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    • 专利摘要:
    The present invention is triazaspiro [5. 5] It is an object to provide an undecane derivative, quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or a medicament containing the same as an active ingredient (symbols in the formula are as described in the specification). . Formula I Since the compound represented by the formula (I) controls the action of the chemokine / chemokine receptor, it is possible to prevent various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis, chronic joint rheumatism and / or the like. Or useful for treatment.
    公开号:KR20030003218A
    申请号:KR1020027007117
    申请日:2000-12-01
    公开日:2003-01-09
    发明作者:히로무 하바시타；신이찌 하마노；시로 시바야마；요시카주 타카오카
    申请人:오노 야꾸힝 고교 가부시키가이샤；
    IPC主号:
    专利说明:

    TRIAZASPIRO [5.5] UNDECANE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT}
    [5] Chemokines are known as basic proteins that have endogenous leukocyte chemotaxis and activation, and have strong heparin binding properties. Currently, chemokines are thought to be involved in inflammation, specific leukocyte infiltration during immune response, as well as in development, homing of lymphocytes, blood cell progenitor cells, and somatic cells under physiological conditions.
    [6] The differentiation, proliferation, and apoptosis of blood cells are controlled by various cytokines. In vivo, inflammation is seen locally, and differentiation and maturation of lymphocytes is performed at certain sites. In other words, the various cells required to move to a specific site, and accumulate, a series of inflammation, immune response occurs. Therefore, in addition to the differentiation, proliferation, and death of cells, cell mobility is also an essential phenomenon in the immune system.
    [7] The movement of blood cells in vivo begins by first translating the hematopoiesis beginning in the AGM region into the development of permanent hematopoiesis in the bone marrow through the fetal liver. Furthermore, T cells and progenitor cells of thymic dendritic cells migrate from the fetal liver and bone marrow to the thymus and differentiate into cells in the thymus environment. The cloned T cells migrate to secondary lymphoid tissues and participate in peripheral immune responses. The Langel Hans cells of the skin that capture, activate and differentiate antigens migrate to the T cell region of local lymph nodes and activate naïve T cells as dendritic cells. Memory T cells pass back through the lymphatic vessels, blood vessels and back to the lymph nodes. In addition, B cells, intestinal epithelial T cells, γδ T cells, NKT cells, and dendritic cells migrate and differentiate in the bone marrow without passing through the thymus and participate in an immune response.
    [8] Chemokines are deeply involved in the movement of these various cells. For example, MIP3β, SLC and its receptor, CCR7, play an important role in the migration and homing of these cells to local lymphoid tissues in order for mature dendritic cells that capture antigens to efficiently meet naïve T cells and memory T cells. . In the secondary lymph nodes of PLT mice lacking SLC expression, few T cells and dendritic cells necessary for an antigen-specific immune response are observed (J. Exp. Med., 189 (3), 451 (1999) . )) .
    [9] MDC, TARC and its receptor, CCR4, play an important role in the local migration of Th2 cells in the immune and inflammatory responses associated with Th2 cells. In rat extreme hepatitis model (P.acnes + LPS), anti-TARC antibody inhibited the increase of blood ALT level and the increase of TNFα, FasL expression level in liver, and further improved rat mortality ( J. Clin. Invest. , 102 , 1933 (1998) . In addition, in the mouse OVA-induced airway hypersensitivity model, anti-MDC antibodies reduced airway hypersensitivity by reducing the number of eosinophils that accumulate in lung epilepsy (J. Immunology, 163 , 403 (1999)) .
    [10] MCP-1 and its receptor, CCR2, are involved in infiltration of macrophages into inflammatory sites. Anti-MCP-1 antibody showed inhibitory effect on monocyte, macrophage infiltration into glomeruli in rat anti-Thy1.1 antibody nephritis model (Kidney Int., 51 , 770 (1997)) .
    [11] As such, chemokine receptors are expressed at various times in various specific cells and are greatly involved in the control of inflammatory and immune responses through a mechanism in which effector cells accumulate where chemokines are produced.
    [12] Acquired immunodeficiency syndrome (abbreviated as AIDS) caused by human immunodeficiency virus (hereinafter abbreviated as HIV) infection is one of the diseases which the therapy is most craving for recently. Once HIV infection occurs in CD4-positive cells, which are major target cells, HIV repeats proliferation in the body of the patient, and then destroys T cells responsible for immune function. In this process, the immune function gradually decreases, and various immunodeficiency states such as fever, diarrhea and swelling of the lymph nodes are easily observed, and various opportunistic infections such as carini pneumonia are easily caused. This condition is the onset of AIDS, and it is well known to cause malignant tumors such as Kaposi's sarcoma and to become addicted.
    [13] Various methods for prevention and treatment of AIDS include, for example, (1) inhibiting the proliferation of HIV by administration of reverse transcriptase inhibitors or protease inhibitors, and (2) preventing and alleviating opportunistic infections caused by the administration of drugs with immunostimulating action. Etc. have been attempted.
    [14] HIV is primarily infected with helper T cells, which are the backbone of the immune system. In that case, it is known since 1985 to use the membrane protein CD4 expressed on the T cell membrane (Cell, 52 , 631 (1985)) . The CD4 molecule consists of 433 amino acid residues and is expressed in macrophages, some B cells, vascular endothelial cells, Langel Hans cells in skin tissue, dendritic cells in lymphoid tissue, and glia cells in the central nervous system in addition to mature helper T cells. You can see it. However, it has been found that CD4 molecules alone do not establish HIV infection, suggesting the possibility of the presence of factors other than the CD4 molecules involved when HIV is infected with cells.
    [15] In 1996, a membrane protein called Fusin was identified as a factor involved in HIV infection other than the CD4 molecule (Science, 272 , 872 (1996)) . This Fusin molecule has been demonstrated to be a receptor (ie, CXCR4) of Stromal Derived Factor-1 (abbreviated as SDF-1). Moreover, it has also been demonstrated that SDF-1 specifically inhibits infection of T cell-directed (X4) HIV in vitro (Nature, 382 , 829 (1996), Nature, 382 , 833 (1996)) . In other words, SDF-1 binds to CXCR4 before HIV, and it is thought that HIV infection was suppressed by eliminating the base for HIV infection.
    [16] At the same time, it was discovered that CCR5, a receptor for RANTES, MIP-1α, and MIP-1β, is also used when macrophage-directed (R5) HIV is infected as another chemokine receptor (Science, 272 , 1955 (1996)). ) .
    [17] Thus, the ability to eliminate HIV and CXCR4 or CCR5 from each other, or to bind the HIV virus and leave the virus incapable of binding to CXCR4 or CCR5, can be an HIV infection inhibitor. There is also an example showing that the small molecule compound originally found as an HIV infection inhibitor is actually an antagonist of CXCR4 (Nature Medicine, 4 , 72 (1998)) .
    [18] From the above, the chemokine / chemokine receptor is considered to be deeply involved in inflammation, immune disease or HIV infection. For example, various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases (allergic bronchial pulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), nephritis, nephritis, nephritis, arthritis, chronic joint rheumatism, psoriasis, Rhinitis, conjunctivitis, suppression of ischemic reperfusion injury, multiple sclerosis, ulcerative colitis, acute respiratory distress syndrome, shock from bacterial infections, diabetes, autoimmune disease treatment, transplant rejection, immune suppression, cancer metastasis prevention, acquired immunity It is thought to be involved in dysfunction syndrome.
    [19] On the other hand, the specification of WO97 / 11940 discloses that the compound represented by the following formula Z is useful for inhibiting platelet aggregation.
    [20]
    [21] Wherein A iZ and B jZ are each independently selected from carbon, nitrogen, oxygen or sulfur, provided that at least one atom of A iZ is carbon and at least one B jZ is carbon;
    [22] Spiro cyclic rings formed by A iz and B j Z may each be partially unsaturated, in some cases,
    [23] pZ and qZ are each independently a number from 2 to 6,
    [24] mZ is a number from 0 to pZ,
    [25] R 10Z is the same or different and is an incoherent substituent, each independently selected from hydrogen, alkyl, halo substituted alkyl, alkenyl, alkynyl, cycloalkyl, ═O , = S, and the like,
    [26] nZ is a number from 0 to qZ,
    [27] R 0Z are the same or different and are incoherent substituents, each independently selected from hydrogen, alkyl, halo substituted alkyl, alkenyl, alkynyl, cycloalkyl, = 0, = S, and the like,
    [28] -(L Z )-is a bond or a divalent substituted or unsubstituted chain of 1 to 10 atoms selected from carbon, nitrogen, sulfur and oxygen,
    [29] Q Z is a basic group containing one or two or more basic radicals, and
    [30] R 3Z is an acidic group containing one or two acidic radicals.
    [31] In addition, the specification of WO98 / 25605 discloses that the compound represented by the formula (Y) is useful as a chemokine receptor modulator.
    [32]
    [33] Wherein mY or lY each independently represent 0, 1, 2, 3, 4 or 5,
    [34] R 1Y represents a hydrogen atom, a C1-8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group, or the like.
    [35] W Y represents a C1-3 alkyl group substituted with a single bond, a C1-3 alkyl group, oxo, or the like, and
    [36] Q Y represents -NR 2- , -O-, -S-, -S (O)-or -SO 2- ,
    [37] X Y represents a C1-3 alkyl group substituted with a single bond, a C1-3 alkyl group, oxo, or the like,
    [38] Y Y -Z Y ring represents phenyl, naphthyl, heteroaryl. However, the definition of each symbol is an excerpt.
    [1] The present invention provides triazaspiro [5. 5] Undecane derivatives and pharmaceuticals containing these as active ingredients.
    [2] More specifically, triazaspiro [5. 5] Undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, methods for their preparation, and pharmaceuticals containing them as active ingredients.
    [3]
    [4] In the above formula, all the symbols have the same meaning as in the latter.
    [39] Disclosure of the Invention
    [40] The inventors of the present invention have made diligent efforts to find compounds that control the action of various chemokine / chemokine receptors. As a result, triazaspiro [5. 5] Undecan derivatives have been found to achieve the object of the present invention to complete the present invention.
    [41] The present invention,
    [42] i) Triazaspiro represented by the following formula (I) [5. 5] undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof,
    [43] ii) a process for the preparation of compounds represented by formula (I), quaternary ammonium salts thereof, N-oxides thereof, or non-toxic salts thereof,
    [44] iii) A pharmaceutical comprising the compound represented by the formula (I), quaternary ammonium salts thereof, N-oxides thereof, or non-toxic salts thereof as an active ingredient.
    [45] Formula I
    [46]
    [47] In which R 1 is
    [48] (1) a hydrogen atom,
    [49] (2) a C1-18 alkyl group,
    [50] (3) a C2-18 alkenyl group,
    [51] (4) a C2-18 alkynyl group,
    [52] (5) -COR 6 ,
    [53] (6) -CONR 7 R 8 ,
    [54] (7) -COOR 9 ,
    [55] (8) -SO 2 R 10 ,
    [56] (9) -COCOOR 11 ,
    [57] (10) -CONR 12 COR 13 ,
    [58] (11) Cyc1, or
    [59] (12) optionally selected 1 to 5 (a) halogen atoms, (b) -CONR 7 R 8 , (c) -COOR 9 , (d) -OR 14 , (e) -SR 15 , (f) -NR 16 R 17 , (g) -NR 18 COR 19 , (h) -SO 2 NR 20 R 21 , (i) -OCOR 22 , (j) -NR 23 SO 2 R 24 , (k) -NR 25 COOR 26 , (l) -NR 27 CONR 28 R 29 , (m) Cyc 1, (n) keto group, (o) C 1-18 alkyl group substituted by -N (SO 2 R 24 ) 2 , C 2-18 alkenyl group, Or a C2-18 alkynyl group,
    [60] (In the group, R 6 to R 9 , R 11 to R 21 , R 23 , R 25, and R 27 to R 29 are each independently.
    [61] (1) a hydrogen atom,
    [62] (2) a C1-8 alkyl group,
    [63] (3) a C2-8 alkenyl group,
    [64] (4) a C2-8 alkynyl group,
    [65] (5) Cyc1, or
    [66] (6) 1 to 5 optionally selected (a) Cyc1, (b) halogen atoms, (c) -OR 30 , (d) -SR 31 , (e) -NR 32 R 33 , (f) -COOR 34 , (g) a C1-8 alkyl group substituted by -CONR 35 R 36 , (h) -NR 37 COR 38 , (i) -NR 39 SO 2 R 40 , (j) -N (SO 2 R 40 ) 2 , C2-8 alkenyl group, or C2-8 alkynyl group, or
    [67] R 7 and R 8 , R 20 and R 21 , R 28 and R 29 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 195 - (C2~6 alkylene) - represents the (in which R 195 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    [68] R 10 , R 22 , R 24 and R 26 are each independently
    [69] (1) a C1-8 alkyl group,
    [70] (2) a C2-8 alkenyl group,
    [71] (3) a C2-8 alkynyl group,
    [72] (4) Cyc1, or
    [73] (5) 1-5 optionally selected (a) Cyc1, (b) halogen atom, (c) -OR 30 , (d) -SR 31 , (e) -NR 32 R 33 , (f) -COOR 34 , (g) a C1-8 alkyl group substituted by -CONR 35 R 36 , (h) -NR 37 COR 38 , (i) -NR 39 SO 2 R 40 , (j) -N (SO 2 R 40 ) 2 , C2-8 alkenyl group, or C2-8 alkynyl group,
    [74] (In the group, R 30 to R 37 and R 39 each independently represent a hydrogen atom, a C 1-8 alkyl group, Cyc 1, or a C 1-8 alkyl group substituted with Cyc 1, or
    [75] R 35 and R 36 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene group) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 196 - (C2~6 alkylene) - a represents (in which, R 196 is hydrogen, C1~8 alkyl group, a phenyl group Or a C1-8 alkyl group substituted with a phenyl group),
    [76] R 38 and R 40 each independently represent a C1-8 alkyl group, Cyc1, or a C1-8 alkyl group substituted by Cyc1)
    [77] Cyc1 is C3-15 monocyclic, cyclic, or tricyclic (condensed or spiro) carbon ring, or 3 to 3 containing 1 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms 15-membered monocyclic, cyclic or tricyclic (condensed or spiro) heterocyclic rings are shown.
    [78] However, Cyc1 may be substituted by 1 to 5 R 51 s ,
    [79] R 51 is
    [80] (1) a C1-8 alkyl group,
    [81] (2) a C2-8 alkenyl group,
    [82] (3) a C2-8 alkynyl group,
    [83] (4) halogen atoms,
    [84] (5) nitro groups,
    [85] (6) trifluoromethyl group
    [86] (7) trifluoromethoxy group,
    [87] (8) nitrile group,
    [88] (9) ketogi,
    [89] (10) Cyc2
    [90] (11) -OR 52 ,
    [91] (12) -SR 53 ,
    [92] (13) -NR 54 R 55 ,
    [93] (14) -COOR 56 ,
    [94] (15) -CONR 57 R 58 ,
    [95] (16) -NR 59 COR 60 ,
    [96] (17) -SO 2 NR 61 R 62 ,
    [97] (18) -OCOR 63 ,
    [98] (19) -NR 64 SO 2 R 65 ,
    [99] (20) -NR 66 COOR 67 ,
    [100] (21) -NR 68 CONR 69 R 70 ,
    [101] (22) -B (OR 71 ) 2 ,
    [102] (23) -SO 2 R 72 ,
    [103] (24) -N (SO 2 R 72 ) 2 , or
    [104] (25) 1-5 optionally selected (a) halogen atoms, (b) Cyc2, (c) -OR 52 , (d) -SR 53 , (e) -NR 54 R 55 , (f) -COOR 56 , (g) -CONR 57 R 58 , (h) -NR 59 COR 60 , (i) -SO 2 NR 61 R 62 , (j) -OCOR 63 , (k) -NR 64 SO 2 R 65 , (l) -NR 66 COOR 67 , (m) -NR 68 CONR 69 R 70 , (n) -B (OR 71 ) 2 , (o) -SO 2 R 72 , (p) -N (SO 2 R 72 ) 2 Substituted C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group)
    [105] (In the group, R 52 to R 62 , R 64 , R 66 and R 68 to R 71 are each independently.
    [106] 1) hydrogen atom, 2) C1-8 alkyl group, 3) C2-8 alkenyl group, 4) C2-8 alkynyl group, 5) Cyc2, or 6) Cyc2, -OR 73 , -COOR 74 , -NR 75 R 76 C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by
    [107] R 57 and R 58 , R 61 and R 62 , R 69 and R 70 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 197 - (C2~6 alkylene) - represents the (in which R 197 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    [108] R 63 , R 65 , R 67 and R 72 are each independently 1) C1-8 alkyl group, 2) C2-8 alkenyl group, 3) C2-8 alkynyl group, 4) Cyc2, or 5) Cyc2, -OR 73 , -COOR 74 , -C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by -NR 75 R 76 ,
    [109] (In the group, R 73 to R 76 each independently represent a hydrogen atom, a C1-8 alkyl group, Cyc2, or a C1-8 alkyl group substituted with Cyc2.)
    [110] Cyc2 has the same meaning as Cyc1.
    [111] However, Cyc2 may be substituted by 1 to 5 R 77 ,
    [112] R 77 is
    [113] 1) a C1-8 alkyl group,
    [114] 2) halogen atoms,
    [115] 3) nitro group,
    [116] 4) trifluoromethyl group,
    [117] 5) trifluoromethoxy group,
    [118] 6) nitrile group,
    [119] 7) -OR 78 ,
    [120] 8) -NR 79 R 80 ,
    [121] 9) -COOR 81 ,
    [122] 10) -SR 82 ,
    [123] 11) -CONR 83 R 84 ,
    [124] 12) a C2-8 alkenyl group,
    [125] 13) a C2-8 alkynyl group,
    [126] 14) ketogi,
    [127] 15) Cyc6,
    [128] 16) -NR 161 COR 162 ,
    [129] 17) -SO 2 NR 163 R 164 ,
    [130] 18) -OCOR 165 ,
    [131] 19) -NR 166 SO 2 R 167 ,
    [132] 20) -NR 168 COOR 169 ,
    [133] 21) -NR 170 CONR 171 R 172 ,
    [134] 22) -SO 2 R 173 ,
    [135] 23) -N (SO 2 R 167 ) 2 ,
    [136] 24) optionally selected 1 to 5 (a) halogen atoms, (b) -OR 78 , (c) -NR 79 R 80 , (d) -COOR 81 , (e) -SR 82 , (f) -CONR 83 R 84 , (g) keto group, (h) Cyc6, (i) -NR 161 COR 162 , (j) -SO 2 NR 163 R 164 , (k) -OCOR 165 , (l) -NR 166 SO 2 R 167 , (m) -NR 168 COOR 169 , (n) -NR 170 CONR 171 R 172 , (o) -SO 2 R 173 , (p) -N (SO 2 R 167 ) 2 substituted by C 1-8 Alkyl group, C2-8 alkenyl group, C2-8 alkynyl group)
    [137] (In the group, R 78 to R 84 , R 161 to R 164 , R 166 , R 168 and R 170 to R 172 each independently represent (a) a hydrogen atom, (b) a C1-8 alkyl group, and (c) C2 to 8 alkenyl group, (d) C2-8 alkynyl group, (e) Cyc6, (f) Cyc6, -OR 174 , -COOR 175 , -NR 176 R 177 , -CONR 178 R 179 substituted by C1-8 alkyl group , C2-8 alkenyl group, C2-8 alkynyl group, or
    [138] R 83 and R 84 , R 163 and R 164 , R 171 and R 172 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 198 - (C2~6 alkylene) - represents the (in which R 198 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted by a phenyl group),
    [139] R 165 , R 167 , R 169 and R 173 each independently represent (a) a C1-8 alkyl group, (b) a C2-8 alkenyl group, (c) a C2-8 alkynyl group, (d) Cyc6, or (e) C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by Cyc6, -OR 174 , -COOR 175 , -NR 176 R 177 , -CONR 178 R 179 )
    [140] (In the group, R 174 to R 177 each independently represent 1) a hydrogen atom, 2) a C 1-8 alkyl group, 3) Cyc 6, or 4) a C 1-8 alkyl group substituted by Cyc 6, or
    [141] R 178 and R 179 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene group) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 199 - (C2~6 alkylene) - a represents (in which, R 199 is hydrogen, C1~8 alkyl group, a phenyl group Or a C1-8 alkyl group substituted with a phenyl group),
    [142] Cyc6 represents a C3-8 monocyclic carbon ring or a 3-8 membered monocyclic ring containing 1-4 nitrogen atoms, 1-2 oxygen atoms and / or 1-2 sulfur atoms.
    [143] However, Cyc6 may be substituted by 1 to 5 R 180 ,
    [144] R 180 is
    [145] (1) a C1-8 alkyl group,
    [146] (2) a halogen atom,
    [147] (3) nitro groups,
    [148] (4) trifluoromethyl group,
    [149] (5) trifluoromethoxy group,
    [150] (6) nitrile group,
    [151] (7) -OR 181 ,
    [152] (8) -NR 182 R 183 ,
    [153] (9) -COOR 184 ,
    [154] (10) -SR 185 , or
    [155] (11) represents -CONR 186 R 187
    [156] (In the group, R 181 to R 187 each independently represent 1) a hydrogen atom, 2) a C1-8 alkyl group, 3) a phenyl group, or 4) a C1-8 alkyl group substituted with a phenyl group,
    [157] R 182 and R 183 , R 186 and R 187 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 200 - (C2~6 alkylene) - represents the (in which, R 200 represents a hydrogen atom, C1-8 alkyl group substituted by C1-8 alkyl group, phenyl group, phenyl group)),
    [158] R 2 is
    [159] (1) a hydrogen atom,
    [160] (2) a C1-8 alkyl group,
    [161] (3) a C2-8 alkenyl group,
    [162] (4) a C2-8 alkynyl group,
    [163] (5) -OR 90 ,
    [164] (6) Cyc3, or
    [165] (7) 1-5 optionally selected (a) halogen atoms, (b) -OR 90 , (c) -SR 91 , (d) -NR 92 R 93 , (e) -COOR 94 , (f) -CONR 95 R 96 , (g) -NR 97 COR 98 , (h) -SO 2 NR 99 R 100 , (i) -OCOR 101 , (j) -NR 102 SO 2 R 103 , (k) -NR 104 COOR 105 , (l) -NR 106 CONR 107 R 108 , (m) Cyc3, (n) keto group, (o) C1-8 alkyl group substituted by -N (SO 2 R 103 ) 2 , C2-8 alkenyl group or A C2-8 alkynyl group,
    [166] (In the group, R 90 to R 100 , R 102 , R 104 and R 106 to R 108 are each independently 1) a hydrogen atom, 2) a C1-8 alkyl group, 3) a C2-8 alkenyl group, 4) C2-8 An alkynyl group, 5) Cyc3, or 6) a C1-8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group substituted by Cyc3, or
    [167] R 95 and R 96 , R 99 and R 100 , R 107 and R 108 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 )-(C2-6 alkylene group) -S- (C2-6 alkylene group)-or 4)-(C2-6 alkylene group) -NR 201- (C2-6 alkylene group)- R 201 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    [168] R 101 , R 103 and R 105 are each independently 1) a C1-8 alkyl group, 2) a C2-8 alkenyl group, 3) a C2-8 alkynyl group, or 4) a C1-8 alkyl group substituted by Cyc3 or Cyc3, C2-8 alkenyl group, C2-8 alkynyl group,
    [169] Cyc3 has the same meaning as Cyc1.
    [170] However, Cyc3 may be substituted by 1 to 5 R 109 ,
    [171] R 109 has the same meaning as R 51 )
    [172] R 3 and R 4 are each independently
    [173] (1) a hydrogen atom,
    [174] (2) a C1-8 alkyl group,
    [175] (3) a C2-8 alkenyl group,
    [176] (4) a C2-8 alkynyl group,
    [177] (5) -COOR 120 ,
    [178] (6) -CONR 121 R 122 ,
    [179] (7) Cyc4, or
    [180] (8) 1-5 optionally selected (a) halogen atoms, (b) nitrile groups, (c) Cyc4, (d) -COOR 120 , (e) -CONR 121 R 122 , (f) -OR 123 , ( g) -SR 124 , (h) -NR 125 R 126 , (i) -NR 127 COR 128 , (j) -SO 2 NR 129 R 130 , (k) -OCOR 131 , (l) -NR 132 SO 2 R 133 , (m) -NR 134 COOR 135 , (n) -NR 136 CONR 137 R 138 , (o) -S-SR 139 , (p) -NHC (= NH) NHR 140 , (q) keto group, (r) C1-8 alkyl group, C2-8 alkenyl group, or C2-8 alkynyl group substituted with -NR 145 CONR 146 COR 147 , (s) -N (SO 2 R 133 ) 2 ,
    [181] (In the group, R 120 to R 130 , R 132 , R 134 , R 136 to R 138 , R 145 and R 146 are each independently 1) a hydrogen atom, 2) a C1-8 alkyl group, and 3) a C2-8 alkenyl group. 4) C2-8 alkynyl group, 5) Cyc4, or 6) Cyc4, a halogen atom, C1-8 alkyl group substituted by -OR 148 , -SR 149 , -COOR 150 , or -NHCOR 141 , C2-8 alkenes Or a C2-8 alkynyl group,
    [182] R 121 and R 122 , R 129 and R 130 , R 137 and R 138 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 202 - (C2~6 alkylene) - represents the (in which R 202 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, a C1-8 alkyl group substituted with a phenyl group),
    [183] R 131 , R 133 , R 135 , R 139 and R 147 are each independently 1) C1-8 alkyl group, 2) C2-8 alkenyl group, 3) C2-8 alkynyl group, 4) Cyc4, or 5) Cyc4, C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by a halogen atom, -OR 148 , -SR 149 , -COOR 150 , or -NHCOR 141 ,
    [184] R 140 represents a hydrogen atom, -COOR 142 , or -SO 2 R 143 ,
    [185] (In the group, R 141 to R 143 are each independently 1) C 1-8 alkyl group, 2) C 2-8 alkenyl group, 3) C 2-8 alkynyl group, 4) Cyc 4, or 5) C 1 -substituted by Cyc 4. 8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group,
    [186] R 148 to R 150 are each independently 1) hydrogen atom, 2) C1-8 alkyl group, 3) C2-8 alkenyl group, 4) C2-8 alkynyl group, 5) Cyc4, or 6) C1 substituted by Cyc4 It represents a -8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group,
    [187] Cyc4 has the same meaning as Cyc1.
    [188] Provided that Cyc4 may be substituted with 1 to 5 R 144 , and R 144 has the same meaning as R 51;
    [189] R 3 and R 4 together
    [190]
    [191] In which R 190 and R 191 each independently represent the same meaning as R 3 or R 4, and
    [192] R 5 is
    [193] (1) a hydrogen atom,
    [194] (2) a C1-8 alkyl group,
    [195] (3) Cyc5, or
    [196] (4) C1-8 alkyl group substituted by Cyc5.
    [197] (In the group, Cyc5 has the same meaning as Cyc1.
    [198] However, Cyc5 may be substituted by 1 to 5 R 160 , and R 160 has the same meaning as R 51 .
    [199] In the present invention, the C1-18 alkyl group is methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl, tetradecyl, pentadecyl, hexadecyl, hepta Decyl, octadecyl groups, and isomers thereof.
    [200] C2-18 alkenyl group means the C2-18 alkylene group which may have 1-9 (preferably 1-4) double bonds. For example, vinyl, propenyl, butenyl, pentenyl, hexenyl, heptenyl, octenyl, nonenyl, decenyl, undecenyl, dodecenyl, tridecenyl, tetradecenyl, pentadecenyl, hexadecenyl, Heptadecenyl, octadecenyl, butadienyl, pentadienyl, hexadienyl, heptadienyl, octadienyl, nonadienyl, decadienyl, undecadienyl, dodecadienyl, tridecadienyl , Tetradecadienyl, pentadecadienyl, hexadecadienyl, heptadecadienyl, octadecadienyl, hexatrienyl, heptatrienyl, octatrienyl, nonatrienyl, decatrienyl , Undecatenyl, dodecatenyl, tridecatenyl, tetradecatenyl, pentadecatenyl, hexadecatenyl, heptadecatrienyl, octadecatenyl, and isomers thereof And the like can be mentioned.
    [201] The C2-18 alkynyl group means a C2-18 alkylene group which may have 1 to 9 triple bonds (preferably 1 to 4). For example, ethynyl, propynyl, butynyl, pentynyl, hexynyl, heptynyl, octinyl, noninyl, decinyl, undecynyl, dodecynyl, tridecynyl, tetradecynyl, pentadecynyl, hexa Decinyl, heptadecinyl, octadecynyl, butadiinyl, pentadiinyl, hexadiinyl, heptadiinyl, octadininyl, nonadidinyl, decadiinyl, undecadiinyl, dodecadiinyl, tridecadinyl Neal, tetradecadiinyl, pentadecadiinyl, hexadecadinyl, heptadecainyl, octadecadiinyl, hexatriinyl, heptatriinyl, octatriinyl, nonatriinyl, decatinyl, undecatinyl , Dodecatinyl, tridecatinyl, tetradecatinyl, pentadecatinyl, hexadecatinyl, heptadecatinyl, octadecatinyl, and isomer groups thereof.
    [202] Examples of the halogen atom include chlorine, bromine, fluorine and iodine atoms.
    [203] The C1-8 alkyl group represents methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl group and isomers thereof.
    [204] The C2-8 alkenyl group means the C2-8 alkylene group which may have 1-4 double bonds. For example, vinyl, propenyl, butenyl, pentenyl, hexenyl, heptenyl, octenyl, butadienyl, pentadienyl, hexadienyl, heptadienyl, octadienyl, hexatrienyl, heptariene And aryl, octatrienyl groups, and isomer groups thereof.
    [205] C2-8 alkynyl group means the C2-8 alkylene group which may have 1-4 triple bonds. For example, ethynyl, propynyl, butynyl, pentynyl, hexynyl, heptynyl, octinyl, butadiinyl, pentadiinyl, hexadiinyl, heptadiinyl, octadiinyl, hexatriinyl, heptatriinyl , Octatriynyl group, and isomer groups thereof.
    [206] Examples of the C2-6 alkylene group include methylene, ethylene, trimethylene, tetramethylene, pentamethylene, hexamethylene group and isomer groups thereof.
    [207] C3-15 monocyclic, cyclic, or tricyclic (condensed or spiro) carbon rings are, for example, cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, cyclooctane, cyclopentene, cyclohexene, cycloheptene, Cyclooctene, cyclopentadiene, cyclohexadiene, cycloheptadiene, cyclooctadiene, benzene, indene, naphthalene, indane, tetrahydronaphthalene, bicyclo [3. 3. 0] octane, bicyclo [4. 3. 0] nonane, bicyclo [4. 4. 0] decane, spiro [4. [4] Nonan, Spiro [4. 5] decane, spiro [5. 5] undecane, bicyclo [3. 1.1] heptane, bicyclo [3. 3. 1] -2-heptene, fluorene, anthracene, etc. are mentioned.
    [208] 3-15 membered monocyclic, cyclic, or tricyclic (condensed or spiro) heterocyclic ring containing 1 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms, for example, 1 3- to 15-membered monocyclic, cyclic, or tricyclic (condensed or spiro) heterocyclic aryl containing 4 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms, or part thereof All is saturated.
    [209] Examples of the 3- to 15-membered monocyclic, cyclic, or tricyclic (condensed or spiro) heterocyclic aryl containing 1 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms include pyrrole, Imidazole, triazole, tetrazole, pyrazole, pyridine, pyrazine, pyrimidine, pyridazine, azepine, diazepine, furan, pyran, oxepin, thiophene, thiaine (thiopyran), thiopine, oxazole , Isoxazole, thiazole, isothiazole, prazan, oxadiazole, oxazine, oxadiazine, oxazine, oxadiazetine, thiadiazole, thiazine, thiadiazine, thiazene, thiadizepine , Indole, isoindole, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, indazole, quinoline, isoquinoline, phthalazine, naphthyridine, quinoxaline, quinazoline, cinnoline, benzoxazole , Benzothiazole, benzoimidazole, benzooxepin, benzooxazepine, benzooxadiasepine, benzothiene, benzo Alas benzodiazepine, benzothiazolyl may be mentioned diazepine, benzoazepine, benzodiazepine, benzo plastic cup, benzo thiadiazole, benzotriazole, carbazole, acridine, dibenzofuran, dibenzothiophene ring and the like.
    [210] 3- to 15-membered monocyclic, cyclic, or tricyclic (condensed or spiro) heterocycles containing 1 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms, Or as fully saturated,
    [211] Pyrroline, pyrrolidine, imidazoline, imidazolidine, pyrazoline, pyrazolidine, triazolin, triazolidine, tetrazoline, tetrazolidine, dihydropyridine, tetrahydropyridine, piperidine, Dihydropyrazine, tetrahydropyrazine, piperazine, dihydropyrimidine, tetrahydropyrimidine, perhydropyrimidine, dihydropyridazine, tetrahydropyridazine, perhydropyridazine, dihydroazine, tetrahydroazine , Perhydroazepine, dihydrodiazepine, tetrahydrodiazepine, perhydrodiazepine, dihydrofuran, tetrahydrofuran, dihydropyran, tetrahydropyran, dihydrothiophene, tetrahydrothiophene, dihydrothiane Phosphorus (dihydrothiopyran), tetrahydrothiaine (tetrahydrothiopyran), dihydrooxazole, tetrahydrooxazole, dihydroisoxazole, tetrahydroisoxazole, di Drothiazole, tetrahydrothiazole, dihydroisothiazole, tetrahydroisothiazole, dihydrooxadiazole, tetrahydrooxadiazole, dihydrothiodiazole, tetrahydrothiodiazole, tetrahydrooxadiazine , Tetrahydrothiadiazine, tetrahydrooxazepine, tetrahydrooxadiazepine, perhydrooxazepine, perhydrooxadiazepine, tetrahydrothiazepine, tetrahydrothiadiazepine, perhydrothiazepine, per Hydrothiadiazepine, morpholine, thiomorpholine, indolin, isoindolin, dihydrobenzofuran, perhydrobenzofuran, dihydroisobenzofuran, perhydroisobenzofuran, dihydrobenzothiophene, perhydrobenzo Thiophene, dihydroisobenzothiophene, perhydroisobenzothiophene, dihydroindazole, perhydroindazole, dihydroquinoline, tetrahydroquinoline, perhydroquinol Lean, dihydroisoquinoline, tetrahydroisoquinoline, perhydroisoquinoline, dihydrophthalazine, tetrahydrophthalazine, perhydrophthalazine, dihydronaphthyridine, tetrahydronaphthyridine, perhydronaph Tilidine, dihydroquinoxaline, tetrahydroquinoxaline, perhydroquinoxaline, dihydroquinazolin, tetrahydroquinazolin, perhydroquinazolin, dihydrocinnoline, tetrahydrocinnoline, perhydrocinnoline, dihydro Benzoxazole, perhydrobenzoxazole, dihydrobenzothiazole, perhydrobenzothiazole, dihydrobenzoimidazole, perhydrobenzoimidazole, dihydrocarbazole, tetrahydrocarbazole, perhydrocarbazole, dihi Droacridin, tetrahydroacridine, perhydroacridine, dihydrodibenzofuran, dihydrodibenzothiophene, tetrahydrodibenzofuran, tetrahydrodibenzothiophene, Perhydrodibenzofuran, perhydrodibenzothiophene, dioxolane, dioxane, dithiolane, dithiane, benzodioxalan, benzodioxane, benzodithiolane, benzodithiane, 2,4,6-trioxaspiro [Bicyclo [3. 3. 0] octane-3,1'-cyclohexane], 1,3-dioxolano [4, 5-g] chromen, 2-oxabicyclo [2. 2. 1] heptane ring etc. are mentioned.
    [212] C3-8 monocyclic carbon ring is, for example, cyclopropane, cyclobutane, cyclopentane, cyclohexane, cycloheptane, cyclooctane, cyclopentene, cyclohexene, cycloheptene, cyclooctene, cyclopentadiene, cyclohexadiene, Cycloheptadiene, cyclooctadiene, benzene, etc. are mentioned.
    [213] A 3-8 membered monocyclic heterocyclic ring containing 1 to 4 nitrogen atoms, 1 to 2 oxygen atoms and / or 1 to 2 sulfur atoms is, for example, 1 to 4 nitrogen atoms or 1 to 2 oxygen atoms. The 3-8 membered monocyclic heterocyclic aryl containing an atom and / or 1-2 sulfur atoms, or part or all thereof is saturated.
    [214] As a 3-8 membered monocyclic heterocyclic aryl containing 1-4 nitrogen atoms, 1-2 oxygen atoms, and / or 1-2 sulfur atoms, pyrrole, imidazole, triazole, tetrazole, pyrazole , Pyridine, pyrazine, pyrimidine, pyridazine, azepine, diazepine, furan, pyran, oxepin, thiophene, thiaine (thiopyran), thiopin, oxazole, isoxazole, thiazole, isothiazole , Prazan, oxadiazole, oxazine, oxadiazine, oxazepine, oxadiazepine, thiadiazole, thiazine, thiadiazine, thiazine, thiadizepine ring and the like.
    [215] 3- to 8-membered monocyclic heterocycle containing 1 to 4 nitrogen atoms, 1 to 2 oxygen atoms and / or 1 to 2 sulfur atoms as described above.
    [216] Some or all saturated ones include pyrroline, pyrrolidine, imidazoline, imidazolidine, pyrazoline, pyrazolidine, triazoline, triazolidine, tetrazoline, tetrazolidine, dihydropyridine, tetrahydro Pyridine, piperidine, dihydropyrazine, tetrahydropyrazine, piperazine, dihydropyrimidine, tetrahydropyrimidine, perhydropyrimidine, dihydropyridazine, tetrahydropyridazine, perhydropyridazine, dehydroase Pin, tetrahydroazepine, perhydroazepine, dihydrodiazepine, tetrahydrodiazepine, perhydrodiazepine, dihydrofuran, tetrahydrofuran, dihydropyran, tetrahydropyran, dihydrothiophene, tetrahydro Thiophene, dihydrothiaine (dihydrothiopyran), tetrahydrothiaine (tetrahydrothiopyran), dihydrooxazole, tetrahydrooxazole, dihydroisooxe Tetraazole, tetrahydroisoxazole, dihydrothiazole, tetrahydrothiazole, dihydroisothiazole, tetrahydroisothiazole, dihydrooxadiazole, tetrahydrooxadiazole, dihydrothiodiazole, tetrahydrothio Diazole, tetrahydrooxadiazine, tetrahydrothiadiazine, tetrahydrooxazepine, tetrahydrooxadiazepine, perhydrooxazepine, perhydrooxadiazepine, tetrahydrothiazepine, tetrahydrothiadiazepine And perhydrothiazepine, perhydrothiadiazepine, morpholine, thiomorpholine, dioxolane, dioxane, dithiolane, dithiane and the like.
    [217] In the present invention, each of the groups represented by the R 1 group, the R 2 group, the R 3 group, the R 4 group, and the R 5 group are all preferable.
    [218] The R 1 group is preferably a C 1-18 alkyl group substituted by Cyc 1, a C 2-18 alkenyl group substituted by Cyc 1, or a C 2-18 alkynyl group substituted by Cyc 1, more preferably substituted by Cyc 1. C1-6 alkyl group.
    [219] As Cyc1, a C3-C10 monocyclic or cyclic (condensed or spiro) carbon ring or a 3- to 10-membered monocyclic ring containing 1 to 4 nitrogen atoms, 1 to 2 oxygen atoms and / or 1 to 2 sulfur atoms Or cyclic (condensed or spiro) heterocycles, more preferably C5-7 monocyclic carbocyclic aryl or containing 1 to 4 nitrogen atoms, 2 oxygen atoms and / or 1 sulfur atom 5- to 10-membered monocyclic or cyclic heterocyclic rings.
    [220] Specifically, Cyc1 is preferably a benzene ring, a pyrazole ring, an imidazole ring, a furan ring, a thiophene ring, a benzodioxane ring, a thiazole ring, or a quinoline ring.
    [221] As R 51 which is a substituent of Cyc 1, Cyc 2, -OR 52 , -SR 53 , and -NR 54 R 55 are preferable. As R <52> , R <53> , R <54> and R <55> , a C1-8 alkyl group and Cyc2 are preferable, More preferably, they are methyl, ethyl, a propyl, and a phenyl group.
    [222] As Cyc2, C5-7 monocyclic carbocyclic aryl or 5-7 membered monocyclic heterocyclic aryl containing 1-4 nitrogen atoms, 1 oxygen atom and / or 1 sulfur atom is preferable, and more preferable. Preferably, it is a benzene ring.
    [223] Examples of R 77 which is a substituent of Cyc2 include a C1-8 alkyl group substituted with -CONR 83 R 84 , -NR 161 COR 162 , -SO 2 NR 163 R 164 , -NR 166 SO 2 R 167 , -CONR 83 R 84 , Preferred are C1-8 alkyl groups substituted by -NR 161 COR 162 , C1-8 alkyl groups substituted by -SO 2 NR 163 R 164 , and C1-8 alkyl groups substituted by -NR 166 SO 2 R 167 . As R 83 , R 84 , R 161 , R 162 , R 163 , R 164 , R 166 and R 167 , a C 1-8 alkyl group substituted with a C 1-8 alkyl group, Cyc 6, -NR 176 R 177 is preferable, and more. Preferably, they are methyl, ethyl, propyl, a phenyl group, and a dimethylaminoethyl group.
    [224] Most preferable R 1 is phenylethyl group, phenylpropyl group, phenylbutyl group, phenylpentyl group, phenylhexyl group, 4-methoxyphenylmethyl group, 4-propyloxyphenylmethyl group, 4-phenyloxyphenylmethyl group, 3,5- Dimethyl-1-phenylpyrazol-4-ylmethyl group, 2-phenylimidazol-4-ylmethyl group, 5-ethylfuran-2-ylmethyl group, 5-ethylthiophen-2-ylmethyl group, 3-chloro- 5-methyl-1-phenylpyrazol-4-ylmethyl group, 1,4-benzodioxan-6ylmethyl group, 4- (4-methylsulfonylaminophenyloxy) phenylmethyl group, 4- (4- (2- Dimethylaminoethylsulfonylamino) phenyloxy) phenylmethyl group, 4- (4-dimethylaminosulfonylphenyloxy) phenylmethyl group, 4- (4-methylcarbonylaminophenyloxy) phenylmethyl group, 4- (4- (2 -Dimethylaminoethylcarbonylamino) phenyloxy) phenylmethyl group, 4- (4-dimethylaminocarbonylphenyloxy) phenylmethyl group, etc. are mentioned.
    [225] As R <2> , a C1-8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group, and the C1-8 alkyl group substituted by Cyc3 are preferable. More preferably, they are a C1-4 alkyl group, a C2-4 alkenyl group, and a C2-4 alkynyl group.
    [226] As most preferable R <2> , an ethyl group, a propyl group, a butyl group, 2-propenyl group, 2-butenyl group, 2-propynyl group, phenylmethyl group, thiophen-2-ylmethyl group, 2-butynyl group, etc. are mentioned.
    [227] Examples of R 3 or R 4, a hydrogen atom, C1~8 alkyl group, a C1~8 alkyl substituted by Cyc4, a C1~8 alkyl group substituted by a C1~8 alkyl, Cyc4 and -OR 123 is substituted by -OR 123 , C1-8 alkyl group substituted by -NR 127 COR 128 , C1-8 alkyl group substituted by -NR 132 SO 2 R 133 , C1-8 alkyl group substituted by -NR 134 COOR 135 , -NR 136 CONR 137 Preferred are C 1-8 alkyl groups substituted by R 138 . More preferably, a C1-4 alkyl group, a C1-4 alkyl group substituted by Cyc4, a C1-4 alkyl group substituted by -OR 123 , a C1-4 alkyl group substituted by Cyc4 and -OR 123 , -NR 127 COR C1-4 alkyl group substituted by 128 , C1-4 alkyl group substituted by -NR 132 SO 2 R 133 , C1-4 alkyl group substituted by -NR 134 COOR 135 , substituted by -NR 136 CONR 137 R 138 It is a C1-4 alkyl group.
    [228] As Cyc4, a benzene ring and a cyclohexane ring are preferable.
    [229] As R 123 , a hydrogen atom, a C1-4 alkyl group, a Cyc4, or a C1-4 alkyl group substituted with Cyc4 is preferable, and more preferably a hydrogen atom, a methyl group, an ethyl group, a phenyl group, or a phenylmethyl group.
    [230] As R 127 , R 132 , R 134 , R 136 and R 138 , a hydrogen atom or a methyl group is preferable.
    [231] As R 128 , R 133 , R 135 , and R 137 , a C 1-4 alkyl group substituted with Cyc 4 or Cyc 4 is preferable, and more preferably, it is a phenyl group, a phenylmethyl group, or a phenylethyl group.
    [232] As R <144> which is a substituent of Cyc4, a C1-4 alkyl group, a halogen atom, a phenyl group, and a phenyloxy group are preferable, More preferably, they are a methyl group, a fluorine atom, a chlorine atom, a phenyl group, and a phenyloxy group.
    [233] Most preferred R 3 or R 4 is a propyl group, 1-methylpropyl group, 2-methylpropyl group, cyclohexylmethyl group, 1-hydroxy-2-methylpropyl group, 1-hydroxy-1-cyclohexylmethyl group, 3 -(Cyclopentylethylcarbonyl) aminobutyl group, 3- (benzyloxycarbonyl) aminopropyl group, 3- (phenylcarbonyl) aminobutyl group, 3- (phenylmethylcarbonyl) aminobutyl group, 3- ( Phenylethylcarbonyl) aminobutyl group, 3- (phenylethenylcarbonyl) aminobutyl group, 3- (4-phenylphenylcarbonyl) aminobutyl group, 3- (4-phenyloxyphenylaminocarbonyl) aminobutyl Group, 3- (4-chlorophenylaminocarbonyl) aminobutyl group, 3- (4-fluorophenylaminocarbonyl) aminobutyl group, 3- (phenylmethylaminocarbonyl) aminobutyl group, 3- (4 -Trifluoromethylsulfonyl) aminobutyl group, 4- (cyclopentylethylcarbonyl) aminobutyl group, 4- (benzyloxycarbonyl) aminobutyl group, 4- (phenylcarbonyl) amino Butyl group, 4- (phenylmethylcarbonyl) aminobutyl group, 4- (phenylethylcarbonyl) aminobutyl group, 4- (phenylethenylcarbonyl) aminobutyl group, 4- (4-phenylphenylcarbonyl) Aminobutyl group, 4- (4-phenyloxyphenylaminocarbonyl) aminobutyl group, 4- (4-chlorophenylaminocarbonyl) aminobutyl group, 4- (4-fluorophenylaminocarbonyl) aminobutyl group And 4- (phenylmethylaminocarbonyl) aminobutyl group and 4- (4-trifluoromethylsulfonyl) aminobutyl group.
    [234] As R 5 , a hydrogen atom or a methyl group is preferable.
    [235] As a preferable compound, the compound represented by the following general formula (Ia) is mentioned among the compound of this invention represented by General formula (I).
    [236]
    [237] In the formula, R 2 represents a C1-8 alkyl group,
    [238] R 3 represents a C 1-8 alkyl group or a C 3-7 cycloalkyl (C 1-4) alkyl group,
    [239] R 5 represents a hydrogen atom or a C 1-8 alkyl group,
    [240] A represents a single bond or a C1-10 alkylene group,
    [241] D ring represents a C3-10 monocyclic or cyclic (fused or spiro) carbon ring or a 3-10 membered monocyclic or cyclic (fused or spiro) heterocycle,
    [242] m represents 0 or an integer of 1 to 4,
    [243] R 300 represents a C1-4 alkyl group, a C1-4 alkoxy group, a phenyl group, a phenoxy group, or a benzyloxy group.
    [244] As C3-10 carbon ring which a D ring represents, C3-10 monocyclic or cyclic carbon ring is preferable, More preferably, C3-7 monocyclic carbon ring or C8-10 cyclic carbon ring to be.
    [245] As the 3 to 10 membered hetero ring represented by the D ring, a 3 to 10 membered monocyclic or cyclic heterocyclic aryl including 1 to 4 nitrogen atoms, 1 to 2 oxygen atoms and / or 1 sulfur atom Or part or all thereof is preferably saturated. More preferably, 5 to 7 membered monocyclic aryl containing 1 to 4 nitrogen atoms, 1 to 2 oxygen atoms and / or 1 sulfur atom, 8 to 10 membered heterocyclic aryl or part thereof or All is saturated.
    [246] In the present invention, unless otherwise indicated, the isomers include all of them. For example, the alkyl group, the alkoxy group and the alkylene group include a straight chain and a branched chain. In addition, isomers (E, Z, cis, trans) in double bonds, rings, condensed rings, isomers (R, S, α, β, enantiomers, diastereomers) due to the presence of asymmetric carbons, etc. The optically active substance (D, L, d, l substance) having optical sensitization, the polar substance (high polar substance, low polar substance) by chromatographic separation, the equilibrium compound, the mixture of any ratio thereof, and the racemic mixture are all present invention. Included in
    [247] [salt]
    [248] In the present invention, all non-toxic salts are included. For example, a general salt, acid addition salt, a hydrate salt, etc. are mentioned.
    [249] The compound of the present invention represented by the formula (I) can be converted into the corresponding salt by a known method. The salt is preferably water soluble with no toxicity. Suitable salts include salts of alkali metals (potassium, sodium, etc.), salts of alkaline earth metals (calcium, magnesium, etc.), ammonium salts, pharmaceutically acceptable organic amines (tetramethylammonium, triethylamine, methylamine, dimethylamine , Cyclopentylamine, benzylamine, phenethylamine, piperidine, monoethanolamine, diethanolamine, tris (hydroxymethyl) amine, lysine, arginine, N-methyl-D-glucamine, etc.) Can be.
    [250] The compound of the present invention represented by the formula (I) can be converted into the corresponding acid addition salt by a known method. Acid addition salts are preferably water-soluble and non-toxic. Suitable acid addition salts include inorganic acid salts such as hydrochloride, hydrobromide, sulfate, phosphate, nitrate, or acetates, trifluoroacetates, lactates, tartarates, oxalates, fumarates, maleates, citrates, benzoates, methane Organic acid salts such as sulfonate, ethanesulfonate, benzenesulfonate, toluenesulfonate, isethionate, glucuronate and gluconate.
    [251] In addition, the compound of the present invention represented by the formula (I) or a salt thereof may be converted into a hydrate by a known method.
    [252] The compounds represented by the formula (I) or their nontoxic salts are all preferred. Specifically, the compound described in the Example or its nontoxic salt is mentioned.
    [253] The quaternary ammonium salt of the compound represented by general formula (I) shows that the nitrogen atom of the compound represented by general formula (I) was quaternized with R <0> group.
    [254] R 0 group represents a C 1-8 alkyl group substituted with a C 1-8 alkyl group and a phenyl group.
    [255] N-oxide of the compound represented by general formula (I) means that the nitrogen atom of the compound represented by general formula (I) was oxidized.
    [256] [Method for Producing Compound of the Invention]
    [257] The compound of the present invention represented by the formula (I) can be produced by the method described in the following method or the examples.
    [258] Among the compounds of the present invention represented by the formula (I), compounds in which the nitrogen atom does not represent quaternary ammonium salts or N-oxides, that is, the compounds represented by the following formula (I-1) can be produced by the method shown below.
    [259]
    [260] Wherein R 1-1 , R 2-1 , R 3-1 , R 4-1 , R 5-1 have the same meaning as R 1 , R 2 , R 3 , R 4 , R 5, and N 1 is Represents a nitrogen atom. However, neither nitrogen atom shall represent quaternary ammonium salt or N-oxide.
    [261] In the formula (I-1), any of R 1-1 , R 2-1 , R 3-1 , R 4-1 , and R 5-1 groups does not represent a group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, that is, , The compound represented by the following general formula (I-1A) can be manufactured by the following method.
    [262]
    [263] Wherein R 1-1A , R 2-1A , R 3-1A , R 4-1A , and R 5-1A are R 1-1 , R 2-1 , R 3-1 , R 4-1 , R 5- The same meaning as 1 is shown. However, all shall not represent the group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, and the other symbols show the same meaning as the above.
    [264] In formula (I-1A), a compound in which R 1 does not represent a hydrogen atom, that is, a compound represented by the following formula (I-1A-1) is a compound represented by the following formula (II-1) or a compound represented by the following formula (II-2) It can manufacture by cyclization reaction.
    [265]
    [266] In the above formula, R 1-1A-1 has the same meaning as R 1-1A . However, R1-1A-1 shall not represent a hydrogen atom, and the other symbols show the same meaning as the above.
    [267]
    [268] In the above formula, X-L-NH- represents the terminal of the terminal amino group polystyrene resin, and other symbols represent the same meaning as above.
    [269]
    [270] In the formula, T represents a C1-8 alkyl group substituted with a C1-8 alkyl group, a C3-8 monocyclic carbon ring, or a C3-8 monocyclic carbon ring.
    [271] The cyclization method of the general formula (II-1) is well-known, for example, is performed by heating to 60-120 degreeC using acid (acetic acid, trifluoroacetic acid, hydrochloric acid, etc.) in an organic solvent (toluene etc.). This reaction is a reaction which is cyclized simultaneously with the cleavage of the polystyrene resin.
    [272] In addition, if necessary, the reaction may be converted to a desired non-toxic salt by a known method.
    [273] The cyclization method of this formula (II-2) is well-known, For example, it heats to 60-120 degreeC using tertiary amine (triethylamine, diisopropylethylamine, etc.) in organic solvent (dichloroethane, toluene, etc.). By doing so. This reaction is a reaction which is cyclized simultaneously with the cleavage of the T group.
    [274] In the formula (I-1A), a compound in which R 1 represents a hydrogen atom, that is, a compound represented by the following formula (I-1A-2), is an amino group of the group R 1A-1 in formula (I-1A-1) prepared by the above method. The compound which shows a protecting group, ie, the compound represented by following formula (I-1A-1-1), can be manufactured by deprotection reaction of an amino group.
    [275]
    [276] In the above formula, all symbols represent the same meanings as above.
    [277]
    [278] In the above formula, R 1-1A-1-1 represents an amino protecting group, and other symbols represent the same meanings as described above.
    [279] Examples of the protecting group for the amino group include benzyl group, benzyloxycarbonyl group, allyloxycarbonyl group, t-butoxycarbonyl group, trifluoroacetyl group and the like.
    [280] The protecting group for the amino group is not particularly limited as long as it is a group which can be easily and selectively released in addition to those described above. For example, those described in the TW Greene team, Protective Groups in Organic Synthesis, Third Edition, Wiley-Interscience, New York, 1999 are used.
    [281] The deprotection reaction of this amino group is known, for example,
    [282] (1) alkali hydrolysis,
    [283] (2) deprotection under acidic conditions,
    [284] (3) deprotection reaction by hydrogenolysis,
    [285] (4) deprotection reaction using metal complexes,
    [286] Specifically, (1) the deprotection reaction (e.g., trifluoroacetyl group) by alkali hydrolysis is performed by the alkali metal in an organic solvent (methanol, tetrahydrofuran, dioxane, etc.). Using a hydroxide (sodium hydroxide, potassium hydroxide, lithium hydroxide, etc.), a hydroxide of alkaline earth metal (barium hydroxide, calcium hydroxide, etc.) or a carbonate (sodium carbonate, potassium carbonate, etc.) or an aqueous solution thereof, or a mixture thereof at a temperature of 0 to 40 ° C. Is done.
    [287] (2) The deprotection reaction under acidic conditions (e.g., t-butoxycarbonyl group) is, for example, an organic acid (acetic acid, trifluoroacetic acid, etc.) in an organic solvent (dichloromethane, chloroform, dioxane, ethyl acetate, anisole, etc.). , Methanesulfonic acid or the like), inorganic acids (hydrochloric acid, sulfuric acid, etc.) or mixtures thereof (hydrogen bromide / acetic acid, etc.) at a temperature of 0 to 100 ° C.
    [288] (3) The deprotection reaction by hydrogenolysis (eg, benzyl group, benzyloxycarbonyl group, allyloxycarbonyl group) is, for example, a solvent (ether type (tetrahydrofuran, dioxane, dimethoxyethane, diethyl ether, etc.) , Alcohols (methanol, ethanol, etc.), benzenes (benzene, toluene, etc.), ketones (acetone, methyl ethyl ketone, etc.), nitrile (acetonitrile, etc.), amides (dimethylformamide, etc.), water, acetic acid In the presence of a catalyst (palladium-carbon, palladium black, palladium hydroxide, platinum oxide, Raney-nickel, etc.) in ethyl, acetic acid or a mixed solvent of two or more thereof, in a hydrogen atmosphere at atmospheric pressure or under pressure, or in the presence of ammonium formate It is performed at a temperature of 200 ° C.
    [289] (4) The deprotection reaction using the metal complex is, for example, a trap reagent (tributyltin hydride, dimethone, etc.) and / or an organic acid (such as acetic acid) in an organic solvent (dichloromethane, dimethylformamide, tetrahydrofuran, etc.). Is carried out at a temperature of 0 to 40 ° C using a metal complex (such as tetrakistriphenylphosphinepalladium (0) complex) in the presence of.
    [290] In addition, the compound represented by general formula (I-1A-1) can be manufactured also by the method shown to the following (a)-(g) using the compound represented by general formula (I-1A-2).
    [291] (a) Formula I-1A-1 of, R 1A-1 is C1~18 alkyl group, an alkenyl group C2~18, C2~18 alkynyl group or a C1~18 alkyl group substituted by various substituent, an alkenyl group C2~18 , A C2-18 alkynyl group, and when R 1A-1 is bonded to an N 1 atom, a compound bonded through -CH 2- , that is, a compound represented by the following formula (I-1A-1a) is represented by formula (I-1A-) The compound represented by 2 and the compound represented by following formula (III) can be manufactured by reductive amination reaction.
    [292]
    [293] Wherein R 1-1A-1a is a C1-17 alkyl group, a C2-17 alkenyl group, a C2-17 alkynyl group, or an optionally selected 1-5 (a) halogen atoms, (b) -CONR 7 R 8 , (c ) -COOR 9 , (d) -OR 14 , (e) -SR 15 , (f) -NR 16 R 17 , (g) -NR 18 COR 19 , (h) -SO 2 NR 20 R 21 , (i ) -OCOR 22 , (j) -NR 23 SO 2 R 24 , (k) -NR 25 COOR 26 , (l) -NR 27 CONR 28 R 29 , (m) Cyc1, (n) keto group, (o) C1-17 alkyl group, C2-17 alkenyl group, or C2-17 alkynyl group substituted by -N (SO 2 R 24 ) 2 . However, R 1-1A-1a shall not represent the group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, and the other symbol shows the same meaning as the above.
    [294]
    [295] In the above formula, all symbols represent the same meanings as above.
    [296] This reductive amination reaction is well known, and for example, reducing agents (such as sodium trihydroacetium boron, sodium cyanoborohydride, etc.) in organic solvents (e.g., dichloroethane, dichloromethane, dimethylformamide, acetic acid and mixtures thereof). ) At a temperature of 0 to 40 ° C.
    [297] In addition, this reductive amination reaction can be performed also in the compound in which the nitrogen atom in a R <1> group shows N-oxide.
    [298] (b) the formula of I-1A-1, 1A-R 1 a C1~18 alkyl group, an alkenyl group C2~18, C2~18 alkynyl group or a C1~18 alkyl group substituted by various substituent, an alkenyl group C2~18 , C2-18 alkynyl group, and when R 1A-1 is bonded to an N 1 atom, -CHR A- 1b-(in the group, R A-1b is a C1-17 alkyl group, a C2-17 alkenyl group, C2- 17 alkynyl group), i.e., the compound represented by the following formula (I-1A-1b) is subjected to reductive amination reaction of the compound represented by the formula (I-1A-2) and the compound represented by the formula (IV) It can manufacture.
    [299]
    [300] In the formula, R A-1b represents a C1-17 alkyl group, a C2-17 alkenyl group, a C2-17 alkynyl group, and other symbols represent the same meaning as described above.
    [301]
    [302] In the above formula, all symbols represent the same meanings as above.
    [303] This reductive amination reaction is well known, for example, Lewis acid (titanium tetrachloride, etc.) in the presence of tertiary amines (such as triethylamine, diisopropylethylamine, etc.) in an organic solvent (eg, dichloroethane, dichloromethane, etc.). The reaction is carried out at 0 to 40 ° C., and is carried out at a temperature of 0 to 40 ° C. in the presence of a reducing agent (sodium hydride triacetoxyborate, sodium cyanoborohydride, etc.).
    [304] (c) In the formula (I-1A-1), a compound in which R 1A-1 represents COR 6 , that is, a compound represented by the following formula (I-1A-1c) is represented by a compound represented by the formula (I-1A-2) and the following formula (V) It can manufacture by amidating reaction of the compound shown.
    [305]
    [306] In the above formula, R 6-1A-1c has the same meaning as R 6 . However, R 6-1A-1c shall not represent a group containing a carboxyl group, a hydroxyl group, an amino group or a thiol group, and neither nitrogen atom shall represent a quaternary ammonium salt or N-oxide, and the other symbols are as described above. The same meaning is indicated.
    [307]
    [308] In the above formula, all symbols represent the same meanings as above.
    [309] This amidation reaction is well known and is a tertiary amine (isopropylethylamine, pyridine, triethylamine, dimethylaniline in an organic solvent (chloroform, dichloromethane, diethyl ether, tetrahydrofuran, dioxane, dimethylformamide, etc.). , Dimethylaminopyridine or the like) or an aqueous alkali solution (such as sodium bicarbonate or sodium hydroxide solution).
    [310] (d) In the formula (I-1A-1), a compound in which R 1-1A-1 represents SO 2 R 10 , that is, a compound represented by the following formula (I-1A-1d) is represented by a compound represented by the formula (I-1A-2). The compound represented by the following formula (VI) can be produced by sulfonamide reaction.
    [311]
    [312] In the above formula, R 10-1A-1d has the same meaning as R 10 . However, it does not represent the group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, and neither nitrogen atom shows a quaternary ammonium salt or N-oxide, and the other symbol shows the same meaning as the above.
    [313]
    [314] In the above formula, all symbols represent the same meanings as above.
    [315] This sulfonamide reaction is well known, and tertiary amines (diisopropylethylamine, pyridine, triethylamine, dimethylaniline, etc.) in an inert organic solvent (chloroform, dichloromethane, dichloroethane, diethyl ether, tetrahydrofuran, etc.) In the presence of dimethylaminopyridine or the like).
    [316] (e) In the formula (I-1A-1), a compound in which R 1A-1 represents CONR 7 R 8 , that is, a compound represented by the following formula (I-1A-1e) is represented by a compound represented by the formula (I-1A-2) It can manufacture by reacting the compound represented by VII-1 or the compound represented by following formula (VII-2).
    [317]
    [318] In the above formula, R 7-1A-1e and R 8-1A-1e have the same meanings as R 7 and R 8 . However, all shall not represent the group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, and neither nitrogen atom shall represent a quaternary ammonium salt or N-oxide, and the other symbol shows the same meaning as the above.
    [319]
    [320] In the above formula, all symbols represent the same meanings as above.
    [321]
    [322] In the above formula, all symbols represent the same meanings as above.
    [323] The reaction with the general formula (VII-1) is known, and tertiary amines (isopropylethylamine, pyridine, triethylamine, dimethylaniline, dimethylamino in organic solvents (chloroform, dichloromethane, diethyl ether, tetrahydrofuran, etc.) are known. Pyridine and the like).
    [324] Reaction with this general formula (VII-2) is well-known, and it is performed by making it react at 0-40 degreeC in an inert organic solvent (chloroform, dichloromethane, dichloroethane, dimethylformamide, diethyl ether, tetrahydrofuran, etc.).
    [325] (f) In formula (I-1A-1), R 1-1A-1 is -CH 2 -CH (OH) -R A-1f (R A-1f is a C1-16 alkyl group, C2-16 alkenyl group, C2- 16 alkynyl group or C1-16 alkyl group, C2-16 alkenyl group, C2-16 alkynyl group substituted by various substituents), that is, the compound represented by the following formula (I-1A-1f) It can manufacture by making the compound represented by 1A-2 and the compound represented by following formula (VIII) react.
    [326]
    [327] Wherein R A-1f is a C1-16 alkyl group, a C2-16 alkenyl group, a C2-16 alkynyl group or an optionally selected 1-4 (a) halogen atoms, (b) -CONR 7 R 8 , (c) -COOR 9 , (d) -OR 14 , (e) -SR 15 , (f) -NR 16 R 17 , (g) -NR 18 COR 19 , (h) -SO 2 NR 20 R 21 , (i) -OCOR 22 , (j) -NR 23 SO 2 R 24 , (k) -NR 25 COOR 26 , (l) -NR 27 CONR 28 R 29 , (m) Cyc1, (n) keto group, (o) -N ( C1-16 alkyl group, C2-16 alkenyl group, C2-16 alkynyl group substituted by SO 2 R 24 ) 2 , and neither nitrogen atom represents quaternary ammonium salt or N-oxide, and the other The symbol shows the same meaning as the above.
    [328]
    [329] In the above formula, all symbols represent the same meanings as above.
    [330] This reaction is well known, in the presence or absence of tertiary amines (triethylamine, N-methylmorpholine, etc.) in an organic solvent (methanol, ethanol, 2-propanol, tetrahydrofuran, acetonitrile, etc.). It is performed by making it react at -100 degreeC.
    [331] (g) In formula (I-1A-1), R 1-1A-1 represents -CH 2 -C (= O) -R A-1g (R A-1g has the same meaning as R A-1f ). A compound, i.e., a compound represented by the following formula (I-1A-1g) may be prepared by reacting a compound represented by the formula (I-1A-2) with a compound represented by the following formula (IX-1) or a compound represented by the following formula (IX-2). Can be.
    [332]
    [333] In the above formula, R A-1g represents the same meaning as R A-1f, and other symbols represent the same meanings as above.
    [334]
    [335] In the above formula, all symbols represent the same meanings as above.
    [336]
    [337] In the above formula, all symbols represent the same meanings as above.
    [338] These reactions are well known, and tertiary amines (isopropylethylamine, pyridine, triethylamine, dimethylaniline, etc.) in organic solvents (chloroform, dichloromethane, diethyl ether, tetrahydrofuran, dioxane, dimethylformamide, etc.) In the presence of dimethylaminopyridine or the like).
    [339] In addition, the compound represented by general formula (I-1A-1) can also be manufactured by the method shown to the following (h).
    [340] (h) In the formula (I-1A-1), a compound in which R 1-1A-1 represents a 2-propenyl group (-CH 2 CH = CH 2 ), that is, a compound represented by the following formula (I-1A-1h) is described above. In the formula (I-1A-1) prepared by the method, a compound in which the R 1-1A-1 group represents a 2-propenyloxycarbonyl group (-COO-CH 2 CH = CH 2 ), that is, the following formula (I-1A-1-) The compound represented by 2 can be manufactured by adding to the reaction using a metal complex.
    [341]
    [342] In the above formula, all symbols represent the same meanings as above.
    [343]
    [344] In the above formula, all symbols represent the same meanings as above.
    [345] Reaction using this metal complex is well-known, For example, in the organic solvent (tetrahydrofuran, acetic acid, etc.), it uses the metal complex (tetrakistriphenylphosphine palladium (0) complex etc.) at the temperature of 0-40 degreeC. Is done.
    [346] In the formula (I-1), a compound in which at least one group of the groups R 1 , R 2 , R 3 , R 4 , and R 5 represents a group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, that is, represented by the following formula (I-1B) The compound is a carboxyl group in which at least one group of R 1-1 , R 2-1 , R 3-1 , R 4-1 , R 5-1 is protected by a protecting group in the formula (I-1A) prepared by the above method. The compound which represents the group containing a hydroxyl group, an amino group, or a thiol group, ie, the compound represented by following formula (I-1A-3), can be manufactured by adding to a deprotection reaction of a protecting group.
    [347]
    [348] Wherein R 1-1B , R 2-1B , R 3-1B , R 4-1B , R 5-1B are R 1-1 , R 2-1 , R 3-1 , R 4-1 , R 5- The same meaning as 1 is shown. However, at least 1 group represents the group containing a carboxyl group, a hydroxyl group, an amino group, or a thiol group, and another symbol shows the same meaning as the above.
    [349]
    [350] Wherein R 1-1A-3 , R 2-1A-3 , R 3-1A-3 , R 4-1A-3 , and R 5-1A-3 are R 1-1 , R 2-1 , R 3- The same meaning as 1 , R 4-1 and R 5-1 is shown. However, at least 1 group represents the group containing the carboxyl group, a hydroxyl group, an amino group, or a thiol group protected by the protecting group, and another symbol shows the same meaning as the above.
    [351] As a protecting group of a carboxyl group, a methyl group, an ethyl group, t-butyl group, benzyl group, and an allyl group are mentioned, for example.
    [352] Examples of the protecting group for the hydroxyl group include a methoxymethyl group, 2-tetrahydropyranyl group, t-butyldimethylsilyl group, t-butyldiphenylsilyl group, acetyl group and benzyl group.
    [353] Examples of the protecting group for the amino group include benzyloxycarbonyl group, allyloxycarbonyl group, t-butoxycarbonyl group, trifluoroacetyl group, and 9-fluorenylmethoxycarbonyl group.
    [354] Examples of the protecting group for the thiol group include benzyl group, methoxybenzyl group, acetamide methyl group, triphenylmethyl group and acetyl group.
    [355] The protecting group for the carboxyl group, hydroxyl group, amino group or thiol group is not particularly limited as long as it is a group which can be easily and selectively released apart from the above. For example, those described in the TW Greene team, Protective Groups in Organic Synthesis, Third Edition, Wiley-Interscience, New York, 1999 are used.
    [356] The deprotection reaction of the protecting group of an amino group is performed by the method mentioned above.
    [357] Deprotection reaction of the protecting group of a carboxyl group, a hydroxyl group, or a thiol group is well known, For example, the following reaction etc. are mentioned.
    [358] (1) alkali hydrolysis
    [359] (2) deprotection under acidic conditions
    [360] (3) deprotection reaction by hydrogenolysis
    [361] (4) Deprotection reaction of silyl group
    [362] (5) deprotection reactions using metal complexes
    [363] Among these methods, (1), (2), (3) and (5) are performed by the same method as the deprotection reaction of the protecting group of an amino group mentioned above.
    [364] When (4) is demonstrated concretely, the deprotection reaction of a silyl group is performed at the temperature of 0-40 degreeC using tetrabutylammonium fluoride, for example in an organic solvent (tetrahydrofuran, acetonitrile, etc.).
    [365] Although a person skilled in the art can easily understand, by using these deprotection reactions separately, the target compound of this invention can be manufactured easily.
    [366] In addition, the compound represented by general formula (I-1A-1) can be manufactured also by the method shown to the following (j)-(m) using the compound represented by following general formula (I-1B-1).
    [367]
    [368] Wherein R 1-1B-1 , R 2-1B-1 , R 3-1B-1 , R 4-1B-1 , and R 5-1B-1 are R 1-1 , R 2-1 , R 3- The same meaning as 1 , R 4-1 and R 5-1 is shown. However, at least 1 group represents the group containing an amino group, and another symbol shows the same meaning as the above.
    [369] (j) a compound in which at least one group of R 1-1A-1 , R 2-1A , R 3-1A , R 4-1A , and R 5-1A in the formula (I-1A-1) represents a group containing an amide group, That is, the compound represented by the following formula (I-1A-1j) can be produced by amidation reaction of the compound represented by the formula (I-1B-1).
    [370]
    [371] Wherein R 1-1A-1j , R 2-1A-1j , R 3-1A-1j , R 4-1A-1j , R 5-1A-1j are R 1-1 , R 2-1 , R 3- 1 , R 4-1 and R 5-1 have the same meaning. However, at least 1 group represents the group containing an amide group, and another symbol shows the same meaning as the above.
    [372] This amidation reaction can be performed by the above-mentioned method.
    [373] (k) A compound in which at least one group of R 1-1A-1 , R 2-1A , R 3-1A , R 4-1A , and R 5-1A represents a group containing a sulfonamide group in the formula (I-1A-1) That is, the compound represented by the following general formula (I-1A-1k) can be produced by sulfonamideization of the compound represented by the general formula (I-1B-1).
    [374]
    [375] Wherein R 1-1A-1k , R 2-1A-1k , R 3-1A-1k , R 4-1A-1k , R 5-1A-1k are R 1-1 , R 2-1 , R 3- The same meaning as 1 , R 4-1 and R 5-1 is shown. However, at least 1 group represents the group containing a sulfonamide group, and the other symbol shows the same meaning as the above.
    [376] This sulfonation reaction can be performed by the method mentioned above.
    [377] (m) a compound in which at least one of R 1-1A-1 , R 2-1A , R 3-1A , R 4-1A , and R 5-1A represents a group containing a urea group in the formula (I-1A-1), That is, the compound represented by the following formula (I-1A-1m) can be produced by urea-reacting the compound represented by the formula (I-1B-1).
    [378]
    [379] Wherein R 1-1A-1m , R 2-1A-1m , R 3-1A-1m , R 4-1A-1m , R 5-1A-1m are R 1-1 , R 2-1 , R 3- The same meaning as 1 , R 4-1 and R 5-1 is shown. However, at least 1 group represents the group containing a urea group, and another symbol shows the same meaning as the above.
    [380] This urea reaction can be performed by the method mentioned above.
    [381] In formula (I-1), at least one group of the groups R 1-1 , R 2-1 , R 3-1 , R 4-1 , R 5-1 represents a group containing a hydroxyl group and / or R 1 is a carboxy group The compound which shows group containing, ie, the compound represented by following formula (I-1B-2), can also be manufactured by the method of the following (n).
    [382]
    [383] Wherein R 1-1B-2 , R 2-1B-2 , R 3-1B-2 , R 4-1B-2 , and R 5-1B-2 are R 1-1 , R 2-1 , R 3- 1 , R 4-1 , R 5-1 has the same meaning. Provided that at least one of the groups R 1-1B-2 , R 2-1B-2 , R 3-1B-2 , R 4-1B-2 , and R 5-1B-2 represents a group containing a hydroxyl group, and / Or R <1B-2> represents group containing a carboxy group, and another symbol shows the same meaning as the above.
    [384] (n) In the formula (I-1B-2), R 1-1B-2 is a C1-18 alkyl group substituted with a C1-18 alkyl group, a C2-18 alkenyl group, a C2-18 alkynyl group, or various substituents, and C2-18. alkenyl group, C2~18 represents an alkynyl, and if combined with the N 1 atom R 1-1B-2 -CH 2 - compounds, i.e. compounds represented by formula I-1B-1n, which is coupled via the In formula (I-1B) prepared by one method, R 1 represents a hydrogen atom and at least one of R 2-1 , R 3-1 , R 4-1 , and R 5-1 represents a group containing a hydroxyl group The compound, ie, the compound represented by the following formula (I-1B-3) and the compound represented by the following formula (X) can be prepared by reductive amination reaction.
    [385]
    [386] Wherein R 1-1B-2n is a C1 to 17 alkyl group, a C2 to 17 alkenyl group, a C2 to 17 alkynyl group or an optionally selected 1 to 5 (a) halogen atom, (b) -CONR 7 R 8 , (c) -COOR 9 , (d) -OR 14 , (e) -SR 15 , (f) -NR 16 R 17 , (g) -NR 18 COR 19 , (h) -SO 2 NR 20 R 21 , (i) -OCOR 22 , (j) -NR 23 SO 2 R 24 , (k) -NR 25 COOR 26 , (l) -NR 27 CONR 28 R 29 , (m) Cyc1, (n) keto group, (o)- N (SO 2 R 24) a C1~17 alkyl group substituted by 2, represents an alkenyl group, or C2~17 C2~17 alkynyl. Provided that at least one of R 1-1B-2n , R 2-1B-2 , R 3-1B-2 , R 4-1B-2 , and R 5-1B-2 groups represents a group containing a hydroxyl group, and And / or R 1B-2n represents a group containing a carboxyl group, and neither nitrogen atom represents a quaternary ammonium salt or N-oxide, and other symbols represent the same meaning as described above.
    [387]
    [388] In the above formula, all symbols represent the same meanings as above.
    [389]
    [390] In the above formula, all symbols represent the same meanings as above.
    [391] This reductive amination reaction is performed by the method mentioned above.
    [392] In addition, this reductive amination reaction can be performed also in the compound in which the nitrogen atom in a R <1> group shows N-oxide.
    [393] Among the compounds of the present invention represented by the formula (I), at least one nitrogen atom exhibits a quaternary ammonium salt, that is, the compound represented by the following formula (I-2) is a compound represented by the formula (I-1) and a compound represented by the formula (XI) It can manufacture by making it react.
    [394]
    [395] In the above formula, R 1-2 , R 2-2 , R 3-2 , R 4-2 , R 5-2 have the same meaning as R 1 , R 2 , R 3 , R 4 , R 5, and N 2 is Represents a nitrogen atom. However, at least one nitrogen atom shall represent a quaternary ammonium salt, and Q shall represent a halogen atom.
    [396] R O -Q
    [397] In the formula, R 0 represents a C 1-8 alkyl group substituted with a C 1-8 alkyl group or a phenyl group, and Q represents a halogen atom.
    [398] This reaction is well-known, and is performed at the temperature of 0-40 degreeC, for example in an organic solvent (acetone, dimethylformamide, methyl ethyl ketone, etc.).
    [399] Among the compounds of the present invention represented by the formula (I), at least one nitrogen atom represents a N-oxide, that is, the compound represented by the following formula (I-3) can be produced by oxidizing the compound represented by the formula (I-1).
    [400]
    [401] In the above formula, R 1-3 , R 2-3 , R 3-3 , R 4-3 , R 5-3 represent the same meaning as R 1 , R 2 , R 3 , R 4 , R 5, and N 3 is Represents a nitrogen atom. However, at least one nitrogen atom shall represent N-oxide.
    [402] This oxidation reaction is well known and, for example, in a suitable organic solvent (dichloromethane, chloroform, benzene, hexane, t-butyl alcohol, etc.), peroxidants (hydrogen peroxide, sodium periodate, acyl nitrite, sodium perborate, peracid (e.g. , 3-chloroperbenzoic acid, peracetic acid, and the like), oxone (trade name, hereinafter abbreviated as oxone; potassium monosulfate), potassium permanganate, chromic acid, and the like.
    [403] The compound represented by general formula (II-1) can be manufactured by the following reaction formulas 1-3.
    [404]
    [405]
    [406]
    [407] In the scheme, X represents a polystyrene resin, L represents a divalent group, and the other symbols represent the same meanings as described above.
    [408] The divalent group represented by L depends on the resin used, and examples thereof include a methylene group and a Rink group. The Rink group means a 4- (2,4-dimethoxybenzyl) phenoxymethyl group.
    [409] In the present invention, as the terminal amino group polystyrene resin, for example, aminomethyl polystyrene resin, 9-fluorenylmethyloxycarbonylamino-Rink resin and the like are used.
    [410] As shown in Scheme 4, a resin represented by the formula (XVI) may be prepared using an aminomethyl polystyrene resin and a 9-fluorenylmethyloxycarbonylamino-Rink resin.
    [411]
    [412] In the reaction using the polystyrene resin of the present invention, the reaction product is purified by washing with plural times with conventional purification means such as a solvent (dimethylformamide, dichloromethane, methanol, tetrahydrofuran, toluene, acetic acid / toluene, etc.). Can be. In addition, the product of the final reaction may be subjected to conventional purification means such as distillation under atmospheric pressure or reduced pressure, high performance liquid chromatography using silica gel or magnesium silicate, thin layer chromatography, or column chromatography or washing, recrystallization or the like. It can refine | purify by.
    [413] In addition, the compound represented by Formula (II-2) can be manufactured by Reaction Scheme 5 shown below.
    [414]
    [415] The starting material and each reagent in the present invention are known per se or can be prepared by known methods.
    [416] Pharmacological activity
    [417] The effectiveness of the compound of the present invention represented by the formula (I) has been demonstrated, for example, by the following experiment.
    [418] As described above, in order to screen compounds that inhibit HIV from binding to CXCR4 or CCR5, which are receptors on CD4-positive cells, it is more directly performed in an assay system using HIV virus. However, the use of the HIV virus for mass screening is not practical because of its handling difficulties. On the other hand, macrophage-directed (R5) HIV-1 and RANTES, MIP-1α and MIP-1β all bind to CCR5, so that both the CCR5 binding site on both the HIV side and the RANTES, MIP-1α and MIP-1β side and RANTES on the CCR5 side , MIP-1α, MIP-1β and HIV binding sites can be expected to have some common features. Therefore, in order to find a compound that inhibits the adsorption of HIV virus, which is a sequence of action different from existing anti-AIDS drugs (reverse transcriptase inhibitors or protease inhibitors), the endogenous ligands of CCR5, RANTES, MIP-1α and MIP-, instead of HIV. An analytical system using 1β can be used.
    [419] Specifically, as a system for screening a compound that inhibits the binding of RANTES and CCR5, for example, since CCR5 is a G protein conjugated membrane transmembrane-type receptor, the effect of RANTES on the transient increase of Ca ions induced by CCR5 The system which measures the can be implemented. The same way of thinking is possible by the binding of T cell-directed (X4) HIV and SDF-1 to CXCR4.
    [420] Experimental Method
    [421] (1) Isolation of the Human CCR5 Gene
    [422] Human placental cDNA was constructed using the Marathon cDNA amplification kit (Clontech). PCR primers hCCR5XbaI-F1: 5'-AGCTAGTCTAGATCCGTTCCCCTACAAGAAACTCTCC-3 '(SEQ ID NO: 1) and hCCR5XbaI-R': 5'-AGCTAGTCTAGAGTGCACAACTCTGACTGGGTCACCA-3 '(SEQ ID NO: 2) were designed based on the sequence of GenBank U54994.
    [423] Human placental cDNA was used as a template, and PCR reaction (2 min at 95 ° C. → [30 sec at 95 ° C., 45 sec at 60 ° C., 1 min at 72 ° C.] × 35 times) was performed using Ex Taq (Takara). It was. The amplified PCR product was subjected to 1% agarose gel electrophoresis, purified using QIAquick Gel Extraction Kit (QIAGEN), and digested with restriction enzyme XbaI. The cleaved fragment was linked to the expression vector pEF-BOS-bsr using DNA Ligation Kit Ver. 2 (Takara), and transformed into E. coli DH5a. This plasmid pEF-BOS-bsr / hCCR5 was prepared and DNA sequence was confirmed.
    [424] (2) CHO cell culture
    [425] CHO-dhfr (−) was cultured using Ham's F-12 (containing fetal bovine serum (10%), penicillin (50 U / ml), streptomycin (50 mg / ml)). In addition, transfected cells were cultured by adding blastodine (5 mg / ml) above.
    [426] (3) Transduction into CHO Cells
    [427] Plasmid pEF-BOS-bsr / hCCR5 was transfected into CHO-dhfr (−) cells using DMRIE-C reagent (Gibco BRL). After 48 hours, selection was made by exchanging with medium containing 5 mg / ml blastodine, to establish stable overexpressing cells.
    [428] (4) Inhibition experiment on the binding of RANTES and CCR5 (Ca ion transient induction activity of RANTES)
    [429] Established human CCR5 stable overexpressing CHO cells (CCR5 / CHO cells) were suspended in Ham's F-12 medium and FBS (10%) and allowed to be 3.0 × 10 6 cells / well in 96 well plates. After 1 day incubation at 37 ° C., the culture supernatant was removed and 80 μl / of Ham's F-12 medium (containing Fura-2 AM (5 μM), Probenecid (2.5 mM) and HEPES (20 mM; pH 7.4)). The well was added and incubated at 37 degreeC for 1 hour in the light shielding state. After washing twice with 1 × Hanks / HEPES (20 mM; pH 7.4) solution, 100 μl / well was added. For CCR5 / CHO cells receiving Fura-2 AM, the recombinant human RANTES (PeproTech) diluted with 1 × Hanks / HEPES (20 mM; pH 7.4) solution was added 3 minutes after the test compound was added. It was added at a concentration of 10 nM. The transient rise in intracellular Ca 2+ concentration induced by human RANTES was measured using a 96 well Ca 2+ detector (Hamamatsu Photonics), and the inhibition rate (%) of the test compound was calculated by the following formula.
    [430] Suppression rate = (Ec-Ea) / Ec × 100
    [431] Ec: Measurement of Ca 2+ transient elevation by RANTES
    [432] Ea: Measurement of Ca 2+ transient rise by RANTES when test compound was added.
    [433] As a result, the compound of the present invention showed more than 50% inhibition at 10 μM. For example, the compound of Example 2 (1) had an IC 50 value of 0.05 μM and the Compound of the Example 2 (2) had an IC 50 value of 0.05 μM.
    [434] Although the system which finds the compound which has an adsorption inhibitory effect with respect to CCR5-directed HIV strain was mentioned above, it is naturally possible to find the compound which suppresses the action of CCR5 or its ligand using this system. Likewise, it is possible to find compounds that inhibit the action of other chemokine receptors and their ligands. For example, CCR2 Alternatively, a system for finding a compound that inhibits the action of the ligand can be constructed. Since CCR2, like CCR5, is a G protein conjugated membrane transmembrane seven times, its ligand is present. For example, it can be carried out by measuring the effect of MCP-1 on the transient rise of Ca ions induced by CCR2.
    [435] (5) Inhibitory experiments on the binding of MCP-1 and CCR2 (Ca-1 transient induction activity of MCP-1)
    [436] Cells expressing human CCR2, such as human monocyte line THP-1 (ATCC No. TIB-202), were treated with FBS (10%), Fura2-AM (5 μM), Probenecid (2.5 mM) and HEPES (20 mM, pH 7.4). ) Was suspended in RPMI1640 medium containing 5.0 × 10 6 cells / ml and kept warm at 37 ° C. for 30 minutes in a shaded state. 4-8 times of 1 × Hanks / HEPES (20 mM, pH 7.4) / Probenecid (2.5 mM) was added and the mixture was further kept warm at 37 ° C. for 30 minutes. After washing the cells with 1 × Hanks / HEPES (20 mM, pH 7.4) / Probenecid (2.5 mM) solution, 2.0 × 10 6 cells / ml were resuspended with the same solution and 100 μl was added to a 96 well plate. After addition of the test compound solution, after 3 minutes, recombinant human MCP-1 (PeproTech) diluted with 1 × Hanks / HEPES (20 mM, pH 7.4) / Probenecid (2.5 mM) was added to a final concentration of 30 nM. Transient increase in intracellular Ca 2+ concentration induced by human MCP-1 was measured using a 96 well Ca 2+ detector (Hamamatsu Photonics), and the inhibition rate (%) of the test compound was calculated by the following formula. .
    [437] Suppression rate = (Ec-Ea) / Ec × 100
    [438] Ec: Measurement of Ca 2+ transient elevation by MCP-1
    [439] Ea: Measurement of Ca 2+ transient increase by MCP-1 when test compound was added.
    [440] As a result, the compound of the present invention showed more than 50% inhibition at 10 μM. For example, the compound of Example 5 (2) had an IC 50 value of 3 μΜ.
    [441] [toxicity]
    [442] The toxicity of the compounds of the present invention is very low and can be judged to be sufficiently safe for use as a medicament.
    [455] Hereinafter, although this invention is demonstrated in detail by reference example and an Example, this invention is not limited to these.
    [456] The solvent in the parenthesis indicated by the point of separation by chromatography and the TLC indicates the elution solvent or the developing solvent used, and the ratio indicates the volume ratio.
    [457] The solvent in parentheses shown in the NMR site represents the solvent used for the measurement.
    [458] R * and S * do not represent absolute positions, only relative positions.
    [459] Reference Example 1: Synthesis of Resin (2)
    [460]
    [461] Aminomethylpolystyrene resin hydrochloride (resin (1); X represents polystyrene resin) (30.0 g) (1% divinylbenzene copolymer, manufactured by Watanabe Kagaku Co., Catalog No. A00062) in dimethylformamide (300 ml ), 10% diisopropylethylamine-dimethylformamide solution (300 ml) and dimethylformamide (300 ml) were washed sequentially and suspended in dimethylformamide (200 ml). Formic acid (10.2 ml) and diisopropylcarbodiimide (42.3 ml) were added to the suspension under ice cooling, followed by stirring at room temperature for 1 hour. The resin was collected by filtration from the reaction solution, washed with dimethylformamide (250 ml × 3 times), dichloromethane (250 ml × 4 times), methanol (250 ml × 2 times) and dichloromethane (250 ml × 4 times). The resin (2) was obtained.
    [462] IR (KBr): ν 1682 cm -1 .
    [463] Reference Example 2: Synthesis of Resin (3)
    [464]
    [465] Triethylamine (18.8 ml), carbon tetrachloride (13.0 ml) and triphenylphosphine (35.4 g) were added to the dichloromethane (300 ml) suspension of Resin (2) obtained in Reference Example 1, and the mixture was heated to reflux for 1 hour. After cooling the reaction solution at room temperature, the resin was collected by filtration. The resin was washed with dichloromethane (250 ml x 3 times), methanol (250 ml x 1 time) and dichloromethane (250 ml x 2 times), and dried under reduced pressure to obtain Resin (3) (28.2 g).
    [466] IR (KBr): ν 2147 cm -1 .
    [467] Reference Example 3: Synthesis of Compound (1)
    [468]
    [469] N-allyloxycarbonyl-4-piperidone (2.15 g), n-propyl in a suspension of tetrahydrofuran / methanol (1: 1; 25 ml) of Resin (3) (2.5 g) prepared in Reference Example 2 Amine (0.97 ml) and N- (t-butyloxycarbonyl) leucine (2.93 g) were added and stirred at 65 ° C. for 16 hours. The reaction solution was cooled at room temperature and the resin was taken by filtration. The obtained resin was washed with tetrahydrofuran (25 ml 2 times), methanol (25 ml 2 times) and dichloromethane (25 ml 2 times) to obtain compound (1).
    [470] Reference Example 4: Synthesis of Compound (2)
    [471]
    [472] To a dichloromethane (25 ml) suspension of compound (1) prepared in Reference Example 3 was added acetic acid (0.81 ml), tributyltin hydride (1.90 ml) and tetrakistriphenylphosphinepalladium (0) complex (270 mg). It was added and stirred at room temperature for 6 hours. The resin was collected by filtration from the reaction solution and washed with dichloromethane (25 ml × 3 times), methanol (25 ml × 2 times), dichloromethane (25 ml × 2 times) and dimethylformamide (25 ml × 3 times). Compound (2) was obtained.
    [473] Reference Example 5: Synthesis of Compound (3)
    [474]
    [475] To a dimethylformamide (25 ml) suspension of compound (2) prepared in Reference Example 4, 3,5-dimethyl-1-phenyl-4-formylpyrazole (1.41 g) and sodium triacetoxyborohydride (1.50 g) And acetic acid (0.2 ml) were added and stirred at room temperature for 16 hours. The resin was collected by filtration from the reaction solution and washed with dimethylformamide (20 ml × 2 times), dichloromethane (20 ml × 2 times), methanol (20 ml × 2 times) and dichloromethane (20 ml × 4 times). Compound (3) was obtained.
    [476] Reference Example 6: Synthesis of Compound (4)
    [477]
    [478] Compound (3) prepared in Reference Example 5 was suspended in a 50% trifluoroacetic acid-dichloromethane (25 ml) solution and stirred at room temperature for 5 minutes. The resin obtained by filtering the reaction solution was again suspended in 50% trifluoroacetic acid-dichloromethane solution (25 ml) and stirred at room temperature for 30 minutes. The resin taken out by filtration from the reaction solution was washed with dichloromethane (25 ml x 4 times), toluene (25 ml x 4 times) and 1.25 M acetate-toluene solution (25 ml x 1 times) to obtain compound (4).
    [479] Reference Example 7: Synthesis of Resin (5)
    [480]
    [481] 9-Fluorenylmethyloxycarbonylamino-Rink resin (resin (4)) (5.0 g) (1% divinylbenzene copolymer, manufactured by Watanabe Kagaku Co., Catalog No. AO0102) in dimethylformamide (50 ml 3 ×), 20% piperidine-dimethylformamide solution (50 ml × 2 times). The washed resin was suspended in 20% piperidine-dimethylformamide solution (50 ml) and stirred at room temperature for 30 minutes. The reaction solution was filtered, and the obtained resin was washed with dimethylformamide (50 ml × 5 times). Ethyl formate (30 ml) was added to a suspension of dimethylformamide (20 ml) of the washed resin, and the mixture was heated to reflux for 6 hours. After cooling at room temperature, the reaction solution was filtered. The filtered resin was washed with dimethylformamide (50 ml × 2 times), dichloromethane (50 ml × 4 times), methanol (50 ml × 4 times) and dichloromethane (50 ml × 4 times), and dried under reduced pressure. The resin (5) (4.34 g) was obtained.
    [482] IR (KBr): ν 1693 cm −1 .
    [483] Reference Example 8: Synthesis of Resin (6)
    [484]
    [485] Resin (6) (3.56 g) was obtained in the same manner as in Reference Example 2 using Resin (4) (4.0 g) prepared in Reference Example 7.
    [486] IR (KBr): ν 2136 cm -1 .
    [487] Reference Example 9: Synthesis of Compound (5)
    [488]
    [489] Resin (6) (1.0 g), N- (6-phenylhexyl) -4-piperidone (0.44 g), n-propylamine (0.14 ml) and N- (t-butyloxycarb) prepared in Reference Example 8 Compound (5) was obtained in the same manner as the Reference Example 3 using carbonyl) -L-leucine (0.42 g).
    [490] Reference Example 10 Synthesis of Compound (6)
    [491]
    [492] To a 1.5 M 2,6-lutidine-dichloromethane (4 ml) suspension of compound (5) prepared in Reference Example 9 was added 1 M trifluoromethanesulfonic acid trimethylsilyl-dichloromethane solution (4 ml) and Stir for 30 minutes. The reaction solution was filtered, and the obtained resin was again suspended in 1.5 M 2,6-lutidine-dichloromethane solution (4 ml), and 1 M trifluoromethanesulfonic acid trimethylsilyl-dichloromethane solution (4 ml) was added. And stirred at room temperature for 30 minutes. The resin was collected by filtration from the reaction solution, and washed with dichloromethane (6 ml x 4 times), methanol (6 ml x 4 times) and toluene (6 ml x 5 times) to obtain compound (6).
    [493] Example 1
    [494] 9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1-propyl-1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [495]
    [496] Compound (4) prepared in Reference Example 6 was suspended in 1.25 M acetic acid-toluene solution (25 ml) and stirred at 90 ° C. for 24 hours and then at room temperature for 16 hours. The reaction solution was filtered, and the resulting resin was washed with chloroform-methanol (1: 1; 20 ml × 2 times). The filtrate and washings were concentrated. The residue was purified by silica gel column chromatography (manufactured by Fuji-Silica Kagaku Co., FL60D; chloroform: methanol = 30: 1). The methanol solution of the obtained residue was made acidic with 1N hydrochloric acid, and then concentrated to give the title compound (703 mg) having the following physical properties.
    [497] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [498] NMR (CD 3 OD): δ 7.68-7.50 (m, 5H), 4.36 (s, 2H), 4.03 (dd, J = 7.8, 5.2 Hz, 1H), 3.83 (m, 2H), 3.64 (m, 2H ), 3.47 (m, 2H), 2.64 (m, 2H), 2.49 (s, 3H), 2.44 (s, 3H), 2.20 (m, 2H), 1.81 (m, 1H), 1.68 (m, 2H) , 1.60 (m, 2 H), 1.05-0.90 (m, 9 H);
    [499] IR (KBr): ν 3424, 3215, 2960, 2873, 2492, 1671, 1645, 1554, 1501, 1468, 1418, 1370, 1330, 1297, 1243, 1148, 958, 928, 754, 698 cm −1 ;
    [500] MS (MALDI, Pos., Α-CHCA): 488 (M + Na) + , 466 (M + H) + , 185.
    [501] Elemental analysis: calculated (C 27 H 39 N 5 O 2 .2HCl) C: 60.22%, H: 7.67%, N: 13.00%.
    [502] Found C: 59.89%, H: 7.67%, N: 12.79%.
    [503] Example 2 (1)-2 (3)
    [504] Using Resin (3) and N-allyloxycarbonyl-4-piperidone prepared in Reference Example 2, instead of n-propylamine and N- (t-butyloxycarbonyl) leucine, the corresponding compounds were used. Reference Example 3-the same operation as Reference Example 4, and using the compound corresponding to instead of 3,5-dimethyl-1-phenyl-4-formylpyrazole, Reference Example 5 → Reference Example 6 → Example 1 and The same operation was carried out to obtain the following compound of the present invention.
    [505] Example 2 (1)
    [506] 9- (1,4-benzodioxane-6-ylmethyl) -1-butyl-3-cyclohexylmethyl-2,5-dioxo-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [507]
    [508] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [509] NMR (CD 3 OD): δ 7.08 (d, J = 2.2 Hz, 1H), 6.99 (dd, J = 8.0, 2.2 Hz, 1H), 6.92 (d, J = 8.0 Hz, 1H), 4.27 (s, 4H), 4.23 (s, 2H), 4.04 (dd, J = 7.6, 4.8 Hz, 1H), 3.74 (m, 2H), 3.60-3.35 (m, 4H), 2.43 (m, 2H), 2.15 (m , 2H), 1.90-1.60 (m, 7H), 1.60-1.45 (m, 2H), 1.45-1.30 (m, 2H), 1.30-1.10 (m, 4H), 1.10-0.80 (m, 5H);
    [510] IR (KBr): ν 3436, 2926, 2852, 2511, 1675, 1645, 1591, 1511, 1418, 1374, 1294, 1261, 1068, 1050, 930, 888 cm −1 ;
    [511] MS (MALDI, Pos., Α-CHCA): 484 (M + H) + , 149.
    [512] Elemental analysis: calculated (C 28 H 41 N 3 O 4 HCl) C: 64.66%, H: 8.14%, N: 8.08%.
    [513] Found C: 64.00%, H: 7.94%, N: 7.90%.
    [514] Example 2 (2)
    [515] 1-Butyl-3-cyclohexylmethyl-2,5-dioxo-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [516]
    [517] TLC: Rf 0.25 (chloroform: methanol = 10: 1);
    [518] NMR (CD 3 OD): δ 8.05-7.94 (m, 3H), 7.75-7.60 (m, 3H), 4.59 (s, 2H), 4.05 (dd, J = 7.4, 4.8 Hz, 1H), 3.88 (m , 2H), 3.65 (m, 2H), 3.51 (m, 2H), 2.68 (m, 2H), 2.19 (m, 2H), 1.90-1.60 (m, 6H), 1.60-1.45 (m, 3H), 1.45-1.30 (m, 3H), 1.30-1.10 (m, 3H), 1.10-0.80 (m, 5H);
    [519] IR (KBr): ν 3423, 2927, 2854, 2664, 1672, 1644, 1421, 1373, 1177, 775, 709, 688 cm −1 ;
    [520] MS (MALDI, Pos., Α-CHCA): 492 (M + H) + .
    [521] Elemental analysis: calculated (C 29 H 41 N 5 O 2 .2HCl.2.8H 2 O) C: 56.63%, H: 7.96%, N: 11.39%.
    [522] Found C: 56.90%, H: 7.23%, N: 10.78%.
    [523] Example 2 (3)
    [524] 1-butyl-3- (2-methyl-1-propyl) -2,5-dioxo-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [525]
    [526] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [527] NMR (CD 3 OD): δ 7.54 (d, J = 8.8 Hz, 2H), 7.40 (m, 2H), 7.18 (m, 1H), 7.11-7.00 (m, 4H), 4.33 (s, 2H), 4.01 (dd, J = 7.6, 4.8 Hz, 1H), 3.80 (m, 2H), 3.60-3.35 (m, 4H), 2.46 (m, 2H), 2.18 (m, 2H), 1.80 (m, 1H) , 1.70 (m, 1 H), 1.54 (m, 2 H), 1.37 (m, 3 H), 1.00-0.90 (m, 9H);
    [528] IR (KBr): ν 3440, 3221, 3066, 2957, 2871, 2559, 1673, 1590, 1509, 1489, 1419, 1371, 1329, 1242, 1172, 873, 693 cm −1 ;
    [529] MS (MALDI, Pos., Α-CHCA): 478 (M + H) + , 183.
    [530] Elemental analysis: calculated (C 29 H 39 N 3 O 3 .HCl) C: 67.75%, H: 7.84%, N: 8.17%.
    [531] Found C: 67.29%, H: 7.70%, N: 8.06%.
    [532] Example 2 (4)
    [533] (3S) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1-propyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [534]
    [535] The title compound (69 mg) having the following physical properties was obtained in the same manner as in Example 1 using compound (6) prepared in Reference Example 10.
    [536] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [537] NMR (CD 3 OD): δ 7.18 (m, 5H), 4.02 (dd, J = 7.6, 4.8 Hz, 1H), 3.70 (m, 2H), 3.56 (m, 2H), 3.39 (m, 2H), 3.11 (m, 2H), 2.63 (dd, J = 7.8, 7.2 Hz, 2H), 2.48 (m, 2H), 2.17 (m, 2H), 1.95-1.50 (m, 9H), 1.42 (m, 4H) , 1.00-0.89 (m, 9 H);
    [538] IR (KBr): ν 3435, 3205, 3082, 3026, 2935, 2870, 2493, 2361, 1674, 1454, 1417, 1370, 1331, 1155, 1071, 1004, 961, 750, 700 cm −1 ;
    [539] MS (FAB, Pos., Glycerin-m-nitrobenzyl alcohol): 442 (M + H) + , 232, 171, 79 (reference peak).
    [540] Elemental analysis: calculated (C 27 H 43 N 3 O 2 HCl) C: 67.83%, H: 9.28%, N: 8.79%.
    [541] Found C: 67.56%, H: 9.50%, N: 8.71%.
    [542] Example 2 (5)
    [543] (3R) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1-propyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [544]
    [545] Resin (6) (1.0 g), N- (6-phenylhexyl) -4-piperidone (0.44 g), n-propylamine (0.14 ml) and N- (t-butyloxycarb) prepared in Reference Example 8 The title compound (63 mg) having the following physical properties was obtained in the same manner as the Reference Example 9-Reference Example 10-Example 1 using carbonyl) -D-leucine (0.42 g).
    [546] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [547] NMR (CD 3 OD): δ 7.18 (m, 5H), 4.02 (dd, J = 7.6, 4.6 Hz, 1H), 3.70 (m, 2H), 3.56 (m, 2H), 3.39 (m, 2H), 3.11 (m, 2H), 2.63 (dd, J = 7.8, 7.2 Hz, 2H), 2.48 (m, 2H), 2.17 (m, 2H), 1.95-1.50 (m, 9H), 1.42 (m, 4H) , 1.00-0.89 (m, 9 H);
    [548] IR (KBr): ν 3441, 3204, 3082, 3026, 2935, 2870, 2660, 2499, 2413, 2361, 1674, 1455, 1417, 1370, 1330, 1267, 1205, 1154, 1070, 1003, 960, 928, 899, 750, 700 cm −1 ;
    [549] MS (FAB, Pos., Glycerin-m-nitrobenzyl alcohol): 442 (M + H) + (reference peak), 294, 232, 202, 171, 79.
    [550] Elemental analysis: calculated (C 27 H 43 N 3 O 2 HCl) C: 67.83%, H: 9.28%, N: 8.79%.
    [551] Found C: 67.52%, H: 9.51%, N: 8.70%.
    [552] Reference Example 3 (1) to 3 (4)
    [553] Using Resin (3) and N-allyloxycarbonyl-4-piperidone prepared in Reference Example 2, instead of n-propylamine and N- (t-butyloxycarbonyl) leucine, the corresponding compounds were used. Reference Example 3-the same operation as Reference Example 4, and using the compound corresponding to instead of 3,5-dimethyl-1-phenyl-4-formylpyrazole, Reference Example 5-Reference Example 6-same as Example 1 The operation was carried out to obtain the following compound of the present invention.
    [554] Example 3 (1)
    [555] 1-butyl-9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [556]
    [557] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [558] NMR (CD 3 OD): δ 7.70-7.48 (m, 5H), 4.35 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.83 (m, 2H), 3.63 (m, 2H ), 3.51 (m, 2H), 2.64 (m, 2H), 2.48 (s, 3H), 2.43 (s, 3H), 2.20 (m, 2H), 1.81 (m, 2H), 1.71 (m, 2H) , 1.55 (m, 2H), 1.50-1.35 (m, 4H), 1.05-0.90 (m, 6H).
    [559] Example 3 (2)
    [560] 1-butyl-3-cyclohexylmethyl-2,5-dioxo-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [561]
    [562] TLC: Rf 0.73 (CHCl 3: MeOH = 10: 1);
    [563] NMR (CD 3 OD): δ 7.74-7.56 (m, 1H), 7.53 (d, J = 8.8 Hz, 2H), 7.40 (m, 2H), 7.18 (m, 1H), 7.10-7.00 (m, 3H ), 4.33 (s, 2H), 4.04 (dd, J = 7.4, 4.8 Hz, 1H), 3.80 (m, 2H), 3.60-3.35 (m, 4H), 2.43 (m, 2H), 2.17 (m, 2H), 1.90-1.60 (m, 7H), 1.60-1.45 (m, 2H), 1.45-1.30 (m, 2H), 1.30-1.15 (m, 4H), 1.10-0.80 (m, 5H).
    [564] Example 3 (3)
    [565] 9- (1,4-benzodioxane-6-ylmethyl) -1-butyl-3- (2-methyl-1-propyl) -2,5-dioxo-1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [566]
    [567] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [568] NMR (CD 3 OD): δ 7.08 (d, J = 2.2 Hz, 1H), 7.01 (dd, J = 8.2, 2.2 Hz, 1H), 6.93 (d, J = 8.2 Hz, 1H), 4.27 (s, 4H), 4.23 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.72 (m, 2H), 3.55-3.35 (m, 4H), 2.43 (m, 2H), 2.16 (m , 2H), 1.80 (m, 1H), 1.67 (m, 2H), 1.55 (m, 2H), 1.37 (m, 2H), 1.00-0.90 (m, 9H).
    [569] Example 3 (4)
    [570] 9- (4-benzyloxyphenylmethyl) -1-butyl-2,5-dioxo-3- (2-methyl-1-propyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [571]
    [572] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [573] NMR (CD 3 OD): δ 7.54-7.25 (m, 7H), 7.10 (m, 2H), 5.13 (s, 2H), 4.27 (s, 2H), 4.00 (dd, J = 8.2, 4.8 Hz, 1H ), 3.72 (m, 2H), 3.55-3.35 (m, 4H), 2.42 (m, 2H), 2.16 (m, 2H), 1.90-1.25 (m, 7H), 1.00-0.90 (m, 9H).
    [574] Example 4
    [575] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [576]
    [577] Reference Example 3 → Reference Example Using Resin (3), N- (6-phenylhexyl) -4-piperidone, n-butylamine and N- (t-butyloxycarbonyl) leucine prepared in Reference Example 2 6 → The same operation as in Example 1 was carried out to obtain a compound of the present invention having the following physical properties.
    [578] TLC: Rf 0.62 (CHCl 3: MeOH = 10: 1);
    [579] NMR (CD 3 OD): δ 7.30-7.06 (m, 5H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.70 (m, 2H), 3.56 (m, 2H), 3.43 (m, 2H ), 3.11 (m, 2H), 2.63 (t, J = 7.8 Hz, 2H), 2.46 (m, 2H), 2.18 (m, 2H), 1.95-1.50 (m, 9H), 1.50-1.25 (m, 6H), 0.97 (m, 9H).
    [580] Example 5 (1)-5 (12)
    [581] Resin (6) prepared in Reference Example 8 with the corresponding compounds in place of N- (6-phenylhexyl) -4-piperidone, n-propylamine and N- (t-butyloxycarbonyl) -L-leucine, respectively The following compounds of the present invention were obtained in the same manner as in Reference Example 9-Reference Example 10-Example 1.
    [582] Example 5 (1)
    [583] (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4, 9-triazaspiro [5.5] undecane hydrochloride
    [584]
    [585] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [586] NMR (CD 3 OD): δ 7.33 (m, 10H), 5.07 (s, 2H), 4.12 (m, 1H), 3.94 (m, 1H), 3.61 (m, 5H), 3.39 (m, 2H), 3.13 (m, 4H), 2.31 (m, 4H), 1.92 (m, 3H), 1.51 (m, 2H), 1.39 (m, 2H), 0.93 (t, J = 6.4 Hz, 6H).
    [587] Example 5 (2)
    [588] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [589]
    [590] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [591] NMR (CD 3 OD): δ 7.33 (m, 10H), 5.06 (m, 2H), 4.07 (m, 1H), 3.86 (m, 1H), 3.76 (m, 1H), 3.63 (m, 2H), 3.37 (m, 4H), 3.12 (m, 4H), 2.43 (m, 2H), 2.21 (m, 2H), 1.86 (m, 2H), 1.55 (m, 4H), 1.37 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [592] Example 5 (3)
    [593] (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [594]
    [595] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [596] NMR (CD 3 OD): δ 7.33 (m, 10H), 5.06 (s, 2H), 4.07 (m, 1H), 3.86 (m, 1H), 3.76 (m, 1H), 3.63 (m, 2H), 3.37 (m, 4H), 3.12 (m, 4H), 2.43 (m, 2H), 2.21 (m, 2H), 1.86 (m, 2H), 1.55 (m, 4H), 1.37 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [597] Example 5 (4)
    [598] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [599]
    [600] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [601] NMR (CD 3 OD): δ 7.33 (m, 5H), 7.26 (m, 5H), 5.05 (s, 2H), 4.05 (m, 1H), 3.85-3.30 (m, 6H), 3.12 (m, 4H ), 2.73 (t, J = 7.6 Hz, 2H), 2.44 (m, 2H), 2.13 (m, 4H), 1.85 (m, 2H), 1.54 (m, 4H), 1.38 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [602] Example 5 (5)
    [603] (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [604]
    [605] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [606] NMR (CD 3 OD): δ 7.33 (m, 5H), 7.26 (m, 5H), 5.05 (s, 2H), 4.05 (m, 1H), 3.85-3.30 (m, 6H), 3.12 (m, 4H ), 2.73 (t, J = 7.2 Hz, 2H), 2.44 (m, 2H), 2.13 (m, 4H), 1.85 (m, 2H), 1.54 (m, 4H), 1.38 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [607] Example 5 (6)
    [608] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [609]
    [610] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [611] NMR (CD 3 OD): δ 7.33 (m, 5H), 7.22 (m, 5H), 5.06 (s, 2H), 4.05 (m, 1H), 3.85-3.38 (m, 6H), 3.12 (m, 4H ), 2.70 (m, 2H), 2.40 (m, 2H), 2.18 (m, 2H), 1.74 (m, 6H), 1.54 (m, 4H), 1.38 (m, 2H), 0.94 (t, J = 7.0 Hz, 3H).
    [612] Example 5 (7)
    [613] (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [614]
    [615] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [616] NMR (CD 3 OD): δ 7.33 (m, 5H), 7.22 (m, 5H), 5.06 (s, 2H), 4.05 (m, 1H), 3.85-3.38 (m, 6H), 3.12 (m, 4H ), 2.70 (m, 2H), 2.40 (m, 2H), 2.18 (m, 2H), 1.74 (m, 6H), 1.54 (m, 4H), 1.38 (m, 2H), 0.94 (t, J = 7.0 Hz, 3H).
    [617] Example 5 (8)
    [618] (3S) -1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [619]
    [620] TLC: Rf 0.57 (CHCl 3: MeOH = 10: 1);
    [621] NMR (CD 3 OD): δ 7.48 (m, 5H), 7.23 (m, 5H), 4.82 (m, 2H), 4.31 (s, 2H), 4.17 (dd, J = 8.0, 4.6 Hz, 1H), 3.72 (m, 2H), 3.40 (m, 2H), 2.52 (m, 2H), 2.08 (m, 2H), 2.00-1.60 (m, 3H), 0.98 (d, J = 6.0 Hz, 6H).
    [622] Example 5 (9)
    [623] (3R) -1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [624]
    [625] TLC: Rf 0.57 (CHCl 3: MeOH = 10: 1);
    [626] NMR (CD 3 OD): δ 7.48 (m, 5H), 7.23 (m, 5H), 4.82 (m, 2H), 4.31 (s, 2H), 4.17 (dd, J = 8.0, 4.6 Hz, 1H), 3.72 (m, 2H), 3.40 (m, 2H), 2.52 (m, 2H), 2.08 (m, 2H), 2.00-1.60 (m, 3H), 0.98 (d, J = 6.0 Hz, 6H).
    [627] Example 5 (10)
    [628] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2- (2-phenyl-5-methyloxazole-4- I) ethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [629]
    [630] TLC: Rf 0.45 (CHCl 3: MeOH = 10: 1);
    [631] NMR (CD 3 OD): δ 8.01 (m, 2H), 7.53 (m, 3H), 7.34 (m, 5H), 5.07 (s, 2H), 4.08 (dd, J = 5.4, 4.4 Hz, 1H), 4.00-3.60 (m, 4H), 3.47 (m, 4H), 3.13 (m, 4H), 2.56 (m, 2H), 2.46 (s, 3H), 2.25 (m, 2H), 1.87 (m, 2H) , 1.75-1.25 (m, 6H), 0.94 (t, J = 7.2 Hz, 3H).
    [632] Example 5 (11)
    [633] (3S) -1-propyl-2,5-dioxo-3- (4- (N- (2-chlorophenylmethyl) oxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] undecane hydrochloride
    [634]
    [635] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [636] NMR (CD 3 OD): δ 7.33 (m, 9H), 5.17 (s, 2H), 4.08 (dd, J = 5.2, 4.8 Hz, 1H), 3.80 (m, 2H), 3.65 (m, 3H), 3.39 (m, 3H), 3.14 (m, 4H), 2.50 (m, 2H), 2.22 (m, 2H), 1.85 (m, 2H), 1.70-1.20 (m, 6H), 0.95 (t, J = 7.2 Hz, 3H).
    [637] Example 5 (12)
    [638] (3S) -1-propyl-2,5-dioxo-3- [3- (3- (2 (4,6-trimethylphenylsulfonyl) guanidino) propyl] -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [639]
    [640] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [641] NMR (CD 3 OD): δ 7.32 (m, 5H), 7.05 (s, 2H), 4.10 (m, 1H), 3.88 (m, 1H), 3.67 (m, 3H), 3.40 (m, 4H), 3.18 (m, 4H), 2.66 (s, 6H), 2.51 (m, 2H), 2.31 (s, 3H), 2.21 (m, 2H), 1.82 (m, 2H), 1.60 (m, 4H), 0.96 (t, J = 7.2 Hz, 3H).
    [642] Example 6 (1)-6 (32)
    [643] The same procedure as in Reference Example 3-Reference Example 4 was performed using the resin (3) prepared in Reference Example 2, N-allyloxycarbonyl-4-piperidone, the corresponding amine derivative, and the corresponding amino acid derivative. The following compounds of the present invention were obtained in the same manner as in Reference Example 5-Reference Example 6-Example 1 using an aldehyde derivative.
    [644] Example 6 (1)
    [645] 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [646]
    [647] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [648] NMR (CD 3 OD): δ 7.55 (m, 2H), 7.40 (m, 2H), 7.18 (m, 1H), 7.05 (m, 4H), 4.33 (s, 2H), 4.01 (dd, J = 7.6 , 4.8 Hz, 1H), 3.79 (m, 2H), 3.60-3.30 (m, 4H), 2.46 (m, 2H), 2.17 (m, 2H), 1.95-1.40 (m, 5H), 0.94 (m, 9H).
    [649] Example 6 (2)
    [650] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [651]
    [652] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [653] NMR (CD 3 OD): δ 7.47 (d, J = 8.8 Hz, 2H), 7.03 (d, J = 8.8 Hz, 2H), 4.29 (s, 2H), 4.04 (dd, J = 7.6, 4.8 Hz, 1H), 3.83 (s, 3H), 3.74 (m, 2H), 3.55-3.35 (m, 4H), 2.41 (m, 2H), 2.15 (m, 2H), 1.85-1.55 (m, 7H), 1.55 -1.42 (m, 3H), 1.42-1.30 (m, 3H), 1.30-1.10 (m, 2H), 1.08-0.80 (m, 5H).
    [654] Example 6 (3)
    [655] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-allyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [656]
    [657] TLC: Rf 0.57 (CHCl 3: MeOH = 10: 1);
    [658] NMR (CD 3 OD): δ 7.46 (d, J = 8.4 Hz, 2H), 7.04 (d, J = 8.4 Hz, 2H), 6.06 (m, 1H), 5.41 (m, 1H), 5.28 (m, 2H), 4.59 (m, 2H), 4.28 (s, 2H), 4.04 (dd, J = 7.2, 4.8 Hz, 1H), 3.77 (m, 2H), 3.55-3.35 (m, 4H), 2.39 (m , 2H), 2.16 (m, 2H), 1.90-1.60 (m, 7H), 1.60-1.45 (m, 2H), 1.45-1.30 (m, 2H), 1.30-1.10 (m, 3H), 1.10-0.80 (m, 5 H).
    [659] Example 6 (4)
    [660] (3S) -1-propyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [661]
    [662] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [663] NMR (CD 3 OD): δ 7.65-7.45 (m, 5H), 4.33 (s, 2H), 4.03 (dd, J = 7.8, 5.2 Hz, 1H), 3.85 (m, 2H), 3.62 (m, 2H ), 3.44 (m, 2H), 2.59 (m, 2H), 2.43 (s, 3H), 2.41 (s, 3H), 2.20 (m, 2H), 1.81 (m, 1H), 1.71 (m, 2H) , 1.64 (m, 2 H), 1.00-0.90 (m, 9H).
    [664] Example 6 (5)
    [665] (3R) -1-propyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [666]
    [667] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [668] NMR (CD 3 OD): δ 7.65-7.45 (m, 5H), 4.33 (s, 2H), 4.03 (dd, J = 7.8, 5.2 Hz, 1H), 3.85 (m, 2H), 3.62 (m, 2H ), 3.44 (m, 2H), 2.59 (m, 2H), 2.43 (s, 3H), 2.41 (s, 3H), 2.20 (m, 2H), 1.81 (m, 1H), 1.71 (m, 2H) , 1.64 (m, 2 H), 1.00-0.90 (m, 9H).
    [669] Example 6 (6)
    [670] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9-phenylmethyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [671]
    [672] TLC: Rf 0.54 (CHCl 3: MeOH = 10: 1);
    [673] NMR (CD 3 OD): δ 7.64-7.44 (m, 5H), 4.36 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.77 (m, 2H), 3.55-3.35 (m , 4H), 2.60-2.30 (m, 2H), 2.17 (m, 2H), 1.95-1.75 (m, 1H), 1.75-1.60 (m, 2H), 1.60-1.45 (m, 2H), 1.45-1.20 (m, 2 H), 1.10-0.80 (m, 9 H).
    [674] Example 6 (7)
    [675] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [676]
    [677] TLC: Rf 0.41 (CHCl 3: MeOH = 20: 1);
    [678] NMR (CDCl 3 ): δ 7.45-7.28 (m, 5H), 6.31 (m, 1H), 5.15 (s, 2H), 4.14 (m, 2H), 3.96 (m, 1H), 3.63 (m, 1H) , 3.44 (m, 1 H), 3.26 (m, 2 H), 1.99-1.14 (m, 11 H), 1.02-0.88 (m, 9H).
    [679] Example 6 (8)
    [680] 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [681]
    [682] TLC: Rf 0.46 (CHCl 3: MeOH = 20: 1);
    [683] NMR (CDCl 3 ): δ 7.40-7.29 (m, 5H), 5.98 (m, 1H), 5.15 (s, 2H), 4.14 (m, 2H), 4.00 (m, 1H), 3.65 (m, 1H) , 3.43 (m, 1H), 3.26 (m, 2H), 2.03-1.81 (m, 4H), 1.80-1.60 (m, 5H), 1.60-1.10 (m, 10H), 1.10-0.85 (m, 5H) .
    [684] Example 6 (9)
    [685] 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [686]
    [687] TLC: Rf 0.66 (CHCl 3: MeOH = 10: 1);
    [688] NMR (CD 3 OD): δ 7.50 (d, J = 8.4 Hz, 2H), 7.45-7.12 (m, 8H), 7.10-6.98 (m, 4H), 4.82 (m, 2H), 4.29 (s, 2H ), 4.18 (dd, J = 8.0, 4.6 Hz, 1H), 3.73 (m, 2H), 3.42 (m, 2H), 2.65-2.30 (m, 2H), 2.20-2.05 (m, 2H), 2.00- 1.60 (m, 3H), 0.98 (d, J = 6.2 Hz, 6H).
    [689] Example 6 (10)
    [690] 1-butyl-2,5-dioxo-3-propyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [691]
    [692] TLC: Rf 0.36 (CHCl 3: MeOH = 10: 1);
    [693] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 ( m, 4H), 4.33 (s, 2H), 4.04 (dd, J = 5.7, 4.5 Hz, 1H), 3.93-3.66 (m, 2H), 3.55-3.31 (m, 4H), 2.47-2.09 (m, 4H), 1.92-1.68 (m, 2H), 1.61-1.21 (m, 6H), 1.01-0.90 (m, 6H).
    [694] Example 6 (11)
    [695] 1-butyl-2,5-dioxo-3-methoxymethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [696]
    [697] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [698] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.2 Hz, 2H), 7.17 (t, J = 7.2 Hz, 1H), 7.09-6.99 ( m, 4H), 4.30 (s, 2H), 4.07 (t, J = 3.0 Hz, 1H), 3.91 (m, 1H), 3.77 (dd, J = 9.0, 3.0 Hz, 1H), 3.67 (m, 1H ), 3.58-3.39 (m, 4H), 3.31 (s, 3H), 3.26 (m, 1H), 2.48-2.13 (m, 4H), 1.65 (m, 1H), 1.53-1.28 (m, 3H), 0.95 (t, J = 7.5 Hz, 3H).
    [699] Example 6 (12)
    [700] 1- (1-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [701]
    [702] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [703] NMR (CD 3 OD): δ 7.46 (d, J = 8.4 Hz, 2H), 7.38 (dd, J = 8.4, 7.5 Hz, 2H), 7.16 (t, J = 7.5 Hz, 1H), 7.08-6.99 ( m, 4H), 4.15 (s, 2H), 3.91-3.82 (m, 1H), 3.81-3.65 (m, 1H), 3.64-3.44 (m, 1H), 3.44-3.15 (m, 3H), 2.42- 2.00 (m, 4H), 1.88-1.56 (m, 5H), 1.46-1.37 (m, 3H), 0.99-0.85 (m, 9H).
    [704] Example 6 (13)
    [705] 1- (2-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [706]
    [707] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [708] NMR (CD 3 OD): δ 7.49 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.2 Hz, 2H), 7.17 (t, J = 7.2 Hz, 1H), 7.08-6.94 ( m, 4H), 4.27 (s, 2H), 4.04 (dd, J = 8.4, 4.5 Hz, 1H), 3.83-3.21 (m, 6H), 2.45-2.12 (m, 4H), 1.92-1.56 (m, 4H), 1.42 (m, 1H), 1.14 (m, 1H), 1.00-0.83 (m, 12H).
    [709] Example 6 (14)
    [710] 1- (2-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [711]
    [712] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [713] NMR (CD 3 OD): δ 7.50 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.13-7.04 ( m, 4H), 4.28 (s, 2H), 4.04 (dd, J = 8.1, 4.2 Hz, 1H), 3.81-3.54 (m, 2H), 3.52-3.21 (m, 4H), 2.46-2.11 (m, 4H), 2.00-1.57 (m, 4H), 0.94 (d, J = 6.3 Hz, 6H), 0.90 (d, J = 6.3 Hz, 3H), 0.90 (d, J = 6.3 Hz, 3H).
    [714] Example 6 (15)
    [715] 1- (2-dimethylaminoethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Khan dihydrochloride
    [716]
    [717] TLC: Rf 0.87 (CHCl 3: MeOH: 28% Ammonia water = 80: 10: 1);
    [718] NMR (CD 3 OD): δ 7.60 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.07-6.99 ( m, 4H), 4.33 (s, 2H), 4.07 (dd, J = 8.4, 4.8 Hz, 1H), 3.99-3.63 (m, 4H), 3.53-3.42 (m, 2H), 3.32-3.21 (m, 2H), 2.99 (s, 3H), 2.96 (s, 3H), 2.70-2.49 (m, 2H), 2.30-2.10 (m, 2H), 1.93-1.56 (m, 3H), 0.94 (d, J = 6.6 Hz, 6H).
    [719] Example 6 (16)
    [720] 1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [721]
    [722] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [723] NMR (CD 3 OD): δ 7.47 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.09-6.99 ( m, 4H), 4.25 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.75-3.34 (m, 8H), 3.31 (s, 3H), 2.48-2.28 (m, 2H) , 2.25-2.06 (m, 2H), 1.90-1.57 (m, 3H), 0.94 (d, J = 6.3 Hz, 3H), 0.93 (d, J = 6.3 Hz, 3H).
    [724] Example 6 (17)
    [725] 1- (2-methylthioethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [726]
    [727] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [728] NMR (CD 3 OD): δ 7.48 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.8 Hz, 2H), 7.17 (t, J = 7.8 Hz, 1H), 7.08-6.99 ( m, 4H), 4.25 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.81-3.49 (m, 4H), 3.48-3.33 (m, 2H), 2.74-2.51 (m, 2H), 2.39-2.10 (m, 7H), 1.90-1.56 (m, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [729] Example 6 (18)
    [730] 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [731]
    [732] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [733] NMR (CD 3 OD): δ 7.40-7.15 (m, 5H), 7.03 (d, J = 2.0 Hz, 1H), 6.96 (dd, J = 8.2, 2.0 Hz, 1H), 6.90 (d, J = 8.2 Hz, 1H), 4.80 (m, 2H), 4.25 (s, 4H), 4.21-4.10 (m, 3H), 3.80-3.55 (m, 2H), 3.50-3.30 (m, 2H), 2.60-2.25 ( m, 2H), 2.20-2.00 (m, 2H), 2.00-1.60 (m, 3H), 0.98 (d, J = 6.4 Hz, 6H).
    [734] Example 6 (19)
    [735] 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [736]
    [737] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [738] NMR (CD 3 OD): δ 7.50-7.15 (m, 12H), 7.07 (d, J = 8.8 Hz, 2H), 5.12 (s, 2H), 4.81 (m, 2H), 4.24 (s, 2H), 4.17 (dd, J = 8.4, 4.8 Hz, 1H), 3.70-3.55 (m, 2H), 3.50-3.35 (m, 2H), 2.60-2.25 (m, 2H), 2.20-2.00 (m, 2H), 2.00-1.60 (m, 3H), 0.98 (d, J = 6.0 Hz, 6H).
    [739] Example 6 (20)
    [740] 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [741]
    [742] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [743] NMR (CD 3 OD): δ 7.70-7.45 (m, 5H), 7.40-7.15 (m, 5H), 4.92 (m, 2H), 4.29 (s, 2H), 4.20 (dd, J = 8.4, 4.8 Hz , 1H), 3.90-3.65 (m, 2H), 3.65-3.45 (m, 2H), 2.85-2.50 (m, 2H), 2.44 (s, 3H), 2.39 (s, 3H), 2.20-2.00 (m , 2H), 2.00-1.60 (m, 3H), 1.00 (d, J = 5.4 Hz, 6H).
    [744] Example 6 (21)
    [745] 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [746]
    [747] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [748] NMR (CD 3 OD): δ 7.18 (t, J = 7.8 Hz, 1H), 7.10-6.85 (m, 6H), 4.77 (m, 2H), 4.25 (s, 4H), 4.19 (m, 3H), 3.68 (m, 2H), 3.40 (m, 2H), 2.60-2.30 (m, 2H), 2.29 (s, 3H), 2.20-2.00 (m, 2H), 2.00-1.60 (m, 3H), 0.99 ( d, J = 6.2 Hz, 6H).
    [749] Example 6 (22)
    [750] 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [751]
    [752] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [753] NMR (CD 3 OD): δ 7.70-7.45 (m, 5H), 7.18 (t, J = 7.4 Hz, 1H), 7.10-7.00 (m, 3H), 4.88 (s, 2H), 4.31 (s, 2H ), 4.20 (dd, J = 8.2, 4.8 Hz, 1H), 3.76 (m, 2H), 3.60 (m, 2H), 2.90-2.50 (m, 2H), 2.47 (s, 3H), 2.41 (s, 3H), 2.30 (s, 3H), 2.10 (m, 2H), 1.88 (m, 1H), 1.85-1.65 (m, 2H), 1.00 (d, J = 5.8 Hz, 6H).
    [754] Example 6 (23)
    [755] 1- (1-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [756]
    [757] TLC: Rf 0.49, 0.56 (chloroform: methanol = 10: 1);
    [758] NMR (CD 3 OD): δ 7.49 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.08-6.99 ( m, 4H), 4.26 (s, 2H), 3.97-3.79 (m, 2H), 3.78-3.60 (m, 1H), 3.54-3.33 (m, 3H), 2.47-2.29 (m, 2H), 2.2 6 -2.03 (m, 3H), 1.87-1.71 (m, 1H), 1.70-1.53 (m, 3H), 1.48-1.16 (m, 5H), 1.02-0.90 (m, 9H).
    [759] Example 6 (24)
    [760] 1- (3-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [761]
    [762] TLC: Rf 0.54 (CHCl 3: MeOH = 10: 1);
    [763] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 ( m, 4H), 4.33 (s, 2H), 4.00 (dd, J = 8.1, 4.8 Hz, 1H), 3.90-3.71 (m, 2H), 3.56-3.34 (m, 4H), 2.46-2.29 (m, 2H), 2.28-2.10 (m, 2H), 1.90-1.56 (m, 4H), 1.55-1.32 (m, 2H), 1.04-0.85 (m, 12H).
    [764] Example 6 (25)
    [765] 1- (2-methoxyphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [766]
    [767] TLC: Rf 0.38 (CHCl 3: MeOH = 20: 1);
    [768] NMR (CD 3 OD): δ 7.59-7.41 (m, 5H), 7.26-7.17 (m, 1H), 6.99-6.84 (m, 3H), 4.74 (brs, 2H), 4.27 (s, 2H), 4.19 (dd, J = 8.4, 4.5 Hz, 1H), 3.88 (s, 3H), 3.90-3.68 (m, 2H), 3.62-3.45 (m, 2H), 2.60-2.14 (m, 4H), 2.35 (s , 3H), 2.33 (s, 3H), 2.00-1.63 (m, 3H), 0.99 (d, J = 6.3 Hz, 6H).
    [769] Example 6 (26)
    [770] 1- (3-methoxyphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [771]
    [772] TLC: Rf 0.33 (CHCl 3: MeOH = 20: 1);
    [773] NMR (CD 3 OD): δ 7.65-7.48 (m, 5H), 7.20 (t, J = 8.1 Hz, 1H), 6.85-6.80 (m, 2H), 6.77 (dd, J = 7.8, 2.1 Hz, 1H ), 4.90 (brs, 2H), 4.31 (s, 2H), 4.20 (dd, J = 8.1, 4.8 Hz, 1H), 3.84-3.65 (m, 2H), 3.75 (s, 3H), 3.65-3.48 ( m, 2H), 2.84-2.56 (m, 2H), 2.47 (s, 3H), 2.40 (s, 3H), 2.19-2.03 (m, 2H), 2.00-1.65 (m, 3H), 0.99 (d, J = 6.3 Hz, 6H).
    [774] Example 6 (27)
    [775] 1- (2-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [776]
    [777] TLC: Rf 0.35 (CHCl 3: MeOH = 20: 1);
    [778] NMR (CD 3 OD): δ 7.63-7.46 (m, 5H), 7.18-7.06 (m, 3H), 6.99-6.91 (m, 1H), 4.81 (brs, 2H), 4.29 (s, 2H), 4.20 (dd, J = 8.4, 4.5 Hz, 1H), 3.90-3.66 (m, 2H), 3.63-3.57 (m, 2H), 2.75-2.40 (m, 2H), 2.44 (s, 3H), 2.40 (s , 3H), 2.38 (s, 3H), 2.30-2.10 (m, 2H), 2.00-1.65 (m, 3H), 0.99 (d, J = 6.3 Hz, 6H).
    [779] Example 6 (28)
    [780] 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [781]
    [782] TLC: Rf 0.48 (CHCl 3: MeOH = 20: 1);
    [783] NMR (CD 3 OD): δ 7.53-7.46 (m, 2H), 7.42-7.36 (m, 2H), 7.22-7.14 (m, 2H), 7.06-6.96 (m, 7H), 4.85-4.65 (m, 2H), 4.28 (s, 2H), 4.18 (dd, J = 8.1, 4.5 Hz, 1H), 3.80-3.62 (m, 2H), 3.50-3.30 (m, 2H), 2.58-2.25 (m, 2H) , 2.29 (s, 3H), 2.18-2.04 (m, 2H), 1.95-1.62 (m, 3H), 0.98 (d, J = 6.3 Hz, 6H).
    [784] Example 6 (29)
    [785] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [786]
    [787] TLC: Rf 0.62 (CHCl 3: MeOH = 20: 1);
    [788] NMR (CD 3 OD): δ 7.17 (d, J = 3.6 Hz, 1H), 6.85 (d, J = 3.6 Hz, 1H), 4.53 (s, 2H), 4.04 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.72 (m, 2H), 3.58-3.45 (m, 2H), 3.43-3.33 (m, 2H), 2.87 (q, J = 7.5 Hz, 2H), 2.50-2.30 (m, 2H) , 2.30-2.08 (m, 2H), 1.83-1.10 (m, 17H), 1.31 (t, J = 7.5 Hz, 3H), 1.05-0.85 (m, 2H), 0.95 (t, J = 7.5 Hz, 3H ).
    [789] Example 6 (30)
    [790] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [791]
    [792] TLC: Rf 0.62 (CHCl 3: MeOH = 20: 1);
    [793] NMR (CD 3 OD): δ 6.63 (d, J = 3.0 Hz, 1H), 6.14 (d, J = 3.0 Hz, 1H), 4.39 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.70 (m, 2H), 3.55-3.40 (m, 2H), 3.40-3.35 (m, 2H), 2.69 (q, J = 7.5 Hz, 2H), 2.50-2.30 (m, 2H) , 2.30-2.10 (m, 2H), 1.85-1.05 (m, 17H), 1.25 (t, J = 7.5 Hz, 3H), 1.05-0.85 (m, 2H), 0.96 (t, J = 7.5 Hz, 3H ).
    [794] Example 6 (31)
    [795] (3S) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [796]
    [797] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [798] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.44-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 (m, 4H), 4.33 (s, 2H), 4.16-4.00 (m, 2H), 3.75-3.40 (m, 5H), 3.26-3.09 (m, 1H), 2.56-2.08 (m, 4H), 1.82-1.60 (m, 2H ), 1.50-1.30 (m, 3H), 1.05-0.89 (m, 9H).
    [799] Example 6 (32)
    [800] (3R) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [801]
    [802] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [803] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.44-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 (m, 4H), 4.33 (s, 2H), 4.16-4.00 (m, 2H), 3.75-3.40 (m, 5H), 3.26-3.09 (m, 1H), 2.56-2.08 (m, 4H), 1.82-1.60 (m, 2H ), 1.50-1.30 (m, 3H), 1.05-0.89 (m, 9H).
    [804] Example 7
    [805] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9-allyloxycarbonyl-1,4,9-triazaspiro [5.5 Undecan
    [806]
    [807] Resin (6), N-allyloxycarbonyl-4-piperidone, n-propylamine and N- (t-butyloxycarbonyl) -N '-(benzyloxycarbonyl) -L prepared in Reference Example 8 The same procedure as in Reference Example 9-Reference Example 10-Example 1 was carried out using lysine to obtain a compound of the present invention having the following physical properties.
    [808] TLC: Rf 0.24 (ethyl acetate: hexane = 4: 1);
    [809] NMR (CD 3 OD): δ 7.35 (m, 5H), 6.40 (m, 1H), 5.96 (ddt, J = 17.2, 10.2, 5.6 Hz, 1H), 5.34 (m, 1H), 5.24 (m, 1H ), 5.12 (s, 2H), 4.88 (m, 1H), 4.62 (m, 2H), 4.10 (m, 2H), 4.00 (m, 1H), 3.75 (m, 1H), 3.36 (m, 2H) , 3.18 (m, 3H), 1.94 (m, 6H), 1.51 (m, 6H), 0.90 (t, J = 7.2 Hz, 3H).
    [810] Example 8
    [811] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -1,4,9-triazaspiro [5.5] undecane
    [812]
    [813] Using the compound prepared in Example 7, the same operation as in Reference Example 4 was carried out, and the mixture was purified by positive ion exchange resin and silica gel column chromatography to obtain a compound of the present invention having the following physical properties.
    [814] TLC: Rf 0.56 (CHCl 3: MeOH: 28% Ammonia = 20: 5: 1);
    [815] NMR (CD 3 OD): δ 7.40-7.20 (m, 10H), 5.06 (s, 2H), 4.03 (t, J = 5.0 Hz, 1H), 3.55-3.18 (m, 4H), 3.12 (t, J = 6.6 Hz, 2H), 3.08-2.98 (m, 2H), 2.20-1.70 (m, 6H), 1.70-1.20 (m, 6H), 0.93 (t, J = 7.2 Hz, 3H).
    [816] Example 8 (1)
    [817] 1-propyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [818]
    [819] Example 7-Same Operation as in Example 8 using N- (t-butyloxycarbonyl) leucine in place of N- (t-butyloxycarbonyl) -N '-(benzyloxycarbonyl) -L-lysine This obtained the compound of this invention which has the following physical properties.
    [820] TLC: Rf 0.44 (CHCl 3: MeOH: Triethylamine = 18: 2: 1);
    [821] NMR (CD 3 OD): δ 3.99 (d, J = 7.8, 4.4 Hz, 1H), 3.50-3.20 (m, 4H), 3.05-2.85 (m, 2H), 2.10-1.75 (m, 5H), 1.75 -1.40 (m, 4H), 1.00-0.85 (m, 9H).
    [822] Example 9
    [823] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [824]
    [825] To a solution of compound (202 mg) in methanol (5 ml) prepared in Example 6 (7) was added 5% palladium-carbon (20 mg). The reaction mixture was stirred at room temperature under hydrogen atmosphere for 3 hours. The reaction mixture was filtered through celite (trade name), and the filtrate was concentrated to give the compound of the present invention (127 mg) having the following physical properties.
    [826] TLC: Rf 0.61 (CHCl 3: MeOH: 28% Ammonia Water = 20: 5: 1);
    [827] NMR (CD 3 OD): δ 3.97 (dd, J = 7.8 Hz, 4.5 Hz, 1H), 3.48-3.22 (m, 4H), 3.00-2.90 (m, 2H), 2.12-1.60 (m, 11H), 0.95 (t, J = 7.2 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [828] Example 9 (1)
    [829] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane
    [830]
    [831] The compound of the present invention was obtained in the same manner as in Example 9 using the compound prepared in Example 6 (8) instead of the compound prepared in Example 6 (7).
    [832] TLC: Rf 0.65 (CHCl 3: MeOH: 28% Ammonia Water = 20: 5: 1);
    [833] NMR (CD 3 OD): δ 4.00 (dd, J = 7.8 Hz, 4.5 Hz, 1H), 3.46-3.24 (m, 4H), 3.03-2.92 (m, 2H), 2.08-1.08 (m, 19H), 1.05-0.84 (m, 5 H).
    [834] Example 10
    [835] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-dihydroxyboranephenylmethyl) -1,4,9 -Triazaspiro [5.5] undecane hydrochloride
    [836]
    [837] The compound prepared in Example 8 (70 mg) was dissolved in a dimethylformamide solution (2 ml) of 1% acetic acid. To this solution was added sodium triacetoxyborate hydride (46 mg) and 4-formylphenylboronic acid (30 mg). The reaction mixture was stirred for 46 hours at room temperature. To the reaction mixture was added 10% methanol solution of acetic acid. The solution was passed through a cation exchange resin (bonderut-SCX, Varian, 0.6 mmol / g, 500 mg / 3 ml) and washed with methanol. It was also eluted with a methanol solution of 10% triethylamine. Only the solution eluted with this methanol solution of 10% triethylamine was concentrated. The obtained residue was purified by silica gel column chromatography (chloroform: methanol = 1: 0 → 30: 1 → 10: 1) to give a compound of the present invention (45 mg) having the following physical properties.
    [838] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [839] NMR (CD 3 OD): δ 7.73 (br, 2H), 7.52 (br, 2H), 7.32 (m, 5H), 5.03 (s, 2H), 4.36 (s, 2H), 4.05 (t, J = 4.8 Hz, 1H), 3.81 (m, 2H), 3.46 (m, 3H), 3.10 (t, J = 6.6 Hz, 2H), 2.37 (br, 2H), 2.22 (br, 2H), 1.92-1.66 (m , 2H), 1.60-1.28 (m, 7H), 0.91 (t, J = 7.5 Hz, 3H).
    [840] Example 10 (1)
    [841] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (1,3-benzodioxalan-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane hydrochloride
    [842]
    [843] The compound of the present invention having the following physical properties was obtained in the same manner as in Example 10 using 2,3- (methylenedioxy) benzoaldehyde instead of 4-formylphenylboronic acid.
    [844] TLC: Rf 0.25 (chloroform: methanol = 10: 1);
    [845] NMR (CD 3 OD): δ 7.32 (m, 5H), 6.96 (m, 3H), 6.05 (s, 2H), 5.04 (s, 2H), 4.33 (s, 2H), 4.05 (t, J = 4.5 Hz, 1H), 3.98-3.54 (m, 2H), 3.53 (m, 2H), 3.38 (m, 3H), 3.11 (t, J = 6.6 Hz, 2H), 2.37 (br, 2H), 2.22 (br , 2H), 1.98-1.76 (m, 2H), 1.61-1.28 (m, 5H), 0.92 (t, J = 7.2 Hz, 3H).
    [846] Example 11
    [847] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (1,4-benzodioxan-6-yl) ethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [848]
    [849] To a solution of compound (315 mg) in dichloromethane (5 ml) prepared in Example 9, 1,4-benzodioxane-6-ylmethylketone (285 mg), triethylamine (0.354 ml), tetrachloride under argon atmosphere Dichloromethane solution of titanium (1.0 M solution, 0.63 ml) was added. The reaction mixture was stirred at rt for 16 h. To the reaction mixture was added a methanol (2 ml) solution of sodium cyanoborohydride (133 mg). The reaction mixture was stirred at rt for 1 h. 2N aqueous sodium hydroxide solution was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The extract was dried over anhydrous sodium sulfate and concentrated. The obtained residue was purified by silica gel column chromatography (Fuji Silysia Kagaku, BW235; chloroform: methanol = 50: 1). The obtained residue was dissolved in methanol, acidified with a 1N aqueous hydrochloric acid solution, and concentrated to give a compound of the present invention (176 mg) having the following physical properties.
    [850] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [851] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.4, 2.1 Hz, 1H), 6.92 (d, J = 8.4 Hz, 1H), 4.40 (q, J = 6.9 Hz, 1H), 4.26 (s, 4H), 3.98 (dd, J = 8.1, 4.5 Hz, 1H), 3.82-3.17 (m, 6H), 2.55-2.04 (m, 4H), 1.87-1.28 (m, 10 H), 1.04-0.85 (m, 9 H).
    [852] Example 11 (1)
    [853] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (4-phenyloxyphenyl) ethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [854]
    [855] The compound of the present invention having the following physical properties was obtained in the same manner as in Example 11 using 4-phenoxyacetophenone instead of 1,4-benzodioxane-6-ylmethyl ketone.
    [856] TLC: Rf 0.58, 0.62 (CHCl 3: MeOH = 10: 1);
    [857] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.09-7.01 ( m, 4H), 4.48 (m, 1H), 3.98 (dd, J = 7.8, 4.8 Hz, 1H), 3.80-3.17 (m, 6H), 2.56-2.28 (m, 2H), 2.28-2.03 (m, 2H), 1.88-1.24 (m, 7H), 1.76 (d, J = 6.9 Hz, 3H), 1.04-0.86 (m, 9H).
    [858] Example 12
    [859] 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1- (1,4-benzodioxan-6-yl) ethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [860]
    [861] Using the compound prepared in Example 9 (1) instead of the compound prepared in Example 9, the same operation as in Example 11 was carried out to obtain a compound of the present invention having the following physical properties.
    [862] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [863] NMR (CD 3 OD): δ 7.02 (d, J = 1.8 Hz, 1H), 6.96 (dd, J = 8.4, 1.8 Hz, 1H), 6.92 (d, J = 8.4 Hz, 1H), 4.39 (m, 1H), 4.26 (s, 4H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.80-3.20 (m, 6H), 2.50-2.02 (m, 4H), 1.82-1.13 (m, 18H) , 1.04-0.83 (m, 5 H).
    [864] Example 13
    [865] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9-allyl-1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [866]
    [867] To a solution of compound (225 mg) in tetrahydrofuran (5 ml) prepared in Example 7 was added tetrakistriphenylphosphinepalladium (0) (51 mg) at room temperature under argon atmosphere. The reaction mixture was stirred at rt for 16 h. The reaction mixture was passed through a cation exchange resin (bond eruth-SCX, Varian, 0.6 mmol / g, 500 mg / 3 ml) and washed with methanol. It was also eluted with a methanol solution (20 ml) of 10% triethylamine. Only the solution eluted with this methanol solution of 10% triethylamine was concentrated. The obtained residue was purified by silica gel column chromatography (chloroform: methanol = 20: 1) to give a compound of the present invention (122 mg) having the following physical properties.
    [868] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [869] NMR (CD 3 OD): δ 7.34 (m, 5H), 6.00 (m, 1H), 5.62 (m, 1H), 5.61 (m, 1H), 5.06 (s, 2H), 4.07 (t, J = 5.2 Hz, 1H), 3.77 (m, 4H), 3.44 (m, 4H), 3.12 (t, J = 6.6 Hz, 2H), 2.39 (m, 2H), 2.20 (m, 2H), 1.84 (m, 2H ), 1.54 (m, 4H), 1.37 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [870] Example 14
    [871] (3S) -1-propyl-2,5-dioxo-3- (4-aminobutyl) -9-phenylethyl-1,4,9-triazaspiro [5.5] undecane
    [872]
    [873] The compound of the present invention was obtained in the same manner as in Example 9 using the compound prepared in Example 5 (11) instead of the compound prepared in Example 6 (7).
    [874] TLC: Rf 0.66 (CHCl 3: MeOH: 28% Ammonia Water = 20: 5: 1);
    [875] NMR (CD 3 OD): δ 7.23 (m, 5H), 4.05 (t, J = 5.2 Hz, 1H), 3.42 (m, 2H), 2.98 (m, 3H), 2.81 (m, 3H), 2.65 ( m, 4H), 2.16 (m, 2H), 1.99 (m, 1H), 1.89 (m, 3H), 1.53 (m, 3H), 1.48 (m, 3H), 0.94 (t, J = 7.2 Hz, 3H ).
    [876] Example 15
    [877] (3S) -1-propyl-2,5-dioxo-3- (4- (N- (4-phenyl) phenylcarbonyl) aminobutyl) -9-phenylethyl-1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [878]
    [879] To a solution of dichloroethane (2 ml) of compound (42 mg) prepared in Example 14, diisopropylethylamine (35 μl) and 4-phenylbenzoyl chloride (33 mg) were added. The reaction mixture was stirred at rt for 3 h. The reaction mixture was passed through a cation exchange resin (bond eruth-SCX, Varian, 0.6 mmol / g, 500 mg / 3 ml) and washed with methanol. It was also eluted with a methanol solution (20 ml) of 10% triethylamine. Only the solution eluted with this methanol solution of 10% triethylamine was concentrated. The obtained residue was purified by silica gel column chromatography (chloroform: methanol = 10: 0 → 10: 1). An ethyl acetate solution of 4N hydrochloric acid was added to the obtained product to obtain a compound of the present invention (66 mg) having the following physical properties.
    [880] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [881] NMR (CD 3 OD): δ 7.89 (d, J = 8.1 Hz, 2H), 7.72 (d, J = 8.1 Hz, 2H), 7.65 (d, J = 7.2 Hz, 2H), 7.45 (t, J = 7.2 Hz, 2H), 7.39-7.26 (m, 6H), 4.11 (m, 1H), 3.86-3.71 (m, 2H), 3.63-3.53 (m, 2H), 3.45-3.30 (m, 4H), 3.07 (m, 2H), 2.42 (br, 2H), 2.19 (m, 2H), 1.99-1.78 (m, 2H), 1.68-1.28 (m, 7H), 0.86 (t, J = 7.5 Hz, 3H).
    [882] Example 16
    [883] Iodide 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-methyl-9- (1- (1,4-benzodioxan-6-yl) ethyl) -1,4, -diaza -9-Azonia Spiro [5.5] Undecan
    [884]
    [885] To a solution of compound (50 mg) in chloroform (2 ml) prepared in Example 2 (1) was added 1N sodium hydroxide (2 ml). The reaction mixture was stirred for 10 minutes at room temperature. The aqueous layer of the reaction mixture was removed. The organic layer was washed with water, dried over anhydrous magnesium sulfate and concentrated. To the acetone (2 ml) solution of the obtained residue was added methyl iodide (118 μl). The reaction mixture was stirred at rt for 18 h. The reaction mixture was concentrated. The obtained residue was solidified with diethyl ether to obtain the compound of the present invention (58 mg) having the following physical properties.
    [886] TLC: Rf 0.23 (ethyl acetate: acetic acid: water = 8: 1: 1);
    [887] NMR (CD 3 OD): δ 7.10-6.90 (m, 3H), 4.60 + 4.49 (s + s, 2H), 4.29 (s, 4H), 4.20-4.00 (m, 3H), 3.70-3.35 (m, 4H), 3.11 + 2.99 (s + s, 3H), 2.80-2.30 (m, 2H), 2.30-2.00 (m, 2H), 1.90-1.10 (m, 15H), 1.10-0.80 (m, 5H).
    [888] Example 17
    [889] (3S) -3- (4- (N-benzyloxycarbonyl) aminobutyl) -2,5-dioxo-9- (2-hydroxy-2-phenylethyl) -1-propyl-1,4, 9-Triazaspiro [5,5] Undecan
    [890]
    [891] Styrene oxide (10 μl) was added to a 2-propanol (0.4 ml) solution of the compound (0.01 g) prepared in Example 8. The reaction mixture was refluxed for 4 hours. After the reaction mixture was cooled to room temperature, the reaction mixture was adsorbed onto an ion exchange resin (OASIS MCX, Waters, 60 mg) washed with methanol (3 mL) in advance. After washing with methanol (2 mL), it was eluted with 10% triethylamine-methanol solution (2 mL). The eluate was concentrated under reduced pressure to obtain a compound of the present invention (13 mg) having the following physical properties.
    [892] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [893] NMR (CD 3 OD): δ 7.40-7.20 (m, 10H), 5.06 (s, 2H), 4.03 (m, 1H), 3.40 (m, 2H), 3.12 (m, 2H), 3.10-2.60 (m , 6H), 2.50 (m, 1H), 2.40-2.00 (m, 2H), 2.00-1.70 (m, 4H), 1.70-1.20 (m, 6H), 0.93 (t, J = 7.2 Hz, 3H).
    [894] Example 18
    [895] (3S) -3- (4- (N-benzyloxycarbonyl) aminobutyl) -2,5-dioxo-9- (2-oxo-2-phenylethyl) -1-propyl-1,4,9 -Triaza spiro [5,5] Undecan
    [896]
    [897] To a solution of dimethylformamide (0.4 ml) of the compound (0.01 g) prepared in Example 8 was added triethylamine (6 μl) and phenacyl bromide (9 mg). The reaction mixture solution was left at room temperature for 24 hours. Acetic acid (0.4 ml) was added to the reaction mixture to make it acidic. The reaction mixture was adsorbed onto an ion exchange resin (OASIS MCX, Waters, 120 mg), previously washed with methanol (6 mL). After washing with methanol (2 ml), eluted with 10% triethylamine-methanol solution (4 ml). The eluate was concentrated under reduced pressure to obtain a compound of the present invention (12 mg) having the following physical properties.
    [898] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [899] NMR (CD 3 OD): δ 8.01 (m, 2H), 7.54 (m, 3H), 7.33 (m, 5H), 5.05 (s, 2H), 4.02 (m, 1H), 4.00 (s, 2H), 3.44 (m, 2H), 3.12 (t, J = 6.6 Hz, 2H), 2.95 (m, 2H), 2.40-2.10 (m, 2H), 2.00-1.70 (m, 5H), 1.68-1.20 (m, 7H), 0.94 (t, J = 7.2 Hz, 3H).
    [900] Example 19
    [901] (3S) -1- (2-methylpropyl) -2,5-dioxo-3-methyl-9-allyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [902]
    [903] In a suspension of tetrahydrofuran (1.5 ml) and methanol (1.5 ml) of Resin (6) (300 mg) prepared in Reference Example 8, N-allyloxycarbonyl-4-piperidone (403 mg), iso Butylamine (0.22 ml) and N- (t-butyloxycarbonyl) -L-alanine (381 mg) were added. The reaction mixture was stirred at 65 ° C. for 20 hours. The reaction solution was cooled at room temperature and the resin was taken by filtration. The obtained resin was washed with tetrahydrofuran (3 ml x 4 times) and methylene chloride (3 ml x 5 times), and dried to obtain a resin (384 mg). To a 1.5 M 2,6-lutidine-methylene chloride (2 ml) suspension of the obtained resin (146 mg) was added 1 M trifluoromethanesulfonic acid trimethylsilyl-methylene chloride solution (2 ml) and stirred at room temperature for 30 minutes. It was. The reaction solution was filtered and washed with methylene chloride (2 ml × 3 times). The obtained resin was again suspended in 1.5 M 2,6-lutidine-methylene chloride solution (2 ml), 1 M trifluoromethanesulfonic acid trimethylsilyl-methylene chloride solution (2 ml) was added, and stirred at room temperature for 30 minutes. It was. The resin was collected by filtration from the reaction solution, washed with methylene chloride (2 ml x 4 times), methanol (2 ml x 4 times) and methylene chloride (2 ml x 4 times), and dried to obtain a resin. The obtained resin was suspended in 1.25 M acetic acid-toluene solution (2 ml). The reaction mixture was stirred at 90 ° C. for 20 hours. The reaction mixture was filtered and washed with toluene (2 ml × 3 times) and methanol (2 ml × 4 times). The filtrate was concentrated to obtain the compound of the present invention (19 mg) having the following physical properties.
    [904] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [905] MS (ESI, Pos., 20 V): 388 (M + H) + ;
    [906] HPLC conditions: F;
    [907] HPLC retention time: 3.40 minutes;
    [908] NMR (CD 3 OD): δ 5.98 (ddt, J = 15.8, 10.4, 5.4 Hz, 1H), 5.30 (m, 1H), 5.21 (m, 1H), 4.59 (m, 2H), 4.20-4.00 (m , 3H), 3.85-3.60 (m, 2H), 3.41 (dd, J = 14.2, 8.0 Hz, 1H), 3.18 (dd, J = 14.2, 7.2 Hz, 1H), 2.10-1.70 (m, 5H), 1.43 (d, J = 6.8 Hz, 3H), 0.89 (t, J = 6.2 Hz, 6H).
    [909] Example 19 (1)
    [910] (3S) -1- (2-methylpropyl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane acetate
    [911]
    [912] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), isobutylamine (0.123 ml) and N- (t-butyloxycarbonyl) prepared in Reference Example 8 ) -L-alanine (235 mg) was used in the same manner as in Example 19 to obtain a compound of the present invention (50 mg) having the following physical properties.
    [913] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [914] MS (ESI, Pos., 20 V): 358 (M + H) + ;
    [915] HPLC conditions: F;
    [916] HPLC retention time: 3.14 minutes;
    [917] NMR (CD 3 OD): δ 7.40-7.20 (m, 5H), 4.15 (q, J = 6.8 Hz, 1H), 3.65 (m, 1H), 3.55-3.35 (m, 3H), 3.25-3.05 (m , 3H), 3.05-2.90 (m, 3H), 2.50-2.05 (m, 4H), 1.98 (s, 3H), 1.92 (m, 1H), 1.43 (d, J = 6.8 Hz, 3H), 0.92 ( t, J = 6.4 Hz, 6H).
    [918] Example 19 (2)
    [919] (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4, 9-triazaspiro [5.5] undecane acetate
    [920]
    [921] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), isobutylamine (0.123 ml) and N- (t-butyloxycarbonyl) prepared in Reference Example 8 ) -N '-(benzyloxycarbonyl) -L-lysine 472 mg) was used in the same manner as in Example 19 to obtain a compound of the present invention (71 mg) having the following physical properties.
    [922] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [923] MS (ESI, Pos., 20 V): 549 (M + H) + ;
    [924] HPLC conditions: F;
    [925] HPLC retention time: 3.49 min;
    [926] NMR (CD 3 OD): δ 7.40-7.20 (m, 10H), 5.06 (s, 2H), 4.10 (m, 1H), 3.67 (m, 1H), 3.60-3.40 (m, 3H), 3.28-3.05 (m, 5H), 3.05-2.90 (m, 3H), 2.50-2.10 (m, 4H), 1.98 (s, 3H), 2.05-1.70 (m, 3H), 1.65-1.20 (m, 4H), 0.92 (t, J = 6.2 Hz, 6H).
    [927] Example 19 (3)
    [928] (3S) -1- (1-benzylpiperidin-4-yl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 Undecane Diacetate
    [929]
    [930] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), 4-amino-1-benzylpiperidine (0.253 ml) and N- prepared in Reference Example 8. (t-butyloxycarbonyl) -L-alanine (235 mg) was used in the same manner as in Example 19 to obtain the compound (41 mg) of the present invention having the following physical properties.
    [931] TLC: Rf 0.10 (CHCl 3: MeOH = 10: 1);
    [932] MS (ESI, Pos., 20 V): 475 (M + H) + ;
    [933] HPLC conditions: F;
    [934] HPLC retention time: 3.09 min;
    [935] NMR (CD 3 OD): δ 7.47 (m, 5H), 7.40-7.20 (m, 5H), 4.19 (s, 2H), 4.00 (q, J = 6.8 Hz, 1H), 3.80-3.53 (m, 4H ), 3.53-3,35 (m, 4H), 3.30-3.15 (m, 2H), 3.15-2.90 (m, 3H), 2,55-2.30 (m, 3H), 2.30-2.00 (m, 2H) , 1.98 (s, 6H), 1.85-1.70 (m, 3H), 1.42 (d, J = 7.0 Hz, 3H).
    [936] Example 19 (4)
    [937] (3S) -1- (1-benzylpiperidin-4-yl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] undecane diacetate
    [938]
    [939] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), 4-amino-1-benzylpiperidine (0.253 ml) and N- prepared in Reference Example 8. (tmg of butyloxycarbonyl) -N '-(benzyloxycarbonyl) -L-lysine (472 mg) Got it.
    [940] TLC: Rf 0.12 (CHCl 3: MeOH = 10: 1);
    [941] MS (ESI, Pos., 20 V): 666 (M + H) + ;
    [942] HPLC conditions: F;
    [943] HPLC retention time: 3.36 minutes;
    [944] NMR (CD 3 OD): δ 7.46 (m, 5H), 7.40-7.20 (m, 10H), 5.03 (s, 2H), 4.19 (s, 2H), 3.99 (m, 1H), 3.80-3.40 (m , 6H), 3.30-2.85 (m, 9H), 2.50-2.10 (m, 6H), 1.98 (s, 6H), 1.95-1.60 (m, 4H), 1.60-1.40 (m, 4H).
    [945] Example 19 (5)
    [946] (3S) -1- (2,2-diphenylpropyl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane ·acetate
    [947]
    [948] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), 2,2-diphenylpropylamine (307 mg) and N- (t prepared in Reference Example 8 The compound of the present invention (22 mg) having the following physical properties was obtained in the same manner as in Example 19 using -butyloxycarbonyl) -L-alanine (235 mg).
    [949] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [950] MS (ESI, Pos., 20 V): 496 (M + H) + ;
    [951] HPLC conditions: F;
    [952] HPLC retention time: 3.58 min;
    [953] NMR (CD 3 OD): δ 7.40-7.10 (m, 15H), 4.79 (m, 1H), 4.16 (m, 1H), 3.93 (m, 1H), 3.71 (s, 2H), 3.23 (m, 1H ), 3.10-2.80 (m, 5H), 1.98 (s, 3H), 1.95-1.82 (m, 2H), 1.70-1.15 (m, 1H), 1.58 (s, 3H), 1.49 (d, J = 6.8 Hz, 3H), 0.70 (m, 1H).
    [954] Example 19 (6)
    [955] (3S) -1- (2,2-diphenylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] undecane acetate
    [956]
    [957] Resin (6) (200 mg), N- (2-phenylethyl) -4-piperidone (252 mg), 2,2-diphenylpropylamine (307 mg) and N- (t prepared in Reference Example 8 The compound of the present invention (18 mg) having the following physical properties was obtained in the same manner as in Example 19 using -butyloxycarbonyl) -N '-(benzyloxycarbonyl) -L-lysine (472 mg).
    [958] MS (ESI, Pos., 20 V): 687 (M + H) + ;
    [959] HPLC conditions: F;
    [960] HPLC retention time: 3.80 minutes;
    [961] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [962] NMR (CD 3 OD): δ 7.40-7.00 (m, 20H), 5.06 (s, 2H), 4.16 (m, 1H), 3.93 (m, 1H), 3.70 (s, 2H), 3.55 (m, 1H ), 3.30-3.10 (m, 2H), 3.10-2.80 (m, 6H), 1.98 (s, 3H), 1.95-1.85 (m, 2H), 1.80 (s, 3H), 1.70-1.30 (m, 8) H).
    [963] Example 19 (7)
    [964] (3S) -1-propyl-2,5-dioxo-3- (4-benzyloxyphenylmethyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane acetate
    [965]
    [966] Resin (6) (0.5 g), N- (2-phenylethyl) -4-piperidone (0.32 g), n-propylamine (0.13 ml) and N- (t-butyloxycarb) prepared in Reference Example 8 The compound of the present invention (68 mg) having the following physical properties was obtained in the same manner as in Example 19 using carbonyl) -O-benzyl-L-tyrosine (0.58 g).
    [967] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [968] NMR (CD 3 OD): δ 7.50-7.10 (m, 10H), 7.06 (d, J = 8.8 Hz, 2H), 6.92 (d, J = 8.8 Hz, 2H), 5.07 (s, 2H), 4.31 ( m, 1H), 3.68 (m, 1H), 3.40 (m, 1H), 3.28-3.13 (m, 4H), 3.13-2.80 (m, 6H), 2.30-2.00 (m, 2H), 1.80-1.35 ( m, 4H), 0.91 (t, J = 7.2 Hz, 3H).
    [969] Example 19 (H1-1) -19 (H13-62)
    [970] The same procedure as in Example 19 was carried out using the resin (6) prepared in Reference Example 8, the corresponding 4-piperidone derivative, the corresponding amine derivative and the corresponding amino acid derivative to obtain the following Tables 1A-1 to 13A-9 The compound of this invention which showed the compound name and showed the structural formula in Table 1B-1-13B-7 was obtained. In addition, the physical properties of these compounds of the present invention are shown in Tables 1C-1 to 13C-3 below.
    [971] In the table of this specification,
    [972] X 1 represents a binding site of R 1 ,
    [973] X 2 represents a binding site of R 2 ,
    [974] X 3 represents a binding site of R 3 ,
    [975] X 4 represents a binding site of R 4 ,
    [976] X 5 represents a binding site of R 5 .
    [977] For example, the structural formula of Example 19 (H1-1) is represented as follows.
    [978]
    [979] In addition, the measurement conditions of high performance liquid chromatography (HPLC) in the table of this specification are shown below.
    [980] Condition A
    [981] Column used: YMC-Pack FL-ODS, 50 × 4.6 mm I.D., S-5um, 120A
    [982] Flow rate used: 1 mL / min
    [983] Solvent used
    [984] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [985] Liquid B: Methanol
    [986] 2 minutes after the start of the measurement, the mixing ratio of the liquid A and the liquid B was fixed at 90/10. Thereafter, the mixing ratio of the liquid A and the liquid B was changed linearly to 20/80 for 20 minutes. Thereafter, the mixing ratio of A liquid and B liquid was fixed at 20/80 for 5 minutes. Thereafter, the mixing ratio of the liquid A and the liquid B was linearly changed to 90/10 in 1 minute.
    [987] Condition B
    [988] Column used: YMC-Pack FL-ODS, 50 × 4.6 mm I.D., S-5um, 120A
    [989] Flow rate used: 1 mL / min
    [990] Solvent used
    [991] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [992] Liquid B: Methanol
    [993] Two minutes after the start of the measurement, the mixing ratio of the liquid A and the liquid B was fixed at 80/20. Thereafter, the mixing ratio of the liquid A and the liquid B was changed linearly to 20/80 for 20 minutes. Thereafter, the mixing ratio of A liquid and B liquid was fixed at 20/80 for 5 minutes. Thereafter, the mixing ratio of A liquid and B liquid was linearly changed to 80/20 for 1 minute.
    [994] Condition C
    [995] Column used: YMC-Pack FL-ODS, 50 × 4.6 mmI.D., S-5um, 120A
    [996] Flow rate used: 1 mL / min
    [997] Solvent used
    [998] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [999] Liquid B: Methanol
    [1000] One minute after the start of the measurement, the mixing ratio of the liquid A and the liquid B was fixed at 90/10. Thereafter, the mixing ratio of A liquid and B liquid was linearly changed to 10/90 for 16 minutes. After that, the mixing ratio of A liquid and B liquid was fixed at 10/90 for 1 minute. Thereafter, the mixing ratio of A liquid and B liquid was linearly changed to 90/10 for 1 minute.
    [1001] Condition D
    [1002] Column used: YMC-Pack FL-ODS, 50 × 4.6 mmI.D., S-5um, 120A
    [1003] Flow rate used: 1 mL / min
    [1004] Solvent used
    [1005] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [1006] Liquid B: Methanol
    [1007] The mixing ratio of A liquid and B liquid was 90/10 at the start of measurement. Thereafter, the mixing ratio of A liquid and B liquid was linearly changed to 10/90 for 16 minutes. Thereafter, the mixing ratio of A liquid and B liquid was fixed at 10/90 for 0.5 minutes. Thereafter, the mixing ratio of the liquid A and the liquid B was changed to 90/10 linearly for 0.5 minutes.
    [1008] Condition E
    [1009] Column used: YMC-Pack FL-ODS, 50 × 4.6 mmI.D., S-5um, 120A
    [1010] Flow rate used: 3 mL / min
    [1011] Solvent used
    [1012] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [1013] Liquid B: Methanol
    [1014] The mixing ratio of A liquid and B liquid was 90/10 at the start of measurement. Thereafter, the mixing ratio of the liquid A and the liquid B was changed linearly to 10/90 for 5 minutes. Thereafter, the mixing ratio of A liquid and B liquid was fixed at 10/90 for 0.5 minutes. Thereafter, the mixing ratio of A liquid and B liquid was changed linearly to 90/10 for 0.1 minute.
    [1015] Condition F
    [1016] Column used: Xterra TM MS C 18 5um, 4.6 × 50 mm ID
    [1017] Flow rate used: 3 mL / min
    [1018] Solvent used
    [1019] Solution A: 0.1% trifluoroacetic acid aqueous solution
    [1020] Liquid B: 0.1% trifluoroacetic acid-acetonitrile solution
    [1021] 0.5 minutes after the start of measurement, the mixing ratio of A liquid and B liquid was fixed at 95/5. Thereafter, the mixing ratio of A liquid and B liquid was changed linearly to 0/100 for 2.5 minutes. Thereafter, the mixing ratio of A liquid and B liquid was fixed at 0/100 for 0.5 minutes. Thereafter, the mixing ratio of the liquid A and the liquid B was changed linearly to 95/5 for 0.01 minutes.
    [1022] TABLE 1A-1
    [1023] Example number Compound name
    [1024] 19 (H1-1) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [1025] 19 (H1-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [1026] 19 (H1-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1027] 19 (H1-4) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1028] 19 (H1-5) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [1029] 19 (H1-6) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1030] 19 (H1-7) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1031] 19 (H1-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1032] 19 (H1-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1033] TABLE 1A-2
    [1034] Example number Compound name
    [1035] 19 (H1-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9 -Triaza Spiro [5.5] Undecan
    [1036] 19 (H1-11) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1037] 19 (H1-12) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1038] 19 (H1-13) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1039] 19 (H1-14) 1-benzyl-2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1040] 19 (H1-15) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1041] 19 (H1-16) 1-benzyl-2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1042] 19 (H1-17) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1043] 19 (H1-18) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1044] Table 1A-3
    [1045] Example number Compound name
    [1046] 19 (H1-19) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1047] 19 (H1-20) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1048] 19 (H1-21) 1- (2,2-diphenylethyl) -2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1049] 19 (H1-22) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1050] 19 (H1-23) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1051] 19 (H1-24) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1052] 19 (H1-25) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1053] 19 (H1-26) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [1054] 19 (H1-27) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1055] TABLE 1A-4
    [1056] Example number Compound name
    [1057] 19 (H1-28) 1- (2-phenylethyl) -2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1058] 19 (H1-29) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1059] 19 (H1-30) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1060] 19 (H1-31) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [1061] 19 (H1-32) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1062] 19 (H1-33) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1063] 19 (H1-34) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1064] 19 (H1-35) 1-propyl-2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1065] 19 (H1-36) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1066] 19 (H1-37) 1-propyl-2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1067] Table 1A-5
    [1068] Example number Compound name
    [1069] 19 (H1-38) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1070] 19 (H1-39) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1071] 19 (H1-40) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1072] 19 (H1-41) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1073] 19 (H1-42) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1074] 19 (H1-43) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triaza Spiro [5.5] Undecan
    [1075] 19 (H1-44) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1076] 19 (H1-45) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1077] 19 (H1-46) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [1078] Table 1A-6
    [1079] Example number Compound name
    [1080] 19 (H1-47) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1081] 19 (H1-48) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1, 4,9-Triaza spiro [5.5] Undecan
    [1082] 19 (H1-49) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [1083] 19 (H1-50) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1084] 19 (H1-51) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [1085] 19 (H1-52) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-benzyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1086] 19 (H1-53) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9-benzyl-1,4,9-triazaspiro [5.5] Undecan
    [1087] 19 (H1-54) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-benzyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1088] Table 1A-7
    [1089] Example number Compound name
    [1090] 19 (H1-55) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4 , 9-triazaspiro [5.5] Undecan
    [1091] TABLE 2A-1
    [1092] Example number Compound name
    [1093] 19 (H2-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1094] 19 (H2-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1095] 19 (H2-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 Undecan
    [1096] 19 (H2-4) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1097] 19 (H2-5) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1098] 19 (H2-6) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1099] 19 (H2-7) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1100] 19 (H2-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1101] TABLE 2A-2
    [1102] Example number Compound name
    [1103] 19 (H2-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1104] 19 (H2-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1105] 19 (H2-11) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1106] 19 (H2-12) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1107] 19 (H2-13) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Cannes
    [1108] 19 (H2-14) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1109] 19 (H2-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1110] 19 (H2-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1111] Table 2A-3
    [1112] Example number Compound name
    [1113] 19 (H2-17) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1114] 19 (H2-18) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1115] 19 (H2-19) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1116] 19 (H2-20) 1-benzyl-2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1117] 19 (H2-21) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1118] 19 (H2-22) 1-benzyl-2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1119] 19 (H2-23) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Cannes
    [1120] 19 (H2-24) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1121] 19 (H2-25) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1122] TABLE 2A-4
    [1123] Example number Compound name
    [1124] 19 (H2-26) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1125] 19 (H2-27) 1- (2,2-diphenylethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1126] 19 (H2-28) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1127] 19 (H2-29) 1- (2,2-Diphenylethyl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 Undecan
    [1128] 19 (H2-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1129] 19 (H2-31) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1130] 19 (H2-32) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1131] 19 (H2-33) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1132] 19 (H2-34) 1- (2-phenylethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1133] Table 2A-5
    [1134] Example number Compound name
    [1135] 19 (H2-35) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1136] 19 (H2-36) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1137] 19 (H2-37) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1138] 19 (H2-38) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Cannes
    [1139] 19 (H2-39) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 Undecan
    [1140] 19 (H2-40) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1141] 19 (H2-41) 1-propyl-2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1142] 19 (H2-42) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1143] 19 (H2-43) 1-propyl-2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1144] Table 2A-6
    [1145] Example number Compound name
    [1146] 19 (H2-44) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Cannes
    [1147] 19 (H2-45) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1148] 19 (H2-46) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1149] 19 (H2-47) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1150] 19 (H2-48) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1151] 19 (H2-49) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1152] 19 (H2-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1153] 19 (H2-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1154] Table 2A-7
    [1155] Example number Compound name
    [1156] 19 (H2-52) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1157] 19 (H2-53) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1158] 19 (H2-54) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [1159] 19 (H2-55) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Cannes
    [1160] 19 (H2-56) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1161] 19 (H2-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1162] 19 (H2-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1163] 19 (H2-59) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1164] Table 2A-8
    [1165] Example number Compound name
    [1166] 19 (H2-60) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1167] 19 (H2-61) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1168] Table 3A-1
    [1169] Example number Compound name
    [1170] 19 (H3-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1171] 19 (H3-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1172] 19 (H3-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1173] 19 (H3-4) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1174] 19 (H3-5) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5 Undecan
    [1175] 19 (H3-6) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecan
    [1176] 19 (H3-7) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1177] 19 (H3-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1178] 19 (H3-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1179] Table 3A-2
    [1180] Example number Compound name
    [1181] 19 (H3-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1182] 19 (H3-11) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1183] 19 (H3-12) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecan
    [1184] 19 (H3-13) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1185] 19 (H3-14) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1186] 19 (H3-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1187] 19 (H3-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1188] 19 (H3-17) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1189] Table 3A-3
    [1190] Example number Compound name
    [1191] 19 (H3-18) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1192] 19 (H3-19) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1193] 19 (H3-20) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1194] 19 (H3-21) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1195] 19 (H3-22) 1-benzyl-2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1196] 19 (H3-23) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1197] 19 (H3-24) 1-benzyl-2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1198] 19 (H3-25) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1199] Table 3A-4
    [1200] Example number Compound name
    [1201] 19 (H3-26) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1202] 19 (H3-27) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1203] 19 (H3-28) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecan
    [1204] 19 (H3-29) 1- (2,2-diphenylethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1205] 19 (H3-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1206] 19 (H3-31) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5 Undecan
    [1207] 19 (H3-32) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1208] 19 (H3-33) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1209] 19 (H3-34) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1210] Table 3A-5
    [1211] Example number Compound name
    [1212] 19 (H3-35) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1213] 19 (H3-36) 1- (2-phenylethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1214] 19 (H3-37) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1215] 19 (H3-38) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1216] 19 (H3-39) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1217] 19 (H3-40) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1218] 19 (H3-41) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5 Undecan
    [1219] 19 (H3-42) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1220] 19 (H3-43) 1-propyl-2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1221] Table 3A-6
    [1222] Example number Compound name
    [1223] 19 (H3-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1224] 19 (H3-45) 1-propyl-2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1225] 19 (H3-46) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1226] 19 (H3-47) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1227] 19 (H3-48) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [1228] 19 (H3-49) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecan
    [1229] 19 (H3-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Undecan
    [1230] 19 (H3-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1231] 19 (H3-52) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1232] Table 3A-7
    [1233] Example number Compound name
    [1234] 19 (H3-53) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1235] 19 (H3-54) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1236] 19 (H3-55) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1237] 19 (H3-56) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenyl Profile) -1,4,9-triazaspiro [5.5] Undecan
    [1238] 19 (H3-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [1239] 19 (H3-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1240] 19 (H3-59) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9- (3-phenylpropyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1241] 19 (H3-60) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (3-phenylpropyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1242] Table 3A-8
    [1243] Example number Compound name
    [1244] 19 (H3-61) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9- (3-phenylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1245] 19 (H3-62) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (3-phenylpropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1246] 19 (H3-63) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1247] Table 4A-1
    [1248] Example number Compound name
    [1249] 19 (H4-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1250] 19 (H4-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1251] 19 (H4-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1252] 19 (H4-4) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1253] 19 (H4-5) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1254] 19 (H4-6) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1255] 19 (H4-7) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1256] 19 (H4-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1257] 19 (H4-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1258] Table 4A-2
    [1259] Example number Compound name
    [1260] 19 (H4-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1261] 19 (H4-11) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1262] 19 (H4-12) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1263] 19 (H4-13) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1264] 19 (H4-14) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1265] 19 (H4-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1266] 19 (H4-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1267] 19 (H4-17) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1268] Table 4A-3
    [1269] Example number Compound name
    [1270] 19 (H4-18) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1271] 19 (H4-19) 1- (2- (Indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1272] 19 (H4-20) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1273] 19 (H4-21) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1274] 19 (H4-22) 1-benzyl-2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1275] 19 (H4-23) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1276] 19 (H4-24) 1-benzyl-2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1277] 19 (H4-25) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1278] 19 (H4-26) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1279] Table 4A-4
    [1280] Example number Compound name
    [1281] 19 (H4-27) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1282] 19 (H4-28) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1283] 19 (H4-29) 1- (2,2-diphenylethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1284] 19 (H4-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1285] 19 (H4-31) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1286] 19 (H4-32) 1- (2,2-Diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1287] 19 (H4-33) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1288] 19 (H4-34) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1289] 19 (H4-35) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1290] Table 4A-5
    [1291] Example number Compound name
    [1292] 19 (H4-36) 1- (2-phenylethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1293] 19 (H4-37) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1294] 19 (H4-38) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1295] 19 (H4-39) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1296] 19 (H4-40) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1297] 19 (H4-41) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1298] 19 (H4-42) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1299] 19 (H4-43) 1-propyl-2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1300] 19 (H4-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1301] Table 4A-6
    [1302] Example number Compound name
    [1303] 19 (H4-45) 1-propyl-2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1304] 19 (H4-46) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1305] 19 (H4-47) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1306] 19 (H4-48) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1307] 19 (H4-49) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1308] 19 (H4-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1309] 19 (H4-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1310] 19 (H4-52) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1311] 19 (H4-53) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1312] Table 4A-7
    [1313] Example number Compound name
    [1314] 19 (H4-54) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1315] 19 (H4-55) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1316] 19 (H4-56) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenyl Butyl) -1,4,9-triazaspiro [5.5] undecane
    [1317] 19 (H4-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Cannes
    [1318] 19 (H4-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1319] 19 (H4-59) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1320] 19 (H4-60) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1321] 19 (H4-61) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1322] Table 4A-8
    [1323] Example number Compound name
    [1324] 19 (H4-62) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1325] 19 (H4-63) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenylbutyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1326] Table 5A-1
    [1327] Example number Compound name
    [1328] 19 (H5-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1329] 19 (H5-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] Cannes
    [1330] 19 (H5-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1331] 19 (H5-4) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [5.5 Undecan
    [1332] 19 (H5-5) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1333] 19 (H5-6) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1334] 19 (H5-7) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1335] 19 (H5-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1336] 19 (H5-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5 Undecan
    [1337] TABLE 5A-2
    [1338] Example number Compound name
    [1339] 19 (H5-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1340] 19 (H5-11) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1341] 19 (H5-12) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1342] 19 (H5-13) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1343] 19 (H5-14) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9 -Triaza Spiro [5.5] Undecan
    [1344] 19 (H5-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1345] 19 (H5-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1346] 19 (H5-17) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Cannes
    [1347] 19 (H5-18) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1348] Table 5A-3
    [1349] Example number Compound name
    [1350] 19 (H5-19) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1351] 19 (H5-20) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1352] 19 (H5-21) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4 , 9-triazaspiro [5.5] Undecan
    [1353] 19 (H5-22) 1-benzyl-2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1354] 19 (H5-23) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1355] 19 (H5-24) 1-benzyl-2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1356] 19 (H5-25) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1357] 19 (H5-26) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1358] 19 (H5-27) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1359] Table 5A-4
    [1360] Example number Compound name
    [1361] 19 (H5-28) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1362] 19 (H5-29) 1- (2,2-diphenylethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1363] 19 (H5-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1364] 19 (H5-31) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1365] 19 (H5-32) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1366] 19 (H5-33) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1367] 19 (H5-34) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Cannes
    [1368] 19 (H5-35) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1369] 19 (H5-36) 1- (2-phenylethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1370] Table 5A-5
    [1371] Example number Compound name
    [1372] 19 (H5-37) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1373] 19 (H5-38) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1374] 19 (H5-39) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [5.5] Cannes
    [1375] 19 (H5-40) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1376] 19 (H5-41) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1377] 19 (H5-42) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1378] 19 (H5-43) 1-propyl-2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1379] 19 (H5-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1380] 19 (H5-45) 1-propyl-2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1381] Table 5A-6
    [1382] Example number Compound name
    [1383] 19 (H5-46) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1384] 19 (H5-47) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1385] 19 (H5-48) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1386] 19 (H5-49) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1387] 19 (H5-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9-phenyl-1,4,9-triazaspiro [5.5] undecane
    [1388] 19 (H5-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triaza Spiro [5.5] Undecan
    [1389] 19 (H5-52) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1390] 19 (H5-53) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1391] 19 (H5-54) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5 Undecan
    [1392] Table 5A-7
    [1393] Example number Compound name
    [1394] 19 (H5-55) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1395] 19 (H5-56) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1, 4,9-Triaza spiro [5.5] Undecan
    [1396] 19 (H5-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1397] 19 (H5-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9-phenyl-1,4,9-triazaspiro [5.5] Cannes
    [1398] 19 (H5-59) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-phenyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1399] 19 (H5-60) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9-phenyl-1,4,9-triazaspiro [5.5] Undecan
    [1400] 19 (H5-61) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-phenyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1401] 19 (H5-62) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-phenyl-1,4 , 9-triazaspiro [5.5] Undecan
    [1402] Table 6A-1
    [1403] Example number Compound name
    [1404] 19 (H6-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1405] 19 (H6-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1406] 19 (H6-3) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1407] 19 (H6-4) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1408] 19 (H6-5) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1409] 19 (H6-6) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1410] 19 (H6-7) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1411] 19 (H6-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1412] Table 6A-2
    [1413] Example number Compound name
    [1414] 19 (H6-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1415] 19 (H6-10) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Cannes
    [1416] 19 (H6-11) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1417] 19 (H6-12) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1418] 19 (H6-13) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1419] 19 (H6-14) 1- (2- (Indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1420] 19 (H6-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1421] 19 (H6-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1422] Table 6A-3
    [1423] Example number Compound name
    [1424] 19 (H6-17) 1-benzyl-2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1425] 19 (H6-18) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1426] 19 (H6-19) 1-benzyl-2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1427] 19 (H6-20) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Cannes
    [1428] 19 (H6-21) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1429] 19 (H6-22) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1430] 19 (H6-23) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1431] 19 (H6-24) 1- (2,2-diphenylethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1432] 19 (H6-25) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1433] Table 6A-4
    [1434] Example number Compound name
    [1435] 19 (H6-26) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1436] 19 (H6-27) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1437] 19 (H6-28) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1438] 19 (H6-29) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1439] 19 (H6-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1440] 19 (H6-31) 1- (2-phenylethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1441] 19 (H6-32) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1442] 19 (H6-33) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1443] Table 6A-5
    [1444] Example number Compound name
    [1445] 19 (H6-34) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1446] 19 (H6-35) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Cannes
    [1447] 19 (H6-36) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1448] 19 (H6-37) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1449] 19 (H6-38) 1-propyl-2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1450] 19 (H6-39) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1451] 19 (H6-40) 1-propyl-2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1452] 19 (H6-41) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Cannes
    [1453] 19 (H6-42) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1454] Table 6A-6
    [1455] Example number Compound name
    [1456] 19 (H6-43) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1457] 19 (H6-44) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1458] 19 (H6-45) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1459] 19 (H6-46) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1460] 19 (H6-47) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1461] 19 (H6-48) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1462] 19 (H6-49) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1463] 19 (H6-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxy.carbonylmethyl-9- (5-phenylpentyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1464] Table 6A-7
    [1465] Example number Compound name
    [1466] 19 (H6-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenyl Pentyl) -1,4,9-triazaspiro [5.5] undecane
    [1467] 19 (H6-52) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Cannes
    [1468] 19 (H6-53) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1469] 19 (H6-54) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9- (5-phenylpentyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1470] 19 (H6-55) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1471] 19 (H6-56) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1472] 19 (H6-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1473] 19 (H6-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1474] Table 7A-1
    [1475] Example number Compound name
    [1476] 19 (H7-1) 1- (furan-2-ylmethyl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1477] 19 (H7-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1478] 19 (H7-3) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1479] 19 (H7-4) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1480] 19 (H7-5) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [1481] 19 (H7-6) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1482] 19 (H7-7) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1483] 19 (H7-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1484] 19 (H7-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1485] Table 7A-2
    [1486] Example number Compound name
    [1487] 19 (H7-10) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1488] 19 (H7-11) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1489] 19 (H7-12) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1490] 19 (H7-13) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1491] 19 (H7-14) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1492] 19 (H7-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1493] 19 (H7-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1494] 19 (H7-17) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1495] Table 7A-3
    [1496] Example number Compound name
    [1497] 19 (H7-18) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1498] 19 (H7-19) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1499] 19 (H7-20) 1-benzyl-2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1500] 19 (H7-21) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1501] 19 (H7-22) 1-benzyl-2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1502] 19 (H7-23) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1503] 19 (H7-24) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1504] 19 (H7-25) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1505] 19 (H7-26) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1506] Table 7A-4
    [1507] Example number Compound name
    [1508] 19 (H7-27) 1- (2,2-diphenylethyl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1509] 19 (H7-28) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1510] 19 (H7-29) 1- (2,2-Diphenylethyl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [1511] 19 (H7-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1512] 19 (H7-31) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1513] 19 (H7-32) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1514] 19 (H7-33) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1515] 19 (H7-34) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1516] Table 7A-5
    [1517] Example number Compound name
    [1518] 19 (H7-35) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1519] 19 (H7-36) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1520] 19 (H7-37) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1521] 19 (H7-38) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [1522] 19 (H7-39) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1523] 19 (H7-40) 1-propyl-2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1524] 19 (H7-41) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1525] 19 (H7-42) 1-propyl-2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1526] 19 (H7-43) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1527] Table 7A-6
    [1528] Example number Compound name
    [1529] 19 (H7-44) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1530] 19 (H7-45) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1531] 19 (H7-46) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1532] 19 (H7-47) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1533] 19 (H7-48) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1534] 19 (H7-49) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1535] 19 (H7-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1536] 19 (H7-51) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1537] Table 7A-7
    [1538] Example number Compound name
    [1539] 19 (H7-52) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1540] 19 (H7-53) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenyl Hexyl) -1,4,9-triazaspiro [5.5] undecane
    [1541] 19 (H7-54) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [1542] 19 (H7-55) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1543] 19 (H7-56) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [1544] 19 (H7-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1545] 19 (H7-58) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1546] 19 (H7-59) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1547] Table 7A-8
    [1548] Example number Compound name
    [1549] 19 (H7-60) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1550] Table 8A-1
    [1551] Example number Compound name
    [1552] 19 (H8-1) 1- (furan-2-ylmethyl) -2,5-dioxo-3-benzyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1553] 19 (H8-2) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [5.5 Undecan
    [1554] 19 (H8-3) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1555] 19 (H8-4) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5 Undecan
    [1556] 19 (H8-5) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1557] 19 (H8-6) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1558] 19 (H8-7) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1559] 19 (H8-8) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1560] 19 (H8-9) 1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4,9 -Triaza Spiro [5.5] Undecan
    [1561] Table 8A-2
    [1562] Example number Compound name
    [1563] 19 (H8-10) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1564] 19 (H8-11) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1565] 19 (H8-12) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Cannes
    [1566] 19 (H8-13) 1- (2- (Indol-3-yl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1567] 19 (H8-14) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1568] 19 (H8-15) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1569] 19 (H8-16) 1- (2- (indol-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4 , 9-triazaspiro [5.5] Undecan
    [1570] 19 (H8-17) 1-benzyl-2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1571] 19 (H8-18) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1572] Table 8A-3
    [1573] Example number Compound name
    [1574] 19 (H8-19) 1-benzyl-2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1575] 19 (H8-20) 1-benzyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1576] 19 (H8-21) 1-benzyl-2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1577] 19 (H8-22) 1-benzyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1578] 19 (H8-23) 1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1579] 19 (H8-24) 1- (2,2-diphenylethyl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1580] 19 (H8-25) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1581] 19 (H8-26) 1- (2,2-diphenylethyl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1582] 19 (H8-27) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1583] Table 8A-4
    [1584] Example number Compound name
    [1585] 19 (H8-28) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1586] 19 (H8-29) 1- (2,2-diphenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Cannes
    [1587] 19 (H8-30) 1- (2,2-diphenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1588] 19 (H8-31) 1- (2-phenylethyl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1589] 19 (H8-32) 1- (2-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1590] 19 (H8-33) 1- (2-phenylethyl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1591] 19 (H8-34) 1- (2-phenylethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [5.5] Cannes
    [1592] 19 (H8-35) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1593] 19 (H8-36) 1- (2-phenylethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1594] Table 8A-5
    [1595] Example number Compound name
    [1596] 19 (H8-37) 1- (2-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1597] 19 (H8-38) 1-propyl-2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1598] 19 (H8-39) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1599] 19 (H8-40) 1-propyl-2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1600] 19 (H8-41) 1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1601] 19 (H8-42) 1-propyl-2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1602] 19 (H8-43) 1-propyl-2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1603] 19 (H8-44) 1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1604] 19 (H8-45) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1605] Table 8A-6
    [1606] Example number Compound name
    [1607] 19 (H8-46) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1608] 19 (H8-47) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9- Triaza Spiro [5.5] Undecan
    [1609] 19 (H8-48) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5 Undecan
    [1610] 19 (H8-49) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1611] 19 (H8-50) 1- (2- (t-butyloxycarbonyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1, 4,9-Triaza spiro [5.5] Undecan
    [1612] 19 (H8-51) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-9-methyl-1,4,9-triazaspiro [5.5] undecane
    [1613] 19 (H8-52) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (2-methylpropyl) -9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1614] 19 (H8-53) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-phenylmethyl-9-methyl-1,4,9-triazaspiro [5.5] Cannes
    [1615] 19 (H8-54) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (indol-3-ylmethyl) -9-methyl-1,4,9-tri Azaspiro [5.5] Undecan
    [1616] Table 8A-7
    [1617] Example number Compound name
    [1618] 19 (H8-55) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxymethyl-9-methyl-1,4,9-triazaspiro [5.5] Undecan
    [1619] 19 (H8-56) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3-benzyloxycarbonylmethyl-9-methyl-1,4,9-triazaspiro [ 5.5] Undecan
    [1620] 19 (H8-57) 1- (1-benzylpyrrolidin-3-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methyl-1,4 , 9-triazaspiro [5.5] Undecan
    [1621] Table 9A-1
    [1622] Example number Compound name
    [1623] 19 (H9-1) (3S) -1-cyclopropyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1624] 19 (H9-2) (3S) -1-cyclobutyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1625] 19 (H9-3) (3S) -1-((1S, 2S, 5S) -6,6-dimethylbicyclo [3.1.1] heptan-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1626] 19 (H9-4) (3S) -1-cyclopentyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1627] 19 (H9-5) (3S) -1-cyclohexyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1628] 19 (H9-6) (3S) -1- (cyclohexylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1629] 19 (H9-7) (3S) -1- (2- (1-methylpyrrolidin-2-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl ) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1630] TABLE 9A-2
    [1631] Example number Compound name
    [1632] 19 (H9-8) (3S) -1-((1-ethylpyrrolidin-2-yl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl)- 9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1633] 19 (H9-9) (3S) -1- (Indan-5-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1634] 19 (H9-10) (3S) -1-cycloheptyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1635] 19 (H9-11) (3S) -1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [1636] 19 (H9-12) (3S) -1- (2- (morpholin-4-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1637] 19 (H9-13) (3S) -1- (3- (morpholin-4-yl) propyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1638] 19 (H9-14) (3S) -1- (2- (pyridin-2-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1639] Table 9A-3
    [1640] Example number Compound name
    [1641] 19 (H9-15) (3S) -1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1642] 19 (H9-16) (3S) -1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1643] 19 (H9-17) (3S) -1- (1- (ethoxycarbonyl) piperidin-4-yl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl ) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1644] 19 (H9-18) (3S) -1- (2- (piperidin-1-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1645] 19 (H9-19) (3S) -1- (1-phenylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1646] 19 (H9-20) (3S) -1- (1-methylethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1647] 19 (H9-21) (3S) -1- (1,3-dimethylbutyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1648] TABLE 9A-4
    [1649] Example number Compound name
    [1650] 19 (H9-22) (3S) -1- (1-methyl-3-phenylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1651] 19 (H9-23) (3S) -1- (1-methylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1652] 19 (H9-24) (3S) -1- (1-methylbutyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1653] 19 (H9-25) (3S) -1-((2-fluorophenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1654] 19 (H9-26) (3S) -1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1655] 19 (H9-27) (3S) -1-((3-fluorophenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1656] 19 (H9-28) (3S) -1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1657] Table 9A-5
    [1658] Example number Compound name
    [1659] 19 (H9-29) (3S) -1-((4-fluorophenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1660] 19 (H9-30) (3S) -1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1661] 19 (H9-31) (3S) -1-((4-methylphenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1662] 19 (H9-32) (3S) -1- (2,2-dimethylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1663] 19 (H9-33) (3S) -1- (2-phenylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1664] 19 (H9-34) (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1665] 19 (H9-35) (3S) -1- (2-methylbutyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1666] Table 9A-6
    [1667] Example number Compound name
    [1668] 19 (H9-36) (3S) -1-benzyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1669] 19 (H9-37) (3S) -1- (2- (N, N-dimethylamino) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1670] 19 (H9-38) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1671] 19 (H9-39) (3S) -1- (2-propynyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1672] 19 (H9-40) (3S) -1- (2-propenyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1673] 19 (H9-41) (3S) -1- (3-hydroxypropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1674] 19 (H9-42) (3S) -1- (3-methylbutyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1675] Table 9A-7
    [1676] Example number Compound name
    [1677] 19 (H9-43) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1678] 19 (H9-44) (3S) -1- (3- (N, N-dimethylamino) propyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1679] 19 (H9-45) (3S) -1- (3-ethoxypropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1680] 19 (H9-46) (3S) -1- (3-phenylpropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1681] 19 (H9-47) (3S) -1- (4-phenylbutyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1682] 19 (H9-48) (3S) -1-pentyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1683] 19 (H9-49) (3S) -1- (3- (imidazol-1-yl) propyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1684] Table 9A-8
    [1685] Example number Compound name
    [1686] 19 (H9-50) (3S) -1-butyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1687] 19 (H9-51) (3S) -1- (2- (1-cyclohexenyl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1688] 19 (H9-52) (3S) -1- (cyclopropylmethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1689] 19 (H9-53) (3S) -1-ethyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1690] 19 (H9-54) (3S) -1- (3-methoxypropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1691] 19 (H9-55) (3S) -1- (2- (pyridin-4-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1692] 19 (H9-56) (3S) -1-((3-chlorophenyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [1693] Table 9A-9
    [1694] Example number Compound name
    [1695] 19 (H9-57) (3S) -1- (3-methylthiopropyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1696] 19 (H9-58) (3S) -1- (2- (thiophen-2-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1697] 19 (H9-59) (3S) -1- (2- (1,1-dimethylethylthio) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1698] 19 (H9-60) (3S) -1-((t-butoxycarbonyl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1699] 19 (H9-61) (3S) -1-((5-methylfuran-2-yl) methyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1700] 19 (H9-62) (3S) -1- (2- (pyridin-3-yl) ethyl) -2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1701] TABLE 10A-1
    [1702] Example number Compound name
    [1703] 19 (H10-1) (3S) -1-cyclopropyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1704] 19 (H10-2) (3S) -1-cyclobutyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1705] 19 (H10-3) (3S) -1-((1S, 2S, 5S) -6,6-dimethylbicyclo [3.1.1] heptan-2-ylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1706] 19 (H10-4) (3S) -1-cyclopentyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1707] 19 (H10-5) (3S) -1-cyclohexyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1708] 19 (H10-6) (3S) -1- (cyclohexylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1709] 19 (H10-7) (3S) -1-cyclooctyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1710] TABLE 10A-2
    [1711] Example number Compound name
    [1712] 19 (H10-8) (3S) -1- (2- (1-methylpyrrolidin-2-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl ) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1713] 19 (H10-9) (3S) -1-((1-ethylpyrrolidin-2-yl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl)- 9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1714] 19 (H10-10) (3S) -1- (Indan-5-yl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1715] 19 (H10-11) (3S) -1-cycloheptyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1716] 19 (H10-12) (3S) -1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [1717] 19 (H10-13) (3S) -1- (2- (morpholin-4-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1718] 19 (H10-14) (3S) -1- (3- (morpholin-4-yl) propyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1719] TABLE 10A-3
    [1720] Example number Compound name
    [1721] 19 (H10-15) (3S) -1- (2- (pyridin-2-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1722] 19 (H10-16) (3S) -1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1723] 19 (H10-17) (3S) -1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1724] 19 (H10-18) (3S) -1- (1- (ethoxycarbonyl) piperidin-4-yl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl ) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1725] 19 (H10-19) (3S) -1- (2- (piperidin-1-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1726] 19 (H10-20) (3S) -1-phenyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1727] 19 (H10-21) (3S) -1- (1-phenylethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1728] TABLE 10A-4
    [1729] Example number Compound name
    [1730] 19 (H10-22) (3S) -1- (1-Methylethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1731] 19 (H10-23) (3S) -1- (1,3-dimethylbutyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1732] 19 (H10-24) (3S) -1- (1-methyl-3-phenylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1733] 19 (H10-25) (3S) -1- (1-methylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1734] 19 (H10-26) (3S) -1- (1-ethylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1735] 19 (H10-27) (3S) -1- (1-Methylbutyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1736] 19 (H10-28) (3S) -1-((2-fluorophenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1737] Table 10A-5
    [1738] Example number Compound name
    [1739] 19 (H10-29) (3S) -1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1740] 19 (H10-30) (3S) -1-((3-fluorophenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1741] 19 (H10-31) (3S) -1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1742] 19 (H10-32) (3S) -1-((4-fluorophenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1743] 19 (H10-33) (3S) -1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1744] 19 (H10-34) (3S) -1-((4-methylphenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1745] 19 (H10-35) (3S) -1- (2,2-dimethylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1746] Table 10A-6
    [1747] Example number Compound name
    [1748] 19 (H10-36) (3S) -1- (2-phenylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1749] 19 (H10-37) (3S) -1- (2-Methylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1750] 19 (H10-38) (3S) -1- (2-methylbutyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1751] 19 (H10-39) (3S) -1-Benzyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1752] 19 (H10-40) (3S) -1- (2- (N, N-dimethylamino) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1753] 19 (H10-41) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1754] 19 (H10-42) (3S) -1- (2-propynyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1755] Table 10A-7
    [1756] Example number Compound name
    [1757] 19 (H10-43) (3S) -1- (2-propenyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1758] 19 (H10-44) (3S) -1- (3-hydroxypropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1759] 19 (H10-45) (3S) -1- (3-Methylbutyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1760] 19 (H10-46) (3S) -1-propyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1761] 19 (H10-47) (3S) -1- (3- (N, N-dimethylamino) propyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1762] 19 (H10-48) (3S) -1- (3-ethoxypropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1763] 19 (H10-49) (3S) -1- (3-phenylpropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1764] Table 10A-8
    [1765] Example number Compound name
    [1766] 19 (H10-50) (3S) -1- (4-phenylbutyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1767] 19 (H10-51) (3S) -1-pentyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1768] 19 (H10-52) (3S) -1- (3- (imidazol-1-yl) propyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1769] 19 (H10-53) (3S) -1-Butyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1770] 19 (H10-54) (3S) -1- (2- (1-cyclohexenyl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1771] 19 (H10-55) (3S) -1- (cyclopropylmethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1772] 19 (H10-56) (3S) -1-Ethyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1773] Table 10A-9
    [1774] Example number Compound name
    [1775] 19 (H10-57) (3S) -1- (3-methoxypropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1776] 19 (H10-58) (3S) -1- (2- (N-ethyl-N- (3-methylphenyl) amino) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino ) Propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1777] 19 (H10-59) (3S) -1- (2- (pyridin-4-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1778] 19 (H10-60) (3S) -1-((3-chlorophenyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [1779] 19 (H10-61) (3S) -1- (3-methylthiopropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [1780] 19 (H10-62) (3S) -1- (2- (thiophen-2-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1781] 19 (H10-63) (3S) -1- (2- (1,1-dimethylethylthio) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1782] Table 10A-10
    [1783] Example number Compound name
    [1784] 19 (H10-64) (3S) -1-((t-butoxycarbonyl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1785] 19 (H10-65) (3S) -1-((2S) -2-hydroxypropyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1786] 19 (H10-66) (3S) -1-((5-methylfuran-2-yl) methyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1787] 19 (H10-67) (3S) -1-((1R) -1- (4-methylphenyl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1788] 19 (H10-68) (3S) -1- (2- (pyridin-3-yl) ethyl) -2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [1789] TABLE 11A-1
    [1790] Example number Compound name
    [1791] 19 (H11-1) (3S) -1-cyclopropyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1792] 19 (H11-2) (3S) -1-cyclobutyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1793] 19 (H11-3) (3S) -1-((1S, 2S, 5S) -6,6-dimethylbicyclo [3.1.1] heptan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1794] 19 (H11-4) (3S) -1-cyclopentyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1795] 19 (H11-5) (3S) -1-cyclohexyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1796] 19 (H11-6) (3S) -1- (cyclohexylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1797] 19 (H11-7) (3S) -1- (2- (1-methylpyrrolidin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4 -Phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1798] 19 (H11-8) (3S) -1-((1-ethylpyrrolidin-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyl Butyl) -1,4,9-triazaspiro [5.5] undecane
    [1799] TABLE 11A-2
    [1800] Example number Compound name
    [1801] 19 (H11-9) (3S) -1- (Indan-5-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1802] 19 (H11-10) (3S) -1-cycloheptyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1803] 19 (H11-11) (3S) -1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1804] 19 (H11-12) (3S) -1- (2- (morpholin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1805] 19 (H11-13) (3S) -1- (3- (morpholin-4-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1806] 19 (H11-14) (3S) -1- (2- (pyridin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1807] 19 (H11-15) (3S) -1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1808] Table 11A-3
    [1809] Example number Compound name
    [1810] 19 (H11-16) (3S) -1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1811] 19 (H11-17) (3S) -1- (1- (ethoxycarbonyl) piperidin-4-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (4 -Phenylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [1812] 19 (H11-18) (3S) -1- (2- (piperidin-1-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1813] 19 (H11-19) (3S) -1- (1-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1814] 19 (H11-20) (3S) -1- (1-methylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1815] 19 (H11-21) (3S) -1-((2-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1816] 19 (H11-22) (3S) -1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1817] TABLE 11A-4
    [1818] Example number Compound name
    [1819] 19 (H11-23) (3S) -1-((3-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1820] 19 (H11-24) (3S) -1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1821] 19 (H11-25) (3S) -1-((4-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1822] 19 (H11-26) (3S) -1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1823] 19 (H11-27) (3S) -1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1824] 19 (H11-28) (3S) -1- (2,2-dimethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1825] 19 (H11-29) (3S) -1- (2-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1826] Table 11A-5
    [1827] Example number Compound name
    [1828] 19 (H11-30) (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1829] 19 (H11-31) (3S) -1- (2-Methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1830] 19 (H11-32) (3S) -1-Benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1831] 19 (H11-33) (3S) -1- (2- (N, N-dimethylamino) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1832] 19 (H11-34) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1833] 19 (H11-35) (3S) -1- (2-propynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1834] 19 (H11-36) (3S) -1- (2-propenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1835] 19 (H11-37) (3S) -1- (3-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1836] Table 11A-6
    [1837] Example number Compound name
    [1838] 19 (H11-38) (3S) -1- (3-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1839] 19 (H11-39) (3S) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1840] 19 (H11-40) (3S) -1- (3- (N, N-dimethylamino) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1841] 19 (H11-41) (3S) -1- (3-ethoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1842] 19 (H11-42) (3S) -1- (3-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1843] 19 (H11-43) (3S) -1- (4-phenylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1844] 19 (H11-44) (3S) -1-pentyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1845] 19 (H11-45) (3S) -1- (3- (imidazol-1-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1846] Table 11A-7
    [1847] Example number Compound name
    [1848] 19 (H11-46) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1849] 19 (H11-47) (3S) -1- (2- (1-cyclohexenyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1850] 19 (H11-48) (3S) -1- (cyclopropylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1851] 19 (H11-49) (3S) -1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5 Undecan
    [1852] 19 (H11-50) (3S) -1- (3-methoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1853] 19 (H11-51) (3S) -1- (2- (pyridin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1854] 19 (H11-52) (3S) -1-((3-chlorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1855] 19 (H11-53) (3S) -1- (3-methylthiopropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1856] Table 11A-8
    [1857] Example number Compound name
    [1858] 19 (H11-54) (3S) -1- (2- (thiophen-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1859] 19 (H11-55) (3S) -1- (2- (1,1-dimethylethylthio) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1860] 19 (H11-56) (3S) -1-((t-butoxycarbonyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1861] 19 (H11-57) (3S) -1-((5-methylfuran-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan
    [1862] 19 (H11-58) (3S) -1- (2- (pyridin-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylbutyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1863] TABLE 12A-1
    [1864] Example number Compound name
    [1865] 19 (H12-1) (3S) -1-cyclopropyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1866] 19 (H12-2) (3S) -1-cyclobutyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1867] 19 (H12-3) (3S) -1-((1S, 2S, 5S) -6,6-dimethylbicyclo [3.1.1] heptan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1868] 19 (H12-4) (3S) -1-cyclopentyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1869] 19 (H12-5) (3S) -1-cyclohexyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1870] 19 (H12-6) (3S) -1- (cyclohexylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1871] 19 (H12-7) (3S) -1- (1,2,3,4-tetrahydronaphthyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1872] 19 (H12-8) (3S) -1-cyclooctyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1873] TABLE 12A-2
    [1874] Example number Compound name
    [1875] 19 (H12-9) (3S) -1- (2- (1-methylpyrrolidin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5 -Phenylpentyl) -1,4,9-triazaspiro [5.5] undecane
    [1876] 19 (H12-10) (3S) -1-((1-ethylpyrrolidin-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenyl Pentyl) -1,4,9-triazaspiro [5.5] undecane
    [1877] 19 (H12-11) (3S) -1- (Indan-5-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1878] 19 (H12-12) (3S) -1-cycloheptyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1879] 19 (H12-13) (3S) -1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1880] 19 (H12-14) (3S) -1- (2- (morpholin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1881] 19 (H12-15) (3S) -1- (3- (morpholin-4-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1882] Table 12A-3
    [1883] Example number Compound name
    [1884] 19 (H12-16) (3S) -1- (2- (pyridin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1885] 19 (H12-17) (3S) -1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1886] 19 (H12-18) (3S) -1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1887] 19 (H12-19) (3S) -1- (2- (piperidin-1-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1888] 19 (H12-20) (3S) -1-phenyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1889] 19 (H12-21) (3S) -1- (1-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1890] 19 (H12-22) (3S) -1- (1-Methylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1891] TABLE 12A-4
    [1892] Example number Compound name
    [1893] 19 (H12-23) (3S) -1- (1,3-dimethylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1894] 19 (H12-24) (3S) -1- (1-methyl-3-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1895] 19 (H12-25) (3S) -1- (1-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1896] 19 (H12-26) (3S) -1- (1-ethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1897] 19 (H12-27) (3S) -1- (1-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1898] 19 (H12-28) (3S) -1-((2-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1899] 19 (H12-29) (3S) -1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1900] Table 12A-5
    [1901] Example number Compound name
    [1902] 19 (H12-30) (3S) -1-((3-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1903] 19 (H12-31) (3S) -1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1904] 19 (H12-32) (3S) -1-((4-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1905] 19 (H12-33) (3S) -1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1906] 19 (H12-34) (3S) -1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1907] 19 (H12-35) (3S) -1- (2,2-dimethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1908] 19 (H12-36) (3S) -1- (2-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1909] Table 12A-6
    [1910] Example number Compound name
    [1911] 19 (H12-37) (3S) -1- (2-Methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1912] 19 (H12-38) (3S) -1- (2-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1913] 19 (H12-39) (3S) -1-Benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1914] 19 (H12-40) (3S) -1- (2- (N, N-dimethylamino) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1915] 19 (H12-41) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1916] 19 (H12-42) (3S) -1- (2-propynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1917] 19 (H12-43) (3S) -1- (2-propenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1918] 19 (H12-44) (3S) -1- (3-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1919] Table 12A-7
    [1920] Example number Compound name
    [1921] 19 (H12-45) (3S) -1- (3-Methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1922] 19 (H12-46) (3S) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1923] 19 (H12-47) (3S) -1- (3- (N, N-dimethylamino) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1924] 19 (H12-48) (3S) -1- (3-ethoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1925] 19 (H12-49) (3S) -1- (3-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1926] 19 (H12-50) (3S) -1- (4-phenylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1927] 19 (H12-51) (3S) -1-pentyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1928] 19 (H12-52) (3S) -1- (3- (imidazol-1-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1929] Table 12A-8
    [1930] Example number Compound name
    [1931] 19 (H12-53) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1932] 19 (H12-54) (3S) -1- (2- (1-cyclohexenyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1933] 19 (H12-55) (3S) -1- (Cyclopropylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1934] 19 (H12-56) (3S) -1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5 Undecan
    [1935] 19 (H12-57) (3S) -1- (1-propylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1936] 19 (H12-58) (3S) -1- (3-methoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1937] 19 (H12-59) (3S) -1- (2- (pyridin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1938] 19 (H12-60) (3S) -1-((3-chlorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1939] Table 12A-9
    [1940] Example number Compound name
    [1941] 19 (H12-61) (3S) -1- (3-methylthiopropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1942] 19 (H12-62) (3S) -1- (2- (thiophen-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1943] 19 (H12-63) (3S) -1- (2- (1,1-dimethylethylthio) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1944] 19 (H12-64) (3S) -1-((t-butoxycarbonyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1945] 19 (H12-65) (3S) -1-((2R) -2-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1946] 19 (H12-66) (3S) -1-((2S) -2-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [1947] 19 (H12-67) (3S) -1-((5-methylfuran-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl) -1,4,9-triazaspiro [5.5] Undecan
    [1948] TABLE 12A-10
    [1949] Example number Compound name
    [1950] 19 (H12-68) (3S) -1-((1R) -1- (4-methylphenyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1951] 19 (H12-69) (3S) -1- (2- (pyridin-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylpentyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1952] Table 13A-1
    [1953] Example number Compound name
    [1954] 19 (H13-1) (3S) -1-cyclopropyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1955] 19 (H13-2) (3S) -1-cyclobutyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1956] 19 (H13-3) (3S) -1-((1S, 2S, 5S) -6,6-dimethylbicyclo [3.1.1] heptan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1957] 19 (H13-4) (3S) -1-cyclopentyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1958] 19 (H13-5) (3S) -1-cyclohexyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1959] 19 (H13-6) (3S) -1- (cyclohexylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [1960] 19 (H13-7) (3S) -1- (1,2,3,4-tetrahydronaphthyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1961] 19 (H13-8) (3S) -1-cyclooctyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1962] Table 13A-2
    [1963] Example number Compound name
    [1964] 19 (H13-9) (3S) -1- (2- (1-methylpyrrolidin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6 -Phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1965] 19 (H13-10) (3S) -1-((1-ethylpyrrolidin-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenyl Hexyl) -1,4,9-triazaspiro [5.5] undecane
    [1966] 19 (H13-11) (3S) -1- (Indan-5-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1967] 19 (H13-12) (3S) -1-cycloheptyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [1968] 19 (H13-13) (3S) -1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [1969] 19 (H13-14) (3S) -1- (2- (morpholin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1970] 19 (H13-15) (3S) -1- (3- (morpholin-4-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1971] Table 13A-3
    [1972] Example number Compound name
    [1973] 19 (H13-16) (3S) -1- (2- (pyridin-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl)- 1,4,9-triazaspiro [5.5] Undecan
    [1974] 19 (H13-17) (3S) -1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1975] 19 (H13-18) (3S) -1- (1- (ethoxycarbonyl) piperidin-4-yl) -2,5-dioxo-3- (2-methylpropyl) -9- (6 -Phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [1976] 19 (H13-19) (3S) -1- (2- (piperidin-1-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl ) -1,4,9-triazaspiro [5.5] Undecan
    [1977] 19 (H13-20) (3S) -1- (1-phenylethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1978] 19 (H13-21) (3S) -1- (1,2-dimethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1979] 19 (H13-22) (3S) -1- (1,3-dimethylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1980] Table 13A-4
    [1981] Example number Compound name
    [1982] 19 (H13-23) (3S) -1- (1-ethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1983] 19 (H13-24) (3S) -1-((2-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1984] 19 (H13-25) (3S) -1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1985] 19 (H13-26) (3S) -1-((3-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1986] 19 (H13-27) (3S) -1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1987] 19 (H13-28) (3S) -1-((4-fluorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1988] 19 (H13-29) (3S) -1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [1989] Table 13A-5
    [1990] Example number Compound name
    [1991] 19 (H13-30) (3S) -1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1992] 19 (H13-31) (3S) -1- (2,2-dimethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [1993] 19 (H13-32) (3S) -1- (2-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1994] 19 (H13-33) (3S) -1- (2-Methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1995] 19 (H13-34) (3S) -1- (2-Methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [1996] 19 (H13-35) (3S) -1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [1997] 19 (H13-36) (3S) -1- (2- (N, N-dimethylamino) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [1998] 19 (H13-37) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [1999] Table 13A-6
    [2000] Example number Compound name
    [2001] 19 (H13-38) (3S) -1- (2-propynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2002] 19 (H13-39) (3S) -1- (2-propenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2003] 19 (H13-40) (3S) -1- (3-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2004] 19 (H13-41) (3S) -1- (3-Methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2005] 19 (H13-42) (3S) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [2006] 19 (H13-43) (3S) -1- (3- (N, N-dimethylamino) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [2007] 19 (H13-44) (3S) -1- (3-ethoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2008] 19 (H13-45) (3S) -1- (3-phenylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2009] Table 13A-7
    [2010] Example number Compound name
    [2011] 19 (H13-46) (3S) -1- (4-phenylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2012] 19 (H13-47) (3S) -1-pentyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [2013] 19 (H13-48) (3S) -1- (3- (imidazol-1-yl) propyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [2014] 19 (H13-49) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [2015] 19 (H13-50) (3S) -1- (2- (1-cyclohexenyl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2016] 19 (H13-51) (3S) -1- (cyclopropylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2017] 19 (H13-52) (3S) -1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [2018] 19 (H13-53) (3S) -1- (1-propylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2019] Table 13A-8
    [2020] Example number Compound name
    [2021] 19 (H13-54) (3S) -1- (3-methoxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2022] 19 (H13-55) (3S) -1- (2- (pyridin-4-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2023] 19 (H13-56) (3S) -1-((3-chlorophenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2024] 19 (H13-57) (3S) -1- (3-Methylthiopropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2025] 19 (H13-58) (3S) -1- (2- (thiophen-2-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [2026] 19 (H13-59) (3S) -1- (2- (1,1-dimethylethylthio) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2027] 19 (H13-60) (3S) -1-((t-butoxycarbonyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2028] Table 13A-9
    [2029] Example number Compound name
    [2030] 19 (H13-61) (3S) -1-((5-methylfuran-2-yl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [2031] 19 (H13-62) (3S) -1- (2- (pyridin-3-yl) ethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2032] TABLE 1B-1
    [2033]
    [2034] TABLE 1B-2
    [2035]
    [2036] TABLE 1B-3
    [2037]
    [2038] TABLE 1B-4
    [2039]
    [2040] Table 1B-5
    [2041]
    [2042] TABLE 1B-6
    [2043]
    [2044] TABLE 1B-7
    [2045]
    [2046] TABLE 2B-1
    [2047]
    [2048] TABLE 2B-2
    [2049]
    [2050] Table 2B-3
    [2051]
    [2052] TABLE 2B-4
    [2053]
    [2054] Table 2B-5
    [2055]
    [2056] Table 2B-6
    [2057]
    [2058] Table 2B-7
    [2059]
    [2060] Table 2B-8
    [2061]
    [2062] TABLE 3B-1
    [2063]
    [2064] TABLE 3B-2
    [2065]
    [2066] Table 3B-3
    [2067]
    [2068] Table 3B-4
    [2069]
    [2070] Table 3B-5
    [2071]
    [2072] Table 3B-6
    [2073]
    [2074] Table 3B-7
    [2075]
    [2076] Table 3B-8
    [2077]
    [2078] Table 4B-1
    [2079]
    [2080] Table 4B-2
    [2081]
    [2082] Table 4B-3
    [2083]
    [2084] Table 4B-4
    [2085]
    [2086] Table 4B-5
    [2087]
    [2088] Table 4B-6
    [2089]
    [2090] Table 4B-7
    [2091]
    [2092] Table 4B-8
    [2093]
    [2094] Table 5B-1
    [2095]
    [2096] TABLE 5B-2
    [2097]
    [2098] Table 5B-3
    [2099]
    [2100] Table 5B-4
    [2101]
    [2102] Table 5B-5
    [2103]
    [2104] Table 5B-6
    [2105]
    [2106] Table 5B-7
    [2107]
    [2108] Table 5B-8
    [2109]
    [2110] Table 6B-1
    [2111]
    [2112] Table 6B-2
    [2113]
    [2114] Table 6B-3
    [2115]
    [2116] Table 6B-4
    [2117]
    [2118] Table 6B-5
    [2119]
    [2120] Table 6B-6
    [2121]
    [2122] Table 6B-7
    [2123]
    [2124] Table 6B-8
    [2125]
    [2126] Table 7B-1
    [2127]
    [2128] Table 7B-2
    [2129]
    [2130] Table 7B-3
    [2131]
    [2132] Table 7B-4
    [2133]
    [2134] Table 7B-5
    [2135]
    [2136] Table 7B-6
    [2137]
    [2138] Table 7B-7
    [2139]
    [2140] Table 7B-8
    [2141]
    [2142] Table 8B-1
    [2143]
    [2144] Table 8B-2
    [2145]
    [2146] Table 8B-3
    [2147]
    [2148] Table 8B-4
    [2149]
    [2150] Table 8B-5
    [2151]
    [2152] Table 8B-6
    [2153]
    [2154] Table 8B-7
    [2155]
    [2156] Table 8B-8
    [2157]
    [2158] TABLE 9B-1
    [2159]
    [2160] Table 9B-2
    [2161]
    [2162] Table 9B-3
    [2163]
    [2164] Table 9B-4
    [2165]
    [2166] Table 9B-5
    [2167]
    [2168] Table 9B-6
    [2169]
    [2170] Table 9B-7
    [2171]
    [2172] TABLE 10B-1
    [2173]
    [2174] TABLE 10B-2
    [2175]
    [2176] Table 10B-3
    [2177]
    [2178] TABLE 10B-4
    [2179]
    [2180] Table 10B-5
    [2181]
    [2182] Table 10B-6
    [2183]
    [2184] Table 10B-7
    [2185]
    [2186] Table 10B-8
    [2187]
    [2188] TABLE 11B-1
    [2189]
    [2190] TABLE 11B-2
    [2191]
    [2192] Table 11B-3
    [2193]
    [2194] TABLE 11B-4
    [2195]
    [2196] Table 11B-5
    [2197]
    [2198] Table 11B-6
    [2199]
    [2200] Table 11B-7
    [2201]
    [2202] TABLE 12B-1
    [2203]
    [2204] TABLE 12B-2
    [2205]
    [2206] Table 12B-3
    [2207]
    [2208] TABLE 12B-4
    [2209]
    [2210] Table 12B-5
    [2211]
    [2212] TABLE 12B-6
    [2213]
    [2214] Table 12B-7
    [2215]
    [2216] Table 12B-8
    [2217]
    [2218] TABLE 13B-1
    [2219]
    [2220] TABLE 13B-2
    [2221]
    [2222] Table 13B-3
    [2223]
    [2224] Table 13B-4
    [2225]
    [2226] Table 13B-5
    [2227]
    [2228] Table 13B-6
    [2229]
    [2230] Table 13B-7
    [2231]
    [2232] TABLE 1C-1
    [2233]
    [2234] TABLE 1C-2
    [2235]
    [2236] Table 1C-3
    [2237]
    [2238] TABLE 2C-1
    [2239]
    [2240] TABLE 2C-2
    [2241]
    [2242] Table 2C-3
    [2243]
    [2244] Table 3C-1
    [2245]
    [2246] Table 3C-2
    [2247]
    [2248] Table 3C-3
    [2249]
    [2250] Table 4C-1
    [2251]
    [2252] Table 4C-2
    [2253]
    [2254] Table 4C-3
    [2255]
    [2256] Table 5C-1
    [2257]
    [2258] Table 5C-2
    [2259]
    [2260] Table 5C-3
    [2261]
    [2262] Table 6C-1
    [2263]
    [2264] TABLE 6C-2
    [2265]
    [2266] Table 6C-3
    [2267]
    [2268] Table 7C-1
    [2269]
    [2270] Table 7C-2
    [2271]
    [2272] Table 7C-3
    [2273]
    [2274] Table 8C-1
    [2275]
    [2276] TABLE 8C-2
    [2277]
    [2278] Table 8C-3
    [2279]
    [2280] Table 9C-1
    [2281]
    [2282] Table 9C-2
    [2283]
    [2284] Table 9C-3
    [2285]
    [2286] TABLE 10C-1
    [2287]
    [2288] TABLE 10C-2
    [2289]
    [2290] Table 10C-3
    [2291]
    [2292] TABLE 11C-1
    [2293]
    [2294] TABLE 11C-2
    [2295]
    [2296] Table 11C-3
    [2297]
    [2298] TABLE 12C-1
    [2299]
    [2300] TABLE 12C-2
    [2301]
    [2302] TABLE 12C-4
    [2303]
    [2304] Table 13C-1
    [2305]
    [2306] TABLE 13C-2
    [2307]
    [2308] Table 13C-3
    [2309]
    [2310] Example 20
    [2311] (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (2,4,6-trimethoxybenzyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2312]
    [2313] To a solution of the compound (0.01 g) prepared in Example 8 in dichloroethane (0.2 ml), 2,4,6-trimethoxybenzaldehyde (0.013 g), sodium triacetoxyborohydride (0.015 g), and dimethylformamide ( 0.2 ml) was added. The reaction mixture was stirred at rt for 50 h. The reaction mixture was adsorbed onto an ion exchange resin (OASIS MCX, Waters, 60 mg) previously washed with methanol (3 ml). Washed with methanol (2 ml) and eluted with 10% triethylamine-methanol solution (2 ml). The eluate was concentrated to give a compound of the present invention (4.4 mg) having the following physical properties.
    [2314] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [2315] NMR (CD 3 OD): δ 7.33 (m, 5H), 6.21 (s, 2H), 5.05 (s, 2H), 4.00 (m, 1H), 3.80 (s, 9H), 3.59 (s, 2H), 3.40 (m, 2H), 3.11 (t, J = 6.6 Hz, 2H), 3.05-2.75 (m, 4H), 2.40-2.00 (m, 2H), 2.00-1.70 (m, 4H), 1.65-1.25 ( m, 6H), 0.90 (t, J = 7.2 Hz, 3H).
    [2316] Example 20 (1)
    [2317] (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (2,2-dimethylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2318]
    [2319] In the same manner as in Example 20, using the compound (0.01 g) and pivalaldehyde (8 μl) prepared in Example 8, the compound (2.5 mg) of the present invention having the following physical properties was obtained.
    [2320] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [2321] NMR (CD 3 OD): δ 7.33 (m, 5H), 5.06 (s, 2H), 4.02 (m, 1H), 3.50-3.30 (m, 2H), 3.20-3.00 (m, 4H), 3.00-2.60 (m, 4H), 2.20-2.00 (m, 2H), 1.90-1.70 (m, 3H), 1.70-1.20 (m, 7H), 0.92 (t, J = 7.4 Hz, 3H), 0.90 (s, 9H ).
    [2322] Example 20 (H14-1)-20 (H15-77)
    [2323] In the same manner as in Example 20 using the compound prepared in Example 8 or 8 (1) and the corresponding aldehyde derivative, the compound names are shown in the following Tables 14A-1 to 15A-10 and Tables 14B-1 to 15B-. The compound of this invention which shows a structural formula in 12 was obtained. In addition, the physical properties of these compounds of the present invention are shown in Tables 14C-1 to 15C-3 below.
    [2324] Table 14A-1
    [2325] Example number Compound name
    [2326] 20 (H14-1) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2,4,6-trimethoxyphenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2327] 20 (H14-2) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-cyanophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2328] 20 (H14-3) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methylbutyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2329] 20 (H14-4) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (1-carboxymethyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2330] 20 (H14-5) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-dimethylaminophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2331] 20 (H14-6) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenoxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2332] 20 (H14-7) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E) -2-methylbutenyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2333] Table 14A-2
    [2334] Example number Compound name
    [2335] 20 (H14-8) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1S, 5S) -6,6-dimethyl Bicyclo [3.3.1] -2-hepten-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2336] 20 (H14-9) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (1-carboxymethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2337] 20 (H14-10) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-cyclopropylmethyl-1,4,9-triaza Spiro [5.5] Undecan
    [2338] 20 (H14-11) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methylthiopropyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2339] 20 (H14-12) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-carboxypropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2340] 20 (H14-13) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2,6-dimethyl-5-heptenyl) -1,4,9-triazaspiro [5.5] Undecan
    [2341] 20 (H14-14) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (quinolin-2-yl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2342] Table 14A-3
    [2343] Example number Compound name
    [2344] 20 (H14-15) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2S, 3R, 4R, 5R) -2 -Acetylamino-3,4,5,6-tetrahydroxyhexanyl) -1,4,9-triazaspiro [5.5] undecane
    [2345] 20 (H14-16) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2,2-dimethylpropyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2346] 20 (H14-17) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4Z) -decenyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2347] 20 (H14-18) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2348] 20 (H14-19) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-butyl-1,4,9-triazaspiro [ 5.5] Undecan
    [2349] 20 (H14-20) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzyl-1,4,9-triazaspiro [ 5.5] Undecan
    [2350] 20 (H14-21) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E) -3- (4-dimethylamino Phenyl) propenyl) -1,4,9-triazaspiro [5.5] undecane
    [2351] Table 14A-4
    [2352] Example number Compound name
    [2353] 20 (H14-22) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E) -3- (furan-2- I) propenyl) -1,4,9-triazaspiro [5.5] undecane
    [2354] 20 (H14-23) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-hydroxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2355] 20 (H14-24) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-hydroxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2356] 20 (H14-25) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-dihydroxyboranephenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2357] 20 (H14-26) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-heptyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2358] 20 (H14-27) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (benzofuran-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2359] 20 (H14-28) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methylbenzothiophen-2-ylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2360] Table 14A-5
    [2361] Example number Compound name
    [2362] 20 (H14-29) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (4-chlorophenylthio) phenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2363] 20 (H14-30) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,7-dimethyl-6-octenyl) -1,4,9-triazaspiro [5.5] Undecan
    [2364] 20 (H14-31) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4- (pyrrolidin-1-yl) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2365] 20 (H14-32) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methyl-3- (4- (2 , 2-dimethylpropyl) phenyl) propyl) -1,4,9-triazaspiro [5.5] undecane
    [2366] 20 (H14-33) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-benzyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2367] 20 (H14-34) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-hydroxy-3,5-bis ( 1,1-dimethylethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2368] Table 14A-6
    [2369] Example number Compound name
    [2370] 20 (H14-35) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methyl-3- (4- (1 -Methylethyl) phenyl) propyl) -1,4,9-triazaspiro [5.5] undecane
    [2371] 20 (H14-36) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,4-di- (benzyloxy) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [2372] 20 (H14-37) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-octyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2373] 20 (H14-38) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,5,5-trimethylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2374] 20 (H14-39) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-butyloxycarbonylmethyl-1,4,9- Triaza Spiro [5.5] Undecan
    [2375] 20 (H14-40) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4- (4-hydroxy-4-methyl Pentyl) -3-cyclohexenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2376] 20 (H14-41) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (5-hydroxypentyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2377] Table 14A-7
    [2378] Example number Compound name
    [2379] 20 (H14-42) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-((1R, 2S, 3R, 5R ) -2-hydroxy-4,6,8-trioxaspiro [bicyclo [3.3.0] octane-7,1'-cyclohexane] -3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2380] 20 (H14-43) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2381] 20 (H14-44) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4- (1,1-dimethylethyl) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [2382] 20 (H14-45) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (1,4-benzodioxan-6-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [2383] 20 (H14-46) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (2,2,6-trimethyl- 1-cyclohexenyl) ethyl) -1,4,9-triazaspiro [5.5] undecane
    [2384] 20 (H14-47) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4- (3-dimethylaminopropyloxy) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [2385] Table 14A-8
    [2386] Example number Compound name
    [2387] 20 (H14-48) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2388] 20 (H14-49) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methylpropyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2389] 20 (H14-50) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-cyclohexylmethyl-1,4,9-triaza Spiro [5.5] Undecan
    [2390] 20 (H14-51) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (thiazol-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2391] 20 (H14-52) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-acetylaminophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2392] 20 (H14-53) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methoxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2393] 20 (H14-54) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-methoxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2394] Table 14A-9
    [2395] Example number Compound name
    [2396] 20 (H14-55) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-biphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2397] 20 (H14-56) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E, 6E) -3,7-dimethyl -2,6-octadienyl) -1,4,9-triazaspiro [5.5] undecane
    [2398] 20 (H14-57) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-dimethylaminophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2399] 20 (H14-58) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-ethylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2400] 20 (H14-59) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-fluorophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2401] 20 (H14-60) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-hydroxyethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2402] 20 (H14-61) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (naphthalen-1-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2403] Table 14A-10
    [2404] Example number Compound name
    [2405] 20 (H14-62) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-propyl-1,4,9-triazaspiro [ 5.5] Undecan
    [2406] 20 (H14-63) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2S, 3S, 4R) -2,3 , 4,5-tetrahydroxypentyl) -1,4,9-triazaspiro [5.5] undecane
    [2407] 20 (H14-64) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (thiophen-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2408] 20 (H14-65) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E) -decenyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2409] 20 (H14-66) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-chlorophenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2410] 20 (H14-67) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (1,3-benzodioxene-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [2411] 20 (H14-68) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3S, 4R) -3,4,5 -Trihydroxypentyl) -1,4,9-triazaspiro [5.5] undecane
    [2412] TABLE 14A-11
    [2413] Example number Compound name
    [2414] 20 (H14-69) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2,3-dimethyl-5-oxo-1 -Phenyl-3-pyrazolin-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2415] 20 (H14-70) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-((2E) -4-methylphene Tenyl) -3-cyclohexenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2416] 20 (H14-71) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methoxy-4-hexyloxyphenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2417] 20 (H14-72) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-fluorophenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2418] 20 (H14-73) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,5,6-trimethyl-3-cyclo Hexenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2419] 20 (H14-74) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,5-dimethyl-1-phenylpyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2420] 20 (H14-75) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-benzyloxyethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2421] TABLE 14A-12
    [2422] Example number Compound name
    [2423] 20 (H14-76) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methoxy-4-benzyloxyphenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2424] 20 (H14-77) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-benzyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2425] 20 (H14-78) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-benzyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2426] 20 (H14-79) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-phenyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2427] 20 (H14-80) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-allyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2428] Table 15A-1
    [2429] Example number Compound name
    [2430] 20 (H15-1) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,4,6-trimethoxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2431] 20 (H15-2) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-cyanophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2432] 20 (H15-3) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylbutyl) -1,4,9-triazaspiro [5.5] undecane
    [2433] 20 (H15-4) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (1-carboxymethyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2434] 20 (H15-5) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dimethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2435] 20 (H15-6) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-phenoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2436] 20 (H15-7) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2E) -2-methylbutenyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2437] 20 (H15-8) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1S, 5S) -6,6-dimethylbicyclo [3.3.1] -2- Hepten-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2438] Table 15A-2
    [2439] Example number Compound name
    [2440] 20 (H15-9) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-carboxymethyl) -1,4,9-triazaspiro [5.5] undecane
    [2441] 20 (H15-10) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-cyclopropylmethyl-1,4,9-triazaspiro [5.5] undecane
    [2442] 20 (H15-11) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylthiopropyl) -1,4,9-triazaspiro [5.5] undecane
    [2443] 20 (H15-12) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-carboxypropyl) -1,4,9-triazaspiro [5.5] undecane
    [2444] 20 (H15-13) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,6-dimethyl-5-heptenyl) -1,4,9-triazaspiro [5.5] Undecan
    [2445] 20 (H15-14) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (quinolin-2-yl) -1,4,9-triazaspiro [5.5] undecane
    [2446] 20 (H15-15) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2S, 3R, 4R, 5R) -2-acetylamino-3,4,5, 6-tetrahydroxyhexanyl) -1,4,9-triazaspiro [5.5] undecane
    [2447] 20 (H15-16) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,2-dimethylpropyl) -1,4,9-triazaspiro [5.5] Cannes
    [2448] 20 (H15-17) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4Z) -decenyl) -1,4,9-triazaspiro [5.5] Cannes
    [2449] Table 15A-3
    [2450] Example number Compound name
    [2451] 20 (H15-18) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [2452] 20 (H15-19) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-butyl-1,4,9-triazaspiro [5.5] undecane
    [2453] 20 (H15-20) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [2454] 20 (H15-21) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2E) -3- (furan-2-yl) propenyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2455] 20 (H15-22) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2456] 20 (H15-23) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2457] 20 (H15-24) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dihydroxyboranephenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [2458] 20 (H15-25) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-heptyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2459] 20 (H15-26) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (benzofuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2460] Table 15A-4
    [2461] Example number Compound name
    [2462] 20 (H15-27) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylbenzothiophen-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2463] 20 (H15-28) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-chlorophenylthio) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2464] 20 (H15-29) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,7-dimethyl-6-octenyl) -1,4,9-triazaspiro [5.5] Undecan
    [2465] 20 (H15-30) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrrolidin-1-yl) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2466] 20 (H15-31) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methyl-3- (4- (2,2-dimethylpropyl) phenyl) propyl) -1,4,9-triazaspiro [5.5] Undecan
    [2467] 20 (H15-32) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2468] 20 (H15-33) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-hydroxy-3,5-di- (1,1-dimethylethyl) phenylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2469] 20 (H15-34) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methyl-3- (4- (1-methylethyl) phenyl) propyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2470] Table 15A-5
    [2471] Example number Compound name
    [2472] 20 (H15-35) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,4-di- (benzyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2473] 20 (H15-36) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-octyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2474] 20 (H15-37) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5,5-trimethylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [2475] 20 (H15-38) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-butyloxycarbonylmethyl-1,4,9-triazaspiro [5.5] undecane
    [2476] 20 (H15-39) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-hydroxy-4-methylpentyl) -3-cyclohexenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2477] 20 (H15-40) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-hydroxypentyl) -1,4,9-triazaspiro [5.5] undecane
    [2478] 20 (H15-41) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-((1R, 2S, 3R, 5R) -2-hydroxy-4,6 , 8-trioxaspiro [bicyclo [3.3.0] octane-7,1'-cyclohexane] -3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2479] 20 (H15-42) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2480] Table 15A-6
    [2481] Example number Compound name
    [2482] 20 (H15-43) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1,1-dimethylethyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2483] 20 (H15-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2484] 20 (H15-45) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (2,2,6-trimethyl-1-cyclohexenyl) ethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2485] 20 (H15-46) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-dimethylaminopropyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2486] 20 (H15-47) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2487] 20 (H15-48) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane
    [2488] 20 (H15-49) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane
    [2489] 20 (H15-50) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (thiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2490] Table 15A-7
    [2491] Example number Compound name
    [2492] 20 (H15-51) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-acetylaminophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2493] 20 (H15-52) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2494] 20 (H15-53) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2495] 20 (H15-54) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-biphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2496] 20 (H15-55) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-ethylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [2497] 20 (H15-56) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2498] 20 (H15-57) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-hydroxyethyl) -1,4,9-triazaspiro [5.5] undecane
    [2499] 20 (H15-58) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (naphthalen-1-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2500] 20 (H15-59) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-propyl-1,4,9-triazaspiro [5.5] undecane
    [2501] Table 15A-8
    [2502] Example number Compound name
    [2503] 20 (H15-60) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2S, 3S, 4R) -2,3,4,5-tetrahydroxypentyl) -1,4,9-triazaspiro [5.5] Undecan
    [2504] 20 (H15-61) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (thiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2505] 20 (H15-62) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2E) -decenyl) -1,4,9-triazaspiro [5.5] Cannes
    [2506] 20 (H15-63) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [2507] 20 (H15-64) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,3-benzodioxoren-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2508] 20 (H15-65) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3S, 4R) -3,4,5-trihydroxypentyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2509] 20 (H15-66) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,3-dimethyl-5-oxo-1-phenyl-3-pyrazoline-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [2510] 20 (H15-67) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-((2E) -4-methylpentenyl) -3-cyclohexenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [2511] Table 15A-9
    [2512] Example number Compound name
    [2513] 20 (H15-68) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methoxy-4-hexyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2514] 20 (H15-69) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2515] 20 (H15-70) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5,6-trimethyl-3-cyclohexenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2516] 20 (H15-71) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2517] 20 (H15-72) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-benzyloxyethyl) -1,4,9-triazaspiro [5.5] undecane
    [2518] 20 (H15-73) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methoxy-4-benzyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2519] 20 (H15-74) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2520] 20 (H15-75) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2521] Table 15A-10
    [2522] Example number Compound name
    [2523] 20 (H15-76) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2524] 20 (H15-77) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-allyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [2525] Table 14B-1
    [2526]
    [2527] Table 14B-2
    [2528]
    [2529] Table 14B-3
    [2530]
    [2531] Table 14B-4
    [2532]
    [2533] Table 14B-5
    [2534]
    [2535] Table 14B-6
    [2536]
    [2537] Table 14B-7
    [2538]
    [2539] Table 14B-8
    [2540]
    [2541] Table 14B-9
    [2542]
    [2543] Table 14B-10
    [2544]
    [2545] Table 14B-11
    [2546]
    [2547] Table 15B-1
    [2548]
    [2549] Table 15B-2
    [2550]
    [2551] Table 15B-3
    [2552]
    [2553] Table 15B-4
    [2554]
    [2555] Table 15B-5
    [2556]
    [2557] Table 15B-6
    [2558]
    [2559] Table 15B-7
    [2560]
    [2561] Table 15B-8
    [2562]
    [2563] Table 15B-9
    [2564]
    [2565] Table 15B-10
    [2566]
    [2567] Table 15B-11
    [2568]
    [2569] TABLE 15B-12
    [2570]
    [2571] Table 14C-1
    [2572]
    [2573] Table 14C-2
    [2574]
    [2575] Table 14C-3
    [2576]
    [2577] Table 14C-4
    [2578]
    [2579] Table 15C-1
    [2580]
    [2581] TABLE 15C-2
    [2582]
    [2583] Table 15C-3
    [2584]
    [2585] Example 21
    [2586] (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (3-phenylpropanoyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2587]
    [2588] Diisopropylethylamine (6 μl) and 3-phenylpropanoylchloride (5 μl) were added to a dichloroethane (0.2 ml) solution of the compound (0.01 g) prepared in Example 8. The reaction mixture was stirred at rt for 1 h. The reaction mixture was added to aminomethylated polystyrene-2% divinylbenzene copolymer resin (NovaBiochem, AM Resin, 50 mg), washed with dichloroethane and filtered. The filtrate was concentrated to obtain the compound of the present invention (14 mg) having the following physical properties.
    [2589] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [2590] NMR (CD 3 OD): δ 7.40-7.10 (m, 10H), 5.06 (s, 2H), 4.03 (m, 1H), 3.70-3.55 (m, 2H), 3.28-3.00 (m, 5H), 3.00 -2.80 (m, 3H), 2.80-2.60 (m, 2H), 2.00-1.65 (m, 6H), 1.65-1.40 (m, 6H), 0.90 (t, J = 7.2 Hz, 3H).
    [2591] Example 21 (1)
    [2592] (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9-benzenesulfonyl-1,4,9-triazaspiro [5.5] undecane
    [2593]
    [2594] Using the compound (0.01 g) and diisopropylethylamine (6 μl) benzenesulfonyl chloride (4.5 μl) prepared in Example 8, the same operation as in Example 21 was carried out to obtain the present compound having the following physical properties (16 mg).
    [2595] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [2596] NMR (CD 3 OD): δ 7.80 (m, 2H), 7.63 (m, 3H), 7.33 (m, 5H), 5.04 (s, 2H), 3.98 (t, J = 4.8 Hz, 1H), 3.60- 3.35 (m, 2H), 3.28-2.90 (m, 6H), 2.20-1.65 (m, 6H), 1.65-1.20 (m, 6H), 0.89 (t, J = 7.2 Hz, 3H).
    [2597] Example 21 (2)
    [2598] (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9-benzylaminocarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2599]
    [2600] Using the compound prepared in Example 8 (0.01 g) and benzyl isocyanate (4 μl), the same operation as in Example 21 was carried out to obtain a compound of the present invention (16 mg) having the following physical properties.
    [2601] TLC: Rf 0.45 (CHCl 3: MeOH = 10: 1);
    [2602] NMR (CD 3 OD): δ 7.40-7.10 (m, 10H), 5.05 (s, 2H), 4.37 (s, 2H), 4.10-3.90 (m, 3H), 3.60-3.45 (m, 2H), 3.30 -3.00 (m, 4H), 2.10-1.70 (m, 6H), 1.65-1.20 (m, 6H), 0.87 (t, J = 7.4 Hz, 3H).
    [2603] Example 21 (H16-1)-21 (H19-71)
    [2604] Using the compound prepared in Example 8 or 8 (1) and the corresponding acid chloride derivative, sulfonyl chloride derivative or isocyanate derivative, the same operation as in Example 21, 21 (1) or 21 (2) was performed. The compound of this invention which showed the compound name in 16A-1-19A-9, and showed the structural formula in Table 16B-1-19B-11 was obtained. In addition, the physical properties of these compounds of the present invention are shown in Tables 16C-1 to 19C-3 below.
    [2605] TABLE 16A-1
    [2606] Example number Compound name
    [2607] 21 (H16-1) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-phenylphenyl) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2608] 21 (H16-2) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-dimethylaminophenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2609] 21 (H16-3) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3- (2-chlorophenyl) -5 -Methylisoxazol-4-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2610] 21 (H16-4) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-fluorophenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2611] 21 (H16-5) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-fluorophenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2612] 21 (H16-6) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-fluorophenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2613] 21 (H16-7) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (cyclopentylcarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2614] TABLE 16A-2
    [2615] Example number Compound name
    [2616] 21 (H16-8) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-methylphenyl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2617] 21 (H16-9) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-methoxyphenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2618] 21 (H16-10) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2,2-dimethylpropanoyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2619] 21 (H16-11) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (pyridin-3-ylcarbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2620] 21 (H16-12) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (pyridin-4-ylcarbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2621] 21 (H16-13) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (pyridin-2-ylcarbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2622] 21 (H16-14) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylacetyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2623] Table 16A-3
    [2624] Example number Compound name
    [2625] 21 (H16-15) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenyloxyacetyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2626] 21 (H16-16) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-ethyl-2,3-dioxopy Ferrazinyl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2627] 21 (H16-17) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-phenylthiopyridin-3-yl) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2628] 21 (H16-18) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-phenyloxypyridin-3-yl) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2629] 21 (H16-19) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methoxyphenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2630] 21 (H16-20) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (thiophen-2-yl) acetyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2631] 21 (H16-21) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-hexanoyl-1,4,9-triazaspiro [5.5] Undecan
    [2632] TABLE 16A-4
    [2633] Example number Compound name
    [2634] 21 (H16-22) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methylphenyl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2635] 21 (H16-23) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methylpropanoyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2636] 21 (H16-24) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-cyclopentylpropanoyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2637] 21 (H16-25) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2E) 3-phenyl-2-prope Noil) -1,4,9-triazaspiro [5.5] Undecan
    [2638] 21 (H16-26) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methylphenyl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2639] 21 (H16-27) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3,3-dimethylbutenoyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2640] 21 (H16-28) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (cyclohexylcarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2641] Table 16A-5
    [2642] Example number Compound name
    [2643] 21 (H16-29) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (phenylcarbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2644] 21 (H16-30) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (thiophen-2-ylcarbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2645] 21 (H16-31) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,6,6-trimethyl-1- Cyclohexenyl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2646] 21 (H16-32) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (ethoxyoxalyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2647] 21 (H16-33) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-phenyl-5-methylisoxazole- 4-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2648] 21 (H16-34) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((5-methyl-2-phenyl-1, 2,3-triazol-4-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2649] 21 (H16-35) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (3-methoxyphenyl) acetyl) -1,4,9-triazaspiro [5.5] Undecan
    [2650] TABLE 16A-6
    [2651] Example number Compound name
    [2652] 21 (H16-36) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-methoxyphenylcarbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2653] 21 (H16-37) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((furan-2-yl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2654] 21 (H16-38) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-benzyloxyacetyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2655] 21 (H16-39) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (cyclobutylcarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2656] 21 (H16-40) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2- (4-methoxyphenyl) acetyl) -1,4,9-triazaspiro [5.5] Undecan
    [2657] 21 (H16-41) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-acetyl-1,4,9-triazaspiro [ 5.5] Undecan
    [2658] 21 (H16-42) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (4-methylpentanol) -1,4, 9-Triaza spiro [5.5] Undecan
    [2659] TABLE 16A-7
    [2660] Example number Compound name
    [2661] 21 (H16-43) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-methoxyacetyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2662] 21 (H16-44) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methylthiopropanoyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2663] 21 (H16-45) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((isoxazol-5-yl) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2664] 21 (H16-46) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-cyclopentylacetyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2665] 21 (H16-47) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-pentanol-1,4,9-triazaspiro [5.5] Undecan
    [2666] 21 (H16-48) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (3-methylbutanoyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2667] 21 (H16-49) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylthioacetyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2668] Table 16A-8
    [2669] Example number Compound name
    [2670] 21 (H16-50) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methyl-1,2,3- Thiadiazol-5-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2671] 21 (H16-51) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-cyanophenyl) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2672] 21 (H16-52) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-butanol-1,4,9-triazaspiro [ 5.5] Undecan
    [2673] 21 (H16-53) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-propanoyl-1,4,9-triaza Spiro [5.5] Undecan
    [2674] 21 (H16-54) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (cyclopropylcarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2675] 21 (H16-55) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2H-benzo [3,4-d] 1 , 3-dioxolane-5-ylcarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2676] 21 (H16-56) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1-phenyl-5-propylpyrazole- 4-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2677] Table 16A-9
    [2678] Example number Compound name
    [2679] 21 (H16-57) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((5- (1,1-dimethylethyl) -2-methylfuran-3-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2680] 21 (H16-58) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1- (1,1-dimethylethyl) -3-methylpyrazol-5-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2681] 21 (H16-59) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-methylsulfonyl-1,4,9-triaza Spiro [5.5] Undecan
    [2682] 21 (H16-60) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-pentylsulfonyl-1,4,9-triaza Spiro [5.5] Undecan
    [2683] 21 (H16-61) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1-methylethyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2684] 21 (H16-62) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-chlorophenyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2685] 21 (H16-63) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-iodinephenyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2686] TABLE 16A-10
    [2687] Example number Compound name
    [2688] 21 (H16-64) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-nitrophenyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2689] 21 (H16-65) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methylsulfonylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2690] 21 (H16-66) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-trifluoromethylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2691] 21 (H16-67) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-biphenyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2692] 21 (H16-68) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-biphenyl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2693] 21 (H16-69) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methoxycarbonylphenyl) sulfonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2694] 21 (H16-70) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3,4-difluorophenyl) sul Ponyl) -1,4,9-triazaspiro [5.5] undecane
    [2695] TABLE 16A-11
    [2696] Example number Compound name
    [2697] 21 (H16-71) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,6-difluorophenyl) sul Ponyl) -1,4,9-triazaspiro [5.5] undecane
    [2698] 21 (H16-72) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,5-difluorophenyl) sul Ponyl) -1,4,9-triazaspiro [5.5] undecane
    [2699] 21 (H16-73) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,5-dimethoxyphenyl) sulfonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2700] 21 (H16-74) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-chloro-4-trifluoromethylphenyl ) Sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2701] 21 (H16-75) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-naphthylsulfonyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2702] 21 (H16-76) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-(((1E) -2-phenylvinyl) sulphate Ponyl) -1,4,9-triazaspiro [5.5] undecane
    [2703] 21 (H16-77) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((furan-2-yl) sulfonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2704] TABLE 16A-12
    [2705] Example number Compound name
    [2706] 21 (H16-78) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((thiophen-2-yl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2707] TABLE 17A-1
    [2708] Example number Compound name
    [2709] 21 (H17-1) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-bromo-2,5-dichloro Thiophen-3-yl) sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2710] 21 (H17-2) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((5-phenylsulfonylthiophen-2-yl ) Sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2711] 21 (H17-3) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((7-chlorobenzoprazan-4-yl ) Sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2712] 21 (H17-4) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methyl-2-acetylaminothiazole -5-yl) sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2713] 21 (H17-5) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methoxy-dibenzofuran-3 -Yl) sulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2714] 21 (H17-6) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3,4-dichlorophenyl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2715] 21 (H17-7) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methoxyphenyl) sulfonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2716] TABLE 17A-2
    [2717] Example number Compound name
    [2718] 21 (H17-8) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-benzylsulfonyl-1,4,9-triaza Spiro [5.5] Undecan
    [2719] 21 (H17-9) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((ethylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2720] 21 (H17-10) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((propylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2721] 21 (H17-11) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1-methylethylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2722] 21 (H17-12) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((ethoxycarbonylmethylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2723] 21 (H17-13) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((butylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2724] 21 (H17-14) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-chlorophenylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2725] Table 17A-3
    [2726] Example number Compound name
    [2727] 21 (H17-15) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((phenylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2728] 21 (H17-16) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methylphenylamino) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2729] 21 (H17-17) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((hexylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2730] 21 (H17-18) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-fluorophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2731] 21 (H17-19) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((benzylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2732] 21 (H17-20) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((cyclohexylamino) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2733] 21 (H17-21) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-methylphenylamino) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2734] TABLE 17A-4
    [2735] Example number Compound name
    [2736] 21 (H17-22) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((octylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2737] 21 (H17-23) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-bromophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2738] 21 (H17-24) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2- (thiophen-2-yl) Ethylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2739] 21 (H17-25) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4- (1-methylethyl) phenylamino ) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2740] 21 (H17-26) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-chlorophenylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2741] 21 (H17-27) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,4,5-trimethylphenylamino) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2742] 21 (H17-28) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,4,6-trimethylphenylamino) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2743] Table 17A-5
    [2744] Example number Compound name
    [2745] 21 (H17-29) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-phenyloxyphenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2746] 21 (H17-30) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-butyloxyphenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2747] 21 (H17-31) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-phenylphenylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2748] 21 (H17-32) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-phenylphenylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2749] 21 (H17-33) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-trifluoromethylphenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2750] 21 (H17-34) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3,4-dichlorophenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2751] 21 (H17-35) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-butyloxycarbonylphenylamino) carb Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2752] Table 17A-6
    [2753] Example number Compound name
    [2754] 21 (H17-36) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,6-di (1-methylethyl ) Phenylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2755] 21 (H17-37) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,5-dimethylphenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2756] 21 (H17-38) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-ethyl-6- (1-methyl Ethyl) phenylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2757] 21 (H17-39) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,4,6-trichlorophenylamino ) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2758] 21 (H17-40) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3,4-dimethylphenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2759] 21 (H17-41) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methylthiophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2760] 21 (H17-42) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-methylthiophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2761] Table 17A-7
    [2762] Example number Compound name
    [2763] 21 (H17-43) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((4-butylphenylamino) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2764] 21 (H17-44) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-chloro-5-trifluoromethylphenyl Amino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2765] 21 (H17-45) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,6-dibromo-4- Ethylphenylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2766] 21 (H17-46) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1-ethoxycarbonyl-2-methyl Propylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2767] 21 (H17-47) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((phenylcarbonylamino) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2768] 21 (H17-48) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,4,6-tribromophenyl Amino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2769] 21 (H17-49) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,5-difluorophenylamino) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2770] Table 17A-8
    [2771] Example number Compound name
    [2772] 21 (H17-50) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3,5-bis (methoxycarbonyl ) Phenylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2773] 21 (H17-51) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((6,7-methylenedioxycoumarin-4 -Ylmethylamino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2774] 21 (H17-52) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,6-dimethylphenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2775] 21 (H17-53) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methylpropyloxy) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2776] 21 (H17-54) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-ethylhexyloxy) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2777] 21 (H17-55) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (ethoxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2778] 21 (H17-56) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (allyloxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2779] Table 17A-9
    [2780] Example number Compound name
    [2781] 21 (H17-57) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (propyloxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2782] 21 (H17-58) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (butyloxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2783] 21 (H17-59) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (hexyloxycarbonyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2784] 21 (H17-60) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2,2,2-trichloroethyloxy ) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2785] 21 (H17-61) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((fluorene-9-ylmethyloxy) car Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2786] 21 (H17-62) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1R, 5R, 2S) -5-methyl 2- (1-methylethyl) cyclohexyloxycarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2787] 21 (H17-63) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2-methoxyethoxy) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2788] Table 17A-10
    [2789] Example number Compound name
    [2790] 21 (H17-64) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (pentyloxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2791] 21 (H17-65) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1-methylethyloxy) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2792] 21 (H17-66) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((3-butenyloxy) carbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2793] 21 (H17-67) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((2R, 1S, 5S) -methyl-2 -(1-methylethyl) cyclohexyloxycarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2794] 21 (H17-68) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (cyclopentyloxycarbonyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2795] 21 (H17-69) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((1,1-dimethylethyloxy) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2796] 21 (H17-70) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (benzyloxycarbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2797] TABLE 17A-11
    [2798] Example number Compound name
    [2799] 21 (H17-71) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((N, N-diphenylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2800] 21 (H17-72) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((N-phenyl-N-methylamino) car Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2801] 21 (H17-73) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((N, N-dimethylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2802] 21 (H17-74) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((N, N-diethylamino) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2803] 21 (H17-75) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9-((N, N-bis (1-methylethyl ) Amino) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2804] 21 (H17-76) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (morpholin-4-ylcarbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2805] 21 (H17-77) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (carbazole-9-ylcarbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2806] TABLE 17A-12
    [2807] Example number Compound name
    [2808] 21 (H17-78) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (pyrrolidin-1-ylcarbonyl)- 1,4,9-triazaspiro [5.5] Undecan
    [2809] Table 18A-1
    [2810] Example Number Compound Name
    [2811] 21 (H18-1) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-biphenyl) carbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2812] 21 (H18-2) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4,7,7-trimethyl-2-oxa-3-oxobicyclo [2.2. 1] heptan-1-yl) carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2813] 21 (H18-3) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-dimethylaminophenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2814] 21 (H18-4) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3- (2-chlorophenyl) -5-methylisoxazol-4-yl) car Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2815] 21 (H18-5) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-fluorophenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2816] 21 (H18-6) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-fluorophenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2817] 21 (H18-7) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-fluorophenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2818] 21 (H18-8) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (cyclopentylcarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2819] Table 18A-2
    [2820] Example number Compound name
    [2821] 21 (H18-9) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-methylphenyl) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2822] 21 (H18-10) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-methoxyphenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2823] 21 (H18-11) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,2-dimethylpropanoyl) -1,4,9-triazaspiro [5.5 Undecan
    [2824] 21 (H18-12) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (pyridin-3-ylcarbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2825] 21 (H18-13) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (pyridin-2-ylcarbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2826] 21 (H18-14) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2827] 21 (H18-15) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenyloxyacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2828] 21 (H18-16) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-ethyl-2,3-dioxopiperazinyl) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2829] 21 (H18-17) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-phenylthiopyridin-3-yl) carbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2830] Table 18A-3
    [2831] Example number Compound name
    [2832] 21 (H18-18) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-phenyloxypyridin-3-yl) carbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2833] 21 (H18-19) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methoxyphenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2834] 21 (H18-20) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (thiophen-2-yl) acetyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2835] 21 (H18-21) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-hexanoyl-1,4,9-triazaspiro [5.5] undecane
    [2836] 21 (H18-22) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methylphenyl) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2837] 21 (H18-23) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methylpropanoyl) -1,4,9-triazaspiro [5.5] Cannes
    [2838] 21 (H18-24) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-cyclopentylpropanoyl) -1,4,9-triazaspiro [5.5] Undecan
    [2839] 21 (H18-25) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2E) -3-phenyl-2-propenyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2840] 21 (H18-26) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methylphenyl) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2841] Table 18A-4
    [2842] Example number Compound name
    [2843] 21 (H18-27) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,3-dimethylbutanoyl) -1,4,9-triazaspiro [5.5] Undecan
    [2844] 21 (H18-28) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-cyclohexylcarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2845] 21 (H18-29) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-phenylcarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2846] 21 (H18-30) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (thiophen-2-ylcarbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2847] 21 (H18-31) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,6,6-trimethyl-1-cyclohexenyl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2848] 21 (H18-32) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((ethoxycarbonyl) carbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2849] 21 (H18-33) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-phenyl-5-methylisoxazol-4-yl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2850] 21 (H18-34) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((5-methyl-2-phenyl-1,2,3-triazol-4-yl ) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2851] Table 18A-5
    [2852] Example number Compound name
    [2853] 21 (H18-35) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (3-methoxyphenyl) acetyl) -1,4,9-triazaspiro [5.5] Undecan
    [2854] 21 (H18-36) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methoxyphenylcarbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2855] 21 (H18-37) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((furan-2-yl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2856] 21 (H18-38) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-benzyloxyacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2857] 21 (H18-39) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (cyclobutylcarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2858] 21 (H18-40) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-methoxyphenyl) acetyl) -1,4,9-triazaspiro [5.5] Undecan
    [2859] 21 (H18-41) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-acetyl-1,4,9-triazaspiro [5.5] undecane
    [2860] 21 (H18-42) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylpentanoyl) -1,4,9-triazaspiro [5.5] undecane
    [2861] 21 (H18-43) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methoxyacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2862] Table 18A-6
    [2863] Example number Compound name
    [2864] 21 (H18-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylthiopropanoyl) -1,4,9-triazaspiro [5.5] Undecan
    [2865] 21 (H18-45) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((isoxazol-5-yl) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2866] 21 (H18-46) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-cyclopentylacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2867] 21 (H18-47) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-pentanoyl-1,4,9-triazaspiro [5.5] undecane
    [2868] 21 (H18-48) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylpropanoyl) -1,4,9-triazaspiro [5.5] Cannes
    [2869] 21 (H18-49) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylthioacetyl) -1,4,9-triazaspiro [5.5] undecane
    [2870] 21 (H18-50) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methyl-1,2,3-thiadiazol-5-yl) carbonyl ) -1,4,9-triazaspiro [5.5] Undecan
    [2871] 21 (H18-51) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-cyanophenyl) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2872] 21 (H18-52) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-butanoyl-1,4,9-triazaspiro [5.5] undecane
    [2873] Table 18A-7
    [2874] Example number Compound name
    [2875] 21 (H18-53) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-propanoyl-1,4,9-triazaspiro [5.5] undecane
    [2876] 21 (H18-54) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-cyclopropylcarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2877] 21 (H18-55) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2H-benzo [3,4-d] 1,3-dioxolane-5-ylcar Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2878] 21 (H18-56) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1-phenyl-5-propylpyrazol-4-yl) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2879] 21 (H18-57) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((5- (1,1-dimethylethyl) -2-methylfuran-3-yl) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2880] 21 (H18-58) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1- (1,1-dimethylethyl) -3-methylpyrazol-5-yl ) Carbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2881] 21 (H18-59) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-methylsulfonyl-1,4,9-triazaspiro [5.5] undecane
    [2882] 21 (H18-60) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-pentylsulfonyl-1,4,9-triazaspiro [5.5] undecane
    [2883] Table 18A-8
    [2884] Example number Compound name
    [2885] 21 (H18-61) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1-methylethyl) sulfonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2886] 21 (H18-62) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-iodinephenyl) sulfonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2887] 21 (H18-63) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methylsulfonylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2888] 21 (H18-64) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-trifluoromethylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2889] 21 (H18-65) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-phenylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2890] 21 (H18-66) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-phenylphenyl) sulfonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2891] 21 (H18-67) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methoxycarbonylphenyl) sulfonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2892] 21 (H18-68) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3,4-difluorophenyl) sulfonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2893] 21 (H18-69) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,6-difluorophenyl) sulfonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2894] Table 18A-9
    [2895] Example number Compound name
    [2896] 21 (H18-70) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,5-difluorophenyl) sulfonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2897] 21 (H18-71) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,5-dimethoxyphenyl) sulfonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2898] 21 (H18-72) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-naphthylsulfonyl) -1,4,9-triazaspiro [5.5] undecane
    [2899] 21 (H18-73) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-(((1E) -2-phenylvinyl) sulfonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2900] 21 (H18-74) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((furan-2-yl) sulfonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2901] 21 (H18-75) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((thiophen-2-yl) sulfonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2902] Table 19A-1
    [2903] Example number Compound name
    [2904] 21 (H19-1) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methyl-2-acetylaminothiazol-5-yl) sulfonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2905] 21 (H19-2) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methoxy-dibenzofuran-3-yl) sulfonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2906] 21 (H19-3) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) sulfonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2907] 21 (H19-4) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-benzylsulfonyl-1,4,9-triazaspiro [5.5] undecane
    [2908] 21 (H19-5) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((ethylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2909] 21 (H19-6) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((propylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2910] 21 (H19-7) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1-methylethylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2911] 21 (H19-8) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((ethoxycarbonylmethylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2912] Table 19A-2
    [2913] Example number Compound name
    [2914] 21 (H19-9) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((butylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2915] 21 (H19-10) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-chlorophenylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2916] 21 (H19-11) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((phenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2917] 21 (H19-12) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methylphenylamino) carbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2918] 21 (H19-13) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((hexylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2919] 21 (H19-14) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-fluorophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2920] 21 (H19-15) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((benzylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2921] 21 (H19-16) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((cyclohexylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2922] 21 (H19-17) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-methylphenylamino) carbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2923] Table 19A-3
    [2924] Example number Compound name
    [2925] 21 (H19-18) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((octylamino) carbonyl) -1,4,9-triazaspiro [5.5] Cannes
    [2926] 21 (H19-19) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-bromophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2927] 21 (H19-20) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2- (thiophen-2-yl) ethylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2928] 21 (H19-21) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4- (1-methylethyl) phenylamino) carbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2929] 21 (H19-22) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-chlorophenylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2930] 21 (H19-23) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,4,5-trimethylphenylamino) carbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2931] 21 (H19-24) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,4,6-trimethylphenylamino) carbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2932] 21 (H19-25) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-phenyloxyphenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2933] Table 19A-4
    [2934] Example number Compound name
    [2935] 21 (H19-26) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-butyloxyphenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2936] 21 (H19-27) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-phenylphenylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2937] 21 (H19-28) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-phenylphenylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2938] 21 (H19-29) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-trifluoromethylphenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2939] 21 (H19-30) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3,4-dichlorophenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2940] 21 (H19-31) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-butyloxycarbonylphenylamino) carbonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2941] 21 (H19-32) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,6-bis (1-methylethyl) phenylamino) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2942] 21 (H19-33) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,5-dimethylphenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2943] Table 19A-5
    [2944] Example number Compound name
    [2945] 21 (H19-34) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-ethyl-6- (1-methylethyl) phenylamino) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2946] 21 (H19-35) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,4,6-trichlorophenylamino) carbonyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [2947] 21 (H19-36) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3,4-dimethylphenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2948] 21 (H19-37) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methylthiophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2949] 21 (H19-38) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methylthiophenylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2950] 21 (H19-39) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-butylphenylamino) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2951] 21 (H19-40) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,6-dibromo-4-ethylphenylamino) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2952] 21 (H19-41) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1-ethoxycarbonyl-2-methylpropylamino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2953] Table 19A-6
    [2954] Example number Compound name
    [2955] 21 (H19-42) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((phenylcarbonylamino) carbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2956] 21 (H19-43) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,4,6-tribromophenylamino) carbonyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [2957] 21 (H19-44) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,5-difluorophenylamino) carbonyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [2958] 21 (H19-45) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3,5-bis (methoxycarbonyl) phenylamino) carbonyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [2959] 21 (H19-46) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((6,7-methylenedioxycoumarin-4-ylmethylamino) carbonyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [2960] 21 (H19-47) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2,6-dimethylphenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2961] 21 (H19-48) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methylpropyloxy) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2962] 21 (H19-49) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-ethylhexyloxy) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2963] Table 19A-7
    [2964] Example number Compound name
    [2965] 21 (H19-50) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-ethoxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2966] 21 (H19-51) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-allyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2967] 21 (H19-52) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-propyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2968] 21 (H19-53) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-butyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2969] 21 (H19-54) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-hexyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2970] 21 (H19-55) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((fluorene-9-ylmethyloxy) carbonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2971] 21 (H19-56) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1R, 5R, 2S) -5-methyl-2- (1-methylethyl) cyclo Hexyloxycarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2972] 21 (H19-57) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2-methoxyethoxy) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2973] 21 (H19-58) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-pentyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2974] Table 19A-8
    [2975] Example number Compound name
    [2976] 21 (H19-59) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((1-methylethyloxy) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2977] 21 (H19-60) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((3-butenyloxy) carbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2978] 21 (H19-61) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((2R, 1S, 5S) -methyl-2- (1-methylethyl) cyclohexyloxy Cicarbonyl) -1,4,9-triazaspiro [5.5] undecane
    [2979] 21 (H19-62) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-cyclopentyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2980] 21 (H19-63) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [2981] 21 (H19-64) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((N, N-diphenylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2982] 21 (H19-65) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((N-phenyl-N-methylamino) carbonyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [2983] 21 (H19-66) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((N, N-dimethylamino) carbonyl) -1,4,9-triazaspiro [5.5] Undecan
    [2984] 21 (H19-67) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((N, N-diethylamino) carbonyl) -1,4,9-triaza Spiro [5.5] Undecan
    [2985] Table 19A-9
    [2986] Example number Compound name
    [2987] 21 (H19-68) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9-((N, N-bis (1-methylethyl) amino) carbonyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [2988] 21 (H19-69) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (morpholin-4-ylcarbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2989] 21 (H19-70) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (carbazole-9-ylcarbonyl) -1,4,9-triazaspiro [5.5 Undecan
    [2990] 21 (H19-71) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (pyrrolidin-1-ylcarbonyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [2991] TABLE 16B-1
    [2992]
    [2993] TABLE 16B-2
    [2994]
    [2995] Table 16B-3
    [2996]
    [2997] TABLE 16B-4
    [2998]
    [2999] Table 16B-5
    [3000]
    [3001] Table 16B-6
    [3002]
    [3003] Table 16B-7
    [3004]
    [3005] Table 16B-8
    [3006]
    [3007] Table 16B-9
    [3008]
    [3009] Table 16B-10
    [3010]
    [3011] TABLE 16B-11
    [3012]
    [3013] TABLE 16B-12
    [3014]
    [3015] Table 17B-1
    [3016]
    [3017] Table 17B-2
    [3018]
    [3019] Table 17B-3
    [3020]
    [3021] Table 17B-4
    [3022]
    [3023] Table 17B-5
    [3024]
    [3025] Table 17B-6
    [3026]
    [3027] Table 17B-7
    [3028]
    [3029] Table 17B-8
    [3030]
    [3031] Table 17B-9
    [3032]
    [3033] Table 17B-10
    [3034]
    [3035] TABLE 17B-11
    [3036]
    [3037] Table 17B-12
    [3038]
    [3039] Table 18B-1
    [3040]
    [3041] Table 18B-2
    [3042]
    [3043] Table 18B-3
    [3044]
    [3045] Table 18B-4
    [3046]
    [3047] Table 18B-5
    [3048]
    [3049] Table 18B-6
    [3050]
    [3051] Table 18B-7
    [3052]
    [3053] Table 18B-8
    [3054]
    [3055] Table 18B-9
    [3056]
    [3057] Table 18B-10
    [3058]
    [3059] Table 18B-11
    [3060]
    [3061] Table 19B-1
    [3062]
    [3063] Table 19B-2
    [3064]
    [3065] Table 19B-3
    [3066]
    [3067] Table 19B-4
    [3068]
    [3069] Table 19B-5
    [3070]
    [3071] Table 19B-6
    [3072]
    [3073] Table 19B-7
    [3074]
    [3075] Table 19B-8
    [3076]
    [3077] Table 19B-9
    [3078]
    [3079] Table 19B-10
    [3080]
    [3081] Table 19B-11
    [3082]
    [3083] TABLE 16C-1
    [3084]
    [3085] TABLE 16C-2
    [3086]
    [3087] Table 16C-3
    [3088]
    [3089] TABLE 17C-1
    [3090]
    [3091] TABLE 17C-2
    [3092]
    [3093] Table 17C-3
    [3094]
    [3095] Table 18C-1
    [3096]
    [3097] Table 18C-2
    [3098]
    [3099] Table 18C-3
    [3100]
    [3101] Table 19C-1
    [3102]
    [3103] Table 19C-2
    [3104]
    [3105] Table 19C-3
    [3106]
    [3107] Example 22
    [3108] (3S) -1-propyl-2,5-dioxo-3- (4- (3-phenylpropanoyl) aminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3109]
    [3110] Dichloroethane (0.5 ml) solution of compound (5 mg) prepared in Example 14 was added pyridine (2 μl), 3-phenylpropanoyl chloride (4 μl). The reaction mixture was stirred at rt for 3 h. Methanol was added to the reaction mixture and adsorbed onto an ion exchange resin (OASIS MCX, Waters, 60 mg) washed with methanol (3 ml) in advance. Washed with methanol (2 ml) and eluted with 10% triethylamine-methanol solution (2 ml). The eluate was concentrated to give a compound of the present invention (1.6 mg) having the following physical properties.
    [3111] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [3112] NMR (CD 3 OD): δ 7.40-7.10 (m, 10H), 4.03 (m, 1H), 3.60-3.30 (m, 2H), 3.14 (m, 2H), 3.06-2.90 (m, 3H), 2.90 -2.75 (m, 4H), 2.75-2.60 (m, 3H), 2.45 (t, J = 7.4 Hz, 2H), 2.30-2.00 (m, 2H), 2.00-1.70 (m, 4H), 1.70-1.20 (m, 6H), 0.93 (t, J = 7.2 Hz, 3H).
    [3113] Example 22 (1)
    [3114] (3S) -1-propyl-2,5-dioxo-3- (4-benzenesulfonylaminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3115]
    [3116] Using the compound prepared in Example 14 (5 mg), pyridine (2 μl) and benzenesulfonyl chloride (3 μl), the same operation as in Example 22 was carried out to obtain the compound (4.4 mg) of the present invention having the following physical properties. Got it.
    [3117] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [3118] NMR (CD 3 OD): δ 7.84 (m, 2H), 7.59 (m, 3H), 7.34-7.10 (m, 5H), 4.01 (t, J = 5.0 Hz, 1H), 3.55-3.30 (m, 2H ), 3.05-2.90 (m, 3H), 2.90-2.75 (m, 4H), 2.75-2.60 (m, 3H), 2.30-2.00 (m, 2H), 1.96 (m, 2H), 1.88-1.70 (m) , 2H), 1.70-1.20 (m, 6H), 0.94 (t, J = 7.4 Hz, 3H).
    [3119] Example 22 (2)
    [3120] (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzylcarbamoyl) aminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3121]
    [3122] In the same manner as in Example 22, using the compound (5 mg) and benzyl isocyanate (3 μl) prepared in Example 14, the present invention compound (7 mg) having the following physical properties was obtained.
    [3123] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [3124] NMR (CD 3 OD): δ 7.40-7.10 (m, 10H), 4.30 (s, 2H), 4.04 (t, J = 5.0 Hz, 1H), 3.55-3.30 (m, 2H), 3.15 (t, J = 6.6 Hz, 3H), 3.05-2.90 (m, 3H), 2.90-2.75 (m, 3H), 2.75-2.60 (m, 2H), 2.35-2.05 (m, 2H), 2.02-1.70 (m, 4H ), 1.70-1.20 (m, 6H), 0.93 (t, J = 7.4 Hz, 3H).
    [3125] Example 22 (H20-1)-22 (H21-77)
    [3126] Using the compound prepared in Example 14 and the corresponding acid chloride derivative, sulfonyl chloride derivative or isocyanate derivative, the same operations as in Example 22, 22 (1) or 22 (2) were carried out to the following Tables 20A-1 to 21A. The compound of the present invention was shown in -11 and the structural formula is shown in Tables 20B-1 to 21B-12. In addition, the physical properties of these compounds of the present invention are shown in Tables 20C-1 to 21C-3 below.
    [3127] Table 20A-1
    [3128] Example number Compound name
    [3129] 22 (H20-1) (3S) -1-propyl-2,5-dioxo-3- (4-((4-biphenyl) carbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3130] 22 (H20-2) (3S) -1-propyl-2,5-dioxo-3- (4-((4,7,7-trimethyl-2-oxa-3-oxobicyclo [2.2.1] Heptan-1-yl) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3131] 22 (H20-3) (3S) -1-propyl-2,5-dioxo-3- (4-((4-dimethylaminophenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3132] 22 (H20-4) (3S) -1-propyl-2,5-dioxo-3- (4-((3- (2-chlorophenyl) -5-methylisoxazol-4-yl) carbonylamino ) Butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3133] 22 (H20-5) (3S) -1-propyl-2,5-dioxo-3- (4-((4-fluorophenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3134] 22 (H20-6) (3S) -1-propyl-2,5-dioxo-3- (4-((3-fluorophenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3135] 22 (H20-7) (3S) -1-propyl-2,5-dioxo-3- (4-((2-fluorophenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3136] Table 20A-2
    [3137] Example number Compound name
    [3138] 22 (H20-8) (3S) -1-propyl-2,5-dioxo-3- (4- (cyclopentylcarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3139] 22 (H20-9) (3S) -1-propyl-2,5-dioxo-3- (4-((3-methylphenyl) carbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3140] 22 (H20-10) (3S) -1-propyl-2,5-dioxo-3- (4-((3-methoxyphenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3141] 22 (H20-11) (3S) -1-propyl-2,5-dioxo-3- (4- (2,2-dimethylpropanoylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3142] 22 (H20-12) (3S) -1-propyl-2,5-dioxo-3- (4- (pyridin-3-ylcarbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3143] 22 (H20-13) (3S) -1-propyl-2,5-dioxo-3- (4- (pyridin-2-ylcarbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3144] 22 (H20-14) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenylacetylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3145] Table 20A-3
    [3146] Example number Compound name
    [3147] 22 (H20-15) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenyloxyacetylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3148] 22 (H20-16) (3S) -1-propyl-2,5-dioxo-3- (4-((4-ethyl-2,3-dioxopiperazinyl) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3149] 22 (H20-17) (3S) -1-propyl-2,5-dioxo-3- (4-((2-phenylthiopyridin-3-yl) carbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3150] 22 (H20-18) (3S) -1-propyl-2,5-dioxo-3- (4-((2-phenyloxypyridin-3-yl) carbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3151] 22 (H20-19) (3S) -1-propyl-2,5-dioxo-3- (4-((2-methoxyphenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3152] 22 (H20-20) (3S) -1-propyl-2,5-dioxo-3- (4- (2- (thiophen-2-yl) acetylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3153] 22 (H20-21) (3S) -1-propyl-2,5-dioxo-3- (4- (hexanoylamino) butyl) -9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3154] TABLE 20A-4
    [3155] Example number Compound name
    [3156] 22 (H20-22) (3S) -1-propyl-2,5-dioxo-3- (4-((4-methylphenyl) carbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3157] 22 (H20-23) (3S) -1-propyl-2,5-dioxo-3- (4- (2-methylpropanoylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3158] 22 (H20-24) (3S) -1-propyl-2,5-dioxo-3- (4- (3-cyclopentylpropanoylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3159] 22 (H20-25) (3S) -1-propyl-2,5-dioxo-3- (4-((2E) -3-phenyl-2-propenylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3160] 22 (H20-26) (3S) -1-propyl-2,5-dioxo-3- (4-((2-methylphenyl) carbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3161] 22 (H20-27) (3S) -1-propyl-2,5-dioxo-3- (4- (3,3-dimethylbutanoylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3162] 22 (H20-28) (3S) -1-propyl-2,5-dioxo-3- (4- (cyclohexylcarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3163] Table 20A-5
    [3164] Example number Compound name
    [3165] 22 (H20-29) (3S) -1-propyl-2,5-dioxo-3- (4- (phenylcarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3166] 22 (H20-30) (3S) -1-propyl-2,5-dioxo-3- (4- (thiophen-2-ylcarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3167] 22 (H20-31) (3S) -1-propyl-2,5-dioxo-3- (4-((2,6,6-trimethyl-1-cyclohexenyl) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3168] 22 (H20-32) (3S) -1-propyl-2,5-dioxo-3- (4-((3-phenyl-5-methylisoxazol-4-yl) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3169] 22 (H20-33) (3S) -1-propyl-2,5-dioxo-3- (4-((5-methyl-2-phenyl-1,2,3-triazol-4-yl) car Carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3170] 22 (H20-34) (3S) -1-propyl-2,5-dioxo-3- (4- (2- (3-methoxyphenyl) acetylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3171] 22 (H20-35) (3S) -1-propyl-2,5-dioxo-3- (4- (4-methoxyphenylcarbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3172] Table 20A-6
    [3173] Example number Compound name
    [3174] 22 (H20-36) (3S) -1-propyl-2,5-dioxo-3- (4-((furan-2-yl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3175] 22 (H20-37) (3S) -1-propyl-2,5-dioxo-3- (4- (2-benzyloxyacetylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3176] 22 (H20-38) (3S) -1-propyl-2,5-dioxo-3- (4- (cyclobutylcarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3177] 22 (H20-39) (3S) -1-propyl-2,5-dioxo-3- (4- (2- (4-methoxyphenyl) acetylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3178] 22 (H20-40) (3S) -1-propyl-2,5-dioxo-3- (4- (acetylamino) butyl) -9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3179] 22 (H20-41) (3S) -1-propyl-2,5-dioxo-3- (4- (4-methylpentanoylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3180] 22 (H20-42) (3S) -1-propyl-2,5-dioxo-3- (4- (2-methoxyacetylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3181] TABLE 20A-7
    [3182] Example number Compound name
    [3183] 22 (H20-43) (3S) -1-propyl-2,5-dioxo-3- (4- (3-methylthiopropanoylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3184] 22 (H20-44) (3S) -1-propyl-2,5-dioxo-3- (4- (2-cyclopentylacetylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3185] 22 (H20-45) (3S) -1-propyl-2,5-dioxo-3- (4- (pentanoylamino) butyl) -9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3186] 22 (H20-46) (3S) -1-propyl-2,5-dioxo-3- (4- (3-methylpropanoylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3187] 22 (H20-47) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenylthioacetylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3188] 22 (H20-48) (3S) -1-propyl-2,5-dioxo-3- (4-((4-methyl-1,2,3-thiadiazol-5-yl) carbonylamino) Butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3189] 22 (H20-49) (3S) -1-propyl-2,5-dioxo-3- (4-((3-cyanophenyl) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3190] Table 20A-8
    [3191] Example number Compound name
    [3192] 22 (H20-50) (3S) -1-propyl-2,5-dioxo-3- (4- (butanoylamino) butyl) -9- (2-phenylethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3193] 22 (H20-51) (3S) -1-propyl-2,5-dioxo-3- (4- (propanoylamino) butyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3194] 22 (H20-52) (3S) -1-propyl-2,5-dioxo-3- (4- (cyclopropylcarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3195] 22 (H20-53) (3S) -1-propyl-2,5-dioxo-3- (4- (2H-benzo [3,4-d] 1,3-dioxolane-5-ylcarbonylamino ) Butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3196] 22 (H20-54) (3S) -1-propyl-2,5-dioxo-3- (4-((1-phenyl-5-propylpyrazol-4-yl) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3197] 22 (H20-55) (3S) -1-propyl-2,5-dioxo-3- (4-((5- (1,1-dimethylethyl) -2-methylfuran-3-yl) carbonyl Amino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3198] 22 (H20-56) (3S) -1-propyl-2,5-dioxo-3- (4-((1- (1,1-dimethylethyl) -3-methylpyrazol-5-yl) car Carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3199] Table 20A-9
    [3200] Example number Compound name
    [3201] 22 (H20-57) (3S) -1-propyl-2,5-dioxo-3- (4- (methylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3202] 22 (H20-58) (3S) -1-propyl-2,5-dioxo-3- (4- (pentylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3203] 22 (H20-59) (3S) -1-propyl-2,5-dioxo-3- (4- (1-methylethylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3204] 22 (H20-60) (3S) -1-propyl-2,5-dioxo-3- (4- (4-chlorophenylsulfonyl) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3205] 22 (H20-61) (3S) -1-propyl-2,5-dioxo-3- (4- (2-iodinephenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3206] 22 (H20-62) (3S) -1-propyl-2,5-dioxo-3- (4- (4-nitrophenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3207] 22 (H20-63) (3S) -1-propyl-2,5-dioxo-3- (4- (4- (methylsulfonyl) phenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3208] Table 20A-10
    [3209] Example number Compound name
    [3210] 22 (H20-64) (3S) -1-propyl-2,5-dioxo-3- (4- (4-trifluoromethylphenylsulfonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3211] 22 (H20-65) (3S) -1-propyl-2,5-dioxo-3- (4- (4-phenylphenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3212] 22 (H20-66) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenylphenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3213] 22 (H20-67) (3S) -1-propyl-2,5-dioxo-3- (4- (3,4-difluorophenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3214] 22 (H20-68) (3S) -1-propyl-2,5-dioxo-3- (4- (2,6-difluorophenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3215] 22 (H20-69) (3S) -1-propyl-2,5-dioxo-3- (4- (2,5-difluorophenylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3216] 22 (H20-70) (3S) -1-propyl-2,5-dioxo-3- (4- (2,5-dimethoxyphenylsulfonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3217] TABLE 20A-11
    [3218] Example number Compound name
    [3219] 22 (H20-71) (3S) -1-propyl-2,5-dioxo-3- (4- (2-chloro-4-trifluoromethylphenylsulfonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [3220] 22 (H20-72) (3S) -1-propyl-2,5-dioxo-3- (4- (2-naphthylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3221] 22 (H20-73) (3S) -1-propyl-2,5-dioxo-3- (4-((1E) -2-phenylvinylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3222] 22 (H20-74) (3S) -1-propyl-2,5-dioxo-3- (4- (furan-2-ylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3223] 22 (H20-75) (3S) -1-propyl-2,5-dioxo-3- (4- (thiophen-2-ylsulfonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3224] TABLE 21A-1
    [3225] Example number Compound name
    [3226] 22 (H21-1) (3S) -1-propyl-2,5-dioxo-3- (4- (4-bromo-2,5-dichlorothiophen-3-ylsulfonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3227] 22 (H21-2) (3S) -1-propyl-2,5-dioxo-3- (4- (5-phenylsulfonylthiophen-2-ylsulfonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3228] 22 (H21-3) (3S) -1-propyl-2,5-dioxo-3- (4- (7-chlorobenzoprazan-4-ylsulfonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3229] 22 (H21-4) (3S) -1-propyl-2,5-dioxo-3- (4- (4-methyl-2-acetylaminothiazol-5-ylsulfonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3230] 22 (H21-5) (3S) -1-propyl-2,5-dioxo-3- (4- (2-methoxy-dibenzofuran-3-ylsulfonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3231] 22 (H21-6) (3S) -1-propyl-2,5-dioxo-3- (4- (3,4-dichlorophenylsulfonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3232] 22 (H21-7) (3S) -1-propyl-2,5-dioxo-3- (4- (4-methoxyphenylsulfonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3233] Table 21A-2
    [3234] Example number Compound name
    [3235] 22 (H21-8) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylsulfonylamino) butyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3236] 22 (H21-9) (3S) -1-propyl-2,5-dioxo-3- (4-((ethylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3237] 22 (H21-10) (3S) -1-propyl-2,5-dioxo-3- (4-((propylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3238] 22 (H21-11) (3S) -1-propyl-2,5-dioxo-3- (4-((1-methylethylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3239] 22 (H21-12) (3S) -1-propyl-2,5-dioxo-3- (4-((butylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3240] 22 (H21-13) (3S) -1-propyl-2,5-dioxo-3- (4-((4-chlorophenylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3241] 22 (H21-14) (3S) -1-propyl-2,5-dioxo-3- (4-((phenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3242] Table 21A-3
    [3243] Example number Compound name
    [3244] 22 (H21-15) (3S) -1-propyl-2,5-dioxo-3- (4-((4-methylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3245] 22 (H21-16) (3S) -1-propyl-2,5-dioxo-3- (4-((hexylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3246] 22 (H21-17) (3S) -1-propyl-2,5-dioxo-3- (4-((4-fluorophenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3247] 22 (H21-18) (3S) -1-propyl-2,5-dioxo-3- (4-((benzylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3248] 22 (H21-19) (3S) -1-propyl-2,5-dioxo-3- (4-((cyclohexylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3249] 22 (H21-20) (3S) -1-propyl-2,5-dioxo-3- (4-((3-methylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3250] 22 (H21-21) (3S) -1-propyl-2,5-dioxo-3- (4-((octylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3251] Table 21A-4
    [3252] Example number Compound name
    [3253] 22 (H21-22) (3S) -1-propyl-2,5-dioxo-3- (4-((4-bromophenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3254] 22 (H21-23) (3S) -1-propyl-2,5-dioxo-3- (4-((2- (thiophen-2-yl) ethylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3255] 22 (H21-24) (3S) -1-propyl-2,5-dioxo-3- (4-((4- (1-methylethyl) phenylamino) carbonylamino) butyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3256] 22 (H21-25) (3S) -1-propyl-2,5-dioxo-3- (4-((3-chlorophenylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3257] 22 (H21-26) (3S) -1-propyl-2,5-dioxo-3- (4-((2,4,5-trimethylphenylamino) carbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3258] 22 (H21-27) (3S) -1-propyl-2,5-dioxo-3- (4-((2,4,6-trimethylphenylamino) carbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3259] 22 (H21-28) (3S) -1-propyl-2,5-dioxo-3- (4-((4-phenyloxyphenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3260] Table 21A-5
    [3261] Example number Compound name
    [3262] 22 (H21-29) (3S) -1-propyl-2,5-dioxo-3- (4-((4-butyloxyphenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3263] 22 (H21-30) (3S) -1-propyl-2,5-dioxo-3- (4-((4-phenylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3264] 22 (H21-31) (3S) -1-propyl-2,5-dioxo-3- (4-((2-phenylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3265] 22 (H21-32) (3S) -1-propyl-2,5-dioxo-3- (4-((4-trifluoromethylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3266] 22 (H21-33) (3S) -1-propyl-2,5-dioxo-3- (4-((3,4-dichlorophenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3267] 22 (H21-34) (3S) -1-propyl-2,5-dioxo-3- (4-((4-butyloxycarbonylphenylamino) carbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [3268] 22 (H21-35) (3S) -1-propyl-2,5-dioxo-3- (4-((2,6-bis (1-methylethyl) phenylamino) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3269] Table 21A-6
    [3270] Example number Compound name
    [3271] 22 (H21-36) (3S) -1-propyl-2,5-dioxo-3- (4-((2,5-dimethylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3272] 22 (H21-37) (3S) -1-propyl-2,5-dioxo-3- (4-((2-ethyl-6- (1-methylethyl) phenylamino) carbonylamino) butyl)- 9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3273] 22 (H21-38) (3S) -1-propyl-2,5-dioxo-3- (4-((2,4,6-trichlorophenylamino) carbonylamino) butyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3274] 22 (H21-39) (3S) -1-propyl-2,5-dioxo-3- (4-((3,4-dimethylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3275] 22 (H21-40) (3S) -1-propyl-2,5-dioxo-3- (4-((2-methylthiophenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3276] 22 (H21-41) (3S) -1-propyl-2,5-dioxo-3- (4-((4-methylthiophenylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3277] 22 (H21-42) (3S) -1-propyl-2,5-dioxo-3- (4-((4-butylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3278] Table 21A-7
    [3279] Example number Compound name
    [3280] 22 (H21-43) (3S) -1-propyl-2,5-dioxo-3- (4-((2-chloro-5-trifluoromethylphenylamino) carbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3281] 22 (H21-44) (3S) -1-propyl-2,5-dioxo-3- (4-((2,6-dibromo-4-ethylphenylamino) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3282] 22 (H21-45) (3S) -1-propyl-2,5-dioxo-3- (4-((1-ethoxycarbonyl-2-methylpropylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3283] 22 (H21-46) (3S) -1-propyl-2,5-dioxo-3- (4-((phenylcarbonylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3284] 22 (H21-47) (3S) -1-propyl-2,5-dioxo-3- (4-((2,4,6-tribromophenylamino) carbonylamino) butyl) -9- ( 2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3285] 22 (H21-48) (3S) -1-propyl-2,5-dioxo-3- (4-((2,5-difluorophenylamino) carbonylamino) butyl) -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3286] 22 (H21-49) (3S) -1-propyl-2,5-dioxo-3- (4-((3,5-bis (methoxycarbonyl) phenylamino) carbonylamino) butyl) -9 -(2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3287] Table 21A-8
    [3288] Example number Compound name
    [3289] 22 (H21-50) (3S) -1-propyl-2,5-dioxo-3- (4-((6,7-methylenedioxycoumarin-4-ylmethylamino) carbonylamino) butyl)- 9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3290] 22 (H21-51) (3S) -1-propyl-2,5-dioxo-3- (4-((2,6-dimethylphenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3291] 22 (H21-52) (3S) -1-propyl-2,5-dioxo-3- (4-((2-methylpropyloxy) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3292] 22 (H21-53) (3S) -1-propyl-2,5-dioxo-3- (4-((2-ethylhexyloxy) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3293] 22 (H21-54) (3S) -1-propyl-2,5-dioxo-3- (4- (ethoxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3294] 22 (H21-55) (3S) -1-propyl-2,5-dioxo-3- (4- (allyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3295] 22 (H21-56) (3S) -1-propyl-2,5-dioxo-3- (4- (propyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3296] Table 21A-9
    [3297] Example number Compound name
    [3298] 22 (H21-57) (3S) -1-propyl-2,5-dioxo-3- (4- (butyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3299] 22 (H21-58) (3S) -1-propyl-2,5-dioxo-3- (4- (hexyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3300] 22 (H21-59) (3S) -1-propyl-2,5-dioxo-3- (4-((2,2,2-trichloroethyloxy) carbonylamino) butyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3301] 22 (H21-60) (3S) -1-propyl-2,5-dioxo-3- (4-((fluorene-9-ylmethyloxy) carbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [3302] 22 (H21-61) (3S) -1-propyl-2,5-dioxo-3- (4-((1S, 5S, 2R) -5-methyl-2- (1-methylethyl) cyclohexyloxy Cycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3303] 22 (H21-62) (3S) -1-propyl-2,5-dioxo-3- (4-((2-methoxyethoxy) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3304] 22 (H21-63) (3S) -1-propyl-2,5-dioxo-3- (4- (pentyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triza spiro [5.5] Undecan
    [3305] Table 21A-10
    [3306] Example number Compound name
    [3307] 22 (H21-64) (3S) -1-propyl-2,5-dioxo-3- (4-((1-methylethyloxy) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3308] 22 (H21-65) (3S) -1-propyl-2,5-dioxo-3- (4-((3-butenyloxy) carbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3309] 22 (H21-66) (3S) -1-propyl-2,5-dioxo-3- (4-((2S, 1R, 5R) -methyl-2- (1-methylethyl) cyclohexyloxycarbo Nylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3310] 22 (H21-67) (3S) -1-propyl-2,5-dioxo-3- (4- (cyclopentyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3311] 22 (H21-68) (3S) -1-propyl-2,5-dioxo-3- (4-((1,1-dimethylethyloxy) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3312] 22 (H21-69) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3313] 22 (H21-70) (3S) -1-propyl-2,5-dioxo-3- (4-((N, N-diphenylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3314] TABLE 21A-11
    [3315] Example number Compound name
    [3316] 22 (H21-71) (3S) -1-propyl-2,5-dioxo-3- (4-((N-phenyl-N-methylamino) carbonylamino) butyl) -9- (2-phenyl Ethyl) -1,4,9-triazaspiro [5.5] undecane
    [3317] 22 (H21-72) (3S) -1-propyl-2,5-dioxo-3- (4-((N, N-dimethylamino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3318] 22 (H21-73) (3S) -1-propyl-2,5-dioxo-3- (4-((N, N-diethylamino) carbonylamino) butyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3319] 22 (H21-74) (3S) -1-propyl-2,5-dioxo-3- (4-((N, N-bis (1-methylethyl) amino) carbonylamino) butyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane
    [3320] 22 (H21-75) (3S) -1-propyl-2,5-dioxo-3- (4- (morpholin-4-ylcarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3321] 22 (H21-76) (3S) -1-propyl-2,5-dioxo-3- (4- (carbazole-9-ylcarbonylamino) butyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3322] 22 (H21-77) (3S) -1-propyl-2,5-dioxo-3- (4- (pyrrolidin-1-ylcarbonylamino) butyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3323] Table 20B-1
    [3324]
    [3325] Table 20B-2
    [3326]
    [3327] Table 20B-3
    [3328]
    [3329] Table 20B-4
    [3330]
    [3331] Table 20B-5
    [3332]
    [3333] Table 20B-6
    [3334]
    [3335] Table 20B-7
    [3336]
    [3337] Table 20B-8
    [3338]
    [3339] Table 20B-9
    [3340]
    [3341] Table 20B-10
    [3342]
    [3343] TABLE 20B-11
    [3344]
    [3345] TABLE 20B-12
    [3346]
    [3347] Table 21B-1
    [3348]
    [3349] Table 21B-2
    [3350]
    [3351] Table 21B-3
    [3352]
    [3353] Table 21B-4
    [3354]
    [3355] Table 21B-5
    [3356]
    [3357] Table 21B-6
    [3358]
    [3359] Table 21B-7
    [3360]
    [3361] Table 21B-8
    [3362]
    [3363] Table 21B-9
    [3364]
    [3365] Table 21B-10
    [3366]
    [3367] Table 21B-11
    [3368]
    [3369] TABLE 21B-12
    [3370]
    [3371] Table 20C-1
    [3372]
    [3373] Table 20C-2
    [3374]
    [3375] Table 20C-3
    [3376]
    [3377] Table 21C-1
    [3378]
    [3379] Table 21C-2
    [3380]
    [3381] Table 21C-3
    [3382]
    [3383] Example 23
    [3384] 1-cyclopropylmethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenoxyphenyl) -1,3,9-triazaspiro [5.5] undecane acetate
    [3385]
    [3386] N-allyloxycarbonyl-4-piperidone (0.396 g) and cyclopropylmethyl in a suspension of tetrahydrofuran / methanol (1: 1; 5 ml) of resin (3) (0.5 g) prepared in Reference Example 2 Amine (0.189 ml) and N- (t-butyloxycarbonyl) leucine (0.542 g) were added and stirred at 65 ° C. for 18 hours. The reaction solution was cooled at room temperature and the resin was taken by filtration. The obtained resin was washed with dimethylformamide (5 ml × 2 times), methylene chloride (5 ml × 2 times), methanol (5 ml × 2 times) and methylene chloride (5 ml × 2 times). Acetic acid (0.149 ml), tributyltin hydride (0.351 ml), and tetrakistriphenylphosphinepalladium (0) complex (50 mg) were added to a methylene chloride (5 ml) suspension of the obtained resin, followed by stirring at room temperature for 6 hours. . The resin was collected by filtration from the reaction solution, and washed with methylene chloride (5 ml × 4 times) and dimethylformamide (5 ml × 3 times). It was suspended in the obtained resin 1% acetic acid-dimethylformamide solution (5 ml), 4-phenyloxybenzoaldehyde (0.252 g) and sodium triacetoxy borohydride (0.277 g) were added there, and it stirred at room temperature for 15 hours. . The resin was collected by filtration from the reaction solution, and washed with methanol (5 ml × 1 time), dimethylformamide (5 ml × 3 times), methanol (5 ml × 4 times) and methylene chloride (5 ml × 4 times). . The obtained resin was suspended in a 50% trifluoroacetic acid-methylene chloride (5 ml) solution and stirred at room temperature for 5 minutes. The reaction solution was filtered, and the obtained resin was again suspended in 50% trifluoroacetic acid-methylene chloride solution (5 ml) and stirred at room temperature for 30 minutes. The resin taken out by filtration from the reaction solution was washed with methylene chloride (5 ml × 3 times) and 1.25 M acetate-toluene solution (5 ml × 3 times). The obtained resin was suspended in 1.25 M acetic acid-toluene solution (5 ml) and stirred at 90 ° C. for 23 hours. The reaction solution was filtered, and the resulting resin was washed with chloroform-methanol (1: 1; 2 ml × 2 times). The filtrate and the washing solution were concentrated to obtain a compound of the present invention (274 mg) having the following physical properties.
    [3387] TLC: Rf 0.40 (CHCl 3: MeOH = 20: 1);
    [3388] NMR (CD 3 OD): δ 7.49 (m, 2H), 7.40 (m, 2H), 7.18 (m, 2H), 7.04 (m, 3H), 4.33 (s, 2H), 4.04 (dd, J = 8.1 , 4.8 Hz, 1H), 3.78 (m, 2H), 3.52 (m, 2H), 3.35 (m, 2H), 2.45-2.10 (m, 4H), 1.98 (s, 3H, CH3COOH), 1.97-1.58 ( m, 4H), 0.94 (d, J = 6.0 Hz, 6H), 0.51 (m, 2H), 0.36 (m, 2H).
    [3389] Example 23 (1)
    [3390] 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenoxyphenyl) -1,3,9-triazaspiro [5.5] Undecane Acetate
    [3391]
    [3392] Resin (3) prepared in Reference Example 2 (0.5 g), N-allyloxycarbonyl-4-piperidone (0.396 g), thiophen-2-ylmethylamine (0.205 ml) and N- (t-butyl In the same manner as in Example 23 using oxycarbonyl) leucine (0.542 g) and 4-phenyloxybenzoaldehyde (0.252 g), the present invention compound (274 mg) having the following physical properties was obtained.
    [3393] TLC: Rf 0.39 (CHCl 3: MeOH = 20: 1);
    [3394] NMR (CD 3 OD): δ 7.48 (m, 2H), 7.39 (m, 2H), 7.28 (m, 1H), 7.18 (m, 2H), 7.04 (m, 4H), 6.91 (m, 1H), 4.86 (s, 2H), 4.32 (s, 2H), 4.12 (dd, J = 8.1, 4.5 Hz, 1H), 3.77 (m, 2H), 3.49 (m, 2H), 2.60-2.30 (m, 2H) , 2.19 (m, 2H), 1.98 (s, 3H), 1.97-1.58 (m, 3H), 0.94 (d, J = 6.0 Hz, 6H).
    [3395] Example 23 (H22-1) -23 (H31-31)
    [3396] The same operation as in Example 23 or 23 (1) was carried out using the resin (3) prepared in Reference Example 2, the corresponding 4-piperidone derivative, the corresponding amine derivative, the corresponding amino acid derivative and the corresponding aldehyde derivative, The compounds of the present invention are shown in Tables 22A-1 to 31A-4, and the structural formulas are shown in Tables 22B-1 to 31B-5. In addition, the physical properties of these compounds of the present invention are shown in Tables 22C-1 to 31C-2 below.
    [3397] TABLE 22A-1
    [3398] Example number Compound name
    [3399] 23 (H22-1) (3S) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [3400] 23 (H22-2) (3R) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [3401] 23 (H22-3) (3S) -1-propyl-2,5-dioxo-3-methyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3402] 23 (H22-4) (3S) -1-propyl-2,5-dioxo-3-benzyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3403] 23 (H22-5) (3S) -1-propyl-2,5-dioxo-3- (1- (benzyloxymethyl) imidazol-5-ylmethyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3404] 23 (H22-6) (3S) -1-propyl-2,5-dioxo-3- (benzyloxymethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3405] 23 (H22-7) (3S) -1-propyl-2,5-dioxo-3- (4-methoxyphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3406] 23 (H22-8) (3S) -1-propyl-2,5-dioxo-3-((1R) -1- (benzyloxy) ethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3407] TABLE 22A-2
    [3408] Example number Compound name
    [3409] 23 (H22-9) (3S) -1-propyl-2,5-dioxo-3- (pyridin-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3410] 23 (H22-10) (3S) -1-propyl-2,5-dioxo-3-butyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3411] 23 (H22-11) (3S) -1-propyl-2,5-dioxo-3- (cyclohexyloxycarbonylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3412] 23 (H22-12) (3S) -1-propyl-2,5-dioxo-3- (cyclohexylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3413] 23 (H22-13) (3R) -1-propyl-2,5-dioxo-3- (cyclohexyloxycarbonylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3414] 23 (H22-14) (3R) -1-propyl-2,5-dioxo-3- (2- (cyclohexyloxycarbonyl) ethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3415] 23 (H22-15) (3R) -1-propyl-2,5-dioxo-3- (4- (benzyloxy) phenylmethyl) -9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3416] 23 (H22-16) (3S) -1-propyl-2,5-dioxo-3-hydroxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3417] Table 22A-3
    [3418] Example number Compound name
    [3419] 23 (H22-17) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxy) phenylmethyl) -9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3420] 23 (H22-18) (3R) -1-propyl-2,5-dioxo-3-butyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3421] 23 (H22-19) (3R) -1-propyl-2,5-dioxo-3- (cyclohexylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3422] 23 (H22-20) (3R) -1-propyl-2,5-dioxo-3-((1S) -1- (benzyloxy) ethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3423] 23 (H22-21) (3R) -1-propyl-2,5-dioxo-3- (benzyloxymethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3424] 23 (H22-22) (3R) -1-propyl-2,5-dioxo-3-((4-methoxyphenylmethylthio) methyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3425] 23 (H22-23) (3R) -1-propyl-2,5-dioxo-3- (benzylthiomethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3426] 23 (H22-24) (3S) -1-propyl-2,5-dioxo-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3427] Table 22A-4
    [3428] Example number Compound name
    [3429] 23 (H22-25) (3S) -1-propyl-2,5-dioxo-3- (imidazol-4-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3430] 23 (H22-26) (3S) -1-propyl-2,5-dioxo-3-hydroxymethyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3431] 23 (H22-27) (3R) -1-propyl-2,5-dioxo-3-((3-nitropyridin-2-yl) disulfanylmethyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3432] 23 (H22-28) (3S) -1-propyl-2,5-dioxo-3- (1-benzylimidazol-4-ylmethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3433] 23 (H22-29) (3R) -1-propyl-2,5-dioxo-3- (4-hydroxyphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3434] 23 (H22-30) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) phenylmethyl) -9- (6-phenylhexyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3435] 23 (H22-31) (3R) -1-propyl-2,5-dioxo-3- (3- (aminocarbonylamino) propyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3436] 23 (H22-32) (3R) -1-propyl-2,5-dioxo-3- (1-naphthylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3437] Table 22A-5
    [3438] Example number Compound name
    [3439] 23 (H22-33) (3S) -1-propyl-2,5-dioxo-3- (3,4-dichlorophenylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3440] 23 (H22-34) (3R) -1-propyl-2,5-dioxo-3-((1,1-dimethylethylthio) methyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3441] 23 (H22-35) (3S) -1-propyl-2,5-dioxo-3- (2-methylpropyl) -4-methyl-9- (6-phenylhexyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3442] 23 (H22-36) (3S) -1-propyl-2,5-dioxo-3-propyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3443] 23 (H22-37) (3S) -1-propyl-2,5-dioxo-3- (4-benzyloxyphenylmethyl) -4-methyl-9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3444] 23 (H22-38) (3S) -1-propyl-2,5-dioxo-3-((1R) -1-hydroxyethyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3445] 23 (H22-39) (3S) -1-propyl-2,5-dioxo-3- (aminocarbonylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5 Undecan
    [3446] 23 (H22-40) (3S) -1-propyl-2,5-dioxo-3-((1R) -1-hydroxyethyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3447] 23 (H22-41) (3R) -1-propyl-2,5-dioxo-3-methyl-9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3448] Table 22A-6
    [3449] Example number Compound name
    [3450] 23 (H22-42) (3R) -1-propyl-2,5-dioxo-3- (pyridin-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3451] 23 (H22-43) (3S) -1-propyl-2,5-dioxo-3- (carboxymethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Cannes
    [3452] 23 (H22-44) (3S) -1-propyl-2,5-dioxo-3- (4-hydroxyphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3453] 23 (H22-45) (3S) -1-propyl-2,5-dioxo-3- (2-methylthioethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3454] 23 (H22-46) (3R) -1-propyl-2,5-dioxo-3-((methylcarbonylamino) methylthiomethyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3455] 23 (H22-47) (3R) -1-propyl-2,5-dioxo-3-((1S) -1-hydroxyethyl) -9- (6-phenylhexyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3456] 23 (H22-48) (3S) -1-propyl-2,5-dioxo-3- (2-chlorophenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3457] 23 (H22-49) (3S) -1-propyl-2,5-dioxo-3- (1-naphthylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3458] 23 (H22-50) (3S) -1-propyl-2,5-dioxo-3- (4-fluorophenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3459] Table 22A-7
    [3460] Example number Compound name
    [3461] 23 (H22-51) (3S) -1-propyl-2,5-dioxo-3- (cyanomethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3462] 23 (H22-52) (3R) -1-propyl-2,5-dioxo-3- (indol-3-ylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3463] 23 (H22-53) (3S) -1-propyl-2,5-dioxo-3- (4- (2-chlorophenylmethyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3464] 23 (H22-54) (3R) -1-propyl-2,5-dioxo-3- (benzyloxycarbonylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3465] 23 (H22-55) (3S) -1-propyl-2,5-dioxo-3- (3- (1-imino-1- (2,4,6-trimethylphenylsulfonylamino) methylamino) Propyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane
    [3466] 23 (H22-56) (3S) -1-propyl-2,5-dioxo-3- (benzyloxycarbonylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3467] 23 (H22-57) (3S) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3468] 23 (H22-58) (3R) -1-propyl-2,5-dioxo-3- (4-methoxyphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3469] Table 22A-8
    [3470] Example number Compound name
    [3471] 23 (H22-59) (3R) -1-propyl-2,5-dioxo-3- (4- (benzyloxycarbonylamino) butyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3472] 23 (H22-60) (3S) -1-propyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (6-phenylhexyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3473] 23 (H22-61) (3R) -1-propyl-2,5-dioxo-3- (1- (benzyloxymethyl) imidazol-4-ylmethyl) -9- (6-phenylhexyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3474] 23 (H22-62) (3R) -1-propyl-2,5-dioxo-3- (4-ethoxyphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] Undecan
    [3475] 23 (H22-63) (3S) -1-propyl-2,5-dioxo-3- (4-phenylphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3476] 23 (H22-64) (3S) -1-propyl-2,5-dioxo-3- (1,1-diphenylmethyl) -9- (6-phenylhexyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3477] TABLE 23A-1
    [3478] Example number Compound name
    [3479] 23 (H23-1) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3480] 23 (H23-2) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3481] 23 (H23-3) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-diethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3482] 23 (H23-4) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3483] 23 (H23-5) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3484] 23 (H23-6) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3485] 23 (H23-7) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-allyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3486] 23 (H23-8) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (dibenzofuran-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3487] 23 (H23-9) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3488] TABLE 23A-2
    [3489] Example number Compound name
    [3490] 23 (H23-10) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3491] 23 (H23-11) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3492] 23 (H23-12) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-diethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3493] 23 (H23-13) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3494] 23 (H23-14) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3495] 23 (H23-15) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3496] 23 (H23-16) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-allyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3497] 23 (H23-17) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (dibenzofuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3498] 23 (H23-18) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3499] Table 24A-1
    [3500] Example number Compound name
    [3501] 23 (H24-1) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3502] 23 (H24-2) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3503] 23 (H24-3) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3504] 23 (H24-4) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3505] 23 (H24-5) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3506] 23 (H24-6) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3507] 23 (H24-7) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3508] 23 (H24-8) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3509] 23 (H24-9) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylimidazol-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3510] Table 24A-2
    [3511] Example number Compound name
    [3512] 23 (H24-10) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3513] 23 (H24-11) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3514] 23 (H24-12) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3515] 23 (H24-13) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (indol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3516] 23 (H24-14) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3517] 23 (H24-15) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (carboxy) thiophen-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3518] 23 (H24-16) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3519] 23 (H24-17) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3520] 23 (H24-18) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3521] Table 24A-3
    [3522] Example number Compound name
    [3523] 23 (H24-19) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3524] 23 (H24-20) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3525] 23 (H24-21) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3526] 23 (H24-22) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3527] 23 (H24-23) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3528] 23 (H24-24) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3529] 23 (H24-25) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3530] Table 24A-4
    [3531] Example number Compound name
    [3532] 23 (H24-26) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3533] 23 (H24-27) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3534] 23 (H24-28) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3535] 23 (H24-29) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3536] 23 (H24-30) 1-ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrole-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3537] 23 (H24-31) 1-Ethyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.6] Undecan
    [3538] TABLE 25A-1
    [3539] Example number Compound name
    [3540] 23 (H25-1) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3541] 23 (H25-2) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3542] 23 (H25-3) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3543] 23 (H25-4) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3544] 23 (H25-5) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3545] 23 (H25-6) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3546] 23 (H25-7) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3547] 23 (H25-8) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylimidazol-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3548] TABLE 25A-2
    [3549] Example number Compound name
    [3550] 23 (H25-9) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3551] 23 (H25-10) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3552] 23 (H25-11) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (indol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3553] 23 (H25-12) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3554] 23 (H25-13) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3555] 23 (H25-14) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3556] 23 (H25-15) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3557] 23 (H25-16) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3558] TABLE 25A-3
    [3559] Example number Compound name
    [3560] 23 (H25-17) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3561] 23 (H25-18) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3562] 23 (H25-19) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3563] 23 (H25-20) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3564] 23 (H25-21) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3565] 23 (H25-22) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3566] 23 (H25-23) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3567] TABLE 25A-4
    [3568] Example number Compound name
    [3569] 23 (H25-24) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3570] 23 (H25-25) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3571] 23 (H25-26) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3572] 23 (H25-27) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrole-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3573] 23 (H25-28) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.6] Undecan
    [3574] TABLE 26A-1
    [3575] Example number Compound name
    [3576] 23 (H26-1) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3577] 23 (H26-2) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3578] 23 (H26-3) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3579] 23 (H26-4) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3580] 23 (H26-5) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3581] 23 (H26-6) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3582] 23 (H26-7) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3583] 23 (H26-8) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3584] 23 (H26-9) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylimidazol-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3585] TABLE 26A-2
    [3586] Example number Compound name
    [3587] 23 (H26-10) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3588] 23 (H26-11) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3589] 23 (H26-12) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3590] 23 (H26-13) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (indol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3591] 23 (H26-14) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3592] 23 (H26-15) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (carboxy) thiophen-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3593] 23 (H26-16) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3594] 23 (H26-17) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3595] 23 (H26-18) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3596] TABLE 26A-3
    [3597] Example number Compound name
    [3598] 23 (H26-19) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3599] 23 (H26-20) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3600] 23 (H26-21) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3601] 23 (H26-22) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3602] 23 (H26-23) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3603] 23 (H26-24) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3604] 23 (H26-25) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3605] TABLE 26A-4
    [3606] Example number Compound name
    [3607] 23 (H26-26) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [3608] 23 (H26-27) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3609] 23 (H26-28) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3610] 23 (H26-29) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3611] 23 (H26-30) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrole-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3612] 23 (H26-31) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.6] Undecan
    [3613] TABLE 27A-1
    [3614] Example number Compound name
    [3615] 23 (H27-1) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [3616] 23 (H27-2) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4,9-triazaspiro [5.5 Undecan
    [3617] 23 (H27-3) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3618] 23 (H27-4) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4,9-triazaspiro [5.5 Undecan
    [3619] 23 (H27-5) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4,9-triazaspiro [5.5 Undecan
    [3620] 23 (H27-6) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3621] 23 (H27-7) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3622] 23 (H27-8) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4,9-triazaspiro [5.5 Undecan
    [3623] 23 (H27-9) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [3624] TABLE 27A-2
    [3625] Example number Compound name
    [3626] 23 (H27-10) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3627] 23 (H27-11) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3628] 23 (H27-12) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3629] 23 (H27-13) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3630] 23 (H27-14) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3631] 23 (H27-15) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3632] 23 (H27-16) 1-((2-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3633] Table 27A-3
    [3634] Example number Compound name
    [3635] 23 (H27-17) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [3636] 23 (H27-18) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3637] 23 (H27-19) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3638] 23 (H27-20) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3639] 23 (H27-21) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3640] 23 (H27-22) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3641] 23 (H27-23) 1-((3-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3642] Table 27A-4
    [3643] Example number Compound name
    [3644] 23 (H27-24) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5 Undecan
    [3645] 23 (H27-25) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3646] 23 (H27-26) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3647] 23 (H27-27) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3648] 23 (H27-28) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3649] 23 (H27-29) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3650] 23 (H27-30) 1-((4-methoxyphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3651] Table 27A-5
    [3652] Example number Compound name
    [3653] 23 (H27-31) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3654] 23 (H27-32) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3655] 23 (H27-33) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2H, 3H-benzo [3,4-e] 1, 4-dioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3656] 23 (H27-34) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3657] 23 (H27-35) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3658] 23 (H27-36) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3659] 23 (H27-37) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3660] Table 27A-6
    [3661] Example number Compound name
    [3662] 23 (H27-38) 1- (pyridin-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3663] 23 (H27-39) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3664] 23 (H27-40) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3665] 23 (H27-41) 1- (Pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3666] 23 (H27-42) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3667] 23 (H27-43) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3668] 23 (H27-44) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3669] Table 27A-7
    [3670] Example number Compound name
    [3671] 23 (H27-45) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3672] 23 (H27-46) 1- (pyridin-3-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3673] 23 (H27-47) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3674] 23 (H27-48) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3675] 23 (H27-49) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3676] 23 (H27-50) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3677] 23 (H27-51) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3678] Table 27A-8
    [3679] Example number Compound name
    [3680] 23 (H27-52) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3681] 23 (H27-53) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3682] 23 (H27-54) 1- (pyridin-4-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3683] 23 (H27-55) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3684] 23 (H27-56) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3685] 23 (H27-57) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3686] 23 (H27-58) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3687] Table 27A-9
    [3688] Example number Compound name
    [3689] 23 (H27-59) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3690] 23 (H27-60) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3691] 23 (H27-61) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3692] 23 (H27-62) 1-((2-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3693] 23 (H27-63) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3694] 23 (H27-64) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3695] 23 (H27-65) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3696] Table 27A-10
    [3697] Example number Compound name
    [3698] 23 (H27-66) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3699] 23 (H27-67) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3700] 23 (H27-68) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3701] 23 (H27-69) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3702] 23 (H27-70) 1-((3-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3703] 23 (H27-71) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] Cannes
    [3704] 23 (H27-72) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-methoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3705] TABLE 27A-11
    [3706] Example number Compound name
    [3707] 23 (H27-73) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3708] 23 (H27-74) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-phenoxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3709] 23 (H27-75) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-benzyloxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3710] 23 (H27-76) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3711] 23 (H27-77) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylimidazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [3712] 23 (H27-78) 1-((4-methylphenyl) methyl) -2,5-dioxo-3- (2-methylpropyl) -9-((4-hydroxyphenyl) methyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3713] TABLE 28A-1
    [3714] Example number Compound name
    [3715] 23 (H28-1) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3716] 23 (H28-2) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3717] 23 (H28-3) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3718] 23 (H28-4) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3719] 23 (H28-5) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3720] 23 (H28-6) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3721] 23 (H28-7) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3722] 23 (H28-8) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3723] 23 (H28-9) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3724] TABLE 28A-2
    [3725] Example number Compound name
    [3726] 23 (H28-10) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3727] 23 (H28-11) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3728] 23 (H28-12) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3729] 23 (H28-13) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3730] 23 (H28-14) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) thiophen-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3731] 23 (H28-15) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3732] 23 (H28-16) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3733] 23 (H28-17) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3734] Table 28A-3
    [3735] Example number Compound name
    [3736] 23 (H28-18) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3737] 23 (H28-19) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3738] 23 (H28-20) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3739] 23 (H28-21) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3740] 23 (H28-22) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3741] 23 (H28-23) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3742] 23 (H28-24) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3743] TABLE 28A-4
    [3744] Example number Compound name
    [3745] 23 (H28-25) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3746] 23 (H28-26) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3747] 23 (H28-27) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3748] 23 (H28-28) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3749] 23 (H28-29) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrol-3-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3750] 23 (H28-30) 1-propyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.6] Undecan
    [3751] TABLE 29A-1
    [3752] Example number Compound name
    [3753] 23 (H29-1) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3754] 23 (H29-2) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3755] 23 (H29-3) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3756] 23 (H29-4) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3757] 23 (H29-5) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3758] 23 (H29-6) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3759] 23 (H29-7) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3760] 23 (H29-8) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3761] 23 (H29-9) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3762] TABLE 29A-2
    [3763] Example number Compound name
    [3764] 23 (H29-10) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3765] 23 (H29-11) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3766] 23 (H29-12) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3767] 23 (H29-13) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (indol-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3768] 23 (H29-14) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3769] 23 (H29-15) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) thiophen-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3770] 23 (H29-16) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3771] 23 (H29-17) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3772] 23 (H29-18) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3773] TABLE 29A-3
    [3774] Example number Compound name
    [3775] 23 (H29-19) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3776] 23 (H29-20) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3777] 23 (H29-21) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3778] 23 (H29-22) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3779] 23 (H29-23) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3780] 23 (H29-24) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3781] 23 (H29-25) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3782] TABLE 29A-4
    [3783] Example number Compound name
    [3784] 23 (H29-26) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3785] 23 (H29-27) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3786] 23 (H29-28) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3787] 23 (H29-29) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3788] 23 (H29-30) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrol-3-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3789] 23 (H29-31) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.6] Undecan
    [3790] TABLE 30A-1
    [3791] Example number Compound name
    [3792] 23 (H30-1) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3793] 23 (H30-2) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3794] 23 (H30-3) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5-methylfuran-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3795] 23 (H30-4) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5-bromothiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3796] 23 (H30-5) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3-methylthiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3797] 23 (H30-6) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3798] 23 (H30-7) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3799] 23 (H30-8) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1-methylindol-3-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3800] TABLE 30A-2
    [3801] Example number Compound name
    [3802] 23 (H30-9) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-methylimidazol-5-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3803] 23 (H30-10) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2,4-dioxo-1,3-dihydropyrimidine-5- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3804] 23 (H30-11) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3805] 23 (H30-12) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3806] 23 (H30-13) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (indol-3-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3807] 23 (H30-14) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [3808] 23 (H30-15) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) thiophen-2-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3809] Table 30A-3
    [3810] Example number Compound name
    [3811] 23 (H30-16) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3812] 23 (H30-17) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3813] 23 (H30-18) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3814] 23 (H30-19) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3815] 23 (H30-20) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3816] 23 (H30-21) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan- 2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3817] 23 (H30-22) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-bromothiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3818] TABLE 30A-4
    [3819] Example number Compound name
    [3820] 23 (H30-23) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3821] 23 (H30-24) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3822] 23 (H30-25) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1-acetylindol-3-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [3823] 23 (H30-26) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (3,5-bis (trifluoromethyl) phenyl) furan- 2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3824] 23 (H30-27) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl ) -1,4,9-triazaspiro [5.5] Undecan
    [3825] 23 (H30-28) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3826] 23 (H30-29) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3827] TABLE 30A-5
    [3828] Example number Compound name
    [3829] 23 (H30-30) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrole-3- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [3830] 23 (H30-31) 1- (2-methoxyethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1, 4,9-triazaspiro [5.6] Undecan
    [3831] TABLE 31A-1
    [3832] Example number Compound name
    [3833] 23 (H31-1) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3834] 23 (H31-2) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3835] 23 (H31-3) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3836] 23 (H31-4) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3837] 23 (H31-5) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3838] 23 (H31-6) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3839] 23 (H31-7) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (pyridin-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3840] 23 (H31-8) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3841] 23 (H31-9) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylimidazol-5-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3842] TABLE 31A-2
    [3843] Example number Compound name
    [3844] 23 (H31-10) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,4-dioxo-1,3-dihydropyrimidin-5-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3845] 23 (H31-11) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3846] 23 (H31-12) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3847] 23 (H31-13) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (indol-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [3848] 23 (H31-14) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (hydroxymethyl) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3849] 23 (H31-15) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) thiophen-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [3850] 23 (H31-16) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (carboxy) furan-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3851] 23 (H31-17) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3852] 23 (H31-18) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-methylbenzoimidazol-2-ylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [3853] Table 31A-3
    [3854] Example number Compound name
    [3855] 23 (H31-19) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethoxyphenyl) furan-2-ylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [3856] 23 (H31-20) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (6- (methoxycarbonyl) indol-3-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [3857] 23 (H31-21) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2,6-dichloro-4-trifluoromethylphenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3858] 23 (H31-22) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-bromothiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [3859] 23 (H31-23) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-chloro-5-trifluoromethylphenyl) furan-2-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3860] 23 (H31-24) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3861] 23 (H31-25) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (1-acetylindol-3-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [3862] TABLE 31A-4
    [3863] Example number Compound name
    [3864] 23 (H31-26) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (3,5-bis (trifluoromethyl) phenyl) furan-2-ylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [3865] 23 (H31-27) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-chloro-3-methyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [3866] 23 (H31-28) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3867] 23 (H31-29) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (2-trifluoromethylphenyl) furan-2-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [3868] 23 (H31-30) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,5-dimethyl-1- (4-carboxyphenyl) pyrrol-3-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [3869] 23 (H31-31) 1-benzyl-2,5-dioxo-3-cyclohexylmethyl-9- (5- (4-chlorophenyl) furan-2-ylmethyl) -1,4,9-triaza Spiro [5.6] Undecan
    [3870] Table 22B-1
    [3871]
    [3872] Table 22B-2
    [3873]
    [3874] Table 22B-3
    [3875]
    [3876] Table 22B-4
    [3877]
    [3878] Table 22B-5
    [3879]
    [3880] Table 22B-6
    [3881]
    [3882] Table 22B-7
    [3883]
    [3884] Table 22B-8
    [3885]
    [3886] Table 22B-9
    [3887]
    [3888] TABLE 23B-1
    [3889]
    [3890] TABLE 23B-2
    [3891]
    [3892] TABLE 23B-3
    [3893]
    [3894] Table 24B-1
    [3895]
    [3896] Table 24B-2
    [3897]
    [3898] Table 24B-3
    [3899]
    [3900] Table 24B-4
    [3901]
    [3902] Table 24B-5
    [3903]
    [3904] TABLE 25B-1
    [3905]
    [3906] Table 25B-2
    [3907]
    [3908] Table 25B-3
    [3909]
    [3910] Table 25B-4
    [3911]
    [3912] Table 25B-5
    [3913]
    [3914] TABLE 26B-1
    [3915]
    [3916] TABLE 26B-2
    [3917]
    [3918] TABLE 26B-3
    [3919]
    [3920] TABLE 26B-4
    [3921]
    [3922] TABLE 26B-5
    [3923]
    [3924] Table 27B-1
    [3925]
    [3926] Table 27B-2
    [3927]
    [3928] Table 27B-3
    [3929]
    [3930] Table 27B-4
    [3931]
    [3932] Table 27B-5
    [3933]
    [3934] Table 27B-6
    [3935]
    [3936] Table 27B-7
    [3937]
    [3938] Table 27B-8
    [3939]
    [3940] Table 27B-9
    [3941]
    [3942] Table 27B-10
    [3943]
    [3944] Table 27B-11
    [3945]
    [3946] Table 28B-1
    [3947]
    [3948] Table 28B-2
    [3949]
    [3950] Table 28B-3
    [3951]
    [3952] TABLE 28B-4
    [3953]
    [3954] Table 28B-5
    [3955]
    [3956] TABLE 29B-1
    [3957]
    [3958] TABLE 29B-2
    [3959]
    [3960] TABLE 29B-3
    [3961]
    [3962] TABLE 29B-4
    [3963]
    [3964] TABLE 29B-5
    [3965]
    [3966] Table 30B-1
    [3967]
    [3968] TABLE 30B-2
    [3969]
    [3970] Table 30B-3
    [3971]
    [3972] Table 30B-4
    [3973]
    [3974] Table 30B-5
    [3975]
    [3976] Table 31B-1
    [3977]
    [3978] Table 31B-2
    [3979]
    [3980] Table 31B-3
    [3981]
    [3982] Table 31B-4
    [3983]
    [3984] Table 31B-5
    [3985]
    [3986] TABLE 22C-1
    [3987]
    [3988] TABLE 22C-2
    [3989]
    [3990] Table 22C-3
    [3991]
    [3992] TABLE 23C
    [3993]
    [3994] TABLE 24C-1
    [3995]
    [3996] Table 24C-2
    [3997]
    [3998] TABLE 25C-1
    [3999]
    [4000] TABLE 25C-2
    [4001]
    [4002] TABLE 26C-1
    [4003]
    [4004] TABLE 26C-2
    [4005]
    [4006] TABLE 27C-1
    [4007]
    [4008] Table 27C-2
    [4009]
    [4010] Table 27C-3
    [4011]
    [4012] Table 28C-1
    [4013]
    [4014] TABLE 28C-2
    [4015]
    [4016] TABLE 29C-1
    [4017]
    [4018] TABLE 29C-2
    [4019]
    [4020] TABLE 30C-1
    [4021]
    [4022] TABLE 30C-2
    [4023]
    [4024] TABLE 31C-1
    [4025]
    [4026] TABLE 31C-2
    [4027]
    [4028] Example 24 (1) -24 (119)
    [4029] Instead of Resin (3) and N-allyloxycarbonyl-4-piperidone prepared in Reference Example 2, and n-propylamine and N- (t-butyloxycarbonyl) leucine, respectively, the corresponding compounds were used for reference. Example 3 → Operation similar to Reference Example 4, and using the compound corresponding to 3,5-dimethyl-1-phenyl-4-formylpyrazole instead of Reference Example 5 → Reference Example 6 → Example 1 The following compounds of the present invention were obtained.
    [4030] Example 24 (1)
    [4031] (3S) -1-butyl-2,5-dioxo-3- (4-methoxyphenylmethyl) -9-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4032]
    [4033] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [4034] NMR (CD 3 OD): δ 7.06 (d, J = 9.0 Hz, 2H), 6.84 (d, J = 9.0 Hz, 2H), 4.31 (dd, J = 4.5, 3.6 Hz, 1H), 3.82-3.67 ( m, 4H), 3.49-3.30 (m, 3H), 3.25 (dd, J = 13.8, 3.6 Hz, 1H), 3.23-3.10 (m, 2H), 2.95-2.87 (m, 2H), 2.87 (dd, J = 13.8, 4.5 Hz, 1H), 2.31 (m, 1H), 2.05 (m, 1H), 1.91-1.64 (m, 7H), 1.56-1.14 (m, 7H), 1.09-0.91 (m, 5H) , 0.26 (m, 1 H).
    [4035] Example 24 (2)
    [4036] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-chlorophenyl) thiophen-5-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [4037]
    [4038] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [4039] NMR (CD 3 OD): δ 7.65 (d, J = 8.7 Hz, 2H), 7.42 (d, J = 8.7 Hz, 2H), 7.42 (d, J = 3.6 Hz, 1H), 7.34 (d, J = 3.6 Hz, 1H), 4.61 (brs, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.95-3.72 (m, 2H), 3.65-3.50 (m, 2H), 3.44-3.34 (m , 2H), 2.50-2.12 (m, 4H), 1.89-1.45 (m, 5H), 1.45-1.28 (m, 2H), 1.13-0.89 (m, 9H).
    [4040] Example 24 (3)
    [4041] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-methoxyphenyl) thiophen-5-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4042]
    [4043] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [4044] NMR (CD 3 OD): δ 7.57 (d, J = 9.0 Hz, 2H), 7.33-7.26 (m, 2H), 6.97 (d, J = 9.0 Hz, 2H), 4.58 (brs, 2H), 4.01 ( dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.71 (m, 5H), 3.64-3.50 (m, 2H), 3.44-3.34 (m, 2H), 2.49-2.12 (m, 4H), 1.90- 1.45 (m, 5H), 1.45-1.28 (m, 2H), 1.03-0.88 (m, 9H).
    [4045] Example 24 (4)
    [4046] 1-((2E) -2-butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [4047]
    [4048] TLC: Rf 0.32 (CHCl 3: MeOH = 20: 1);
    [4049] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.44-7.35 (m, 2H), 7.22-7.14 (m, 1H), 7.06 (d, J = 8.7 Hz, 2H), 7.10-7.00 (m, 2H), 5.75-5.60 (m, 1H), 5.52-5.38 (m, 1H), 4.33 (s, 2H), 4.15-3.93 (m, 2H), 4.03 (dd, J = 7.8 , 4.5 Hz, 1H), 3.88-3.66 (m, 2H), 3.55-3.42 (m, 2H), 2.52-2.35 (m, 2H), 2.28-2.08 (m, 2H), 1.90-1.57 (m, 3H ), 1.65 (dd, J = 6.3, 1.5 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4050] Example 24 (5)
    [4051] 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4052]
    [4053] TLC: Rf 0.33 (CHCl 3: MeOH = 20: 1);
    [4054] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.43-7.36 (m, 3H), 7.18 (t, J = 7.2 Hz, 1H), 7.09-6.99 (m, 4H), 6.33 (m, 1H), 6.28 (d, J = 3.0 Hz, 1H), 4.69 (s, 2H), 4.33 (s, 2H), 4.08 (dd, J = 7.8, 4.5 Hz, 1H), 3.87-3.72 (m, 2H), 3.57-3.42 (m, 2H), 2.65-2.38 (m, 2H), 2.30-2.12 (m, 2H), 1.90-1.56 (m, 3H), 0.93 (d, J = 6.6 Hz , 3H), 0.91 (d, J = 6.6 Hz, 3H).
    [4055] Example 24 (6)
    [4056] 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4057]
    [4058] TLC: Rf 0.39 (CHCl 3: MeOH = 20: 1);
    [4059] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.43-7.34 (m, 2H), 7.27 (dd, J = 5.1, 1.2 Hz, 1H), 7.18 (t, J = 7.2 Hz, 1H), 7.09-7.00 (m, 5H), 6.91 (dd, J = 5.1, 3.3 Hz, 1H), 4.92 (brs, 2H), 4.32 (s, 2H), 4.11 (dd, J = 7.8, 4.5 Hz, 1H), 3.84-3.66 (m, 2H), 3.53-3.41 (m, 2H), 2.68-2.46 (m, 2H), 2.23-2.06 (m, 2H), 1.95-1.59 (m, 3H) , 0.95 (d, J = 6.6 Hz, 6H).
    [4060] Example 24 (7)
    [4061] 1-cyclopropylmethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4062]
    [4063] TLC: Rf 0.40 (CHCl 3: MeOH = 20: 1);
    [4064] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.43-7.35 (m, 2H), 7.18 (t, J = 7.2 Hz, 1H), 7.08-7.00 (m, 4H), 4.33 (s, 2H), 4.04 (dd, J = 7.8, 4.5 Hz, 1H), 3.87-3.68 (m, 2H), 3.56-3.43 (m, 2H), 3.46-3.35 (m, 2H), 2.56- 2.35 (m, 2H), 2.23-2.12 (m, 2H), 1.95-1.58 (m, 3H), 1.10-0.95 (m, 1H), 0.95 (d, J = 6.6 Hz, 6H), 0.56-0.45 ( m, 2H), 0.42-0.34 (m, 2H).
    [4065] Example 24 (8)
    [4066] 1- (2-fluorophenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4067]
    [4068] TLC: Rf 0.43 (CHCl 3: MeOH = 20: 1);
    [4069] NMR (CD 3 OD): δ 7.48 (d, J = 9.0 Hz, 2H), 7.42-7.34 (m, 2H), 7.32-7.21 (m, 1H), 7.17 (t, J = 7.5 Hz, 1H), 7.14-7.06 (m, 3H), 7.06-6.98 (m, 4H), 4.80 (brs, 2H), 4.30 (s, 2H), 4.18 (dd, J = 8.1, 4.8 Hz, 1H), 3.86-3.68 ( m, 2H), 3.50-3.35 (m, 2H), 2.50-2.30 (m, 1H), 2.30-2.14 (m, 3H), 1.94-1.62 (m, 3H), 0.97 (d, J = 6.3 Hz, 6H).
    [4070] Example 24 (9)
    [4071] 1- (3-methyl-2-butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [4072]
    [4073] TLC: Rf 0.29 (CHCl 3: MeOH = 20: 1);
    [4074] NMR (CD 3 OD): δ 7.52 (d, J = 8.4 Hz, 2H), 7.43-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.09-7.00 (m, 4H), 4.97 (br, 1H), 4.32 (s, 2H), 4.20-4.00 (m, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.90-3.68 (m, 2H), 3.55-3.45 ( m, 2H), 2.52-2.32 (m, 2H), 2.30-2.08 (m, 2H), 1.90-1.56 (m, 3H), 1.74 (s, 3H), 1.69 (s, 3H), 0.94 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4075] Example 24 (10)
    [4076] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (quinolin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4077]
    [4078] TLC: Rf 0.25 (CHCl 3: MeOH = 20: 1);
    [4079] NMR (CD 3 OD): δ 9.52 (d, J = 1.5 Hz, 1H), 9.35 (d, J = 1.5 Hz, 1H), 8.35 (d, J = 8.7 Hz, 1H), 8.27 (d, J = 8.7 Hz, 1H), 8.24-8.16 (m, 1H), 8.04-7.96 (m, 1H), 4.76 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 4.00-3.85 (m , 2H), 3.68-3.55 (m, 2H), 3.55-3.43 (m, 2H), 2.76-2.56 (m, 2H), 2.27-2.05 (m, 2H), 1.82-1.10 (m, 15H), 1.05 -0.83 (m, 2H), 0.92 (t, J = 7.2 Hz, 3H).
    [4080] Example 24 (11)
    [4081] 1-butyl-2,5-dioxo-3- (benzyloxycarbonylmethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4082]
    [4083] TLC: Rf 0.74 (CHCl 3: MeOH = 9: 1);
    [4084] NMR (CD 3 OD): δ 7.52 (d, J = 7.0 Hz, 2H), 7.40 (t, J = 7.5 Hz, 2H), 7.33 (m, 5H), 7.18 (t, J = 7.5 Hz, 1H) , 7.05 (m, 4H), 5.12 (s, 2H), 4.33 (s, 2H), 4.31 (m, 1H), 3.88 (m, 1H), 3.66 (m, 1H), 3.50-3.35 (m, 4H ), 3.08 (dd, J = 17.7, 4.8 Hz, 1H), 2.86 (dd, J = 17.7, 3.0 Hz, 1H), 2.34 (m, 2H), 2.25 (m, 2H), 1.50 (m, 2H) , 1.36 (m, 2H), 0.94 (t, J = 7.5 Hz, 3H).
    [4085] Example 24 (12)
    [4086] 1- (3-methyl-2-butenyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4087]
    [4088] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [4089] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.96 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.96 (m, 1H), 4.26 (s, 4H), 4.22 (s, 2H), 4.10-4.00 (m, 3H), 3.84-3.68 (m, 2H), 3.52-3.40 (m, 2H), 2.43-2.08 (m, 4H), 1.84-1.42 (m, 13H), 1.38-1.12 (m, 4H), 1.04-0.85 (m, 2H).
    [4090] Example 24 (13)
    [4091] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-((2E) -3-phenyl-2-propenyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4092]
    [4093] TLC: Rf 0.28 (CHCl 3: MeOH = 20: 1);
    [4094] NMR (CD 3 OD): δ 7.53-7.48 (m, 2H), 7.30-7.40 (m, 3H), 6.95 (d, J = 16.2 Hz, 1H), 6.36 (dd, J = 16.2, 8.1 Hz, 1H ), 4.07 (dd, J = 7.5, 4.5 Hz, 1H), 3.96 (d, J = 8.1 Hz, 2H), 3.86-3.75 (m, 2H), 3.60-3.52 (m, 2H), 3.42-3.34 ( m, 2H), 2.42-2.18 (m, 4H), 1.82-1.14 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [4095] Example 24 (14)
    [4096] (3S) -1-butyl-2,5-dioxo-3- (1,1-dimethylethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4097]
    [4098] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [4099] NMR (CD 3 OD): δ 7.54 (d, J = 8.5 Hz, 2H), 7.39 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.08-7.02 (m, 4H), 4.34 ( s, 2H), 3.88 (m, 2H), 3.62 (s, 1H), 3.46 (m, 4H), 2.45 (m, 2H), 2.13 (m, 2H), 1.66-1.47 (m, 2H), 1.36 (m, 2H), 1.02 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H).
    [4100] Example 24 (15)
    [4101] (3S) -1-Butyl-2,5-dioxo-3- (1,1-dimethylethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4102]
    [4103] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4104] NMR (CD 3 OD): δ 7.07 (m, 1H), 6.99 (d, J = 8.0 Hz, 1H), 6.91 (d, J = 8.0 Hz, 1H), 4.26 (m, 4H), 4.24 (s, 2H), 3.83 (m, 2H), 3.62 (s, 1H), 3.45 (m, 4H), 2.42 (m, 2H), 2.11 (m, 2H), 1.64-1.5 (m, 2H), 1.38 (m , 2H), 1.01 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H).
    [4105] Example 24 (16)
    [4106] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4107]
    [4108] TLC: Rf 0.67 (CHCl 3: MeOH = 10: 1);
    [4109] NMR (CD 3 OD): δ 7.34 (s, 1H), 4.73 (s, 2H), 4.01 (dd, J = 8.0, 4.5 Hz, 1H), 3.93 (m, 2H), 3.65 (m, 2H), 3.41 (m, 2H), 2.53-2.41 (m, 2H), 2.48 (s, 3H), 2.23 (m, 2H), 1.85-1.52 (m, 5H), 1.38 (m, 2H), 0.96 (t, J = 7.0 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [4110] Example 24 (17)
    [4111] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4112]
    [4113] TLC: Rf 0.66 (CHCl 3: MeOH = 10: 1);
    [4114] NMR (CD 3 OD): δ 7.34 (s, 1H), 4.72 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.98-3.86 (m, 2H), 3.67-3.63 (m , 2H), 3.44-3.38 (m, 2H), 2.56-2.42 (m, 2H), 2.48 (s, 3H), 2.30-2.14 (m, 2H), 1.84-1.18 (m, 15H), 0.96 (t , J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [4115] Example 24 (18)
    [4116] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4117]
    [4118] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [4119] NMR (CD 3 OD): δ 7.63 (s, 1 H), 4.69 (s, 2 H), 4.03 (dd, J = 7.3, 4.5 Hz, 1 H), 3.96-3.82 (m, 2H), 3.72-3,58 (m, 2H), 3.42-3.37 (m, 2H), 2.52 (s, 3H), 2.56-2.36 (m, 2H), 2.28-2.12 (m, 2H), 1.80-1.12 (m, 15H), 0.96 (t, J = 7.5 Hz, 3H), 0.96 (m, 2H).
    [4120] Example 24 (19)
    [4121] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4122]
    [4123] TLC: Rf 0.70 (CHCl 3: MeOH = 10: 1);
    [4124] NMR (CD 3 OD): δ 7.63 (s, 1H), 4.69 (brs, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.99-3.83 (m, 2H), 3.70-3.58 (m , 2H), 3.44-3.34 (m, 2H), 2.53 (s, 3H), 2.50-2.33 (m, 2H), 2.32-2.12 (m, 2H), 1.88-1.46 (m, 5H), 1.45-1.31 (m, 2 H), 1.01-0.90 (m, 9 H).
    [4125] Example 24 (20)
    [4126] (3R) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4127]
    [4128] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4129] NMR (CD 3 OD): δ 7.04 (d, J = 2.0 Hz, 1H), 6.97 (dd, J = 8.5, 2.0 Hz, 1H), 6.93 (d, J = 8.5 Hz, 1H), 4.26 (s, 4H), 4.24 (s, 2H), 4.04 (dd, J = 7.5, 5.0 Hz, 1H), 3.76 (m, 2H), 3.46 (m, 4H), 2.39-2.11 (m, 4H), 1.78-1.17 (m, 15H), 0.95 (t, J = 7.0 Hz, 3H), 0.95 (m, 2H).
    [4130] HPLC conditions
    [4131] Column used: YMC CHIRAL-CD BR, 0.46 × 25 cm, YMC, DB12S05-2546 WTI;
    [4132] Flow rate used: 0.5 mL / min;
    [4133] Solvent used
    [4134] Solution A: 0.1 M aqueous potassium dihydrogen phosphate solution
    [4135] Liquid B: Acetonitrile
    [4136] A: B = 84: 16;
    [4137] UV used: 235 nm;
    [4138] Retention time: 18 minutes.
    [4139] Example 24 (21)
    [4140] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4141]
    [4142] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4143] NMR (CD 3 OD): δ 7.04 (d, J = 2.0 Hz, 1H), 6.97 (dd, J = 8.5, 2.0 Hz, 1H), 6.93 (d, J = 8.5 Hz, 1H), 4.26 (s, 4H), 4.24 (s, 2H), 4.04 (dd, J = 7.5, 5.0 Hz, 1H), 3.76 (m, 2H), 3.46 (m, 4H), 2.39-2.11 (m, 4H), 1.78-1.17 (m, 15H), 0.95 (t, J = 7.0 Hz, 3H), 0.95 (m, 2H).
    [4144] HPLC conditions
    [4145] Column used: YMC CHIRAL-CD BR, 0.46 × 25 cm, YMC, DB12S05-2546 WTI;
    [4146] Flow rate used: 0.5 mL / min;
    [4147] Solvent used
    [4148] Solution A: 0.1 M aqueous potassium dihydrogen phosphate solution
    [4149] Liquid B: Acetonitrile
    [4150] A: B = 84: 16;
    [4151] UV used: 235 nm;
    [4152] Retention time: 20 minutes.
    [4153] Example 24 (22)
    [4154] (3R) -1-butyl-2,5-dioxo-3-((1R) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4155]
    [4156] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4157] NMR (CD 3 OD): δ 7.53 (d, J = 8.5 Hz, 2H), 7.39 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.08-7.01 (m, 4H), 4.33 ( s, 2H), 3.96 (d, J = 2.5 Hz, 1H), 3.92 (m, 1H), 3.75 (m, 1H), 3.53-3.44 (m, 4H), 2.49-2.32 (m, 2H), 2.16 (m, 2H), 2.06-1.98 (m, 1H), 1.61-1.21 (m, 6H), 1.00-0.89 (m, 9H).
    [4158] Example 24 (23)
    [4159] (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4160]
    [4161] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4162] NMR (CD 3 OD): δ 7.53 (d, J = 8.5 Hz, 2H), 7.39 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.08-7.01 (m, 4H), 4.33 ( s, 2H), 3.96 (d, J = 2.5 Hz, 1H), 3.92 (m, 1H), 3.75 (m, 1H), 3.53-3.44 (m, 4H), 2.49-2.32 (m, 2H), 2.16 (m, 2H), 2.06-1.98 (m, 1H), 1.61-1.21 (m, 6H), 1.00-0.89 (m, 9H).
    [4163] Example 24 (24)
    [4164] 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4165]
    [4166] TLC: Rf 0.70 (CHCl 3: MeOH = 10: 1);
    [4167] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.2 Hz, 2H), 7.18 (t, J = 7.2 Hz, 1H), 7.09-7.00 ( m, 4H), 4.33 (brs, 2H), 4.28-4.10 (m, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.86-3.70 (m, 2H), 3.56-3.43 (m, 2H), 2.59-2.40 (m, 2H), 2.34-2.15 (m, 2H), 1.89-1.57 (m, 6H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz , 3H).
    [4168] Example 24 (25)
    [4169] 1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4170]
    [4171] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [4172] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.4, 2.1 Hz, 1H), 6.93 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.18 (brs, 2H), 4.07 (dd, J = 6.9, 4.8 Hz, 1H), 3.84-3.68 (m, 2H), 3.55-3.42 (m, 2H), 2.57 -2.40 (m, 2H), 2.32-2.12 (m, 2H), 1.85-1.42 (m, 11H), 1.38-1.13 (m, 3H), 1.04-0.85 (m, 2H).
    [4173] Example 24 (26)
    [4174] 1-pentyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4175]
    [4176] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4177] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.4, 2.1 Hz, 1H), 6.92 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.22 (brs, 2H), 4.03 (dd, J = 7.2, 4.5 Hz, 1H), 3.84-3.67 (m, 2H), 3.52-3.33 (m, 4H), 2.43-2.07 (m, 4H) , 1.83-1.42 (m, 9H), 1.41-1.13 (m, 8H), 1.04-0.85 (m, 5H).
    [4178] Example 24 (27)
    [4179] 1- (3-methoxyphenylmethyl) -2,5-dioxo-3- (benzyloxymethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4180]
    [4181] TLC: Rf 0.45 (CHCl 3: MeOH = 10: 1);
    [4182] NMR (CD 3 OD): δ 7.60-7.43 (m, 5H), 7.38-7.24 (m, 5H), 7.14 (t, J = 8.4 Hz, 1H), 6.83-6.72 (m, 3H), 4.96-4.70 (m, 2H), 4.60 (d, J = 11.4 Hz, 1H), 4.50 (d, J = 11.4 Hz, 1H), 4.29 (t, J = 2.4 Hz, 1H), 4.24 (s, 2H), 4.02 (dd, J = 9.6, 2.4Hz, 1H), 3.93-3.79 (m, 1H), 3.72 (s, 3H), 3.70 (dd, J = 9.6, 2.4Hz, 1H), 3.70-3.60 (m, 1H ), 3.55-3.44 (m, 1H), 3.35-3.23 (m, 1H), 2.58-2.05 (m, 10H).
    [4183] Example 24 (28)
    [4184] (3R) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4185]
    [4186] TLC: Rf 0.29 (CHCl 3: MeOH = 10: 1);
    [4187] NMR (CD 3 OD): δ 7.54 (d, J = 8.7 Hz, 2H), 7.42-7.36 (m, 2H), 7.18 (m, 1H), 7.05 (d, J = 8.7 Hz, 2H), 7.05- 7.02 (m, 2H), 4.32 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.85-3.72 (m, 2H), 3.50-3.39 (m, 4H), 2.52-2.38 ( m, 2H), 2.24-2.11 (m, 2H), 1.84-1.20 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.93 (d , J = 6.3 Hz, 3H).
    [4188] HPLC conditions
    [4189] Column used: CHIRALCEL OD-R, 0.46 × 25 cm, DAICEL, ODR0CE-HD028;
    [4190] Flow rate used: 0.4 mL / min;
    [4191] Solvent used
    [4192] Solution A: 0.2 M aqueous potassium dihydrogen phosphate
    [4193] Liquid B: Acetonitrile
    [4194] A: B = 64: 36;
    [4195] UV used: 235 nm;
    [4196] Retention time: 30 minutes.
    [4197] Example 24 (29)
    [4198] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4199]
    [4200] TLC: Rf 0.29 (CHCl 3: MeOH = 10: 1);
    [4201] NMR (CD 3 OD): δ 7.54 (d, J = 8.7 Hz, 2H), 7.42-7.36 (m, 2H), 7.18 (m, 1H), 7.05 (d, J = 8.7 Hz, 2H), 7.05- 7.02 (m, 2H), 4.33 (s, 2H), 3.98 (dd, J = 8 .. 1, 4.5 Hz, 1H), 3.86-3.72 (m, 2H), 3.53-3.37 (m, 4H), 2.47 -2.36 (m, 2H), 2.24-2.12 (m, 2H), 1.80-1.30 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.93 (d, J = 6.3 Hz, 3H).
    [4202] HPLC conditions
    [4203] Column used: CHIRALCEL OD-R, 0.46 × 25 cm, DAICEL, ODR0CE-HD028;
    [4204] Flow rate used: 0.4 mL / min;
    [4205] Solvent used
    [4206] Solution A: 0.2 M aqueous potassium dihydrogen phosphate
    [4207] Liquid B: Acetonitrile
    [4208] A: B = 64: 36;
    [4209] UV used: 235 nm;
    [4210] Retention time: 28 minutes.
    [4211] Example 24 (30)
    [4212] 1-butyl-2,5-dioxo-3-cyclopentylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4213]
    [4214] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [4215] NMR (CD 3 OD): δ 7.05 (d, J = 2.0 Hz, 1H), 6.98 (dd, J = 8.5, 2.0 Hz, 1H), 6.93 (d, J = 8.5 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 3.99 (t, J = 6.0 Hz, 1H), 3.77 (m, 2H), 3.46 (m, 2H), 3.37 (m, 2H), 2.36 (m, 2H), 2.15 (m, 2H), 1.96 (m, 1H), 1.81 (m, 4H), 1.59 (m, 6H), 1.36 (m, 2H), 1.15 (m, 2H), 0.95 (t, J = 7.0 Hz , 3H).
    [4216] Example 24 (31)
    [4217] 1-propyl-2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4218]
    [4219] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [4220] NMR (CD 3 OD): δ 7.59-7.46 (m, 5H), 4.33 (s, 2H), 4.08 (m, 1H), 4.00 (m, 1H), 3.83 (m, 1H), 3.77 (m, 1H ), 3.59 (m, 2H), 3.52 (m, 1H), 3.25 (d, J = 6.5 Hz, 2H), 2.53 (m, 2H), 2.42 (m, 1H), 2.40 (s, 3H), 2.39 (s, 3H), 2.21 (m, 2H), 1.69 (m, 6H), 1.52 (m, 2H), 1.21 (m, 4H), 0.95 (t, J = 7.0 Hz, 3H), 0.88 (m, 2H).
    [4221] Example 24 (32)
    [4222] (3S) -1-Butyl-2,5-dioxo-3- (1-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4223]
    [4224] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4225] NMR (CD 3 OD): δ 7.06-6.90 (m, 3H), 4.26 (s, 4H), 4.23 (s, 2H), 3.95 (d, J = 3.3 Hz, 1H), 3.87 (m, 1H), 3.70 (m, 1H), 3.58-3.42 (m, 4H), 2.56-2.30 (m, 2H), 2.20-1.98 (m, 2H), 1.54-1.00 (m, 7H), 0.99 (d, J = 7.2 Hz, 3H), 0.95 (t, J = 7.5 Hz, 3H), 0.91 (t, J = 7.5 Hz, 3H).
    [4226] Example 24 (33)
    [4227] (3R) -1-butyl-2,5-dioxo-3- (1-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4228]
    [4229] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4230] NMR (CD 3 OD): δ 7.06-6.91 (m, 3H), 4.26 (s, 4H), 4.23 (s, 2H), 3.95 (d, J = 3.3 Hz, 1H), 3.87 (m, 1H), 3.70 (m, 1H), 3.56-3.40 (m, 4H), 2.50-2.32 (m, 2H), 2.18-1.96 (m, 2H), 1.62-1.17 (m, 7H), 0.99 (d, J = 7.2 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H), 0.91 (t, J = 7.5 Hz, 3H).
    [4231] Example 24 (34)
    [4232] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylmethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4233]
    [4234] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [4235] NMR (CD 3 OD): δ 7.32-7.21 (m, 5H), 7.17 (d, J = 3.6 Hz, 1H), 6.89 (d, J = 3.6 Hz, 1H), 4.51 (s, 2H), 4.17 ( s, 2H), 4.00 (dd, J = 7.8 Hz, 4.5 Hz, 1H), 3.84-3.72 (m, 2H), 3.56-3.44 (m, 2H), 3.38-3.32 (m, 2H), 2.42-2.14 (m, 4H), 1.84-1.30 (m, 7H), 0.95 (t, J = 6.9 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H), 0.92 (d, J = 6.3 Hz, 3H) .
    [4236] Example 24 (35)
    [4237] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenylmethylthiophen-5-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4238]
    [4239] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4240] NMR (CD 3 OD): δ 7.32-7.21 (m, 5H), 7.18 (d, J = 3.6 Hz, 1H), 6.89 (d, J = 3.6 Hz, 1H), 4.51 (s, 2H), 4.17 ( s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.72 (m, 2H), 3.58-3.44 (m, 2H), 3.40-3.36 (m, 2H), 2.44-2.08 ( m, 4H), 1.81-1.07 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [4241] Example 24 (36)
    [4242] (3R) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4243]
    [4244] TLC: Rf 0.41 (CHCl 3: MeOH = 20: 1);
    [4245] NMR (CD 3 OD): δ 7.05 (s, 1H), 6.98 (d, J = 8.4 Hz, 1H), 6.92 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.00 (dd, J = 7.0, 3.0 Hz, 1H), 3.83-3.64 (m, 2H), 3.50 (m, 2H), 3.38 (m, 2H), 2.35 (m, 2H), 2.25 (m , 2H), 1.99 (m, 1H), 1.55 (m, 1H), 1.50 (m, 2H), 1.35 (m, 2H), 0.99 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H) .
    [4246] Example 24 (37)
    [4247] (3S) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4248]
    [4249] TLC: Rf 0.41 (CHCl 3: MeOH = 20: 1);
    [4250] NMR (CD 3 OD): δ 7.05 (s, 1H), 6.98 (d, J = 8.4 Hz, 1H), 6.92 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.00 (dd, J = 7.0, 3.0 Hz, 1H), 3.83-3.63 (m, 2H), 3.50 (m, 2H), 3.38 (m, 2H), 2.35 (m, 2H), 2.25 (m , 2H), 1.99 (dd, J = 14.0, 3.0 Hz, 1H), 1.55 (dd, J = 14.0, 7.0 Hz, 1H), 1.50 (m, 2H), 1.35 (m, 2H), 0.99 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H).
    [4251] Example 24 (38)
    [4252] (3R) -1- (2-butynyl) -2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [4253]
    [4254] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [4255] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 ( m, 4H), 4.33 (brs, 2H), 4.33-4.09 (m, 2H), 4.03 (dd, J = 6.9, 3.3 Hz, 1H), 3.85-3.68 (m, 2H), 3.58-3.43 (m, 2H), 2.59-2.41 (m, 2H), 2.40-2.20 (m, 2H), 2.03 (dd, J = 14.4, 3.3 Hz, 1H), 1.75 (brs, 3H), 1.56 (dd, J = 14.4, 6.9 Hz, 1H), 0.99 (s, 9H).
    [4256] Example 24 (39)
    [4257] (3S) -1- (2-butynyl) -2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [4258]
    [4259] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [4260] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 ( m, 4H), 4.33 (brs, 2H), 4.33-4.09 (m, 2H), 4.03 (dd, J = 6.9, 3.3 Hz, 1H), 3.85-3.68 (m, 2H), 3.58-3.43 (m, 2H), 2.59-2.41 (m, 2H), 2.40-2.20 (m, 2H), 2.03 (dd, J = 14.4, 3.3 Hz, 1H), 1.75 (brs, 3H), 1.56 (dd, J = 14.4, 6.9 Hz, 1H), 0.99 (s, 9H).
    [4261] Example 24 (40)
    [4262] 1-butyl-2,5-dioxo-3-cycloheptylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4263]
    [4264] TLC: Rf 0.70 (CHCl 3: MeOH = 10: 1);
    [4265] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.4, 2.1 Hz, 1H), 6.93 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.24 (s, 2H), 3.99 (dd, J = 8.1, 4.2 Hz, 1H), 3.84-3.70 (m, 2H), 3.45 (m, 2H), 3.36 (m, 2H), 2.37-2.11 (m, 4H), 1.80-1.49 (m, 15H), 1.36 (m, 2H), 1.22 (m, 2H), 0.95 (t, J = 7.5 Hz, 3H).
    [4266] Example 24 (41)
    [4267] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,4,6-trimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4268]
    [4269] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [4270] NMR (CD 3 OD): δ 6.31 (s, 2H), 4.26 (s, 2H), 4.03 (dd, J = 7.8, 4.5 Hz, 1H), 3.89 (s, 6H), 3.84 (s, 3H), 3.84-3.73 (m, 2H), 3.54-3.33 (m, 4H), 2.44-2.25 (m, 2H), 2.24-2.03 (m, 2H), 1.84-1.12 (m, 15H), 1.06-0.85 (m , 5H).
    [4271] Example 24 (42)
    [4272] 1-Butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4273]
    [4274] TLC: Rf 0.71 (CHCl 3: MeOH = 10: 1);
    [4275] NMR (CD 3 OD): δ 7.05-6.91 (m, 3H), 4.26 (s, 4H), 4.22 (s, 2H), 4.04 (t, J = 5.4 Hz, 1H), 3.84 (m, 1H), 3.67 (m, 1H), 3.54-3.40 (m, 3H), 3.35 (m, 1H), 2.44-2.08 (m, 4H), 1.90-1.16 (m, 19H), 0.95 (t, J = 7.5 Hz, 3H), 0.95 (m, 2H).
    [4276] Example 24 (43)
    [4277] 1-butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4278]
    [4279] TLC: Rf 0.76 (CHCl 3: MeOH = 10: 1);
    [4280] NMR (CD 3 OD): δ 7.53-7.49 (m, 2H), 7.42-7.36 (m, 2H), 7.18 (m, 1H), 7.10-7.02 (m, 4H), 4.32 (s, 2H), 4.04 (t, J = 4.8 Hz, 1H), 3.87 (m, 1H), 3.71 (m, 1H), 3.56-3.40 (m, 3H), 3.35 (m, 1H), 2.48-2.12 (m, 4H), 1.86-1.10 (m, 19 H), 0.95 (t, J = 7.5 Hz, 3 H), 0.95 (m, 2H).
    [4281] Example 24 (44)
    [4282] 1-butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4283]
    [4284] TLC: Rf 0.64 (CHCl 3: MeOH = 10: 1);
    [4285] NMR (CD 3 OD): δ 7.59-7.45 (m, 5H), 4.31 (s, 2H), 4.06 (t, J = 5.0 Hz, 1H), 3.92 (m, 1H), 3.77 (m, 1H), 3.63-3.37 (m, 4H), 2.44 (m, 2H), 2.39 (s, 3H), 2.38 (s, 3H), 2.21 (m, 2H), 1.85-1.6 8 (m, 7H), 1.54 (m , 2H), 1.39 (m, 4H), 1.23 (m, 6H), 0.96 (t, J = 7.5 Hz, 3H), 0.89 (m, 2H).
    [4286] Example 24 (45)
    [4287] 1-butyl-2,5-dioxo-3- (2-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4288]
    [4289] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [4290] NMR (CD 3 OD): δ 7.50 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.09-7.00 ( m, 4H), 4.32 (brs, 2H), 4.29 (dd, J = 9.9, 3.0 Hz, 1H), 4.04-3.88 (m, 2H), 3.59-3.40 (m, 4H), 2.46-2.21 (m, 4H), 2.18 (dd, J = 14.4, 3.0 Hz, 1H), 1.75 (dd, J = 14.4, 9.9 Hz, 1H), 1.61-1.43 (m, 2H), 1.42-1.29 (m, 2H), 1.28 (s, 6H), 0.95 (t, J = 7.5 Hz, 3H).
    [4291] Example 24 (46)
    [4292] 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [4293]
    [4294] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [4295] NMR (CD 3 OD): δ 7.61-7.45 (m, 5H), 4.32 (s, 2H), 4.31-4.18 (m, 2H), 4.06 (dd, J = 7.8, 4.5 Hz, 1H), 3.93-3.77 (m, 2H), 3.68-3.57 (m, 2H), 2.72-2.57 (m, 2H), 2.40 (s, 3H), 2.38 (s, 3H), 2.36-2.16 (m, 2H), 1.92-1.59 (m, 6H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4296] Example 24 (47)
    [4297] 1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [4298]
    [4299] TLC: Rf 0.37 (CHCl 3: MeOH = 10: 1);
    [4300] NMR (CD 3 OD): δ 7.60-7.43 (m, 5H), 4.32 (s, 2H), 4.23 (d, J = 2.1 Hz, 2H), 4.09 (dd, J = 7.2, 4.8 Hz, 1H), 3.92-3.78 (m, 2H), 3.68-3.56 (m, 2H), 2.66-2.51 (m, 2H), 2.38 (s, 3H), 2.36 (s, 3H), 2.36-2.16 (m, 2H), 1.83-1.60 (m, 10H), 1.59-1.43 (m, 1H), 1.38-1.12 (m, 3H), 1.06-0.87 (m, 2H).
    [4301] Example 24 (48)
    [4302] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [4303]
    [4304] TLC: Rf 0.35 (CHCl 3: MeOH = 20: 1);
    [4305] NMR (CD 3 OD): δ 7.63-7.48 (m, 5H), 4.33 (s, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.95-3.74 (m, 2H), 3.67-3.56 (m, 2H), 3.48 (m, 2H), 2.72-2.58 (m, 2H), 2.45 (s, 3H), 2.41 (s, 3H), 2.30-2.07 (m, 2H), 1.84-1.10 (m , 15H), 1.02-0.92 (m, 2H), 0.96 (t, J = 7.2 Hz, 3H).
    [4306] Example 24 (49)
    [4307] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4308]
    [4309] TLC: Rf 0.23 (CHCl 3: MeOH = 10: 1);
    [4310] NMR (CD 3 OD): δ 8.19 (m, 1H), 8.07 (m, 1H), 7.47-7.42 (m, 2H), 7.29-7.19 (m, 4H), 4.55 (s, 2H), 4.03 (dd) , J = 7.8, 4.5 Hz, 1H), 3.94 (m, 2H), 3.64 (m, 2H), 3.38 (m, 2H), 2.54-2.16 (m, 4H), 1.90-1.28 (m, 7H), 0.96 (t, J = 6.9 Hz, 3H), 0.96 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4311] Example 24 (50)
    [4312] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4313]
    [4314] TLC: Rf 0.62 (CHCl 3: MeOH = 10: 1);
    [4315] NMR (CD 3 OD): δ 8.19 (m, 1H), 8.09 (m, 1H), 7.47-7.42 (m, 2H), 7.29-7.19 (m, 4H), 4.55 (s, 2H), 4.05 (dd , J = 7.8, 4.8 Hz, 1H), 3.96 (m, 2H), 3.64 (m, 2H), 3.42 (m, 2H), 2.48 (m, 2H), 2.36-2.16 (m, 2H), 1.82- 1.14 (m, 15 H), 0.96 (t, J = 7.5 Hz, 3 H), 0.95-0.84 (m, 2H).
    [4316] Example 24 (51)
    [4317] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylbenzomorpholin-7-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4318]
    [4319] TLC: Rf 0.69 (CHCl 3: MeOH = 10: 1);
    [4320] NMR (CDCl3): δ 6.93 (d, J = 8.7 Hz, 1H), 6.86 (s, 1H), 6.75 (d, J = 8.7 Hz, 1H), 4.28-4.25 (m, 2H), 4.17 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.80-3.65 (m, 2H), 3.50-3.40 (m, 2H), 3.40-3.30 (m, 2H), 2.91 (s, 3H) , 2.38-2.06 (m, 4H), 1.78-1.63 (m, 8H), 1.63-1.42 (m, 3H), 1.40-1.18 (m, 6H), 1.05-0.90 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [4321] Example 24 (52)
    [4322] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylbenzomorpholin-7-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4323]
    [4324] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [4325] NMR (CDCl 3): δ 7.00 (d, J = 7.2 Hz, 1H), 6.94 (s, 1H), 6.85 (d, J = 7.2 Hz, 1H), 4.31-4.29 (m, 2H), 4.19 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.79-3.66 (m, 2H), 3.47-3.34 (m, 6H), 2.97 (s, 3H), 2.45-2.34 (m, 2H) , 2.22-2.10 (m, 2H), 1.84-1.75 (m, 1H), 1.71-1.46 (m, 4H), 1.42-1.32 (m, 2H), 0.97-0.92 (m, 9H).
    [4326] Example 24 (53)
    [4327] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (N-methyl-N-phenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Dihydrochloride
    [4328]
    [4329] TLC: Rf 0.40 (CHCl 3: MeOH = 20: 1);
    [4330] NMR (CD 3 OD): δ 7.40-7.28 (m, 4H), 7.19-7.10 (m, 3H), 6.94-6.86 (m, 2H), 4.23 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.86-3.63 (m, 2H), 3.55-3.30 (m, 4H), 3.31 (s, 3H), 2.46-2.27 (m, 2H), 2.26-2.06 (m, 2H), 1.90 -1.42 (m, 5H), 1.44-1.26 (m, 2H), 0.98-0.91 (m, 9H).
    [4331] Example 24 (54)
    [4332] 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (N-methyl-N-phenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4333]
    [4334] TLC: Rf 0.52 (CHCl 3: MeOH = 20: 1);
    [4335] NMR (CD 3 OD): δ 7.40-7.28 (m, 4H), 7.20-7.12 (m, 3H), 6.93-6.86 (m, 2H), 4.24 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.85-3.66 (m, 2H), 3.55-3.40 (m, 2H), 3.40-3.30 (m, 2H), 3.32 (s, 3H), 2.44-2.07 (m, 4H), 1.84 -1.40 (m, 10H), 1.40-1.10 (m, 5H), 1.06-0.85 (m, 2H), 0.95 (t, J = 7.5 Hz, 3H).
    [4336] Example 24 (55)
    [4337] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (3,5-dimethylpyrazol-1-yl) -5-methoxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4338]
    [4339] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [4340] NMR (CD 3 OD): δ 7.53 (d, J = 3.0 Hz, 1H), 7.44 (d, J = 8.7 Hz, 1H), 7.22 (dd, J = 8.7, 3.0 Hz, 1H), 6.29 (s, 1H), 4.09 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.94 (s, 3H), 3.74 (m, 2H), 3.42 (m, 4H), 2.44 (m, 2H ), 2.37 (s, 3H), 2.22 (s, 3H), 2.22 (m, 2H), 1.86-1.30 (m, 7H), 0.96 (t, J = 7.8Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4341] Example 24 (56)
    [4342] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2- (3,5-dimethylpyrazol-1-yl) -5-methoxyphenylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [4343]
    [4344] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4345] NMR (CD 3 OD): δ 7.43 (d, J = 8.7 Hz, 1H), 7.40 (d, J = 2.7 Hz, 1H), 7.22 (dd, J = 8.7, 2.7 Hz, 1H), 6.22 (s, 1H), 4.09 (s, 2H), 4.06 (dd, J = 7.5, 4.2 Hz, 1H), 3.93 (s, 3H), 3.80 (m, 2H), 3.42 (m, 4H), 2.38 (m, 2H ), 2.34 (s, 3H), 2.22 (s, 3H), 2.20 (m, 2H), 1.80-1.16 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H) .
    [4346] Example 24 (57)
    [4347] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-diethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4348]
    [4349] TLC: Rf 0.47 (CHCl 3: MeOH = 20: 1);
    [4350] NMR (CD 3 OD): δ 7.53 (d, J = 9.0 Hz, 2H), 7.49 (d, J = 9.0 Hz, 2H), 4.31 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.73 (m, 2H), 3.65-3.54 (m, 2H), 3.49-3.38 (m, 2H), 2.88 (q, J = 7.5 Hz, 2H), 2.77 (q, J = 7.5 Hz , 2H), 2.58-2.38 (m, 2H), 2.30-2.12 (m, 2H), 1.90-1.56 (m, 5H), 1.55-1.30 (m, 2H), 1.31 (t, J = 7.5 Hz, 3H ), 0.99-0.94 (m, 12H).
    [4351] Example 24 (58)
    [4352] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-diethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [4353]
    [4354] TLC: Rf 0.51 (CHCl 3: MeOH = 20: 1);
    [4355] NMR (CD 3 OD): δ 7.58 (d, J = 9.0 Hz, 2H), 7.48 (d, J = 9.0 Hz, 2H), 4.31 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.73 (m, 2H), 3.65-3.54 (m, 2H), 3.50-3.38 (m, 2H), 2.88 (q, J = 7.5 Hz, 2H), 2.77 (q, J = 7.5 Hz , 2H), 2.60-2.40 (m, 2H), 2.28-2.09 (m, 2H), 1.85-1.10 (m, 15H), 1.31 (t, J = 7.5 Hz, 3H), 1.04-0.85 (m, 2H ), 0.96 (t, J = 7.5 Hz, 3H), 0.94 (t, J = 7.5 Hz, 3H).
    [4356] Example 24 (59)
    [4357] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4358]
    [4359] TLC: Rf 0.65 (CHCl 3: MeOH = 10: 1);
    [4360] NMR (CD 3 OD): δ 8.32 (s, 1H), 8.06 (m, 1H), 7.44 (t, J = 7.5 Hz, 2H), 7.26 (t, J = 7.5 Hz, 1H), 7.14 (d, J = 7.5 Hz, 2H), 7.06 (d, J = 8.7 Hz, 1H), 4.39 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.70 (m, 2H), 3.53-3.41 (m, 4H), 2.45 (m, 2H), 2.25-2.12 (m, 2H), 1.78 (m, 1H), 1.72-1.50 (m, 4H), 1.36 (m, 2H), 0.97- 0.93 (m, 9 H).
    [4361] Example 24 (60)
    [4362] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4363]
    [4364] TLC: Rf 0.67 (CHCl 3: MeOH = 10: 1);
    [4365] NMR (CD 3 OD): δ 8.31 (s, 1H), 8.07 (d, J = 8.3 Hz, 1H), 7.44 (t, J = 7.5 Hz, 2H), 7.26 (t, J = 7.5 Hz, 1H) , 7.14 (d, J = 7.5 Hz, 2H), 7.06 (d, J = 8.3 Hz, 1H), 4.39 (s, 2H), 4.04 (dd, J = 7.8, 4.6 Hz, 1H), 3.90-3.76 ( m, 2H), 3.52-3.38 (m, 4H), 2.58-2.36 (m, 2H), 2.25-2.11 (m, 2H), 1.80-1.42 (m, 10H), 1.42-1.17 (m, 5H), 1.05-0.85 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [4366] Example 24 (61)
    [4367] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,3-benzodioxolan-5-ylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4368]
    [4369] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [4370] NMR (CD 3 OD): δ 7.05-7.00 (m, 2H), 6.92 (m, 1H), 6.03 (s, 2H), 4.26 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H ), 3.84-3.68 (m, 2H), 3.52-3.36 (m, 4H), 2.42-2.10 (m, 4H), 1.88-1.32 (m, 7H), 0.96 (t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4371] Example 24 (62)
    [4372] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,3-benzodioxolan-5-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4373]
    [4374] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [4375] NMR (CD 3 OD): δ 7.06-7.01 (m, 2H), 6.92 (m, 1H), 6.03 (s, 2H), 4.27 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H ), 3.82-3.70 (m, 2H), 3.56-3.36 (m, 4H), 2.48-2.10 (m, 4H), 1.82-1.16 (m, 15H), 0.96 (t, J = 7.5 Hz, 3H) , 0.96 (m, 2 H).
    [4376] Example 24 (63)
    [4377] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-hydroxy-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4378]
    [4379] TLC: Rf 0.88 (CHCl 3: MeOH = 10: 1);
    [4380] NMR (CD 3 OD): δ 7.26 (d, J = 8.5 Hz, 1H), 6.51 (dd, J = 8.5, 2.5 Hz, 1H), 6.48 (d, J = 2.5 Hz, 1H), 4.26 (s, 2H), 4.03 (m, 1H), 3.77 (m, 5H), 3.47 (m, 2H), 3.37 (m, 2H), 2.34 (m, 2H), 2.15 (m, 2H), 1.69 (m, 6H) ), 1.52 (m, 4H), 1.31 (m, 5H), 0.95 (m, 5H).
    [4381] Example 24 (64)
    [4382] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylthiophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4383]
    [4384] TLC: Rf 0.83 (chloroform: methanol = 10: 1);
    [4385] NMR (CD 3 OD): δ 7.44 (d, J = 8.7 Hz, 2H), 7.36 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.80 (m, 2H), 3.49 (m, 2H), 3.34 (m, 2H), 2.50 (s, 3H), 2.36-2.11 (m, 4H), 1.69 (m, 10H), 1.39-1.23 (m, 5H), 0.95 (m, 5H).
    [4386] Example 24 (65)
    [4387] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (N, N-diphenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4388]
    [4389] TLC: Rf 0.48 (CHCl 3: MeOH = 20: 1);
    [4390] NMR (CD 3 OD): δ 7.40-7.25 (m, 6H), 7.13-7.01 (m, 8H), 4.27 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.87-3.68 (m, 2H), 3.56-3.44 (m, 2H), 3.44-3.32 (m, 2H), 2.48-2.32 (m, 2H), 2.29-2.10 (m, 2H), 1.90-1.44 (m, 5H) , 1.44-1.30 (m, 2H), 0.96 (t, J = 6.9 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4391] Example 24 (66)
    [4392] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (N, N-diphenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4393]
    [4394] TLC: Rf 0.53 (CHCl 3: MeOH = 20: 1);
    [4395] NMR (CD 3 OD): δ 7.41-7.26 (m, 6H), 7.14-7.00 (m, 8H), 4.27 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.88-3.68 (m, 2H), 3.57-3.45 (m, 2H), 3.44-3.36 (m, 2H), 2.48-2.32 (m, 2H), 2.28-2.07 (m, 2H), 1.84-1.44 (m, 10H) , 1.44-1.14 (m, 5H), 1.00-0.90 (m, 2H), 0.96 (t, J = 6.9 Hz, 3H).
    [4396] Example 24 (67)
    [4397] (3S) -1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4398]
    [4399] TLC: Rf 0.32 (CHCl 3: MeOH = 20: 1);
    [4400] NMR (CD 3 OD): δ 7.59-7.46 (m, 5H), 4.32 (s, 2H), 4.24 (s, 2H), 4.09 (dd, J = 7.5, 4.5 Hz, 1H), 3.86 (m, 2H ), 3.65 (m, 2H), 2.60 (m, 2H), 2.39 (s, 3H), 2.38 (s, 3H), 2.26 (m, 2H), 1.88-1.66 (m, 10H), 1.53 (m, 1H), 1.25 (m, 3H), 0.96 (m, 2H).
    [4401] Example 24 (68)
    [4402] (3S) -1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4403]
    [4404] TLC: Rf 0.43 (CHCl 3: MeOH = 20: 1);
    [4405] NMR (CD 3 OD): δ 7.60-7.46 (m, 5H), 4.32 (s, 2H), 4.26 (m, 2H), 4.06 (dd, J = 7.5, 4.5 Hz, 1H), 3.85 (m, 2H ), 3.62 (m, 2H), 2.60 (m, 2H), 2.39 (s, 3H), 2.38 (s, 3H), 2.27 (m, 2H), 1.89-1.61 (m, 6H), 0.95 (d, J = 6.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H).
    [4406] Example 24 (69)
    [4407] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4408]
    [4409] TLC: Rf 0.57 (CHCl 3: MeOH = 20: 1);
    [4410] NMR (CD 3 OD): δ 7.59-7.45 (m, 5H), 4.32 (s, 2H), 4.06 (dd, J = 7.8, 4.5 Hz, 1H), 3.85 (m, 2H), 3.60 (m, 2H ), 3.43 (m, 2H), 2.53-2.44 (m, 2H), 2.45 (s, 3H), 2.41 (s, 3H), 2.32-2.16 (m, 2H), 1.80-1.17 (m, 15H), 1.02-0.93 (m, 2H), 0.96 (d, J = 7.0 Hz, 3H).
    [4411] Example 24 (70)
    [4412] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9 -Triazaspiro [5.5] undecane, dihydrochloride
    [4413]
    [4414] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [4415] NMR (CD 3 OD): δ 7.36 (d, J = 8.4 Hz, 2H), 7.31 (d, J = 8.4 Hz, 2H), 4.30 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.84 (m, 2H), 3.60 (m, 2H), 3.38 (m, 2H), 2.42 (s, 3H), 2.37 (s, 3H), 2.35 (s, 3H), 2.52-2.18 (m , 4H), 1.90-1.32 (m, 7H), 0.96 (t, J = 7.8 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4416] Example 24 (71)
    [4417] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4418]
    [4419] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [4420] NMR (CD 3 OD): δ 7.38 (d, J = 8.4 Hz, 2H), 7.33 (d, J = 8.4 Hz, 2H), 4.31 (s, 2H), 4.06 (dd, J = 7.5, 4.5 Hz, 1H), 3.82 (m, 2H), 3.60 (m, 2H), 3.42 (m, 2H), 2.43 (s, 3H), 2.38 (s, 3H), 2.36 (s, 3H), 2.56-2.14 (m , 3H), 1.84-1.16 (m, 15H), 0.97 (t, J = 7.2 Hz, 3H), 0.97 (m, 2H).
    [4421] Example 24 (72)
    [4422] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [4423]
    [4424] TLC: Rf 0.30 (CHCl 3: MeOH = 20: 1);
    [4425] NMR (CD 3 OD): δ 7.57 (d, J = 9.0 Hz, 2H), 7.49 (d, J = 9.0 Hz, 2H), 4.31 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.91-3.80 (m, 2H), 3.60 (m, 2H), 3.46 (m, 2H), 2.52 (m, 2H), 2.40 (s, 3H), 2.39 (s, 3H), 2.27-2.15 (m, 2H), 1.86-1.81 (m, 1H), 1.76-1.51 (m, 4H), 1.44-1.32 (m, 2H), 0.96 (t, J = 7.0 Hz, 3H), 0.95 (d, J = 6.0 Hz, 3H), 0.94 (d, J = 6.0 Hz, 3H).
    [4426] Example 24 (73)
    [4427] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [4428]
    [4429] TLC: Rf 0.27 (CHCl 3: MeOH = 20: 1);
    [4430] NMR (CD 3 OD): δ 7.57 (d, J = 8.5 Hz, 2H), 7.48 (d, J = 8.5 Hz, 2H), 4.31 (s, 2H), 4.04 (dd, J = 7.8, 4.5 Hz, 1H), 3.91-3.77 (m, 2H), 3.60 (m, 2H), 3.45 (m, 2H), 2.50 (m, 2H), 2.39 (s, 6H), 2.27-2.14 (m, 2H), 1.80 -1.51 (m, 9H), 1.44-1.17 (m, 6H), 1.03-0.89 (m, 5H).
    [4431] Example 24 (74)
    [4432] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-trifluoromethylphenyl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4433]
    [4434] TLC: Rf 0.23 (CHCl 3: MeOH = 20: 1);
    [4435] NMR (CD 3 OD): δ 7.87 (d, J = 8.7 Hz, 2H), 7.72 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.93-3.78 (m, 2H), 3.60 (m, 2H), 3.43 (m, 2H), 2.50 (m, 2H), 2.45 (s, 3H), 2.40 (s, 3H), 2.29-2.16 (m, 2H), 1.86-1.77 (m, 1H), 1.74-1.54 (m, 4H), 1.44-1.34 (m, 2H), 0.96 (t, J = 7.0 Hz, 3H), 0.95 (d, J = 6.0 Hz, 3H), 0.94 (d, J = 6.0 Hz, 3H).
    [4436] Example 24 (75)
    [4437] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-trifluoromethylphenyl) pyrazol-4-ylmethyl) -1,4,9 -Triazaspiro [5.5] undecane, dihydrochloride
    [4438]
    [4439] TLC: Rf 0.37 (CHCl 3: MeOH = 20: 1);
    [4440] NMR (CD 3 OD): δ 7.87 (d, J = 8.4 Hz, 2H), 7.72 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.92-3.78 (m, 2H), 3.60 (m, 2H), 3.45 (m, 2H), 2.50 (m, 2H), 2.45 (s, 3H), 2.40 (s, 3H), 2.28-2.15 (m, 2H), 1.80-1.51 (m, 9H), 1.44-1.21 (m, 6H), 1.03-0.93 (m, 5H).
    [4441] Example 24 (76)
    [4442] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-diethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4443]
    [4444] TLC: Rf 0.70 (CHCl 3: MeOH = 10: 1);
    [4445] NMR (CD 3 OD): δ 7.61-7.53 (m, 3H), 7.53-7.46 (m, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.79 (m, 2H), 3.65-3.58 (m, 2H), 3.50-3.38 (m, 2H), 2.85-2.75 (m, 4H), 2.47 (br, 2H), 2.28-2.16 (m, 2H), 1 83-1.46 (m, 3H), 1.41-1.29 (m, 4H), 0.98-0.91 (m, 15H).
    [4446] Example 24 (77)
    [4447] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-diethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Dihydrochloride
    [4448]
    [4449] TLC: Rf 0.67 (CHCl 3: MeOH = 10: 1);
    [4450] NMR (CD 3 OD): δ 7.61-7.53 (m, 3H), 7.53-7.46 (m, 2H), 4.32 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.79 (m, 2H), 3.70-3.55 (m, 2H), 3.47-3.31 (m, 2H), 2.91-2.75 (m, 4H), 2.60-2.45 (m, 2H), 2.30-2.14 (m, 2H) , 1.80-1.43 (m, 9H), 1.43-1.15 (m, 8H), 0.98-0.91 (m, 9H).
    [4451] Example 24 (78)
    [4452] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenylthiazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4453]
    [4454] TLC: Rf 0.62 (CHCl 3: MeOH = 10: 1);
    [4455] NMR (CD 3 OD): δ 8.03-8.00 (m, 2H), 7.87 (s, 1H), 7.52-7.49 (m, 3H), 4.54 (s, 2H), 4.04 (dd, J = 7.6, 4.8 Hz , 1H), 4.04-3.87 (m, 2H), 3.70-3.58 (m, 2H), 3.51-3.39 (m, 2H), 2.58-2.38 (m, 2H), 2.26-2.13 (m, 2H), 1.7 8-1.43 (m, 9H), 1.40-1.15 (m, 6H), 1.10-0.90 (m, 5H).
    [4456] Example 24 (79)
    [4457] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylthiazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4458]
    [4459] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [4460] NMR (CD 3 OD): δ 8.02-8.01 (m, 2H), 7.85 (s, 1H), 7.51-7.50 (m, 3H), 4.55 (s, 2H), 4.03-3.86 (m, 3H), 3.68 -3.59 (m, 2H), 3.45-3.36 (m, 2H), 2.50-2.34 (m, 2H), 2.29-2.16 (m, 2H), 1.88-1.45 (m, 5H), 1.36 (q, J = 7.2 Hz, 2H), 0.97-0.93 (m, 9H).
    [4461] Example 24 (80)
    [4462] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (1,4-benzodioxan-2-yl) thiazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane hydrochloride
    [4463]
    [4464] TLC: Rf 0.36 (CHCl 3: MeOH = 10: 1);
    [4465] NMR (CD 3 OD): δ 7.88 (s, 1 H), 7.00 (m, 1 H), 6.94-6.87 (m, 3 H), 5.66 (dd, J = 6.0, 2.7 Hz, 1 H), 4.62 (dd, J) = 11.7, 2.7 Hz, 1H), 4.51 (s, 2H), 4.42 (dd, J = 11.7,6.0 Hz, 1H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.88 (m, 2H) , 3.58 (m, 2H), 3.40 (m, 2H), 2.48-2.16 (m, 4H), 1.90-1.28 (m, 7H), 0.97 (t, J = 7.5 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4466] Example 24 (81)
    [4467] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-trifluoromethyl-2- (morpholin-1-yl) thiazol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4468]
    [4469] TLC: Rf 0.78 (CHCl 3: MeOH = 10: 1);
    [4470] NMR (CD 3 OD): δ 4.63 (s, 2H), 4.03 (dd, J = 7.8, 4,8 Hz, 1H), 3.86-3.78 (m, 6H), 3.58 (m, 6H), 3.40 (m, 2H), 2.44 (m, 2H), 2.22 (m, 2H), 1.88-1.32 (m, 8H), 0.97 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4471] Example 24 (82)
    [4472] 1-butyl-2,5-dioxo-3- (tetrahydropyran-4-ylmethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triazaspiro [5.5] undecane, dihydrochloride
    [4473]
    [4474] TLC: Rf 0.31 (CHCl 3: MeOH = 10: 1);
    [4475] NMR (CD 3 OD): δ 7.60-7.46 (m, 5H), 4.33 (s, 2H), 4.09 (dd, J = 7.5, 4.5 Hz, 1H), 3.98-3.78 (m, 4H), 3.68-3.56 (m, 2H), 3.50-3.36 (m, 4H), 2.58-2.16 (m, 4H), 2.40 (s, 3H), 2.39 (s, 3H), 1.84-1.20 (m, 11H), 0.97 (t , J = 7.2 Hz, 3H).
    [4476] Example 24 (83)
    [4477] 1-Butyl-2,5-dioxo-3- (tetrahydropyran-4-ylmethyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4478]
    [4479] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [4480] NMR (CD 3 OD): δ 7.06-6.92 (m, 3H), 4.27 (s, 4H), 4,24 (s, 2H), 4.07 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.86 (m, 2H), 3.84-3.68 (m, 2H), 3.52-3.36 (m, 6H), 2.44-2.10 (m, 4H), 1.82-1.22 (m, 11H), 0.96 (t, J = 7.2 Hz , 3H).
    [4481] Example 24 (84)
    [4482] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-carboxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4483]
    [4484] TLC: Rf 0.58 (CHCl 3: MeOH: Acetic Acid = 20: 2: 1);
    [4485] NMR (CD 3 OD): δ 8.14 (d, J = 8.4 Hz, 2H), 7.68 (d, J = 8.4 Hz, 2H), 4.45 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.76 (m, 2H), 3.56-3.43 (m, 2H), 3.43-3.34 (m, 2H), 2.50-2.31 (m, 2H), 2.28-2.08 (m, 2H), 1.84- 1.12 (m, 15 H), 1.06-0.90 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [4486] Example 24 (85)
    [4487] 1-butyl-2,5-dioxo-3- (2-cyclohexylethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4488]
    [4489] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4490] NMR (CD 3 OD): δ 7.56-7.45 (m, 5H), 4.32 (s, 2H), 4.02 (t, J = 4.8 Hz, 1H), 3.98-3.85 (m, 1H), 3.85-3.70 (m , 1H), 3.65-3.56 (m, 2H), 3.56-3.42 (m, 1H), 3.42-3.30 (m, 1H), 2.55-2.37 (m, 2H), 2.38 (s, 3H), 2.37 (s , 3H), 2.30-2.13 (m, 2H), 1.92-1.78 (m, 2H), 1.78-1.60 (m, 5H), 1.60-1.48 (m, 2H), 1.48-1.32 (m, 2H), 1.32 -1.08 (m, 6H), 0.96 (t, J = 7.2 Hz, 3H), 0.96-0.85 (m, 2H).
    [4491] Example 24 (86)
    [4492] 1-butyl-2,5-dioxo-3- (2-cyclohexylethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4493]
    [4494] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [4495] NMR (CD 3 OD): δ 7.05 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.03 (t, J = 4.8 Hz, 1H), 3.90-3.79 (m, 1H), 3.76-3.62 (m, 1H), 3.50-3.38 (m, 3H), 3 . 38-3.30 (m, 1H), 2.43-2.06 (m, 4H), 1.92-1.78 (m, 2H), 1.78-1.60 (m, 5H), 1.60-1.45 (m, 2H), 1.42-1.30 (m , 2H), 1.30-1.08 (m, 6H), 0.95 (t, J = 7.2 Hz, 3H), 0.97-0.88 (m, 2H).
    [4496] Example 24 (87)
    [4497] (3R) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4498]
    [4499] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [4500] NMR (CD 3 OD): δ 7.61-7.48 (m, 5H), 4.33 (s, 2H), 4.06 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.78 (m, 2H), 3.68-3.58 (m, 2H), 3.50-3.40 (m, 2H), 2.62-2.45 (m, 2H), 2.42 (s, 3H), 2.40 (s, 3H), 2.30-2.12 (m, 2H), 1.82-1.12 (m, 15H), 0.97 (t, J = 7.2 Hz, 3H), 0.97 (m, 2H).
    [4501] Example 24 (88)
    [4502] 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methyl-2-phenylthiazol-5-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4503]
    [4504] TLC: Rf 0.75 (CHCl 3: MeOH = 10: 1);
    [4505] NMR (CD 3 OD): δ 7.98-7.95 (m, 2H), 7.55-7.50 (m, 3H), 4.69 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.98-3.78 (m, 2H), 3.65-3.56 (m, 2H), 3.50-3.40 (m, 2H), 2.58 (s, 3H), 2.60-2.48 (m, 2H), 2.27-2.14 (m, 2H), 1.88 -1.48 (m, 5H), 1.48-1.30 (m, 2H), 0.97-0.93 (m, 9H).
    [4506] Example 24 (89)
    [4507] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (thiophen-1-yl) thiazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [4508]
    [4509] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [4510] NMR (CD 3 OD): δ 7.81 (s, 1H), 7.67 (d, J = 3.9 Hz, 1H), 7.60 (d, J = 5.4 Hz, 1H), 7.14 (dd, J = 5.4, 3.9 Hz, 1H), 4.49 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.82 (m, 2H), 3.62-3.55 (m, 2H), 3.42 (t, J = 7. 5 Hz, 2H), 2.58-2.40 (m, 2H), 2.28-2.10 (m, 2H), 1.86-1.42 (m, 5H), 1.46-1.30 (m, 2H), 0.97-0.93 (m, 9H).
    [4511] Example 24 (90)
    [4512] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (pyridin-4-yl) thiazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [4513]
    [4514] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [4515] NMR (CD 3 OD): δ 8.98 (d, J = 6.9 Hz, 2H), 8.71 (d, J = 6.9 Hz, 2H), 8.37 (s, 1H), 4.66 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 4.00-3.87 (m, 2H), 3.70-3.59 (m, 2H), 3.50 (t, J = 7.8 Hz, 2H), 2.72-2.58 (m, 2H), 2.25 -2.08 (m, 2H), 1.88-1.46 (m, 5H), 1.46-1.35 (m, 2H), 0.97-0.92 (m, 9H).
    [4516] Example 24 (91)
    [4517] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,4-dimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4518]
    [4519] TLC: Rf 0.28 (CHCl 3: MeOH = 10: 1);
    [4520] NMR (CD 3 OD): δ 7.23 (s, 1H), 7.09 (d, J = 8.4 Hz, 1H), 7.03 (d, J = 8.4 Hz, 1H), 4.29 (s, 2H), 4.04 (dd, J = 7.5, 4.8 Hz, 1H), 3.90 (s, 3H), 3.86 (s, 3H), 3.88-3.64 (m, 2H), 3.56-3.38 (m, 4H), 2.58-2.37 (m, 2H) , 2.24-2.08 (m, 2H), 1.82-1.10 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [4521] Example 24 (92)
    [4522] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4523]
    [4524] TLC: Rf 0.31 (CHCl 3: MeOH = 10: 1);
    [4525] NMR (CD 3 OD): δ 6.74 (d, J = 1.8 Hz, 2H), 6.60 (t, J = 1.8 Hz, 1H), 4.28 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.86-3.70 (m, 2H), 3.83 (s, 6H), 3.58-3.36 (m, 4H), 2.52-2.36 (m, 2H), 2.24-2.08 (m, 2H), 1.82-1.10 ( m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [4526] Example 24 (93)
    [4527] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-2-yl) furan-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [4528]
    [4529] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [4530] NMR (CD 3 OD): δ 8.76 (dd, J = 5.4, 1.5 Hz, 1H), 8.51 (ddd, J = 8.1, 7.5, 1.5 Hz, 1H), 8.39 (d, J = 7.5 Hz, 1H), 7.85 (dd, J = 8.1, 5.4 Hz, 1H), 7.61 (d, J = 3.6 Hz, 1H), 7.08 (d, J = 3.6 Hz, 1H), 4.63 (s, 2H), 4.00 (dd , J = 7.8, 4.5 Hz, 1H), 3.98-3.81 (m, 2H), 3.65-3.55 (m, 2H), 3.49 (t, J = 8.1 Hz, 2H), 2.72-2.55 (m, 2H), 2.28-2.10 (m, 2H), 1.90-1.27 (m, 7H), 1.00-0.89 (m, 9H).
    [4531] Example 24 (94)
    [4532] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-3-yl) furan-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [4533]
    [4534] TLC: Rf 0.45 (CHCl 3: MeOH = 10: 1);
    [4535] NMR (CD 3 OD): δ 9.34 (d, J = 1.8 Hz, 1H), 8.94 (dd, J = 8.1, 1.8 Hz, 1H), 8.75 (d, J = 5.4 Hz, 1H), 8.10 (dd, J = 8.1, 5.4Hz, 1H), 7.34 (d, J = 3.6Hz, 1H), 6.98 (d, J = 3.6Hz, 1H), 4.57 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.77 (m, 2H), 3.63-3.43 (m, 4H), 2.73-2.55 (m, 2H), 2.28-2.09 (m, 2H), 1.89-1.27 (m, 7H), 1.00-0.89 (m, 9 H).
    [4536] Example 24 (95)
    [4537] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3,5-dimethylpyrazol-1-yl) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4538]
    [4539] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [4540] NMR (CD 3 OD): δ 7.94 (d, J = 8.1 Hz, 2H), 7.71 (d, J = 8.1 Hz, 2H), 6.51 (s, 1H), 4.49 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.85-3.76 (m, 2H), 3.58-3.48 (m, 4H), 2.72-2.58 (m, 2H), 2.45 (s, 3H), 2.39 (s, 3H) , 2.23-2.06 (m, 2H), 1.88-1.45 (m, 5H), 1.45-1.34 (m, 2H), 0.97-0.92 (m, 9H).
    [4541] Example 24 (96)
    [4542] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-chloropyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [4543]
    [4544] TLC: Rf 0.57 (CHCl 3: MeOH = 10: 1);
    [4545] NMR (CD 3 OD): δ 8.54 (bs, 1H), 8.45 (bs, 1H), 7.87 (bs, 1H), 7.71 (d, J = 8.4 Hz, 2H), 7.26 (d, J = 8.4 Hz, 2H), 4.39 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.73 (m, 2H), 3.56-3.40 (m, 4H), 2.64-2.46 (m, 2H) , 2.24-2.09 (m, 2H), 1.86-1.42 (m, 5H), 1.42-1.30 (m, 2H), 0.97-0.92 (m, 9H).
    [4546] Example 24 (97)
    [4547] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrimidin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [4548]
    [4549] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4550] NMR (CD 3 OD): δ 8.62 (d, J = 4.8 Hz, 2H), 7.68 (d, J = 8.4 Hz, 2H), 7.32 (d, J = 8.4 Hz, 2H), 7.26 (t, J = 4.8 Hz, 1H), 4.40 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.72 (m, 2H), 3.60-3.35 (m, 4H), 2.58-2.40 (m , 2H), 2.28-2.07 (m, 2H), 1.90-1.45 (m, 5H), 1.45-1.36 (m, 2H), 0.98-0.90 (m, 9H).
    [4551] Example 24 (98)
    [4552] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Khan dihydrochloride
    [4553]
    [4554] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4555] NMR (CD 3 OD): δ 8.76 (d, J = 2.7 Hz, 1H), 8.63 (d, J = 5.7 Hz, 1H), 8.28 (dd, J = 8.7, 2.7 Hz, 1H), 8.07 (dd, J = 8.7, 5.7 Hz, 1H), 7.78 (d, J = 8.4 Hz, 2H), 7.35 (d, J = 8.4 Hz, 2H), 4.41 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.93-3.72 (m, 2H), 3.58-3.40 (m, 4H), 2.68-2.48 (m, 2H), 2.26-2.06 (m, 2H), 1.90-1.46 (m, 5H), 1.46-1.30 (m, 2 H), 0.98-0.91 (m, 9 H).
    [4556] Example 24 (99)
    [4557] 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4558]
    [4559] TLC: Rf 0.28 (CHCl 3: MeOH = 19: 1);
    [4560] NMR (CD 3 OD): δ 7.39-7.29 (m, 4H), 4.31 (s, 2H), 4.27-4.20 (m, 2H), 4.06 (dd, J = 7.5, 4.8 Hz, 1H), 3.84 (m , 2H), 3.62 (m, 2H), 2.59 (m, 2H), 2.42 (s, 3H), 2.37 (s, 3H), 2.34 (s, 3H), 2.28 (m, 2H), 1.92-1.60 ( m, 6H), 0.96 (d, J = 6.3 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H).
    [4561] Example 24 (100)
    [4562] (3R) -1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4563]
    [4564] TLC: Rf 0.29 (CHCl 3: MeOH = 19: 1);
    [4565] NMR (CD 3 OD): δ 7.59-7.43 (m, 5H), 4.31 (s, 2H), 4.25 (q, J = 2.1 Hz, 2H), 4.09 (dd, J = 7.2, 4.8 Hz, 1H), 3.85 (dt, J = 3.0, 12.3 Hz, 2H), 3.68-3.56 (m, 2H), 2.61 (m, 2H), 2.38 (s, 3H), 2.37 (s, 3H), 2.26 (m, 2H) , 1.83-1.43 (m, 8H), 1.75 (t, J = 2.1 Hz, 3H), 1.38-1.12 (m, 3H), 0.96 (m, 2H).
    [4566] Example 24 (101)
    [4567] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-hydroxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4568]
    [4569] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [4570] NMR (CD 3 OD): δ 7.47 (d, J = 9.0 Hz, 2H), 6.97 (d, J = 9.0 Hz, 2H), 6.88 (d, J = 9.0 Hz, 2H), 6.80 (d, J = 9.0 Hz, 2H), 4.30 (s, 2H), 4.00 (dd, J = 7.5, 4.8 Hz, 1H), 3.86-3.70 (m, 2H), 3.52-3.34 (m, 4H), 2.48-2.3 0 ( m, 2H), 2.28-2.10 (m, 2H), 1.88-1.44 (m, 5H), 1.44-1.28 (m, 2H), 0.97-0.92 (m, 9H).
    [4571] Example 24 (102)
    [4572] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-2-yl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4573]
    [4574] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [4575] NMR (CD 3 OD): δ 8.89 (d, J = 7.8 Hz, 1H), 8.70 (t, J = 7.8 Hz, 1H), 8.43 (d, J = 8.4 Hz, 1H), 8.10-8.06 (m, 3H), 7.98 (d, J = 8.7 Hz, 2H), 4.51 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.96-3.78 (m, 2H), 3.56-3.45 (m , 4H), 2.72-2.58 (m, 2H), 2.24-2.08 (m, 2H), 1.84-1.44 (m, 5H), 1.44-1.34 (m, 2H), 0.97-0.92 (m, 9H).
    [4576] Example 24 (103)
    [4577] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-3-yl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4578]
    [4579] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4580] NMR (CD 3 OD): δ 9.24 (s, 1H), 8.98 (d, J = 8.4 Hz, 1H), 8.88 (d, J = 8.4 Hz, 1H), 8.21 (dd, J = 8.4, 5.7 Hz, 1H), 7.96 (d, J = 8.4 Hz, 2H), 7.87 (d, J = 8.4 Hz, 2H), 4.47 (s, 2H), 4.01 (dd, J = 7.5, 4.8 Hz, 1H), 3.96- 3.75 (m, 2H), 3.58-3.44 (m, 4H), 2.64-2.50 (m, 2H), 2.25-2.08 (m, 2H), 1.88-1.48 (m, 5H), 1.48-1.32 (m, 2H ), 0.97-0.92 (m, 9H).
    [4581] Example 24 (104)
    [4582] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-carboxyphenyl) pyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [4583]
    [4584] TLC: Rf 0.27 (CHCl 3: MeOH = 10: 1);
    [4585] NMR (CD 3 OD): δ 8.19 (d, J = 8.4 Hz, 2H), 7.61 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.74 (m, 2H), 3.66-3.55 (m, 2H), 3.48-3.36 (m, 2H), 2.58-2.40 (m, 2H), 2.45 (s, 3H), 2.40 (s, 3H), 2.32-2.14 (m, 2H), 1.90-1.46 (m, 5H), 1.46-1.30 (m, 2H), 0.99-0.95 (m, 9H).
    [4586] Example 24 (105)
    [4587] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrazin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Khan dihydrochloride
    [4588]
    [4589] TLC: Rf 0.48 (CHCl 3: MeOH = 20: 1);
    [4590] NMR (CD 3 OD): δ 8.47 (d, J = 1.5 Hz, 1H), 8.32 (d, J = 2.7 Hz, 1H), 8.13 (dd, J = 2.7, 1.5 Hz, 1H), 7.65 (d, J = 8.4 Hz, 2H), 7.32 (d, J = 8.4 Hz, 2H), 4.40 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.73 (m, 2H), 3.58-3.46 (m, 2H), 3.44-3.34 (m, 2H), 2.52-2.34 (m, 2H), 2.30-2.10 (m, 2H), 1.90-1.43 (m, 5H), 1.43-1.26 (m , 2H), 0.99-0.90 (m, 9H).
    [4591] Example 24 (106)
    [4592] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-carboxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4593]
    [4594] TLC: Rf 0.20 (CHCl 3: MeOH = 10: 1);
    [4595] NMR (CD 3 OD): δ 8.11 (d, J = 8.4 Hz, 2H), 7.83 (d, J = 8.4 Hz, 2H), 7.77 (d, J = 8.4 Hz, 2H), 7.69 (d, J = 8.4 Hz, 2H), 4.43 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.96-3.74 (m, 2H), 3.58-3.36 (m, 4H), 2.55-2.3 8 ( m, 2H), 2.28-2.10 (m, 2H), 1.88-1.44 (m, 5H), 1.44-1.30 (m, 2H), 0.97-0.92 (m, 9H).
    [4596] Example 24 (107)
    [4597] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-4-yl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4598]
    [4599] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [4600] NMR (CD 3 OD): δ 8.91 (d, J = 6.9 Hz, 2H), 8.45 (d, J = 6.9 Hz, 2H), 8.11 (d, J = 7.8 Hz, 2H), 7.91 (d, J = 7.8 Hz, 2H), 4.49 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.96-3.78 (m, 2H), 3.58-3.40 (m, 4H), 2.64-2.48 (m , 2H), 2.26-2.08 (m, 2H), 1.90-1.28 (m, 7H), 0.96-0.93 (m, 9H).
    [4601] Example 24 (108)
    [4602] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Khan dihydrochloride
    [4603]
    [4604] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [4605] NMR (CD 3 OD): δ 8.44-8.15 (m, 2H), 7.82 (d, J = 7.2 Hz, 2H), 7.60-7.40 (m, 1H), 7.42 (d, J = 7.2 Hz, 2H), 7.27-7.24 (m, 1H), 4.43 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.70 (m, 2H), 3.58-3.40 (m, 4H), 2.6 4 -2.42 (m, 2H), 2.28-2.06 (m, 2H), 1.92-1.28 (m, 7H), 0.97-0.94 (m, 9H).
    [4606] Example 24 (109)
    [4607] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (naphthalen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4608]
    [4609] TLC: Rf 0.71 (CHCl 3: MeOH = 10: 1);
    [4610] NMR (CD 3 OD): δ 8.08-7.93 (m, 4H), 7.64-7.57 (m, 3H), 4.54 (s, 2H), 4.04 (dd, J = 7.5, 4.8 Hz, 1H), 3.96-3.80 (m, 2H), 3.60-3.44 (m, 2H), 3.42-3.36 (m, 2H), 2.42-2.08 (m, 4H), 1.82-1.16 (m, 15H), 0.95 (t, J = 7.5 Hz , 3H), 0.95 (m, 2H).
    [4611] Example 24 (110)
    [4612] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-methoxynaphthalen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4613]
    [4614] TLC: Rf 0.75 (CHCl 3: MeOH = 10: 1);
    [4615] NMR (CD 3 OD): δ 7.98 (s, 1H), 7.91 (d, J = 8.7 Hz, 1H), 7.85 (d, J = 8.7 Hz, 1H), 7.58 (d, J = 8.7 Hz, 1H) , 7.31 (d, J = 2.4 Hz, 1H), 7.22 (dd, J = 8.7, 2.4 Hz, 1H), 4.48 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.94- 3.78 (m, 2H), 3.93 (s, 3H), 3.58-3.44 (m, 2H), 3.42-3.36 (m, 2H), 2.48-2.30 (m, 2H), 2.24-2.08 (m, 2H), 1.82-1.10 (m, 15 H), 0.95 (t, J = 7.2 Hz, 3 H), 0.95 (m, 2H).
    [4616] Example 24 (111)
    [4617] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4618]
    [4619] TLC: Rf 0.27 (CHCl 3: MeOH = 10: 1);
    [4620] NMR (CD 3 OD): δ 8.03 (d, J = 8.7 Hz, 2H), 7.63 (d, J = 8.4 Hz, 2H), 7.17 (d, J = 8.4 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 4.37 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.70 (m, 2H), 3.56-3.36 (m, 4H), 2.56-2.3 8 ( m, 2H), 2.25-2.10 (m, 2H), 1.84-1.44 (m, 5H), 1.44-1.39 (m, 2H), 0.98-0.93 (m, 9H).
    [4621] Example 24 (112)
    [4622] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-4-yl) furan-2-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [4623]
    [4624] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [4625] NMR (CD 3 OD): δ 8.80 (d, J = 6.9 Hz, 2H), 8.39 (d, J = 6.9 Hz, 2H), 7.69 (d, J = 3.6 Hz, 1H), 7.08 (d, J = 3.6 Hz, 1H), 4.62 (s, 2H), 4.00 (dd, J = 7.8, 4.5, Hz, 1H), 3.99-3.79 (m, 2H), 3.65-3.43 (m, 4H), 2.72-2. 54 (m, 2H), 2.30-2.10 (m, 2H), 1.88-1.26 (m, 7H), 1.00-0.84 (m, 9H).
    [4626] Example 24 (113)
    [4627] 1-butyl-2,5-dioxo-3-cyclopentylmethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4628]
    [4629] TLC: Rf 0.66 (CHCl 3: MeOH = 10: 1);
    [4630] NMR (CD 3 OD): δ 7.52 (d, J = 8.5 Hz, 2H), 7.40 (t, J = 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.05 (m, 4H) , 4.34 (s, 2H), 4.00 (t, J = 6.0 Hz, 1H), 3.82 (m, 2H), 3.49 (m, 2H), 3.39 (m, 2H), 2.37 (m, 2H), 2.17 ( m, 2H), 1.96 (m, 1H), 1.81 (m, 4H), 1.58 (m, 6H), 1.38 (m, 2H), 1.17 (m, 2H), 0.95 (t, J = 7.0 Hz, 3H ).
    [4631] Example 24 (114)
    [4632] (3R) -1-butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4633]
    [4634] TLC: Rf 0.52 (CHCl 3: MeOH = 20: 1);
    [4635] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.40 (t, J = 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.04 (m, 4H) , 4.33 (s, 2H), 4.01 (dd, J = 7.2, 3.3 Hz, 1H), 3.82 (m, 1H), 3.71 (m, 1H), 3.50 (m, 2H), 3.43 (m, 2H), 2.38 (m, 2H), 2.24 (m, 2H), 2.00 (dd, J = 14.0, 3.3 Hz, 1H), 1.55 (dd, J = 14.0, 7.2 Hz, 1H), 1.50 (m, 2H), 1.36 (m, 2H), 0.99 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H).
    [4636] Example 24 115
    [4637] (3S) -1-butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4638]
    [4639] TLC: Rf 0.52 (CHCl 3: MeOH = 20: 1);
    [4640] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.40 (t, J = 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.04 (m, 4H) , 4.33 (s, 2H), 4.01 (dd, J = 7.2, 3.3 Hz, 1H), 3.82 (m, 1H), 3.71 (m, 1H), 3.50 (m, 2H), 3.43 (m, 2H), 2.38 (m, 2H), 2.24 (m, 2H), 2.00 (dd, J = 14.0, 3.3 Hz, 1H), 1.55 (dd, J = 14.0, 7.2 Hz, 1H), 1.50 (m, 2H), 1.36 (m, 2H), 0.99 (s, 9H), 0.95 (t, J = 7.0 Hz, 3H).
    [4641] Example 24 (116)
    [4642] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-nitrophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4643]
    [4644] TLC: Rf 0.68 (CHCl 3: MeOH = 10: 1);
    [4645] NMR (CD 3 OD): δ 8.33 (d, J = 8.7 Hz, 2H), 7.78 (d, J = 8.7 Hz, 2H), 4.49 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.76 (m, 2H), 3.55-3.43 (m, 2H), 3.40-3.31 (m, 2H), 2.45-2.28 (m, 2H), 2.27-2.08 (m, 2H), 1.83- 1.14 (m, 15 H), 1.04-0.86 (m, 5 H).
    [4646] Example 24 (117)
    [4647] (3R) -1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4648]
    [4649] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [4650] NMR (CDCl 3): δ 7.38-7.14 (m, 10H), 6.00-5.75 (m, 1H), 4.40-4.15 (m, 2H), 3.92-3.58 (m, 3H), 3.58-2.25 (m, 13H) , 2.18-1.45 (m, 10 H).
    [4651] Example 24 (118)
    [4652] (3S) -1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4653]
    [4654] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [4655] NMR (CDCl 3): δ 7.40-7.15 (m, 10H), 6.05-5.80 (m, 1H), 4.40-4.10 (m, 2H), 3.90-3.55 (m, 3H), 3.55-2.20 (m, 13H) , 2.18-1.45 (m, 10 H).
    [4656] Example 24 (119)
    [4657] (3S) -1-propyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4658]
    [4659] TLC: Rf 0.32 (CHCl 3: MeOH = 10: 1);
    [4660] NMR (CD 3 OD): δ 7.40-7.20 (m, 10H), 5.06 (s, 2H), 4.09 (dd, J = 5.2, 4.6 Hz, 1H), 4.00-3.70 (m, 2H), 3.70-3.55 (m, 2H), 3.50-3.30 (m, 4H), 3.20-3.00 (m, 4H), 2.65-2.35 (m, 2H), 2.30-2.10 (m, 2H), 2.00-1.75 (m, 2H) , 1.70-1.40 (m, 4H), 0.96 (t, J = 7.4 Hz, 3H).
    [4661] Example 25
    [4662] 1-butyl-2,5-dioxo-3- (carboxymethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4663]
    [4664] To a solution of compound (173 mg) in methanol (5 mL) prepared in Example 24 (11) was added 2N aqueous sodium hydroxide solution (2 ml). The reaction mixture was stirred at rt for 3 h. 2N aqueous hydrochloric acid solution was added to the reaction mixture until pH was 4, and extracted with ethyl acetate. The extract was washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate and concentrated. The obtained residue was dissolved in 1,4-dioxane and 4N hydrochloric acid and 1,4-dioxane solution were added. The residue obtained by concentrating the reaction mixture was washed with diethyl ether and dried to obtain the compound of the present invention (127 mg) having the following physical properties.
    [4665] TLC: Rf 0.51 (CHCl 3: MeOH: Acetic Acid = 20: 4: 1);
    [4666] NMR (CD 3 OD): 7.55-7.53 (m, 2H), 7.42-7.36 (m, 2H), 7.20-7.15 (m, 1H), 7.07-7.02 (m, 4H), 4.33 (s, 2H), 4.27 (t, J = 4.5 Hz, 1H), 3.96-3.90 (m, 1H), 3.72-3.66 (m, 1H), 3.54-3.38 (m, 4H), 2.97 (dd, J = 18.0, 4.8 H z , 1H), 2.79 (dd, J = 18.0, 4.8 Hz, 1H), 2.50-2.36 (m, 3H), 2.27-2.16 (m, 1H), 1.62-1.48 (m, 2H), 1.41-1.30 (m , 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [4667] Example 26 (1) -26 (3)
    [4668] Resin (3) and N-allyloxycarbonyl-4-piperidone prepared in Reference Example 2 were used, and instead of n-propylamine and N- (t-butyloxycarbonyl) leucine, the corresponding compounds were used. Reference Example 3-the same operation as Reference Example 4, and by using a compound instead of 3,5-dimethyl-1-phenyl-4-formylpyrazole Reference Example 5 → Reference Example 6 → Example 1 and Since the same operation was carried out and the hydroxyl group was partially acetylated, the same operation as in Example 25 was carried out to obtain the following compound of the present invention.
    [4669] Example 26 (1)
    [4670] 1- (3-hydroxybutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4671]
    [4672] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4673] NMR (CD 3 OD): δ 7.54 (d, J = 8.5 Hz, 2H), 7.39 (t, J = 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.04 (m, 4H) , 4.33 (s, 2H), 4.02 (m, 1H), 3.80 (m, 3H), 3.51 (m, 4H), 2.46 (m, 2H), 2.19 (m, 2H), 1.85-1.57 (m, 5H ), 1. 17 (d, J = 6.0 Hz, 3H), 0.94 (d, J = 9.0 Hz, 6H).
    [4674] Example 26 (2)
    [4675] 1- (3-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4676]
    [4677] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [4678] NMR (CD 3 OD): δ 7.51 (d, J = 8.5 Hz, 2H), 7.40 (t, J = 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.04 (m, 4H) , 4.34 (s, 2H), 4.02 (dd, J = 7.5, 4.0 Hz, 1H), 3.80 (m, 2H), 3.60 (t, J = 6.0 Hz, 2H), 3.48 (m, 4H), 2.40 ( m, 2H), 2.20 (m, 2H), 1.82-1.58 (m, 5H), 0.94 (d, J = 6.0 Hz, 3H), 0.93 (d, J = 6.0 Hz, 3H).
    [4679] Example 26 (3)
    [4680] 1- (2-hydroxybutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [4681]
    [4682] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4683] NMR (CD 3 OD): δ 7.50 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 ( m, 4H), 4.32 (s, 2H), 4.03 (dd, J = 8.1, 4.8 Hz, 1H), 3.96-3.41 (m, 6H), 3.27-3.14 (m, 1H), 2.68-2.53 (m, 1H), 2.37-2.26 (m, 3H), 1.94-1.24 (m, 5H), 1.08-0.82 (m, 9H).
    [4684] Example 27
    [4685] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-aminophenylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4686]
    [4687] To a methanol solution of compound (50 mg) prepared in Example 24 (116) was added 5% palladium-carbon (10 mg) under argon. The reaction mixture was stirred for 20 minutes at room temperature under hydrogen gas atmosphere. The reaction mixture was filtered through celite (trade name) and the filtrate was concentrated. The residue was purified by silica gel column chromatography (chloroform: methanol = 50: 1 → 30: 1 → 20: 1). The obtained compound was dissolved in methanol and concentrated by adding 4N hydrochloric acid / ethyl acetate solution. The obtained residue was washed with diethyl ether and dried to obtain the compound (34 mg) of the present invention having the following physical properties.
    [4688] TLC: Rf 0.21 (CHCl 3: MeOH = 10: 1);
    [4689] NMR (CD 3 OD): δ 7.80 (d, J = 8.4 Hz, 2H), 7.47 (d, J = 8.4 Hz, 2H), 4.41 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.74 (m, 2H), 3.52-3.45 (m, 4H), 2.65-2.52 (m, 2H), 2.24-2.08 (m, 2H), 1.80-1.16 (m, 15H), 0.94 ( t, J = 7.5 Hz, 3H), 0.94 (m, 2H).
    [4690] Example 28
    [4691] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-((4-methylphenyl) sulfonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4692]
    [4693] To the pyridine (2 ml) solution of compound (33 mg) prepared in Example 28 was added p-toluenesulfonylchloride (21 mg). The reaction mixture was stirred at rt for 27 h. The reaction mixture was concentrated and extracted with ethyl acetate by adding saturated aqueous sodium hydrogen carbonate solution. The extract was washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate and concentrated. The residue was purified by silica gel column chromatography (chloroform: methanol = 10: 1). The obtained compound was dissolved in methanol, and concentrated by adding 4N hydrochloric acid / ethyl acetate solution. The obtained residue was washed with diethyl ether and dried to obtain the compound (27 mg) of the present invention having the following physical properties.
    [4694] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [4695] NMR (CD 3 OD): δ 7.70 (d, J = 8.4 Hz, 2H), 7.41 (d, J = 8.4 Hz, 2H), 7.30 (d, J = 8.4 Hz, 2H), 7.22 (d, J = 8.4 Hz, 2H), 4.25 (s, 2H), 4.03 (dd, J = 7.2, 4.5 Hz, 1H), 3.78 (m, 2H), 3.42 (m, 4H), 2.42-2.06 (m, 4H), 2.37 (s, 3H), 1.82-1.10 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [4696] Example 28 (1)
    [4697] 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylcarbonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4698]
    [4699] The compound of the present invention having the following physical properties was obtained in the same manner as in Example 28 using benzoyl chloride instead of p-toluenesulfonyl chloride.
    [4700] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [4701] NMR (CD 3 OD): δ 7.93 (d, J = 8.4 Hz, 2H), 7.88 (d, J = 8.4 Hz, 2H), 7.61-7.50 (m, 5H), 4.34 (s, 2H), 4.05 ( dd, J = 7.8, 4.5 Hz, 1H), 3.80 (m, 2H), 3.42 (m, 4H), 2.24 (m, 4H), 1.82-1.16 (m, 15H), 0.96 (t, J = 7.2 Hz , 3H), 0.96 (m, 2H).
    [4702] Example 29
    [4703] (3S) -1-butyl-2,5-dioxo-3-benzyloxymethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [4704]
    [4705] Reference Example 3 → Reference Example Using Resin (3) and N-benzyloxycarbonyl-4-piperidone and O-benzyl-N- (t-butyloxycarbonyl) -L-serine prepared in Reference Example 2 6 → The same operation as in Example 1 was carried out to obtain a compound of the present invention having the following physical properties.
    [4706] TLC: Rf 0.66 (CHCl 3: MeOH = 20: 1);
    [4707] NMR (CDCl 3 ): δ 7.40-7.25 (m, 10H), 6.09 (brs, 1H), 5.15 (s, 2H), 4.54 (s, 2H), 4.20-3.98 (br, 2H), 4.18 (dd, J = 8.4, 3.6 Hz, 1H), 3.93 (dd, J = 9.3, 3.6 Hz, 1H), 3.80-3.56 (br, 1H), 3.66 (dd, J = 9.3, 8.4, Hz, 1H), 3.45- 3.12 (m, 3H), 2.02-1.75 (m, 4H), 1.57-1.39 (m, 2H), 1.38-1.20 (m, 2H), 0.91 (t, J = 7.2 Hz, 3H).
    [4708] Example 30
    [4709] (3S) -1-butyl-2,5-dioxo-3-hydroxymethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [4710]
    [4711] To a solution of the compound (245 mg) of dichloromethane (5 ml) prepared in Example 29 was added 1M dichloromethane solution of boron tribromide (1.4 ml) at -40 ° C and stirred at -20 ° C for 3 hours. Water and saturated aqueous sodium hydrogen carbonate solution were added to the reaction mixture, which was then extracted with ethyl acetate. The extract was washed with water and saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate and concentrated. The residue was purified by silica gel column chromatography (chloroform: methanol = 30: 1) to give the compound (173 mg) of the present invention having the following physical properties.
    [4712] TLC: Rf 0.29 (CHCl 3: MeOH = 20: 1);
    [4713] NMR (CDCl 3 ): δ 7.42-7.27 (m, 5H), 6.26-6.15 (br, 1H), 5.16 (s, 2H), 4.26-4.00 (m, 2H), 3.98-3.82 (m, 2H), 3.84-3.60 (br, 1H), 3.43-3.13 (m, 4H), 2.80-2.68 (br, 1H), 2.05-1.75 (m, 4H), 1.58-1.40 (m, 2H), 1.40-1.20 (m , 2H), 0.92 (t, J = 7.5 Hz, 3H).
    [4714] Example 31
    [4715] (3S) -1-butyl-2,5-dioxo-3-hydroxymethyl-1,4,9-triazaspiro [5.5] undecane
    [4716]
    [4717] Using the compound prepared in Example 30, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [4718] TLC: Rf 0.21 (CHCl 3: MeOH: Acetic Acid = 20: 4: 1);
    [4719] NMR (d 6 -DMSO): δ 7.83 (brs, 1H), 5.10-4.90 (br, 1H), 3.88-3.78 (m, 1H), 3.76-3.65 (m, 1H), 3.58-3.48 (m, 1H ), 3.28-3.18 (m, 1H), 3.18-3.04 (m, 3H), 2.88-2.75 (m, 2H), 1.94-1.83 (m, 1H), 1.83-1.64 (m, 3H), 1.56-1.42 (m, 1H), 1.42-1.20 (m, 3H), 0.88 (t, J = 7.2 Hz, 3H).
    [4720] Example 32 (1)
    [4721] (3S) -1-butyl-2,5-dioxo-3-hydroxymethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4722]
    [4723] The compound of the present invention having the following physical properties was obtained in the same manner as in Example 10 using 4-phenyloxybenzaldehyde and the compound prepared in Example 31.
    [4724] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4725] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.43-7.35 (m, 2H), 7.22-7.14 (m, 1H), 7.06 (d, J = 8.7 Hz, 2H), 7.06-7.00 (m, 2H), 4.33 (s, 2H), 4.03-3.90 (m, 3H), 3.79-3.66 (m, 1H), 3.65 (dd, J = 10.5, 2.4 Hz, 1H), 3.61- 3.42 (m, 3H), 3.30-3.18 (m, 1H), 2.50-2.24 (m, 3H), 2.24-2.12 (m, 1H), 1.76-1.58 (m, 1H), 1.54-1.26 (m, 3H ), 0.95 (t, J = 7.5 Hz, 3H).
    [4726] Example 32 (2)
    [4727] (3S) -1-Butyl-2,5-dioxo-3-hydroxymethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [4728]
    [4729] In the same manner as in Example 10, using 1-phenyl-3,5-dimethyl-4-formylpyrazole and the compound prepared in Example 31, the compound of the present invention having the following physical property values was obtained.
    [4730] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4731] NMR (CD 3 OD): δ 7.61-7.46 (m, 5H), 4.32 (s, 2H), 4.08-3.92 (m, 3H), 3.83-3.70 (m, 1H), 3.66 (dd, J = 10.5, 2.4 Hz, 1H), 3.66-3.52 (m, 3H), 3.40-3.25 (m, 1H), 2.64-2.50 (m, 1H), 2.50-2.40 (m, 2H), 2.41 (s, 3H), 2.39 (s, 3H), 2.28-2.15 (m, 1H), 1.80-1.58 (m, 1H), 1.58-1.30 (m, 3H), 0.96 (t, J = 7.5 Hz, 3H).
    [4732] Reference Example 11: Synthesis of Compound (7)
    [4733]
    [4734] Reference Example 3 → Reference Example 4 with Resin (3) and N-allyloxycarbonyl-4-piperidone, n-butylamine and N- (t-butyloxycarbonyl) leucine prepared in Reference Example 2 The same operation was carried out, and the compound (7) was obtained by the same operation as in Reference Example 5 using 4-hydroxybenzaldehyde instead of 3,5-dimethyl-1-phenyl-4-formylpyrazole.
    [4735] Reference Example 12 Synthesis of Compound (8)
    [4736]
    [4737] In a dichloromethane (2 ml) suspension of the compound (60 mg) prepared in Reference Example 11, a dichloromethane solution (0.302 ml) and diethylazodicarboxylate of triphenylphosphine (80 mg) and 1M cyclopentanol (0.137 ml) was added. The reaction mixture was stirred at rt for 18 h. The resin obtained by filtering the reaction solution was washed with dichloromethane (2 ml x 4 times), methanol (2 ml x 3 times) and dichloromethane (3 ml x 4 times) to obtain compound (8).
    [4738] Example 33
    [4739] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopentyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4740]
    [4741] Using the compound prepared in Reference Example 12, the same operation as in Reference Example 6-Example 1 was carried out to obtain a compound of the present invention having the following physical properties.
    [4742] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4743] NMR (CD 3 OD): δ 7.41 (d, J = 8.7 Hz, 2H), 6.98 (d, J = 8.7 Hz, 2H), 4.83 (m, 1H), 4.25 (brs, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.86-3.65 (m, 2H), 3.53-3.27 (m, 4H), 2.40-2.06 (m, 4H), 2.02-1.43 (m, 13H), 1.43-1.24 ( m, 2H), 1.01-0.90 (m, 9H).
    [4744] Example 33 (1) -33 (6)
    [4745] The same procedure as in Reference Example 11 was carried out using a compound corresponding to n-butylamine and N- (t-butyloxycarbonyl) leucine, and Reference Example 12-> Example using a compound corresponding to cyclopentanol. The same operation as in 33 was performed to obtain the compound of the present invention shown below.
    [4746] Example 33 (1)
    [4747] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-diethylaminoethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4748]
    [4749] TLC: Rf 0.54 (CHCl 3: MeOH: 28% Ammonia = 80: 10: 1);
    [4750] NMR (CD 3 OD): δ 7.57 (d, J = 8.7 Hz, 2H), 7.12 (d, J = 8.7 Hz, 2H), 4.40 (t, J = 4.8 Hz, 2H), 4.30 (s, 2H) , 4.03 (dd, J = 7.5, 5.1 Hz, 1H), 3.84-3.67 (m, 2H), 3.63 (t, J = 4.8 Hz, 2H), 3.50-3.40 (m, 4H), 3.40-3.31 (m , 4H), 2.58-2.41 (m, 2H), 2.23-2.04 (m, 2H), 1.82-1.42 (m, 10H), 1.41-1.12 (m, 11H), 1.04-0.87 (m, 5H).
    [4751] Example 33 (2)
    [4752] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-dimethylaminoethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4753]
    [4754] TLC: Rf 0.46 (CHCl 3: MeOH: 28% Ammonia = 80: 10: 1);
    [4755] NMR (CD 3 OD): δ 7.57 (d, J = 8.7 Hz, 2H), 7.13 (d, J = 8.7 Hz, 2H), 4.39 (t, J = 4.8 Hz, 2H), 4.30 (s, 2H) , 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.84-3.67 (m, 2H), 3.61 (t, J = 4.8 Hz, 2H), 3.50-3.38 (m, 4H), 2.98 (s, 6H ), 2.59-2.42 (m, 2H), 2.24-2.03 (m, 2H), 1.83-1.12 (m, 15H), 1.04-0.86 (m, 5H).
    [4756] Example 33 (3)
    [4757] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-propyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4758]
    [4759] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [4760] NMR (CD 3 OD): δ 7.43 (d, J = 8.7 Hz, 2H), 7.01 (d, J = 8.7 Hz, 2H), 4.27 (brs, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.96 (t, J = 6.6 Hz, 2H), 3.85-3.67 (m, 2H), 3.53-3.33 (m, 4H), 2.45-2.27 (m, 2H), 2.26-2.07 (m, 2H) , 1.86-1.14 (m, 17H), 1.03 (t, J = 7.2 Hz, 3H), 1.00-0.89 (m, 5H).
    [4761] Example 33 (4)
    [4762] 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4763]
    [4764] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4765] NMR (CD 3 OD): δ 7.42 (d, J = 8.7 Hz, 2H), 7.27 (dd, J = 5.4, 0.9 Hz, 1H), 7.06-6.97 (m, 3H), 6.91 (dd, J = 5.4 , 3.6 Hz, 1H), 4.95-4.85 (m, 2H), 4.27 (brs, 2H), 4.14 (dd, J = 7.5, 4.5 Hz, 1H), 3.84 (d, J = 6.6 Hz, 2H), 3.84 -3.66 (m, 2H), 3.51-3.39 (m, 2H), 2.59-2.36 (m, 2H), 2.24-2.07 (m, 2H), 1.84-1.44 (m, 8H), 1.35-1.12 (m, 4H), 1.04-0.85 (m, 2H), 0.66-0.57 (m, 2H), 0.38-0.31 (m, 2H).
    [4766] Example 33 (5)
    [4767] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4768]
    [4769] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4770] NMR (CD 3 OD): δ 7.42 (d, J = 8.4 Hz, 2H), 7.01 (d, J = 8.4 Hz, 2H), 4.26 (brs, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.84 (d, J = 6.9 Hz, 2H), 3.83-3.66 (m, 2H), 3.51-3.33 (m, 4H), 2.44-2.26 (m, 2H), 2.25-2.06 (m, 2H) , 1.82-1.12 (m, 16H), 1.04-0.86 (m, 5H), 0.66-0.57 (m, 2H), 0.38-0.31 (m, 2H).
    [4771] Example 33 (6)
    [4772] 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4773]
    [4774] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [4775] NMR (CD 3 OD): δ 7.42 (d, J = 8.7 Hz, 2H), 7.01 (d, J = 8.7 Hz, 2H), 4.26 (brs, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.84 (d, J = 6.9 Hz, 2H), 3.84-3.66 (m, 2H), 3.50-3.33 (m, 4H), 2.43-2.26 (m, 2H), 2.26-2.08 (m, 2H) , 1.89-1.43 (m, 5H), 1.43-1.17 (m, 3H), 1.00-0.88 (m, 9H), 0.66-0.58 (m, 2H), 0.38-0.31 (m, 2H).
    [4776] Example 34
    [4777] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4778]
    [4779] In the same manner as in Example 10, using 4-dimethylaminobenzaldehyde and the compound prepared in Example 9 (1), the compound of the present invention having the following physical property values was obtained.
    [4780] TLC: Rf 0.26 (CHCl 3: MeOH = 10: 1);
    [4781] NMR (CD 3 OD): δ 7.78 (d, J = 8.7 Hz, 2H), 7.59 (d, J = 8.7 Hz, 2H), 4.39 (s, 2H), 4.03 (dd, J = 7.5, 4.8, Hz , 1H), 3.90-3.70 (m, 2H), 3.52-3.40 (m, 4H), 3.26 (s, 6H), 2.64-2.47 (m, 2H), 2.24-2.04 (m, 2H), 1.82-1 . 12 (m, 15 H), 1.04-0.88 (m, 5 H).
    [4782] Example 34 (1)
    [4783] 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (diethylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4784]
    [4785] In the same manner as in Example 34 using 4-diethylaminobenzaldehyde instead of 4-dimethylaminobenzaldehyde, the compound of the present invention having the following physical properties was obtained.
    [4786] TLC: Rf 0.28 (CHCl 3: MeOH: Acetic Acid = 10: 1);
    [4787] NMR (CD 3 OD): δ 7.94-7.78 (m, 2H), 7.72-7.52 (m, 2H), 4.43 (s, 2H), 4.03 (dd, J = 7.5, 4.8, Hz, 1H), 3.92- 3.73 (m, 2H), 3.73-3.60 (m, 4H), 3.54-3.40 (m, 4H), 2.63-2.45 (m, 2H), 2.25-2.05 (m, 2H), 1.82-1.10 (m, 21H ), 1.04-0.86 (m, 5 H).
    [4788] Example 35
    [4789] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [4790]
    [4791] Reference Example 3 → Reference using Resin (3) prepared in Reference Example 2, N-benzyloxycarbonyl-4-piperidone, n-butylamine, N- (t-butyloxycarbonyl) -L-leucine Example 6 → The same operation as in Example 1 was carried out to obtain a compound of the present invention having the following physical properties.
    [4792] TLC: Rf 0.67 (CHCl 3: MeOH = 20: 1);
    [4793] NMR (CD 3 OD): δ 7.35 (m, 5H), 6.50 (brs, 1H), 5.15 (s, 2H), 4.08 (m, 2H), 3.96 (m, 1H), 3.62 (brs, 1H), 3.44 (brs, 1H), 3.26 (m, 2H), 1.95-1.76 (m, 4H), 1.61-1.45 (m, 5H), 1.31 (m, 2H), 0.96 (d, J = 6.3 Hz, 3H) , 0.93 (d, J = 6.3 Hz, 3H), 0.91 (t, J = 7.2 Hz, 3H).
    [4794] Example 36
    [4795] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4796]
    [4797] Using the compound prepared in Example 35, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [4798] TLC: Rf 0.18 (CHCl 3: MeOH = 4: 1);
    [4799] NMR (CD 3 OD): δ 4.02 (dd, J = 7.8, 4.6 Hz, 1H), 3.80 (dd, J = 12.5, 4.0 Hz, 1H), 3.72 (dd, J = 12.5, 4.0 Hz, 1H), 3.39 (m, 4H), 2.34-2.09 (m, 4H), 1.88-1.50 (m, 5H), 1.37 (m, 2H), 0.96 (t, J = 7.5 Hz, 3H), 0.95 (d, J = 6.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H).
    [4800] Example 37 (1) -37 (88)
    [4801] Using the compound prepared in Example 36 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [4802] Example 37 (1)
    [4803] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-methyl-4-chlorophenyl) -1- (4-methylphenylmethyl) pyrazole 3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4804]
    [4805] TLC: Rf 0.46 (CHCl 3: MeOH = 20: 1);
    [4806] NMR (CD 3 OD): δ 7.42 (d, J = 8.1 Hz, 1H), 7.28 (d, J = 1.5 Hz, 1H), 7.19 (dd, J = 8.1, 1.5 Hz, 1H), 7.11 (d, J = 8.1Hz, 2H), 6.92 (d, J = 8.1Hz, 2H), 6.65 (s, 1H), 5.35 (s, 2H), 4.40 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.97-3.76 (m, 2H), 3.64-3.52 (m, 2H), 3.46-3.35 (m, 2H), 2.56-2.38 (m, 2H), 2.35 (s, 3H), 2.28 ( s, 3H), 2.30-2.10 (m, 2H), 1.91-1.46 (m, 5H), 1.46-1.30 (m, 2H), 0.96 (t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.3 Hz, 6H).
    [4807] Example 37 (2)
    [4808] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dimethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4809]
    [4810] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [4811] NMR (CD 3 OD): δ 7.78 (d, J = 8.7 Hz, 2H), 7.58 (d, J = 8.7 Hz, 2H), 4.40 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.82 (m, 2H), 3.42 (m, 4H), 3.26 (s, 6H), 2.56 (m, 2H), 2.18 (m, 2H), 1.88-1.30 (m, 7H), 0.95 (t , J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4812] Example 37 (3)
    [4813] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-diethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [4814]
    [4815] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [4816] NMR (CD 3 OD): δ 7.96-7.82 (m, 2H), 7.74-7.55 (m, 2H), 4.40 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.60 (m, 6H), 3.55-3.40 (m, 4H), 2.65-2.48 (m, 2H), 2.25-2.06 (m, 2H), 1.89-1.26 (m, 7H), 1.15 (t, J = 7.2 Hz , 6H), 1.00-0.87 (m, 9H).
    [4817] Example 37 (4)
    [4818] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclohexyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4819]
    [4820] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [4821] NMR (CD 3 OD): δ 7.45-7.42 (m, 2H), 7.02-6.99 (m, 2H), 4.40-4.31 (m, 1H), 4.27 (s, 2H), 4.00 (dd, J = 8.0, 4.5 Hz, 1H), 3.83-3.70 (m, 2H), 3.47 (brd, 2H), 3.42-3.35 (m, 2H), 2.43-2.32 (m, 2H), 2.24-2.11 (m, 2H), 2.00 -1.93 (m, 2H), 1.86-1.32 (m, 15H), 0.97-0.92 (m, 9H).
    [4822] Example 37 (5)
    [4823] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4824]
    [4825] TLC: Rf 0.70 (CHCl 3: MeOH = 10: 1);
    [4826] NMR (CD 3 OD): δ 7.52-7.47 (m, 2H), 7.22-7.19 (m, 2H), 7.04-7.00 (m, 2H), 6.94-6.90 (m, 2H), 4.32 (s, 2H) , 4.01 (dd, J = 8.0, 4.5 Hz, 1H), 3.86-3.73 (m, 2H), 3.48 (brd, 2H), 3.42-3.34 (m, 2H), 2.45-2.33 (m, 5H), 2.25 -2.12 (m, 2H), 1.85-1.48 (m, 5H), 1.41-1.31 (m, 2H), 0.97-0.92 (m, 9H).
    [4827] Example 37 (6)
    [4828] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4829]
    [4830] TLC: Rf 0.65 (CHCl 3: MeOH = 10: 1);
    [4831] NMR (CD 3 OD): δ 7.49-7.46 (m, 2H), 7.00-6.94 (m, 6H), 4.31 (s, 2H), 4.01 (dd, J = 8.0, 4.5 Hz, 1H), 3.84-3.71 (m, 5H), 3.48 (brd, 2H), 3.40-3.31 (m, 2H), 2.42-2.30 (m, 2H), 2.25-2.12 (m, 2H), 1.83-1.48 (m, 5H), 1.41 -1.30 (m, 2H), 0.97-0.92 (m, 9H).
    [4832] Example 37 (7)
    [4833] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-butylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4834]
    [4835] TLC: Rf 0.35 (CHCl 3: MeOH = 10: 1);
    [4836] NMR (CD 3 OD): δ 7.46 (d, J = 8.1 Hz, 2H), 7.32 (d, J = 8.1 Hz, 2H), 4.31 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.84-3.68 (m, 2H), 3.54-3.36 (m, 4H), 2.67 (t, J = 7.8 Hz, 2H), 2.48-2.30 (m, 2H), 2.26-2.08 (m, 2H) , 1.90-1.28 (m, 11H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H), 0.94 (t, J = 7.2 Hz, 3H).
    [4837] Example 37 (8)
    [4838] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-methylpropyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4839]
    [4840] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [4841] NMR (CD 3 OD): δ 7.47 (d, J = 6.9 Hz, 2H), 7.30 (d, J = 6.9 Hz, 2H), 4.33 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.70 (m, 2H), 3.56-3.34 (m, 4H), 2.53 (d, J = 7.2 Hz, 2H), 2.53-2.30 (m, 2H), 2.24-2.08 (m, 2H) , 1.96-1.26 (m, 8H), 0.95 (t, J = 7.8 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.91 (d, J = 6.6 Hz, 6H).
    [4842] Example 37 (9)
    [4843] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-fluorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4844]
    [4845] TLC: Rf 0.36 (CHCl 3: MeOH = 10: 1);
    [4846] NMR (CD 3 OD): δ 7.53 (d, J = 8.4 Hz, 2H), 7.17 (d, J = 8.4 Hz, 2H), 7.16-7.04 (m, 4H), 4.33 (s, 2H), 4.02 ( dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.68 (m, 2H), 3.58-3.36 (m, 4H), 2.46-2.10 (m, 4H), 1.90-1.24 (m, 7H), 0.96 ( t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4847] Example 37 (10)
    [4848] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-hydroxy-4-methoxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [4849]
    [4850] TLC: Rf 0.20 (CHCl 3: MeOH = 10: 1);
    [4851] NMR (CD 3 OD): δ 7.03-6.94 (m, 3H), 4.23 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.89 (s, 3H), 3.84-3.68 (m , 2H), 3.56-3.36 (m, 4H), 2.42-2.08 (m, 4H), 1.88-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4852] Example 37 (11)
    [4853] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4854]
    [4855] TLC: Rf 0.48 (hexane: AcOEt = 1: 1);
    [4856] NMR (CD 3 OD): δ 7.64-7.54 (m, 2H), 7.37-7.27 (m, 2H), 4.45 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.81 (m, 2H), 3.54 (m, 2H), 3.36 (m, 2H), 2.38 (m, 2H), 2.19 (m, 2H), 1.82-1.49 (m, 5H), 1.35 (m, 2H), 0.95 (t, J = 7.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [4857] Example 37 (12)
    [4858] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4859]
    [4860] TLC: Rf 0.52 (hexane: ethyl acetate = 1: 1);
    [4861] NMR (CD 3 OD): δ 7.52 (dt, J = 8.3, 6.0 Hz, 1H), 7.41-7.37 (m, 2H), 7.26 (t, J = 8.3 Hz, 1H), 4.39 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.89-3.76 (m, 2H), 3.50-3.38 (m, 4H), 2.48-2.38 (m, 2H), 2.25-2.12 (m, 2H), 1.84-1.75 (m, 1H), 1.72-1.46 (m, 4H), 1.42-1.28 (m, 2H), 0.99-0.92 (m, 9H).
    [4862] Example 37 (13)
    [4863] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4864]
    [4865] TLC: Rf 0.33 (hexane: AcOEt = 1: 1);
    [4866] NMR (CD 3 OD): δ 7.60 (dd, J = 8.7, 5.4 Hz, 2H), 7.24 (t, J = 8.7 Hz, 2H), 4.36 (s, 2H), 3.99 (dd, J = 7.5, 4.5 Hz, 1H), 3.78 (m, 2H), 3.49-3.35 (m, 4H), 2.44-2.13 (m, 4H), 1.84-1.46 (m, 5H), 1.37 (m, 2H), 0.99-0.95 ( m, 9H).
    [4867] Example 37 (14)
    [4868] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4869]
    [4870] TLC: Rf 0.62 (hexane: ethyl acetate = 1: 1);
    [4871] NMR (CD 3 OD): δ 7.72 (d, J = 7.0 Hz, 1H), 7.60 (dd, J = 8.0, 1.5 Hz, 1H), 7.56-7.45 (m, 2H), 4.55 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.94 (m, 2H), 3.55 (m, 2H), 3.42-3.32 (m, 2H), 2.43-2.37 (m, 2H), 2.26-2. 13 (m, 2H), 1.85-1.46 (m, 5H), 1.35 (m, 2H), 0.97-0.92 (m, 9H).
    [4872] Example 37 (15)
    [4873] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4874]
    [4875] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [4876] NMR (CD 3 OD): δ 7.55 (d, J = 8.7 Hz, 2H), 7.51 (d, J = 8.7 Hz, 2H), 4.34 (s, 2H), 4.00 (dd, J = 7.8, 4.5, Hz , 1H), 3.88-3.68 (m, 2H), 3.51-3.34 (m, 4H), 2.49-2.52 (m, 2H), 2.26-2.08 (m, 2H), 1.90-1.44 (m, 5H), 1 44-1.29 (m, 2H), 1.00-0.89 (m, 9H).
    [4877] Example 37 (16)
    [4878] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4879]
    [4880] TLC: Rf 0.55 (CHCl 3: MeOH = 20: 1);
    [4881] NMR (CD 3 OD): δ 7.68-7.64 (m, 1H), 7.56-7.45 (m, 3H), 4.37 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.91-3.72 (m, 2H), 3.54-3.32 (m, 4H), 2.53-2.34 (m, 2H), 2.27-2.08 (m, 2H), 1.90-1.44 (m, 5H), 1.44-1.27 (m, 2H) , 0.99-0.89 (m, 9H).
    [4882] Example 37 (17)
    [4883] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methyl-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4884]
    [4885] TLC: Rf 0.34 (CHCl 3: MeOH = 20: 1);
    [4886] NMR (CD 3 OD): δ 7.38-7.30 (m, 2H), 6.99 (d, J = 8.1 Hz, 1H), 4.25 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.85 (s, 3H), 3.85-3.65 (m, 2H), 3.52-3.33 (m, 4H), 2.50-2.30 (m, 2H), 2.22 (s, 3H), 2.20-2.07 (m, 2H), 1.90-1.43 (m, 5H), 1.43-1.28 (m, 2H), 0.99-0.88 (m, 9H).
    [4887] Example 37 (18)
    [4888] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (7-methoxy-1,3-benzodioxolan-5-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane hydrochloride
    [4889]
    [4890] TLC: Rf 0.36 (CHCl 3: MeOH = 20: 1);
    [4891] NMR (CD 3 OD): δ 6.85 (d, J = 1.8 Hz, 1H), 6.74 (d, J = 1.8 Hz, 1H), 5.99 (s, 2H), 4.25 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.92 (s, 3H), 3.87-3.66 (m, 2H), 3.52-3.32 (m, 4H), 2.52-2.34 (m, 2H), 2.26-2.08 (m, 2H), 1.90-1.43 (m, 5H), 1.43-1.29 (m, 2H), 0.99-0.90 (m, 9H).
    [4892] Example 37 (19)
    [4893] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylthiophenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [4894]
    [4895] TLC: Rf 0.52 (CHCl 3: MeOH = 20: 1);
    [4896] NMR (CD 3 OD): δ 7.50-7.36 (m, 7H), 7.30 (d, J = 8.7 Hz, 2H), 4.31 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.68 (m, 2H), 3.53-3.32 (m, 4H), 2.50-2.30 (m, 2H), 2.26-2.06 (m, 2H), 1.90-1.42 (m, 5H), 1.42-1.27 (m , 2H), 0.98-0.89 (m, 9H).
    [4897] Example 37 (20)
    [4898] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4899]
    [4900] TLC: Rf 0.41 (CHCl 3: MeOH = 19: 1);
    [4901] NMR (CD 3 OD): δ 7.57 (d, J = 7.8 Hz, 1H), 7.42-7.28 (m, 3H), 4.41 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.89 (m, 2H), 3.53 (m, 2H), 3.42 (m, 2H), 2.48 (s, 3H), 2.48 (m, 2H), 2.16 (m, 2H), 1.90-1.42 (m, 5H) , 1.36 (sextet, J = 7.2 Hz, 2H), 0.94 (d, J = 6.6 Hz, 3H), 0.94 (t, J = 7.2 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [4902] Example 37 (21)
    [4903] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4904]
    [4905] TLC: Rf 0.31 (CHCl 3: MeOH = 19: 1);
    [4906] NMR (CD 3 OD): δ 7.41-7.29 (m, 4H), 4.31 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.79 (m, 2H), 3.52-3.34 (m , 4H), 2.40 (m, 2H), 2.40 (s, 3H), 2.17 (m, 2H), 1.90-1.44 (m, 5H), 1.36 (sextet, J = 7.5 Hz, 2H), 0.94 (t, J = 7.5 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [4907] Example 37 (22)
    [4908] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [4909]
    [4910] TLC: Rf 0.31 (CHCl 3: MeOH = 19: 1);
    [4911] NMR (CD 3 OD): δ 7.43 (d, J = 7.8 Hz, 2H), 7.31 (d, J = 7.8 Hz, 2H), 4.31 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.78 (m, 2H), 3.52-3.35 (m, 4H), 2.40 (m, 2H), 2.37 (s, 3H), 2.17 (m, 2H), 1.88-1.44 (m, 5H), 1.36 (sextet, J = 7.5 Hz, 2H), 0.94 (t, J = 7.5 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [4912] Example 37 (23)
    [4913] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1-methylethyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [4914]
    [4915] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4916] NMR (CD 3 OD): δ 7.48 (d, J = 8.4 Hz, 2H), 7.38 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.70 (m, 2H), 3.54-3.36 (m, 4H), 3.04-2.88 (m, 1H), 2.48-2.30 (m, 2H), 2.28-2.08 (m, 2H), 1.90- 1.28 (m, 7H), 1.26 (d, J = 6.9 Hz, 6H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.9 Hz, 3H), 0.94 (d, J = 6.9 Hz, 3H).
    [4917] Example 37 (24)
    [4918] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-fluoro-4-methoxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [4919]
    [4920] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [4921] NMR (CD 3 OD): δ 7.40-7.32 (m, 2H), 7.21 (m, 1H), 4.31 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.92 (s, 3H ), 3.86-3.64 (m, 2H), 3.58-3.36 (m, 4H), 2.56-2.32 (m, 2H), 2.28-2.08 (m, 2H), 1.90-1.26 (m, 7H), 0.96 (t , J = 7.2 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4922] Example 37 (25)
    [4923] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-hydroxyethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4924]
    [4925] TLC: Rf 0.22 (CHCl 3: MeOH = 10: 1);
    [4926] NMR (CD 3 OD): δ 7.48 (d, J = 8.7 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 4.29 (s, 2H), 4.09 (t, J = 5.1 Hz, 2H) , 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.88 (t, J = 5.1 Hz, 2H), 3.86-3.64 (m, 2H), 3.54-3.36 (m, 4H), 2.50-2.30 (m , 2H), 2.26-2.08 (m, 2H), 1.90-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4927] Example 37 (26)
    [4928] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-hydroxy-3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4929]
    [4930] TLC: Rf 0.66 (CHCl 3: MeOH = 10: 1);
    [4931] NMR (CD 3 OD): δ 7.24 (d, J = 7.7 Hz, 2H), 6.89 (t, J = 7.7 Hz, 1H), 4.36 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.76 (m, 2H), 3.58-3.36 (m, 4H), 2.44-2.08 (m, 4H), 2.89 (s, 3H), 1.90-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4932] Example 37 (27)
    [4933] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-trifluoromethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4934]
    [4935] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [4936] NMR (CD 3 OD): δ 7.71 (d, J = 7.8 Hz, 2H), 7.42 (d, J = 7.8 Hz, 2H), 4.41 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.56-3.36 (m, 4H), 2.56-2.36 (m, 2H), 2.26-2.08 (m, 2H), 1.90-1.28 (m, 7H), 0.95 ( t, J = 7.5 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4937] Example 37 (28)
    [4938] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methyl-5-chloro-1-phenylpyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [4939]
    [4940] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [4941] NMR (CD 3 OD): δ 7.59-7.50 (m, 5H), 4.35 (s, 2H), 4.03 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.80 (m, 2H), 3.72-3.58 (m, 2H), 3.46-3.38 (m, 2H), 2.58-2.38 (m, 2H), 2.45 (s, 3H), 2.36-2.18 (m, 2H), 1.92-1.24 (m, 7H), 0.97 (t, J = 7.5 Hz, 3H), 0.96 (d, J = 6.6 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H).
    [4942] Example 37 (29)
    [4943] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylpyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [4944]
    [4945] TLC: Rf 0.28 (CHCl 3: MeOH = 10: 1);
    [4946] NMR (CD3OD): δ 9.17 (s, 1H), 8.80 (m, 1H), 8.39 (m, 1H), 8.03-7.97 (m, 2H), 7.73-7.65 (m, 3H), 4.65 (s, 2H ), 4.03 (dd, J = 7.2, 4.2 Hz, 1H), 4.02-3.82 (m, 2H), 3.64-3.42 (m, 2H), 3.78-3.56 (m, 2H), 2.30-2.08 (m, 2H) ), 1.88-1.24 (m, 7H), 0.96 (d, J = 6.3 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H).
    [4947] Example 37 (30)
    [4948] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4949]
    [4950] TLC: Rf 0.18 (CHCl 3: MeOH = 10: 1);
    [4951] NMR (CD 3 OD): δ 7.54 (d, J = 8.7 Hz, 2H), 7.30 (d, J = 9.0 Hz, 2H), 7.08 (d, J = 8.7 Hz, 2H), 7.04 (d, J = 9.0 Hz, 2H), 4.34 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.68 (m, 2H), 3.56-3.35 (m, 4H), 2.96 (s, 3H ), 2.50-2.08 (m, 4H), 1.88-1.26 (m, 7H), 0.96 (t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4952] Example 37 (31)
    [4953] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylsulfonylaminophenyl) pyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [4954]
    [4955] TLC: Rf 0.15 (CHCl 3: MeOH = 10: 1);
    [4956] NMR (CD 3 OD): δ 7.49 (d, J = 8.7 Hz, 2H), 7.43 (d, J = 8.7 Hz, 2H), 4.33 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.96-3.76 (m, 2H), 3.66-3.58 (m, 2H), 3.56-3.42 (m, 2H), 3.05 (s, 3H), 2.68-2.46 (m, 2H), 2.44 (s, 3H), 2.41 (s, 3H), 2.32-2.10 (m, 2H), 1.90-1.28 (m, 7H), 0.97 (t, J = 6.6 Hz, 3H), 0.96 (d, J = 6.3 Hz, 3H ), 0.95 (d, J = 6.3 Hz, 3H).
    [4957] Example 37 (32)
    [4958] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-methylpyridin-2-yloxy) phenylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [4959]
    [4960] TLC: Rf 0.29 (CHCl 3: MeOH = 10: 1);
    [4961] NMR (CD 3 OD): δ 8.12 (s, 1H), 7.93 (d, J = 8.4 Hz, 1H), 7.68 (d, J = 8.7 Hz, 2H), 7.30 (d, J = 8.7 Hz, 2H) , 7.06 (d, J = 8.4 Hz, 1H), 4.40 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.94-3.76 (m, 2H), 3.58-3.40 (m, 4H ), 2.56-2.36 (m, 2H), 2.38 (s, 3H), 2.30-2.08 (m, 2H), 1.88-1.24 (m, 7H), 0.96 (t, J = 7.8 Hz, 3H), 0.96 ( d, J = 6.6 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H).
    [4962] Example 37 (33)
    [4963] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (6-methylpyridine-1-oxide-3-yloxy) phenylmethyl) -1, 4,9-triazaspiro [5.5] undecane hydrochloride
    [4964]
    [4965] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [4966] NMR (CD 3 OD): δ 8.47 (s, 1H), 7.71 (d, J = 8.7 Hz, 2H), 7.62-7.48 (m, 2H), 7.29 (d, J = 8.7 Hz, 2H), 4.40 ( s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.92-3.72 (m, 2H), 3.58-3.38 (m, 4H), 2.64-2.40 (m, 2H), 2.60 (s, 3H), 2.28-2.10 (m, 2H), 1.90-1.28 (m, 7H), 0.96 (t, J = 7.8 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [4967] Example 37 (34)
    [4968] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (2-methylpropyloxycarbonyl) indol-5-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane hydrochloride
    [4969]
    [4970] TLC: Rf 0.23 (CHCl 3: MeOH = 10: 1);
    [4971] NMR (CD 3 OD): δ 8.16 (d, J = 8.4 Hz, 1H), 7.82 (d, J = 1.5 Hz, 1H), 7.78 (d, J = 3.6 Hz, 1H), 7.50 (dd, J = 8.4, 1.5 Hz, 1H), 6.75 (d, J = 3.6 Hz, 1H), 4.46 (s, 2H), 4.27 (d, J = 6.6 Hz, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.82-3.74 (m, 2H), 3.58-3.36 (m, 4H), 2.48-2.30 (m, 2H), 2.26-2.08 (m, 3H), 1.88-1.24 (m, 7H), 1.09 ( s, 3H), 1.06 (s, 3H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4972] Example 37 (35)
    [4973] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenyl-5-methyloxazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4974]
    [4975] TLC: Rf 0.32 (CHCl 3: MeOH = 10: 1);
    [4976] NMR (CD 3 OD): δ 8.05-8.02 (m, 2H), 7.52-7.50 (m, 3H), 4.35 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.80 (m, 2H), 3.70-3.58 (m, 2H), 3.44-3.38 (m, 2H), 2.53 (s, 3H), 2.53-2.36 (m, 2H), 2.34-2.14 (m, 2H), 1.90 -1.26 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [4977] Example 37 (36)
    [4978] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [4979]
    [4980] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [4981] NMR (CD 3 OD): δ 7.47 (d, J = 8.4 Hz, 2H), 7.07 (d, J = 8.4 Hz, 2H), 4.64 (m, 1H), 4.29 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.98-3.91 (m, 2H), 3.84-3.68 (m, 2H), 3.64-3.56 (m, 2H), 3.50-3.37 (m, 4H), 2.50-2.30 ( m, 2H), 2.24-1.98 (m, 4H), 1.88-1.26 (m, 9H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d , J = 6.3 Hz, 3H).
    [4982] Example 37 (37)
    [4983] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (6-methylpyridin-3-yloxy) phenylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [4984]
    [4985] TLC: Rf 0.22 (CHCl 3: MeOH = 10: 1);
    [4986] NMR (CD 3 OD): δ 8.55 (d, J = 2.7 Hz, 1H), 8.10 (dd, J = 9.0, 2.7 Hz, 1H), 7.84 (d, J = 9.0 Hz, 1H), 7.72 (d, J = 8.7 Hz, 2H), 7.29 (d, J = 8.7 Hz, 2H), 4.40 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.70 (m, 2H), 3.58-3.38 (m, 4H), 2.74 (s, 3H), 2.60-2.42 (m, 2H), 2.28-2.08 (m, 2H), 1.90-1.26 (m, 7H), 0.96 (t, J = 7.5 Hz, 3H), 0.96 (d, J = 6.6 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H).
    [4987] Example 37 (38)
    [4988] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4989]
    [4990] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [4991] NMR (CD 3 OD): δ 7.55-7.46 (m, 2H), 7.36-7.25 (m, 2H), 4.30 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.95-3.73 (m, 2H), 3.66-3.55 (m, 2H), 3.52-3.40 (m, 2H), 2.63-2.45 (m, 2H), 2.39 (s, 3H), 2.37 (s, 3H), 2.30-2.10 (m, 2H), 1.90-1.43 (m, 5H), 1.43-1.30 (m, 2H), 0.99-0.91 (m, 9H).
    [4992] Example 37 (39)
    [4993] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (pyridin-2-yl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4994]
    [4995] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [4996] NMR (CD 3 OD): δ 8.55 (d, J = 4.8 Hz, 1H), 8.12 (dd, J = 8.4, 7.2 Hz, 1H), 7.87 (d, J = 8.4 Hz, 1H), 7.50 (dd, J = 7.2, 4.8 Hz, 1H), 4.32 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.96-3.73 (m, 2H), 3.67-3.55 (m, 2H), 3.54 -3.40 (m, 2H), 2.69 (s, 3H), 2.70-2.48 (m, 2H), 2.44 (s, 3H), 2.28-2.08 (m, 2H), 1.92-1.43 (m, 5H), 1.43 -1.26 (m, 2H), 0.99-0.90 (m, 9H).
    [4997] Example 37 (40)
    [4998] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-hydroxyphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [4999]
    [5000] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5001] NMR (CD 3 OD): δ 7.30 (d, J = 9.0 Hz, 2H), 6.95 (d, J = 9.0 Hz, 2H), 4.33 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.77 (m, 2H), 3.61 (m, 2H), 3.47 (m, 2H), 2.58 (m, 2H), 2.45 (s, 3H), 2.36 (s, 3H), 2.20 (m , 2H), 1.88-1.76 (m, 1H), 1.73-1.32 (m, 6H), 0.96 (t, J = 7.5 Hz, 3H), 0.95 (d, J = 6.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H).
    [5002] Example 37 (41)
    [5003] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-carboxyethyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5004]
    [5005] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [5006] NMR (CD 3 OD): δ 7.47 (d, J = 8.0 Hz, 2H), 7.37 (d, J = 8.0 Hz, 2H), 4.31 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.73 (m, 2H), 3.49-3.35 (m, 4H), 2.96 (t, J = 7.5 Hz, 2H), 2.62 (t, J = 7.5 Hz, 2H), 2.44-2.33 (m , 2H), 2.23-2.11 (m, 2H), 1.84-1.32 (m, 7H), 0.94 (t, J = 7.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [5007] Example 37 (42)
    [5008] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (dimethylaminosulfonyl) phenyl) pyrazole-4 -Ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5009]
    [5010] TLC: Rf 0.54 (CHCl 3: MeOH = 9: 1);
    [5011] NMR (CD 3 OD): δ 7.96 (d, J = 8.7 Hz, 2H), 7.77 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.95-3.75 (m, 2H), 3.66-3.56 (m, 2H), 3.47 (m, 2H), 2.74 (s, 6H), 2.56 (m, 2H), 2.48 (s, 3H), 2.41 (s, 3H), 2.30-2.12 (m, 2H), 1.90-1.46 (m, 5H), 1.38 (sextet, J = 7.2 Hz, 2H), 0.98-0.93 (m, 9H).
    [5012] Example 37 (43)
    [5013] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-methylpyridin-1-oxide-2-yloxy) phenylmethyl) -1, 4,9-triazaspiro [5.5] undecane hydrochloride
    [5014]
    [5015] TLC: Rf 0.41 (CHCl 3: MeOH = 9: 1);
    [5016] NMR (CD 3 OD): δ 7.77 (brs, 1 H), 7.65-7.59 (m, 2 H), 7.56 (dd, J = 9.3, 2.4 Hz, 1 H), 7.03-6.97 (m, 2H), 6.73 (d , J = 9.3 Hz, 1H), 4.33 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.86-3.68 (m, 2H), 3.51-3.36 (m, 4H), 2.46 ( m, 2H), 2.25-2.07 (m, 2H), 2.18 (s, 3H), 1.90-1.44 (m, 5H), 1.36 (sextet, J = 7.2 Hz, 2H), 0.97-0.91 (m, 9H) .
    [5017] Example 37 (44)
    [5018] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-carboxy-1-ethenyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [5019]
    [5020] TLC: Rf 0.20 (CHCl 3: MeOH = 10: 1);
    [5021] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.70 (d, J = 16.2 Hz, 1H), 7.61 (d, J = 8.4 Hz, 2H), 6.58 (d, J = 16.2 Hz, 2H), 4.39 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.92-3.74 (m, 2H), 3.58-3.36 (m, 4H), 2.50-2.32 (m , 2H), 2.30-2.10 (m, 2H), 1.90-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5022] Example 37 (45)
    [5023] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4- (2-carboxy-1-ethenyl) phenyloxy) phenylmethyl) -1 , 4,9-triazaspiro [5.5] undecane hydrochloride
    [5024]
    [5025] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [5026] NMR (CD 3 OD): δ 7.69-7.57 (m, 5H), 7.14 (d, J = 8.4 Hz, 2H), 7.05 (d, J = 8.7 Hz, 2H), 6.42 (d, J = 15.9 Hz, 1H), 4.36 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.92-3.70 (m, 2H), 3.56-3.35 (m, 4H), 2.48-2.30 (m, 2H) , 2.30-2.12 (m, 2H), 1.88-1.25 (m, 7H), 0.98-0.88 (m, 9H).
    [5027] Example 37 (46)
    [5028] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-aminocarbonylphenyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5029]
    [5030] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [5031] NMR (CD 3 OD): δ 7.90 (d, J = 8.7 Hz, 2H), 7.60 (d, J = 8.7 Hz, 2H), 7.15 (d, J = 8.7 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 4.36 (s, 2H), 4.01 (dd, J = 7.8, 4.5, Hz, 1H), 3.90-3.70 (m, 2H), 3.58-3.35 (m, 4H), 2.54-2.36 ( m, 2H), 2.30-2.10 (m, 2H), 1.90-1.26 (m, 7H), 1.00-0.86 (m, 9H).
    [5032] Example 37 (47)
    [5033] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-aminosulfonylphenyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5034]
    [5035] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [5036] NMR (CD 3 OD): δ 7.90 (d, J = 8.7 Hz, 2H), 7.57 (d, J = 8.7 Hz, 2H), 7.17 (d, J = 8.7 Hz, 2H), 7.13 (d, J = 8.7 Hz, 2H), 4.28 (brs, 2H), 4.01 (dd, J = 7.8, 4.5, Hz, 1H), 3.83-3.60 (m, 2H), 3.49-3.34 (m, 4H), 2.44-2.26 ( m, 2H), 2.26-2.09 (m, 2H), 1.89-1.26 (m, 7H), 1.00-0.88 (m, 9H).
    [5037] Example 37 (48)
    [5038] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-benzylpyrazol-4-ylmethyl) -1,4,9 -Triazaspiro [5.5] undecane, dihydrochloride
    [5039]
    [5040] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5041] NMR (CD 3 OD): δ 7.41-7.33 (m, 3H), 7.21-7.19 (m, 2H), 5.45 (s, 2H), 4.30 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz , 1H), 3.89-3.73 (m, 2H), 3.60-3.46 (m, 4H), 2.61 (m, 2H), 2.48 (s, 3H), 2.46 (s, 3H), 2.23-2.11 (m, 2H ), 1.87-1.31 (m, 7H), 0.95 (t, J = 7.0 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [5042] Example 37 (49)
    [5043] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (2,4-difluorophenyl) pyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5044]
    [5045] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5046] NMR (CD 3 OD): δ 7.61-7.53 (m, 1 H), 7.33-7.26 (m, 1 H), 7.23-7.16 (m, 1 H), 4.31 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.76 (m, 2H), 3.63-3.56 (m, 2H), 3.49-3.45 (m, 2H), 2.57 (m, 2H), 2.40 (s, 3H), 2.29 (s , 3H), 2.19 (m, 2H), 1.86-1.34 (m, 7H), 0.96 (t, J = 7.0 Hz, 3H), 0.95 (d, J = 6.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H).
    [5047] Example 37 (50)
    [5048] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrrolidin-1-ylmethyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [5049]
    [5050] TLC: Rf 0.10 (CHCl 3: MeOH = 10: 1);
    [5051] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.65 (d, J = 8.4 Hz, 2H), 4.43 (s, 2H), 4.40 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.70 (m, 2H), 3.56-3.40 (m, 6H), 3.25-3.12 (m, 2H), 2.68-2.48 (m, 2H), 2.28-1.95 ( m, 6H), 1.88-1.42 (m, 5H), 1.42-1.30 (m, 2H), 0.98-0.90 (m, 9H).
    [5052] Example 37 (51)
    [5053] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (morpholin-4-ylsulfonyl) phenyl) pyra Zol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5054]
    [5055] TLC: Rf 0.43 (CHCl 3: MeOH = 20: 1);
    [5056] NMR (CD 3 OD): δ 7.95 (d, J = 8.7 Hz, 2H), 7.80 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.95-3.72 (m, 2H), 3.76-3.67 (m, 4H), 3.66-3.57 (m, 2H), 3.56-3.42 (m, 2H), 3.08-2.95 (m, 4H), 2.70- 2.50 (m, 2H), 2.50 (s, 3H), 2.42 (s, 3H), 2.31-2.10 (m, 2H), 1.90-1.44 (m, 5H), 1.44-1.30 (m, 2H), 1.00- 0.91 (m, 9 H).
    [5057] Example 37 (52)
    [5058] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (methylaminosulfonyl) phenyl) pyrazole-4 -Ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5059]
    [5060] TLC: Rf 0.21 (CHCl 3: MeOH = 10: 1);
    [5061] NMR (CD 3 OD): δ 8.01 (d, J = 8.4 Hz, 2H), 7.73 (d, J = 8.4 Hz, 2H), 4.34 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.98-3.78 (m, 2H), 3.66-3.58 (m, 2H), 3.44-3.30 (m, 2H), 2.59 (s, 3H), 2.54-2.38 (m, 2H), 2.47 (s, 3H), 2.40 (s, 3H), 2.36-2.16 (m, 2H), 1.90-1.26 (m, 7H), 0.97 (t, J = 7.5 Hz, 3H), 0.96 (d, J = 6.6 Hz, 6H ).
    [5062] Example 37 (53)
    [5063] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-cyanophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5064]
    [5065] TLC: Rf 0.30 (CHCl 3: MeOH = 10: 1);
    [5066] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.66 (d, J = 8.7 Hz, 2H), 7.21 (d, J = 8.4 Hz, 2H), 7.14 (d, J = 8.7 Hz, 2H), 4.39 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.72 (m, 2H), 3.58-3.36 (m, 4H), 2.58-2.38 (m , 2H), 2.28-2.08 (m, 2H), 1.88-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5067] Example 37 (54)
    [5068] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (dimethylaminomethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5069]
    [5070] TLC: Rf 0.16 (CHCl 3: MeOH = 10: 1);
    [5071] NMR (CD 3 OD): δ 7.76 (d, J = 8.1 Hz, 2H), 7.63 (d, J = 8.1 Hz, 2H), 4.41 (s, 2H), 4.37 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.50-3.42 (m, 4H), 2.87 (s, 6H), 2.65-2.50 (m, 2H), 2.22-2.04 (m, 2H), 1.88-1.32 (m, 7H), 0.97-0.92 (m, 9H).
    [5072] Example 37 (55)
    [5073] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (2-dimethylaminoethylaminosulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane trihydrochloride
    [5074]
    [5075] TLC: Rf 0.13 (CHCl 3: MeOH = 10: 1);
    [5076] NMR (CD 3 OD): δ 8.07 (d, J = 8.7 Hz, 2H), 7.78 (d, J = 8.7 Hz, 2H), 4.31 (s, 2H), 4.01 (dd, J = 8.1, 5.1 Hz, 1H), 3.95-3.74 (m, 2H), 3.68-3.45 (m, 4H), 3.40-3.20 (m, 4H), 2.95 (s, 6H), 2.70-2.50 (m, 2H), 2.49 (s, 3H), 2.41 (s, 3H), 2.28-2.12 (m, 2H), 1.88-1.34 (m, 7H), 0.98-0.92 (m, 9H).
    [5077] Example 37 (56)
    [5078] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (4-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5079]
    [5080] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [5081] NMR (CD 3 OD): δ 7.81 (s, 1H), 7.69 (d, J = 7.5 Hz, 1H), 7.53 (d, J = 9.0 Hz, 2H), 7.55-7.48 (m, 1H), 7.45 ( d, J = 7.5 Hz, 1H), 6.87 (d, J = 9.0 Hz, 2H), 4.40 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.73 (m, 2H ), 3.56-3.44 (m, 2H), 3.44-3.30 (m, 2H), 2.53-2.33 (m, 2H), 2.26-2.08 (m, 2H), 1.90-1.40 (m, 5H), 1.43-1.25 (m, 2H), 0.94 (d, J = 6.3 Hz, 3H), 0.94 (t, J = 7.2 Hz, 3H), 0.93 (d, J = 6.3 Hz, 3H).
    [5082] Example 37 (57)
    [5083] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5084]
    [5085] TLC: Rf 0.54 (CHCl 3: MeOH = 10: 1);
    [5086] NMR (CD 3 OD): δ 7.53 (d, J = 8.5 Hz, 2H), 7.28 (t, J = 8.3 Hz, 1H), 7.07 (d, J = 8.5 Hz, 2H), 6.75 (ddd, J = 8.3, 2.3, 1.0 Hz, 1H), 6.60-6.57 (m, 2H), 4.33 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.73 (m, 2H), 3.77 (s, 3H), 3.51-3.34 (m, 4H), 2.41 (m, 2H), 2.42-2.12 (m, 2H), 1.84-1.33 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H ), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [5087] Example 37 (58)
    [5088] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (quinoxalin-2-yl) pyrazol-4-ylmethyl ) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5089]
    [5090] TLC: Rf 0.52 (CHCl 3: MeOH = 10: 1);
    [5091] NMR (CD 3 OD): δ 9.51 (s, 1H), 8.12 (d, J = 8.0 Hz, 1H), 8.04 (d, J = 8.0 Hz, 1H), 7.90-7.80 (m, 2H), 4.37 ( s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.81 (m, 2H), 3.63 (m, 2H), 3.44 (m, 2H), 2.92 (s, 3H), 2.47 (s, 3H), 2.47 (m, 2H), 2.29-2.17 (m, 2H), 1.86-1.33 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.5 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H).
    [5092] Example 37 (59)
    [5093] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylcarbonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5094]
    [5095] TLC: Rf 0.76 (CHCl 3: MeOH = 10: 1);
    [5096] NMR (CD 3 OD): δ 7.88 (d, J = 8.4 Hz, 2H), 7.81-7.67 (m, 5H), 7.57-7.52 (m, 2H), 4.49 (s, 2H), 4.01 (dd, J = 8.1, 4.8 Hz, 1H), 4.00-3.78 (m, 2H), 3.59-3.48 (m, 2H), 3.44-3.35 (m, 2H), 2.50-2.32 (m, 2H), 2.32-2.14 (m , 2H), 1.88-1.24 (m, 7H), 1.02-0.88 (m, 9H).
    [5097] Example 37 (60)
    [5098] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (N- (2-hydroxyethyl) -N -Methylaminosulfonyl) phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5099]
    [5100] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [5101] NMR (CD 3 OD): δ 8.00 (d, J = 8.7 Hz, 2H), 7.76 (d, J = 8.7 Hz, 2H), 4.34 (s, 2H), 4.04 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.76 (m, 2H), 3.70 (t, J = 5.7 Hz, 2H), 3.68-3.58 (m, 2H), 3.50-3.38 (m, 2H), 3.20 (t, J = 5.7 Hz , 2H), 2.88 (s, 3H), 2.58-2.38 (m, 2H), 2.48 (s, 3H), 2.41 (s, 3H), 2.36-2.16 (m, 2H), 1.90-1.24 (m, 7H ), 0.97 (t, J = 6.9 Hz, 3H), 0.96 (d, J = 6.3 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H).
    [5102] Example 37 (61)
    [5103] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (2-phenylethyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5104]
    [5105] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [5106] NMR (CD 3 OD): δ 7.31-7.23 (m, 3H), 7.10 (d, J = 6.6 Hz, 2H), 4.44 (t, J = 6.3 Hz, 2H), 4.21 (s, 2H), 4.03 ( dd, J = 7.8, 4.8 Hz, 1H), 3.82-3.60 (m, 2H), 3.58-3.32 (m, 4H), 3.13 (t, J = 6.3 Hz, 2H), 2.72-2.52 (m, 2H) , 2.50 (s, 3H), 2.24-2.04 (m, 2H), 1.99 (s, 3H), 1.90-1.36 (m, 7H), 0.97 (t, J = 7.2Hz, 3H), 0.96 (d, J = 6.6 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H).
    [5107] Example 37 (62)
    [5108] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,3,5-trimethylpyrazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [5109]
    [5110] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5111] NMR (CD 3 OD): δ 4.28 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.87 (s, 3H), 3.87-3.69 (m, 2H), 3.60-3.43 (m , 4H), 2.69-2.50 (m, 2H), 2.46 (s, 3H), 2.44 (s, 3H), 2.26-2.08 (m, 2H), 1.90-1.28 (m, 7H), 0.98-0.85 (m , 9H).
    [5112] Example 37 (63)
    [5113] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (morpholin-4-ylmethyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [5114]
    [5115] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [5116] NMR (CD 3 OD): δ 7.74 (d, J = 8.4 Hz, 2H), 7.66 (d, J = 8.4 Hz, 2H), 4.40 (s, 4H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 4.10-3.70 (m, 6H), 3.54-3.42 (m, 4H), 3.40-3.16 (m, 4H), 2.65-2.46 (m, 2H), 2.24-2.03 (m, 2H), 1.88- 1.28 (m, 7 H), 1.02-0.88 (m, 9 H).
    [5117] Example 37 (64)
    [5118] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylpiperazin-1-ylmethyl) phenylmethyl) -1,4,9 -Triazaspiro [5.5] undecane trihydrochloride
    [5119]
    [5120] TLC: Rf 0.64 (CHCl 3: MeOH = 5: 1);
    [5121] NMR (CD 3 OD): δ 7.45 (m, 4H), 4.55 (s, 2H), 4.42 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.88-3.56 (m, 10H ), 3.53-3.43 (m, 4H), 3.01 (s, 3H), 2.59-2.47 (m, 2H), 2.22-2.09 (m, 2H), 1.85-1.33 (m, 7H), 0.94 (t, J = 7.2 Hz, 3H), 0.94 (d, J = 6.5 Hz, 3H), 0.93 (d, J = 6.5 Hz, 3H).
    [5122] Example 37 (65)
    [5123] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylsulfonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5124]
    [5125] TLC: Rf 0.70 (ethyl acetate: methanol = 9: 1);
    [5126] NMR (CD 3 OD): δ 8.08 (d, J = 8.4 Hz, 2H), 8.02-7.96 (m, 2H), 7.80 (d, J = 8.4 Hz, 2H), 7.70-7.55 (m, 3H), 4.43 (s, 2H), 3.99 (dd, J = 7.8, 4.8 Hz, 1H), 3.91-3.72 (m, 2H), 3.48-3.34 (m, 4H), 2.48-2.32 (m, 2H), 2.23- 2.06 (m, 2H), 1.88-1.43 (m, 5H), 1.34 (sextet, J = 7.2 Hz, 2H), 0.96-0.90 (m, 9H).
    [5127] Example 37 (66)
    [5128] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-cyclohexylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [5129]
    [5130] TLC: Rf 0.28 (ethyl acetate: methanol = 9: 1);
    [5131] NMR (CD 3 OD): δ 4.35-4.20 (m, 3H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.68 (m, 2H), 3.58-3.41 (m, 4H), 2.60 -2.46 (m, 2H), 2.45 (s, 3H), 2.40 (s, 3H), 2.26-2.08 (m, 2H), 1.98-1.26 (m, 17H), 0.98-0.91 (m, 9H).
    [5132] Example 37 (67)
    [5133] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5134]
    [5135] TLC: Rf 0.11 (ethyl acetate: methanol = 9: 1);
    [5136] NMR (CD 3 OD): δ 7.83 (ddd, J = 7.8, 1.5, 0.9 Hz, 1H), 7.61 (dd, J = 2.4, 1.5 Hz, 1H), 7.58 (d, J = 8.7 Hz, 2H), 7.51 (t, J = 7.8 Hz, 1H), 7.29 (ddd, J = 7.8, 2.4, 0.9 Hz, 1H), 7.11 (d, J = 8.7 Hz, 2H), 4.35 (s, 2H), 4.01 (dd , J = 7.8, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.57-3.36 (m, 4H), 2.50-2.34 (m, 2H), 2.28-2.09 (m, 2H), 1.89-1.44 (m, 5H), 1.36 (sextet, J = 7.2 Hz, 2H), 0.98-0.91 (m, 9H).
    [5137] Example 37 (68)
    [5138] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (piperidin-1-ylmethyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [5139]
    [5140] TLC: Rf 0.52 (CHCl 3: MeOH = 9: 1);
    [5141] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.65 (d, J = 8.4 Hz, 2H), 4.41 (s, 2H), 4.34 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.91-3.71 (m, 2H), 3.54-3.41 (m, 6H), 3.05-2.91 (m, 2H), 2.67-2.49 (m, 2H), 2.25-2.05 ( m, 2H), 2.00-1.28 (m, 13H), 0.98-0.91 (m, 9H).
    [5142] Example 37 (69)
    [5143] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (pyrrolidin-1-ylsulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5144]
    [5145] TLC: Rf 0.36 (ethyl acetate: methanol = 9: 1);
    [5146] NMR (CD 3 OD): δ 8.01 (d, J = 8.7 Hz, 2H), 7.76 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.95-3.74 (m, 2H), 3.66-3.55 (m, 2H), 3.50-3.40 (m, 2H), 3.34-3.24 (m, 4H), 2.62-2.47 (m, 2H), 2.48 ( s, 3H), 2.40 (s, 3H), 2.30-2.11 (m, 2H), 1.90-1.45 (m, 9H), 1.38 (sextet, J = 7.2 Hz, 2H), 1.00-0.90 (m, 9H) .
    [5147] Example 37 (70)
    [5148] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,3-dihydrobenzofuran-5-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5149]
    [5150] TLC: Rf 0.56 (ethyl acetate: methanol = 9: 1);
    [5151] NMR (CD 3 OD): δ 7.40 (brs, 1 H), 7.26 (dd, J = 8.1, 1.8 Hz, 1H), 6.80 (d, J = 8.1 Hz, 1H), 4.59 (t, J = 8.7 Hz, 2H), 4.26 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.66 (m, 2H), 3.52-3.36 (m, 4H), 3.24 (t, J = 8.7 Hz , 2H), 2.49-2.35 (m, 2H), 2.25-2.08 (m, 2H), 1.89-1.43 (m, 5H), 1.36 (sextet, J = 7.2 Hz, 2H), 0.98-0.91 (m, 9H ).
    [5152] Example 37 (71)
    [5153] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (2-hydroxyethylaminosulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5154]
    [5155] TLC: Rf 0.35 (CHCl 3: MeOH = 10: 1);
    [5156] NMR (CD 3 OD): δ 8.03 (d, J = 8.7 Hz, 2H), 7.72 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.02 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.73 (m, 2H), 3.67-3.57 (m, 2H), 3.56 (t, J = 5.7 Hz, 2H), 3.51-3.40 (m, 2H), 3.01 (t, J = 5.7 Hz , 2H), 2.63-2.42 (m, 2H), 2.47 (s, 3H), 2.41 (s, 3H), 2.32-2.12 (m, 2H), 1.92-1.44 (m, 5H), 1.44-1.30 (m , 2H), 1.00-0.91 (m, 9H).
    [5157] Example 37 (72)
    [5158] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (carboxymethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5159]
    [5160] TLC: Rf 0.30 (CHCl 3: MeOH = 10: 1);
    [5161] NMR (CD 3 OD): δ 7.47 (d, J = 8.7 Hz, 2H), 7.04 (d, J = 8.7 Hz, 2H), 4.71 (s, 2H), 4.29 (s, 2H), 4.00 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.67 (m, 2H), 3.53-3.33 (m, 4H), 2.46-2.28 (m, 2H), 2.26-2.08 (m, 2H), 1.90-1.27 ( m, 7H), 0.99-0.90 (m, 9H).
    [5162] Example 37 (73)
    [5163] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1-phenyl-1-hydroxymethyl) phenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [5164]
    [5165] TLC: Rf 0.23 (CHCl 3: MeOH = 10: 1);
    [5166] NMR (CD 3 OD): δ 7.62-7.18 (m, 9H), 5.82 (s, 1H), 4.33 (s, 2H), 4.00 (dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.68 (m , 2H), 3.56-3.36 (m, 4H), 2.48-2.28 (m, 2H), 2.24-2.06 (m, 2H), 1.88-1.24 (m, 7H), 0.95 (t, J = 6.6 Hz, 3H ), 0.94 (d, J = 6.3 Hz, 3H), 0.93 (d, J = 6.3 Hz, 3H).
    [5167] Example 37 (74)
    [5168] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-hydroxypiperidin-1-ylmethyl) phenylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [5169]
    [5170] TLC: Rf 0.16 (CHCl 3: MeOH = 10: 1);
    [5171] NMR (CD 3 OD): δ 7.73 (d, J = 7.8 Hz, 2H), 7.69-7.61 (m, 2H), 4.42 (s, 2H), 4.40-4.34 (m, 2H), 4.11-4.05 (m , 1H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.72 (m, 2H), 3.55-3.38 (m, 4H), 3.16-3.00 (m, 1H), 2.60-2.38 (m , 2H), 2.26-2.06 (m, 3H), 2.00-1.88 (m, 2H), 1.88-1.43 (m, 9H), 1.43-1.14 (m, 2H), 0.98-0.90 (m, 9H).
    [5172] Example 37 (75)
    [5173] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-carboxyphenylmethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5174]
    [5175] TLC: Rf 0.58 (CHCl 3: MeOH = 5: 1);
    [5176] NMR (CD 3 OD): δ 8.10 (s, 1H), 7.98 (d, J = 8.1 Hz, 1H), 7.68 (d, J = 8.7 Hz, 1H), 7.50 (t, J = 8.1 Hz, 1H) , 7.47 (d, J = 8.7 Hz, 2H), 7.13 (d, J = 8.7 Hz, 2H), 5.22 (s, 2H), 4.29 (s, 2H), 4.01 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.68 (m, 2H), 3.54-3.32 (m, 4H), 2.42-2.08 (m, 4H), 1.90-1.28 (m, 7H), 0.95 (t, J = 6.9 Hz, 3H) , 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5177] Example 37 (76)
    [5178] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (bis (methylsulfonyl) amino) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5179]
    [5180] TLC: Rf 0.64 (CHCl 3: MeOH = 5: 1);
    [5181] NMR (CD 3 OD): δ 7.72 (d, J = 8.4 Hz, 2H), 7.61 (d, J = 8.4 Hz, 2H), 4.44 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.78 (m, 2H), 3.58-3.36 (m, 4H), 3.47 (s, 6H), 2.50-2.12 (m, 4H), 1.92-1.28 (m, 7H), 0.96 (t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5182] Example 37 (77)
    [5183] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1,4-benzodioxan-6-yloxy) phenylmethyl) -1,4 , 9-triazaspiro [5.5] undecane hydrochloride
    [5184]
    [5185] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [5186] NMR (CD 3 OD): δ 7.49 (d, J = 8.7 Hz, 2H), 7.02 (d, J = 8.7 Hz, 2H), 6.85 (m, 1H), 6.55-6.51 (m, 2H), 4.33 ( s, 2H), 4.24 (s, 4H), 4.02 (dd, J = 7.5, 4.8 Hz, 1H), 3.88-3.70 (m, 2H), 3.56-3.32 (m, 4H), 2.42-2.10 (m, 4H), 1.92-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.6 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H).
    [5187] Example 37 (78)
    [5188] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (3-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5189]
    [5190] TLC: Rf 0.19 (CHCl 3: MeOH = 10: 1);
    [5191] NMR (CD 3 OD): δ 7.83 (s, 1H), 7.74 (m, 1H), 7.59-7.51 (m, 2H), 7.28 (m, 1H), 7.16-7.09 (m, 2H), 6.81 (m , 1H), 4.44 (s, 2H), 4.01 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.76 (m, 2H), 3.58-3.32 (m, 4H), 2.50-2.32 (m, 2H ), 2.28-2.08 (m, 2H), 1.88-1.26 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5192] Example 37 (79)
    [5193] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (methylsulfonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5194]
    [5195] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5196] NMR (CD 3 OD): δ 7.52 (d, J = 8.4 Hz, 2H), 7.34 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.72 (m, 2H), 3.52-3.14 (m, 4H), 3.01 (s, 3H), 2.46-2.30 (m, 2H), 2.28-2.10 (m, 2H), 1.88-1.1 0 (m, 7 H), 0.98-0.90 (m, 9 H).
    [5197] Example 37 (80)
    [5198] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6- (4-methoxyphenyloxy) pyridin-3-ylmethyl) -1,4,9 -Triazaspiro [5.5] undecane, dihydrochloride
    [5199]
    [5200] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5201] NMR (CD 3 OD): δ 8.30 (m, 1H), 8.05 (m, 1H), 7.10-6.86 (m, 5H), 4.39 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H ), 3.90-3.74 (m, 2H), 3.81 (s, 3H), 3.54-3.32 (m, 4H), 2.54-2.32 (m, 2H), 2.28-2.05 (m, 2H), 1.88-1.26 (m) , 7H), 0.98-0.90 (m, 9H).
    [5202] Example 37 (81)
    [5203] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylaminocarbonylphenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [5204]
    [5205] TLC: Rf 0.54 (CHCl 3: MeOH = 10: 1);
    [5206] NMR (CD 3 OD): δ 8.39 (brd, J = 4.5 Hz, 1H), 7.84 (d, J = 9.0 Hz, 2H), 7.59 (d, J = 9.0 Hz, 2H), 7.15 (d, J = 9.0 Hz, 2H), 7.07 (d, J = 9.0 Hz, 2H), 4.35 (s, 2H), 4.01 (m, 1H), 3.86-3.73 (m, 2H), 3.53-3.41 (m, 4H), 2.91 (d, J = 4.5 Hz, 3H), 2.55-2.30 (m, 2H), 2.30-2.10 (m, 2H), 1.90-1.30 (m, 7H), 0.95 (t, J = 6.9 Hz, 3H) , 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [5207] Example 37 (82)
    [5208] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-chlorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5209]
    [5210] TLC: Rf 0.59 (CHCl 3: MeOH = 10: 1);
    [5211] NMR (CD 3 OD): δ 7.53 (d, J = 8.4 Hz, 2H), 7.38 (d, J = 9.0 Hz, 2H), 7.08 (d, J = 8.4 Hz, 2H), 7.02 (d, J = 9.0 Hz, 2H), 4.31 (s, 2H), 4.01 (m, 1H), 3.90-3.70 (m, 2H), 3.60-3.30 (m, 4H), 2.50-2.10 (m, 4H), 1.90-1 . 30 (m, 7H), 0.95 (t, J = 7.2 Hz, 3H), 0.94 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [5212] Example 37 (83)
    [5213] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (4-carboxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5214]
    [5215] TLC: Rf 0.60 (CHCl 3: MeOH = 5: 1);
    [5216] NMR (CD 3 OD): δ 8.13 (d, J = 9.0 Hz, 2H), 7.93 (s, 1H), 7.84 (m, 1H), 7.81 (d, J = 9.0 Hz, 2H), 7.66-7.56 ( m, 2H), 4.46 (s, 2H), 4.02 (dd, J = 7.5, 4.8 Hz, 1H), 3.96-3.74 (m, 2H), 3.58-3.36 (m, 4H), 2.48-2.08 (m, 4H), 1.88-1.24 (m, 7H), 0.95 (t, J = 6.9 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5217] Example 37 (84)
    [5218] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (phenylaminocarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5219]
    [5220] TLC: Rf 0.27 (CHCl 3: MeOH = 10: 1);
    [5221] NMR (CD 3 OD): δ 8.07 (d, J = 8.4 Hz, 2H), 7.74 (d, J = 8.4 Hz, 2H), 7.72-7.67 (m, 2H), 7.38 (t, J = 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 4.47 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.96-3.76 (m, 2H), 3.58-3.36 (m , 4H), 2.54-2.36 (m, 2H), 2.28-2.12 (m, 2H), 1.90-1.24 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5222] Example 37 (85)
    [5223] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylthiophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5224]
    [5225] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [5226] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.33 (d, J = 8.7 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 7.00 (d, J = 8.7 Hz, 2H), 4.34 (s, 2H), 4.02 (dd, J = 7.8, 4.5 Hz, 1H), 3.88-3.68 (m, 2H), 3.56-3.36 (m, 4H), 2.48 (s, 3H ), 2.48-2.32 (m, 2H), 2.28-2.08 (m, 2H), 1.90-1.28 (m, 7H), 0.96 (t, J = 7.2 Hz, 3H), 0.95 (d, J = 6.3 Hz, 3H), 0.94 (d, J = 6.3 Hz, 3H).
    [5227] Example 37 (86)
    [5228] (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4- (2-dimethylaminoethylaminocarbonyl) phenyloxy) phenylmethyl) -1 , 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5229]
    [5230] TLC: Rf 0.11 (CHCl 3: MeOH = 10: 1);
    [5231] NMR (CD 3 OD): δ 7.93 (d, J = 9.0 Hz, 2H), 7.64 (d, J = 8.7 Hz, 2H), 7.15 (d, J = 8.7 Hz, 2H), 7.10 (d, J = 9.0 Hz, 2H), 4.36 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.70 (m, 4H), 3.54-3.36 (m, 6H), 2.98 (s, 6H ), 2.62-2.44 (m, 2H), 2.24-2.08 (m, 2H), 1.88-1.30 (m, 7H), 0.98-0.90 (m, 9H).
    [5232] Example 37 (87)
    [5233] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-aminocarbonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5234]
    [5235] TLC: Rf 0.17 (CHCl 3: MeOH = 10: 1);
    [5236] NMR (CD 3 OD): δ 7.98 (d, J = 8.7 Hz, 2H), 7.70 (d, J = 8.7 Hz, 2H), 4.43 (s, 2H), 4.00 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.74 (m, 2H), 3.52-3.36 (m, 4H), 2.58-2.40 (m, 2H), 2.26-2.08 (m, 2H), 1.88-1.28 (m, 7H), 0.98- 0.88 (m, 9 H).
    [5237] Example 37 (88)
    [5238] (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dimethylaminocarbonylphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5239]
    [5240] TLC: Rf 0.31 (CHCl 3: MeOH = 10: 1);
    [5241] NMR (CD 3 OD): δ 7.68 (d, J = 8.1 Hz, 2H), 7.54 (d, J = 8.1 Hz, 2H), 4.41 (s, 2H), 4.01 (dd, J = 7.8, 4.8 Hz, 1H), 3.92-3.82 (m, 2H), 3.54-3.36 (m, 4H), 3.11 (s, 3H), 2.99 (s, 3H), 2.56-2.38 (m, 2H), 2.26-2.08 (m, 2H), 1.86-1.28 (m, 7H), 1.00-0.86 (m, 9H).
    [5242] Example 38
    [5243] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [5244]
    [5245] The present invention having the following physical properties by performing the same operation as in Example 35 using N- (t-butyloxycarbonyl) -L-cyclohexylalanine instead of N- (t-butyloxycarbonyl) -L-leucine The compound was obtained.
    [5246] TLC: Rf 0.35 (hexane: AcOEt = 1: 1);
    [5247] NMR (CDCl 3 ): δ 7.39-7.31 (m, 5H), 6.48 (brs, 1H), 5.16 (s, 2H), 4.15 (brs, 2H), 4.00 (ddd, J = 9.6, 4.8, 1.5 Hz, 1H), 3.76-3.16 (m, 4H), 2.02-1.12 (m, 19H), 1.08-0.88 (m, 2H), 0.92 (t, J = 7.2 Hz, 3H).
    [5248] Example 39
    [5249] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5250]
    [5251] Using the compound prepared in Example 38, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [5252] TLC: Rf 0.08 (CHCl 3: MeOH: Acetic Acid = 90: 10: 1);
    [5253] NMR (CD 3 OD): δ 4.05 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.68 (m, 2H), 3.46-3.34 (m, 4H), 2.40-2.04 (m, 4H), 1.83 -1.46 (m, 10H), 1.39 (sextet, J = 7.5 Hz, 2H), 1.33-1.15 (m, 3H), 1.05-0.86 (m, 2H), 0.97 (t, J = 7.2 Hz, 3H).
    [5254] Example 40 (1)-40 (90)
    [5255] Using the compound prepared in Example 39 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5256] Example 40 (1)
    [5257] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5258]
    [5259] TLC: Rf 0.71 (ethyl acetate);
    [5260] NMR (CD 3 OD): δ 7.50 (d, J = 8.7 Hz, 2H), 7.19 (d, J = 8.7 Hz, 2H), 7.02 (d, J = 8.7 Hz, 2H), 6.92 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.87-3.69 (m, 2H), 3.55-3.42 (m, 2H), 3.42-3.34 (m , 2H), 2.49-2.30 (m, 2H), 2.33 (s, 3H), 2.30-2.08 (m, 2H), 1.82-1.10 (m, 15H), 1.05-0.85 (m, 2H), 0.95 (t , J = 7.2 Hz, 3H).
    [5261] Example 40 (2)
    [5262] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5263]
    [5264] TLC: Rf 0.67 (ethyl acetate);
    [5265] NMR (CD 3 OD): δ 7.49 (d, J = 8.4 Hz, 2H), 7.02-6.92 (m, 6H), 4.31 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.69 (m, 2H), 3.79 (s, 3H), 3.54-3.30 (m, 4H), 2.50-2.30 (m, 2H), 2.28-2.06 (m, 2H), 1.83-1.10 (m, 15H ), 1.05-0.83 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5266] Example 40 (3)
    [5267] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5268]
    [5269] TLC: Rf 0.38 (hexane: AcOEt = 1: 1);
    [5270] NMR (CD 3 OD): δ 7.70-7.53 (m, 2H), 7.38-7.23 (m, 2H), 4.44 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.77 (m, 2H), 3.60-3.45 (m, 2H), 3.45-3.30 (m, 2H), 2.53-2.34 (m, 2H), 2.28-2.08 (m, 2H), 1.83-1.10 (m, 15H) , 1.05-0.82 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5271] Example 40 (4)
    [5272] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5273]
    [5274] TLC: Rf 0.40 (hexane: AcOEt = 1: 1);
    [5275] NMR (CD 3 OD): δ 7.57-7.48 (m, 1H), 7.44-7.37 (m, 2H), 7.30-7.21 (m, 1H), 4.38 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.55-3.33 (m, 4H), 2.56-2.37 (m, 2H), 2.25-2.04 (m, 2H), 1.82-1.08 (m, 15H) , 1.06-0.83 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5276] Example 40 (5)
    [5277] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5278]
    [5279] TLC: Rf 0.27 (hexane: AcOEt = 1: 1);
    [5280] NMR (CD 3 OD): δ 7.62 (dd, J = 8.7, 5.1 Hz, 2H), 7.23 (dd, J = 8.7, 8.7 Hz, 2H), 4.36 (s, 2H), 4.03 (dd, J = 7.8 , 4.8 Hz, 1H), 3.88-3.71 (m, 2H), 3.53-3.33 (m, 4H), 2.53-2.35 (m, 2H), 2.27-2.04 (m, 2H), 1.82-1.10 (m, 15H ), 1.05-0.82 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5281] Example 40 (6)
    [5282] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5283]
    [5284] TLC: Rf 0.60 (hexane: AcOEt = 1: 1);
    [5285] NMR (CD 3 OD): δ 7.65 (m, 1H), 7.55-7.49 (m, 3H), 4.37 (s, 2H), 4.04 (dd, J = 7.0, 4.5 Hz, 1H), 3.83 (m, 2H ), 3.54-3.47 (m, 2H), 3.41-3.35 (m, 2H), 2.38 (m, 2H), 2.18 (m, 2H), 1.78-1.47 (m, 9H), 1.42-1.17 (m, 6H) ), 0.95 (t, J = 7.5 Hz, 3H), 0.97-0.92 (m, 2H).
    [5286] Example 40 (7)
    [5287] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclohexyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5288]
    [5289] TLC: Rf 0.36 (CHCl 3: MeOH = 10: 1);
    [5290] NMR (CD 3 OD): δ 7.41 (d, J = 8.7 Hz, 2H), 7.00 (d, J = 8.7 Hz, 2H), 4.36 (m, 1H), 4.24 (s, 2H), 4.03 (dd, J = 7.8, 4.5 Hz, 1H), 3.82-3.65 (m, 2H), 3.50-3.30 (m, 4H), 2.42-2.25 (m, 2H), 2.25-2.06 (m, 2H), 2.02-1.92 ( m, 2H), 1.84-1.14 (m, 23H), 1.04-0.89 (m, 5H).
    [5291] Example 40 (8)
    [5292] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxy-3-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5293]
    [5294] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [5295] NMR (CD 3 OD): δ 7.01 (d, J = 7.8 Hz, 1H), 6.99-6.93 (m, 2H), 4.22 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.87 (s, 3H), 3.83-3.67 (m, 2H), 3.52-3.42 (m, 2H), 3.42-3.33 (m, 2H), 2.44-2.27 (m, 2H), 2.26-2.07 (m, 2H ), 1.83-1.12 (m, 15 H), 1.04-0.89 (m, 5 H).
    [5296] Example 40 (9)
    [5297] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5298]
    [5299] TLC: Rf 0.77 (CHCl 3: MeOH = 10: 1);
    [5300] NMR (CD 3 OD): δ 7.69 (dd, J = 7.5, 2.1 Hz, 1H), 7.60 (dd, J = 7.5, 2.1 Hz, 1H), 7.51 (dt, J = 2.1, 7.5 Hz, 1H), 7.47 (dt, J = 2.1, 7.5 Hz, 1H), 4.52 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 4.00-3.82 (m, 2H), 3.60-3.48 (m, 2H), 3.43-3.34 (m, 2H), 2.48-2.29 (m, 2H), 2.28-2.07 (m, 2H), 1.83-1.44 (m, 10H), 1.43-1.12 (m, 5H), 1.04- 0.88 (m, 5 H).
    [5301] Example 40 (10)
    [5302] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5303]
    [5304] TLC: Rf 0.77 (CHCl 3: MeOH = 10: 1);
    [5305] NMR (CD 3 OD): δ 7.56 (d, J = 7.2 Hz, 1H), 7.41-7.30 (m, 3H), 4.41 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.98-3.79 (m, 2H), 3.57-3.48 (m, 2H), 3.44-3.39 (m, 2H), 2.56-2.38 (m, 2H), 2.48 (s, 3H), 2.26-2.06 (m, 2H ), 1.82-1.15 (m, 15 H), 1.02-0.84 (m, 5 H).
    [5306] Example 40 (11)
    [5307] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5308]
    [5309] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [5310] NMR (CD 3 OD): δ 7.40-7.28 (m, 4H), 4.31 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.84-3.70 (m, 2H), 3.52-3.46 (m, 4H), 2.51-2.30 (m, 2H), 2.39 (s, 3H), 2.24-2.04 (m, 2H), 1.80-1.12 (m, 15H), 1.02-0.84 (m, 5H).
    [5311] Example 40 (12)
    [5312] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5313]
    [5314] TLC: Rf 0.61 (CHCl 3: MeOH = 10: 1);
    [5315] NMR (CD 3 OD): δ 7.44 (d, J = 8.4 Hz, 2H), 7.31 (d, J = 8.4 Hz, 2H), 4.31 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.88-3.70 (m, 2H), 3.52-3.36 (m, 4H), 2.48-2.30 (m, 2H), 2.38 (s, 3H), 2.30-2.08 (m, 2H), 1.81-1.1 0 (m, 15 H), 1.04-0.82 (m, 5 H).
    [5316] Example 40 (13)
    [5317] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenylthiophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5318]
    [5319] TLC: Rf 0.74 (chloroform: methanol = 10: 1);
    [5320] NMR (CD 3 OD): δ 7.50-7.37 (m, 7H), 7.29 (d, J = 8.4 Hz, 2H), 4.31 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.84-3.70 (m, 2H), 3.50-3.32 (m, 4H), 2.56-2.38 (m, 2H), 2.24-2.05 (m, 2H), 1.81-1.06 (m, 15H), 1.02-0.84 (m , 5H).
    [5321] Example 40 (14)
    [5322] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (2-methylpropyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5323]
    [5324] TLC: Rf 0.41 (CHCl 3: MeOH = 19: 1);
    [5325] NMR (CD 3 OD): δ 7.47 (d, J = 7.5 Hz, 2H), 7.29 (d, J = 7.5 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.80 (m, 2H), 3.56-3.36 (m, 4H), 2.52 (d, J = 7.2 Hz, 2H), 2.45 (m, 2H), 2.16 (m, 2H), 1.96-1.14 (m , 16H), 0.97-0.89 (m, 11H).
    [5326] Example 40 (15)
    [5327] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-butylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5328]
    [5329] TLC: Rf 0.37 (CHCl 3: MeOH = 19: 1);
    [5330] NMR (CD 3 OD): δ 7.46 (d, J = 8.4 Hz, 2H), 7.32 (d, J = 8.4 Hz, 2H), 4.31 (s, 2H), 4.03 (dd, J = 7.2, 4.8 Hz, 1H), 3.79 (m, 2H), 3.56-3.36 (m, 4H), 2.66 (t, J = 7.5 Hz, 2H), 2.41 (m, 2H), 2.16 (m, 2H), 1.82-1.20 (m , 19H), 1.00-0.89 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H), 0.93 (t, J = 7.2 Hz, 3H).
    [5331] Example 40 (16)
    [5332] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5333]
    [5334] TLC: Rf 0.63 (CHCl 3: MeOH = 10: 1);
    [5335] NMR (CD 3 OD): δ 7.46 (d, J = 8.4 Hz, 2H), 7.37 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.74 (m, 2H), 3.52-3.43 (m, 2H), 3.43-3.32 (m, 2H), 3.02-2.90 (m, 1H), 2.45-2.25 (m, 2H), 2.2 5 -2.08 (m, 2H), 1.80-1.12 (m, 21H), 1.04-0.88 (m, 5H).
    [5336] Example 40 (17)
    [5337] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxy-3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5338]
    [5339] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [5340] NMR (CD 3 OD): δ 7.40-7.31 (m, 2H), 7.22-7.17 (m, 1H), 4.30 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.90 (s , 3H), 3.86-3.70 (m, 2H), 3.50-3.38 (m, 4H), 2.52-2.32 (m, 2H), 2.26-2.05 (m, 2H), 1.80-1.15 (m, 15H), 1.01 -0.88 (m, 5 H).
    [5341] Example 40 (18)
    [5342] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-hydroxyethoxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5343]
    [5344] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5345] NMR (CD 3 OD): δ 7.47 (d, J = 8.7 Hz, 2H), 7.06 (d, J = 8.7 Hz, 2H), 4.29 (s, 2H), 4.08-4.00 (m, 3H), 3.89- 3.84 (m, 2H), 3.84-3.68 (m, 2H), 3.52-3.36 (m, 4H), 2.48-2.30 (m, 2H), 2.25-2.08 (m, 2H), 1.80-1.10 (m, 15H ), 1.04-0.86 (m, 5 H).
    [5346] Example 40 (19)
    [5347] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-hydroxy-3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5348]
    [5349] TLC: Rf 0.85 (CHCl 3: MeOH = 10: 1);
    [5350] NMR (CD 3 OD): δ 7.30-7.21 (m, 2H), 6.88 (t, J = 7.5 Hz, 1H), 4.36 (s, 2H), 4.03 (dd, J = 7.8, 4.2 Hz, 1H), 3.94-3.78 (m, 2H), 3.56-3.46 (m, 2H), 3.42-3.32 (m, 2H), 2.50-2.30 (m, 2H), 2.28 (s, 3H), 2.28-2.06 (m, 2H ), 1.82-1.01 (m, 15 H), 1.00-0.87 (m, 5H).
    [5351] Example 40 (20)
    [5352] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5353]
    [5354] TLC: Rf 0.60 (CHCl 3: MeOH = 20: 1);
    [5355] NMR (CD 3 OD): δ 7.57 (d, J = 8.7 Hz, 2H), 7.51 (d, J = 8.7 Hz, 2H), 4.36 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.89-3.71 (m, 2H), 3.53-3.33 (m, 4H), 2.52-2.32 (m, 2H), 2.26-2.07 (m, 2H), 1.83-1.06 (m, 15H), 1.04- 0.84 (m, 2H), 0.95 (t, J = 6.9 Hz, 3H).
    [5356] Example 40 (21)
    [5357] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (7-methoxy-1,3-benzodioxolan-5-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [5358]
    [5359] TLC: Rf 0.43 (CHCl 3: MeOH = 20: 1);
    [5360] NMR (CD 3 OD): δ 6.85 (s, 1H), 6.74 (s, 1H), 5.99 (s, 2H), 4.25 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.92 (s, 3H), 3.87-3.67 (m, 2H), 3.54-3.34 (m, 4H), 2.53-2.30 (m, 2H), 2.25-2.05 (m, 2H), 1.83-1.10 (m, 15H ), 1.06-0.83 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5361] Example 40 (22)
    [5362] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methyl-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5363]
    [5364] TLC: Rf 0.38 (CHCl 3: MeOH = 20: 1);
    [5365] NMR (CD 3 OD): δ 7.37-7.28 (m, 2H), 6.99 (d, J = 8.1 Hz, 1H), 4.25 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.85 (s, 3H), 3.84-3.66 (m, 2H), 3.52-3.32 (m, 4H), 2.48-2.28 (m, 2H), 2.22 (s, 3H), 2.22-2.05 (m, 2H), 1.83-1.10 (m, 15H), 1.06-0.83 (m, 2H), 0.94 (t, J = 6.9 Hz, 3H).
    [5366] Example 40 (23)
    [5367] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-fluorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5368]
    [5369] TLC: Rf 0.53 (CHCl 3: MeOH = 20: 1);
    [5370] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.18-7.00 (m, 6H), 4.33 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.87-3.69 (m, 2H), 3.55-3.32 (m, 4H), 2.52-2.32 (m, 2H), 2.28-2.08 (m, 2H), 1.83-1.12 (m, 15H), 1.06-0.83 (m , 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5371] Example 40 (24)
    [5372] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-trifluoromethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5373]
    [5374] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [5375] NMR (CD 3 OD): δ 7.72-7.69 (m, 2H), 7.41 (d, J = 7.8 Hz, 2H), 4.40 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.75 (m, 2H), 3.52-3.38 (m, 4H), 2.54-2.32 (m, 2H), 2.28-2.10 (m, 2H), 1.80-1.10 (m, 15H), 1.02-0.88 (m , 5H).
    [5376] Example 40 (25)
    [5377] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methyl-5-chloro-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [5378]
    [5379] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [5380] NMR (CD 3 OD): δ 7.56-7.50 (m, 5H), 4.33 (s, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.98-3.80 (m, 2H), 3.70-3.59 (m, 2H), 3.50-3.40 (m, 2H), 2.60-2.38 (m, 2H), 2.45 (s, 3H), 2.32-2.14 (m, 2H), 1.82-1.14 (m, 15H), 1 02-0.86 (m, 5 H).
    [5381] Example 40 (26)
    [5382] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,3-dimethyl-5-oxo-1-phenylpyrazolin-4-ylmethyl) -1,4, 9-triazaspiro [5.5] undecane dihydrochloride
    [5383]
    [5384] TLC: Rf 0.27 (CHCl 3: MeOH = 10: 1);
    [5385] NMR (CD 3 OD): δ 7.62-7.48 (m, 3H), 7.44-7.38 (m, 2H), 4.13 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.88-3.72 (m, 2H), 3.64-3.52 (m, 2H), 3.50-3.38 (m, 2H), 3.35 (s, 3H), 2.60-2.40 (m, 2H), 2.48 (s, 3H), 2.28-2.1 0 (m, 2H), 1.82-1.10 (m, 15H), 1.02-0.84 (m, 5H).
    [5386] Example 40 (27)
    [5387] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1- (2-methylpropyloxycarbonyl) indol-5-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane hydrochloride
    [5388]
    [5389] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [5390] NMR (CD 3 OD): δ 8.26 (d, J = 8.4 Hz, 1H), 7.82 (s, 1H), 7.76 (d, J = 3.6 Hz, 1H), 7.50 (dd, J = 8.4, 1.8 Hz, 1H), 6.74 (d, J = 3.6 Hz, 1H), 4.44 (s, 2H), 4.25 (d, J = 6.6 Hz, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.86- 3.72 (m, 2H), 3.52-3.40 (m, 4H), 2.52-2.36 (m, 2H), 2.25-2.06 (m, 3H), 1.80-1.10 (m, 15H), 1.07 (d, J = 9.0 Hz, 6H), 1.00-0.84 (m, 5H).
    [5391] Example 40 (28)
    [5392] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methyl-2-phenyloxazol-4-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5393]
    [5394] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5395] NMR (CD 3 OD): δ 8.04-8.00 (m, 2H), 7.51-7.49 (m, 3H), 4.34 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.98-3.82 (m, 2H), 3.70-3.60 (m, 2H), 3.44-3.38 (m, 2H), 2.52 (s, 3H), 2.50-2.36 (m, 2H), 2.28-2.12 (m, 2H), 1.80 -1.12 (m, 15 H), 1.00-0.86 (m, 5H).
    [5396] Example 40 (29)
    [5397] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylsulfonylaminophenyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5398]
    [5399] TLC: Rf 0.32 (CHCl 3: MeOH = 10: 1);
    [5400] NMR (CD 3 OD): δ 7.47 (d, J = 9.0 Hz, 2H), 7.41 (d, J = 9.0 Hz, 2H), 4.32 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.92-3.76 (m, 2H), 3.65-3.58 (m, 2H), 3.52-3.45 (m, 2H), 3.04 (s, 3H), 2.64-2.50 (m, 2H), 2.43 (s, 3H), 2.40 (s, 3H), 2.28-2.12 (m, 2H), 1.82-1.10 (m, 15H), 1.00-0.88 (m, 5H).
    [5401] Example 40 (30)
    [5402] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5403]
    [5404] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [5405] NMR (CD 3 OD): δ 7.53 (d, J = 9.0 Hz, 2H), 7.29 (d, J = 9.0 Hz, 2H), 7.08-7.00 (m, 4H), 4.33 (s, 2H), 4.03 ( dd, J = 7.5, 4.8 Hz, 1H), 3.85-3.72 (m, 2H), 3.54-3.36 (m, 4H), 2.95 (s, 3H), 2.48-2.34 (m, 2H), 2.25-2.08 ( m, 2H), 1.80-1.14 (m, 15H), 0.98-0.88 (m, 5H).
    [5406] Example 40 (31)
    [5407] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (6-methylpyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5408]
    [5409] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [5410] NMR (CD 3 OD): δ 8.58 (d, J = 2.7 Hz, 1H), 8.17 (m, 1H), 7.90 (d, J = 8.4 Hz, 1H), 7.75 (d, J = 9.0 Hz, 2H) , 7.30 (d, J = 9.0 Hz, 2H), 4.39 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.88-3.72 (m, 2H), 3.56-3.44 (m, 4H ), 2.76 (s, 3H), 2.68-2.50 (m, 2H), 2.24-2.06 (m, 2H), 1.82-1.14 (m, 15H), 1.02-0.88 (m, 5H).
    [5411] Example 40 (32)
    [5412] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (6-methylpyridin-1-oxide-3-yloxy) phenylmethyl) -1,4,9 -Triazaspiro [5.5] undecane hydrochloride
    [5413]
    [5414] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [5415] NMR (CD 3 OD): δ 8.40 (m, 1H), 7.69 (d, J = 8.4 Hz, 2H), 7.69 (m, 1H), 7.54 (m, 1H), 7.27 (d, J = 8.4 Hz, 2H), 4.39 (s, 2H), 4.04 (dd, J = 7.5, 4.8 Hz, 1H), 3.88-3.72 (m, 2H), 3.58-3.39 (m, 4H), 2.59 (s, 3H), 2.58 -2.40 (m, 2H), 2.28-2.06 (m, 2H), 1.82-1.10 (m, 15H), 1.02-0.84 (m, 5H).
    [5416] Example 40 (33)
    [5417] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5418]
    [5419] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5420] NMR (CD 3 OD): δ 7.49 (d, J = 8.4 Hz, 2H), 7.05 (d, J = 8.4 Hz, 2H), 4.63 (m, 1H), 4.27 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.97-3.90 (m, 2H), 3.84-3.66 (m, 2H), 3.62-3.52 (m, 2H), 3.50-3.38 (m, 3H), 2.5 4-2.38 (m, 2H), 2.22-1.98 (m, 4H), 1.80-1.10 (m, 18H), 1.00-0.86 (m, 5H).
    [5421] Example 40 (34)
    [5422] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-phenylpyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5423]
    [5424] TLC: Rf 0.50 (CHCl 3: MeOH = 10: 1);
    [5425] NMR (CD 3 OD): δ 9.14 (m, 1H), 8.75 (m, 1H), 8.36 (m, 1H), 8.02-7.99 (m, 2H), 7.68-7.62 (m, 3H), 4.63 (s , 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 4.02-3.94 (m, 2H), 3.64-3.42 (m, 4H), 2.72-2.56 (m, 2H), 2.25-2.06 (m , 2H), 1.80-1.10 (m, 15H), 1.00-0.86 (m, 5H).
    [5426] Example 40 (35)
    [5427] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5428]
    [5429] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [5430] NMR (CD 3 OD): δ 7.58-7.50 (m, 2H), 7.37-7.28 (m, 2H), 4.32 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.73 (m, 2H), 3.67-3.55 (m, 2H), 3.53-3.42 (m, 2H), 2.70-2.48 (m, 2H), 2.43 (s, 3H), 2.39 (s, 3H), 2.30-2.08 (m, 2H), 1.84-1.10 (m, 15H), 1.08-0.93 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5431] Example 40 (36)
    [5432] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (pyridin-2-yl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5433]
    [5434] TLC: Rf 0.60 (CHCl 3: MeOH = 10: 1);
    [5435] NMR (CD 3 OD): δ 8.53 (dd, J = 4.8, 1.5 Hz, 1H), 8.11-8.00 (m, 1H), 7.84 (d, J = 8.4 Hz, 1H), 7.49-7.41 (m, 1H ), 4.32 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.95-3.74 (m, 2H), 3.66-3.54 (m, 2H), 3.50-3.37 (m, 2H), 2.68 (s, 3H), 2.64-2.40 (m, 2H), 2.43 (s, 3H), 2.30-2.08 (m, 2H), 1.93-1.10 (m, 15H), 1.08-0.92 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5436] Example 40 (37)
    [5437] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-hydroxyphenyl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5438]
    [5439] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5440] NMR (CD 3 OD): δ 7.34 (d, J = 9.0 Hz, 2H), 6.96 (d, J = 9.0 Hz, 2H), 4.35 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.78 (m, 2H), 3.64-3.61 (m, 2H), 3.50 (t, J = 8.0 Hz, 2H), 2.68-2.56 (m, 2H), 2.49 (s, 3H), 2.3 9 (s, 3H), 2.25-2.12 (m, 2H), 1.81-1.19 (m, 15H), 0.95 (t, J = 7.5 Hz, 3H), 0.99-0.91 (m, 2H).
    [5441] Example 40 (38)
    [5442] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-carboxyethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5443]
    [5444] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5445] NMR (CD 3 OD): δ 7.46 (d, J = 8.3 Hz, 2H), 7.38 (d, J = 8.3 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.85-3.74 (m, 2H), 3.50-3.46 (m, 2H), 3.40-3.35 (m, 2H), 2.96 (t, J = 7.2 Hz, 2H), 2.62 (t, J = 7.2 Hz , 2H), 2.42-2.30 (m, 2H), 2.34-2.10 (m, 2H), 1.78-1.18 (m, 15H), 0.94 (t, J = 7.2 Hz, 3H), 0.94 (m, 2H).
    [5446] Example 40 (39)
    [5447] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-hydroxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5448]
    [5449] TLC: Rf 0.54 (CHCl 3: MeOH = 10: 1);
    [5450] NMR (CD 3 OD): δ 7.47 (d, J = 8.4 Hz, 2H), 6.97 (d, J = 8.4 Hz, 2H), 6.88 (d, J = 9.0 Hz, 2H), 6.80 (d, J = 9.0 Hz, 2H), 4.30 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.83-3.72 (m, 2H), 3.49-3.34 (m, 4H), 2.38 (m, 2H ), 2.23-2.10 (m, 2H), 1.78-1.16 (m, 15H), 1.02-0.92 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5451] Example 40 (40)
    [5452] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-carboxyphenyl) pyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [5453]
    [5454] TLC: Rf 0.25 (chloroform: methanol = 10: 1);
    [5455] NMR (CD 3 OD): δ 8.19 (d, J = 8.4 Hz, 2H), 7.61 (d, J = 8.4 Hz, 2H), 4.33 (s, 2H), 4.06 (dd, J = 7.5, 4.5 Hz, 1H), 3.93-3.80 (m, 2H), 3.61 (m, 2H), 3.43-3.38 (m, 2H), 2.44 (s, 3H), 2.40 (m, 2H), 2.39 (s, 3H), 2.21 (m, 2H), 1.75-1.18 (m, 15H), 0.96 (m, 2H), 0.96 (t, J = 7.2 Hz, 3H).
    [5456] Example 40 (41)
    [5457] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (dimethylaminosulfonyl) phenyl) pyrazol-4-ylmethyl ) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5458]
    [5459] TLC: Rf 0.54 (CHCl 3: MeOH = 9: 1);
    [5460] NMR (CD 3 OD): δ 7.96 (d, J = 8.7 Hz, 2H), 7.78 (d, J = 8.7 Hz, 2H), 4.31 (s, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.74 (m, 2H), 3.66-3.56 (m, 2H), 3.48 (m, 2H), 2.74 (s, 6H), 2.59 (m, 2H), 2.49 (s, 3H), 2.41 (s, 3H), 2.29-2.10 (m, 2H), 1.84-1.16 (m, 13H), 1.06-0.86 (m, 5H).
    [5461] Example 40 (42)
    [5462] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (5-methylpyridin-1-oxide-2-yloxy) phenylmethyl) -1,4,9 -Triazaspiro [5.5] undecane hydrochloride
    [5463]
    [5464] TLC: Rf 0.49 (CHCl 3: MeOH = 9: 1);
    [5465] NMR (CD 3 OD): δ 7.77 (brs, 1 H), 7.61 (d, J = 7.5 Hz, 2H), 7.56 (dd, J = 9.3, 2.4 Hz, 1H), 7.00 (d, J = 7.5 Hz, 2H), 6.73 (d, J = 9.3 Hz, 1H), 4.34 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.86-3.69 (m, 2H), 3.52-3.35 (m , 4H), 2.44 (m, 2H), 2.25-2.06 (m, 2H), 2.18 (s, 3H), 1.84-1.14 (m, 15H), 1.04-0.96 (m, 5H).
    [5466] Example 40 (43)
    [5467] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-carboxy-1-ethynyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5468]
    [5469] TLC: Rf 0.17 (CHCl 3: MeOH = 10: 1);
    [5470] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.70 (d, J = 15.9 Hz, 1H), 7.61 (d, J = 8.4 Hz, 2H), 6.57 (d, J = 15.9 Hz, 1H), 4.39 (s, 2H), 4.04 (dd, J = 7.2, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.58-3.36 (m, 4H), 2.50-2.32 (m , 2H), 2.28-2.08 (m, 2H), 1.92-1.10 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5471] Example 40 (44)
    [5472] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-((1E) -2-carboxy-1-ethynyl) phenyloxy) phenylmethyl)- 1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5473]
    [5474] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [5475] NMR (CD 3 OD): δ 7.69-7.63 (m, 3H), 7.57 (d, J = 8.7 Hz, 2H), 7.14 (d, J = 8.7 Hz, 2H), 7.05 (d, J = 8.4 Hz, 2H), 6.42 (d, J = 15.9 Hz, 1H), 4.36 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.74 (m, 2H), 3.55-3.36 (m , 4H), 2.50-2.30 (m, 2H), 2.30-2.08 (m, 2H), 1.82-1.10 (m, 15H), 1.02-0.88 (m, 5H).
    [5476] Example 40 (45)
    [5477] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-aminocarbonylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5478]
    [5479] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [5480] NMR (CD 3 OD): δ 7.90 (d, J = 9.0 Hz, 2H), 7.60 (d, J = 9.0 Hz, 2H), 7.15 (d, J = 9.0 Hz, 2H), 7.07 (d, J = 9.0 Hz, 2H), 4.36 (s, 2H), 4.04 (dd, J = 7.5, 4.5, Hz, 1H), 3.90-3.72 (m, 2H), 3.56-3.35 (m, 4H), 2.53-2.35 ( m, 2H), 2.28-2.08 (m, 2H), 1.84-1.13 (m, 15H), 1.06-0.86 (m, 5H).
    [5481] Example 40 (46)
    [5482] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-aminosulfonylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5483]
    [5484] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5485] NMR (d 6 -DMSO): δ 11.03 (brs, 1 H), 8.42 (brs, 1 H), 7.82 (d, J = 8.7 Hz, 2H), 7.71 (d, J = 8.7 Hz, 2H), 7.33 (brs , 2H), 7.16 (d, J = 8.7 Hz, 4H), 4.38-4.23 (m, 2H), 3.91 (m, 1H), 3.61-3.23 (m, 6H), 2.58-2.30 (m, 2H), 2.18-1.91 (m, 2H), 1.76-1.00 (m, 15H), 0.98-0.71 (m, 5H).
    [5486] Example 40 (47)
    [5487] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-benzylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane, dihydrochloride
    [5488]
    [5489] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5490] NMR (CD 3 OD): δ 7.41-7.33 (m, 3H), 7.22-7.20 (m, 2H), 5.46 (s, 2H), 4.31 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz , 1H), 3.88-3.74 (m, 2H), 3.58-3.48 (m, 4H), 2.61 (m, 2H), 2.47 (s, 6H), 2.24-2.09 (m, 2H), 1.80-1.16 (m , 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [5491] Example 40 (48)
    [5492] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (2,4-difluorophenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5493]
    [5494] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5495] NMR (CD 3 OD): δ 7.58-7.51 (m, 1 H), 7.33-7.25 (m, 1 H), 7.22-7.16 (m, 1 H), 4.31 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.91-3.78 (m, 2H), 3.59 (m, 2H), 3.44 (m, 2H), 2.49 (m, 2H), 2.38 (s, 3H), 2.28 (s, 3H), 2.27-2.15 (m, 2H), 1.81-1.16 (m, 15H), 0.96 (t, J = 7.0 Hz, 3H), 0.96 (m, 2H).
    [5496] Example 40 (49)
    [5497] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (pyrrolidin-1-ylmethyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [5498]
    [5499] TLC: Rf 0.14 (CHCl 3: MeOH = 10: 1);
    [5500] NMR (CD 3 OD): δ 7.74 (d, J = 8.4 Hz, 2H), 7.65 (d, J = 8.4 Hz, 2H), 4.43 (s, 2H), 4.40 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.70 (m, 2H), 3.56-3.38 (m, 6H), 3.28-3.10 (m, 2H), 2.66-2.48 (m, 2H), 2.26-1.92 ( m, 6H), 1.83-1.10 (m, 15H), 1.06-0.83 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5501] Example 40 (50)
    [5502] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (morphon-4-ylsulfonyl) phenyl) pyrazole-4 -Ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5503]
    [5504] TLC: Rf 0.46 (CHCl 3: MeOH = 20: 1);
    [5505] NMR (CD 3 OD): δ 7.95 (d, J = 8.7 Hz, 2H), 7.80 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.05 (dd, J = 7.8, 4.5 Hz, 1H), 3.94-3.74 (m, 2H), 3.76-3.67 (m, 4H), 3.66-3.56 (m, 2H), 3.56-3.42 (m, 2H), 3.10-2.92 (m, 4H), 2.68- 2.50 (m, 2H), 2.50 (s, 3H), 2.42 (s, 3H), 2.30-2.08 (m, 2H), 1.84-1.08 (m, 15H), 1.08-0.83 (m, 2H), 0.95 ( t, J = 7.2 Hz, 3H).
    [5506] Example 40 (51)
    [5507] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-cyanophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5508]
    [5509] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5510] NMR (CD 3 OD): δ 7.75 (d, J = 9.3 Hz, 2H), 7.64 (d, J = 9.0 Hz, 2H), 7.22 (d, J = 9.0 Hz, 2H), 7.14 (d, J = 9.3 Hz, 2H), 4.40 (s, 2H), 4.05 (dd, J = 7.5, 4.8 Hz, 1H), 3.92-3.74 (m, 2H), 3.58-3.36 (m, 4H), 2.52-2.36 (m , 2H), 2.32-2.08 (m, 2H), 1.84-1.12 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5511] Example 40 (52)
    [5512] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (N- (2-hydroxyethyl) -N-methylamino Sulfonyl) phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5513]
    [5514] TLC: Rf 0.68 (CHCl 3: MeOH = 5: 1);
    [5515] NMR (CD 3 OD): δ 8.00 (d, J = 8.7 Hz, 2H), 7.78 (d, J = 8.7 Hz, 2H), 4.33 (s, 2H), 4.06 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.76 (m, 2H), 3.70 (t, J = 5.7 Hz, 2H), 3.68-3.60 (m, 2H), 3.58-3.42 (m, 2H), 3.20 (t, J = 5.7 Hz , 2H), 2.88 (s, 3H), 2.72-2.58 (m, 2H), 2.50 (s, 3H), 2.44 (s, 3H), 2.28-2.06 (m, 2H), 1.82-1.10 (m, 15H ), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5516] Example 40 (53)
    [5517] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (2-phenylethyl) pyrazol-4-ylmethyl) -1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [5518]
    [5519] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [5520] NMR (CD 3 OD): δ 7.28-7.23 (m, 3H), 7.10-7.07 (m, 2H), 4.40 (t, J = 6.6 Hz, 2H), 4.19 (s, 2H), 4.06 (dd, J = 7.2, 4.8 Hz, 1H), 3.80-3.60 (m, 2H), 3.58-3.36 (m, 4H), 3.12 (t, J = 6.6 Hz, 2H), 2.64-2.45 (m, 2H), 2.45 ( s, 3H), 2.26-2.04 (m, 2H), 1.95 (s, 3H), 1.84-1.14 (m, 15H), 0.97 (t, J = 7.5 Hz, 3H), 0.97 (m, 2H).
    [5521] Example 40 (54)
    [5522] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylaminomethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5523]
    [5524] TLC: Rf 0.16 (CHCl 3: MeOH = 10: 1);
    [5525] NMR (CD 3 OD): δ 7.76 (d, J = 8.1 Hz, 2H), 7.63 (d, J = 8.1 Hz, 2H), 4.41 (s, 2H), 4.37 (s, 2H), 4.03 (dd, J = 7.8, 5.1 Hz, 1H), 3.90-3.75 (m, 2H), 3.52-3.38 (m, 4H), 2.87 (s, 6H), 2.64-2.48 (m, 2H), 2.22-2.04 (m, 2H), 1.80-1.15 (m, 15H), 1.00-0.86 (m, 5H).
    [5526] Example 40 (55)
    [5527] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (4-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5528]
    [5529] TLC: Rf 0.58 (CHCl 3: MeOH = 10: 1);
    [5530] NMR (CD 3 OD): δ 7.81 (s, 1H), 7.69 (d, J = 7.5 Hz, 1H), 7.54 (d, J = 9.0 Hz, 2H), 7.55-7.48 (m, 1H), 7.45 ( d, J = 7.5 Hz, 1H), 6.87 (d, J = 9.0 Hz, 2H), 4.40 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.92-3.73 (m, 2H ), 3.58-3.43 (m, 2H), 3.43-3.32 (m, 2H), 2.55-2.35 (m, 2H), 2.28-2.06 (m, 2H), 1.82-1.10 (m, 15H), 1.08-0.83 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5531] Example 40 (56)
    [5532] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (quinoxalin-2-yl) pyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5533]
    [5534] TLC: Rf 0.67 (CHCl 3: MeOH = 10: 1);
    [5535] NMR (CD 3 OD): δ 9.51 (s, 1H), 8.13 (d, J = 8.0 Hz, 1H), 8.05 (d, J = 8.0 Hz, 1H), 7.91-7.80 (m, 2H), 4.38 ( s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.82 (m, 2H), 3.63 (m, 2H), 3.42 (m, 2H), 2.92 (s, 3H), 2.47 (s, 3H), 2.47 (m, 2H), 2.29-2.16 (m, 2H), 1.80-1.18 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [5536] Example 40 (57)
    [5537] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylcarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5538]
    [5539] TLC: Rf 0.68 (CHCl 3: MeOH = 10: 1);
    [5540] NMR (CD 3 OD): δ 7.87 (d, J = 8.4 Hz, 2H), 7.82-7.74 (m, 4H), 7.67 (t, J = 8.4 Hz, 1H), 7.57-7.51 (m, 2H), 4.48 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.78 (m, 2H), 3.58-3.38 (m, 4H), 2.58-2.40 (m, 2H), 2.30- 2.10 (m, 2 H), 1.82-1.14 (m, 15 H), 1.02-0.86 (m, 5H).
    [5541] Example 40 (58)
    [5542] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylaminosulfonylphenyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane, dihydrochloride
    [5543]
    [5544] TLC: Rf 0.30 (CHCl 3: MeOH = 10: 1);
    [5545] NMR (CD 3 OD): δ 8.01 (d, J = 8.7 Hz, 2H), 7.74 (d, J = 8.7 Hz, 2H), 4.33 (s, 2H), 4.06 (dd, J = 7.8, 4.5 Hz, 1H), 3.86-3.78 (m, 2H), 3.68-3.58 (m, 2H), 3.52-3.36 (m, 2H), 2.59 (s, 3H), 2.59-2.38 (m, 2H), 2.48 (s, 3H), 2.41 (s, 3H), 2.34-2.10 (m, 2H), 1.84-1.16 (m, 15H), 0.97 (t, J = 7.2 Hz, 3H), 0.97 (m, 2H).
    [5546] Example 40 (59)
    [5547] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,3,5-trimethylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [5548]
    [5549] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5550] NMR (CD 3 OD): δ 4.28 (s, 2H), 4.03 (dd, J = 7.8, 4.5 Hz, 1H), 3.87 (s, 3H), 3.87-3.69 (m, 2H), 3.61-3.43 (m , 4H), 2.69-2.50 (m, 2H), 2.46 (s, 3H), 2.44 (s, 3H), 2.25-2.06 (m, 2H), 1.83-1.12 (m, 15H), 1.05-0.86 (m , 5H).
    [5551] Example 40 (60)
    [5552] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (morpholin-4-ylmethyl) phenylmethyl) -1,4,9-triazaspiro [5.5 Undecane Dihydrochloride
    [5553]
    [5554] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [5555] NMR (CD 3 OD): δ 7.74 (d, J = 8.4 Hz, 2H), 7.66 (d, J = 8.4 Hz, 2H), 4.40 (s, 4H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 4.00-3.70 (m, 6H), 3.54-3.40 (m, 4H), 3.35-3.18 (m, 4H), 2.63-2.47 (m, 2H), 2.24-2.02 (m, 2H), 1.83- 1.12 (m, 15 H), 1.06-0.85 (m, 5H).
    [5556] Example 40 (61)
    [5557] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5558]
    [5559] TLC: Rf 0.57 (CHCl 3: MeOH = 10: 1);
    [5560] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.28 (t, J = 8.4 Hz, 1H), 7.07 (d, J = 8.7 Hz, 2H), 6.75 (ddd, J = 8.4, 2.4, 1.0 Hz, 1H), 6.61-6.57 (m, 2H), 4.34 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.85-3.55 (m, 2H), 3.77 (s, 3H), 3.53-3.47 (m, 2H), 3.40 (m, 2H), 2.50-2.35 (m, 2H), 2.25-2.11 (m, 2H), 1.80-1.23 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [5561] Example 40 (62)
    [5562] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylpiperazin-1-ylmethyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane trihydrochloride
    [5563]
    [5564] TLC: Rf 0.69 (CHCl 3: MeOH = 5: 1);
    [5565] NMR (CD 3 OD): δ 7.74 (s, 4H), 4.54 (s, 2H), 4.41 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.87-3.42 (m, 14H ), 3.00 (s, 3H), 2.61-2.46 (m, 2H), 2.21-2.07 (m, 2H), 1.79-1.15 (m, 15H), 1.02-0.92 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5566] Example 40 (63)
    [5567] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (pyridine-1-oxide-3-yloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5568]
    [5569] TLC: Rf 0.42 (CHCl 3: MeOH = 9: 1);
    [5570] NMR (CD 3 OD): δ 8.45 (t, J = 1.8 Hz, 1H), 8.37 (brd, J = 6.3 Hz, 1H), 7.71 (dd, J = 8.4, 6.3 Hz, 1H), 7.72 (d, J = 8.7 Hz, 2H), 7.59 (brdd, J = 8.4, 1.8 Hz, 1H), 7.31 (d, J = 8.7 Hz, 2H), 4.40 (s, 2H), 4.04 (dd, J = 7.8 Hz, 1H), 3.90-3.74 (m, 2H), 3.57-3.40 (m, 4H), 2.58-2.40 (m, 2H), 2.28-2.08 (m, 2H), 1.82-1.14 (m, 15H), 1.04- 0.90 (m, 5 H).
    [5571] Example 40 (64)
    [5572] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenylsulfonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5573]
    [5574] TLC: Rf 0.77 (ethyl acetate: methanol = 9: 1);
    [5575] NMR (CD 3 OD): δ 8.08 (d, J = 8.4 Hz, 2H), 8.02-7.96 (m, 2H), 7.80 (d, J = 8.4 Hz, 2H), 7.70-7.55 (m, 3H), 4.43 (s, 2H), 4.02 (dd, J = 7.8, 4.8 Hz, 1H), 3.89-3.73 (m, 2H), 3.49-3.34 (m, 4H), 2.48-2.33 (m, 2H), 2.23- 2.04 (m, 2H), 1.82-1.14 (m, 15H), 1.03-0.85 (m, 5H).
    [5576] Example 40 (65)
    [5577] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-cyclohexylpyrazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] undecane, dihydrochloride
    [5578]
    [5579] TLC: Rf 0.32 (ethyl acetate: methanol = 9: 1);
    [5580] NMR (CD 3 OD): δ 4.42-4.28 (m, 1H), 4.28 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.72 (m, 2H), 3.60-3.43 (m, 4H), 2.68-2.50 (m, 2H), 2.50 (s, 3H), 2.46 (s, 3H), 2.25-2.06 (m, 2H), 2.04-1.15 (m, 25H), 1.05-0.89 (m, 5 H).
    [5581] Example 40 (66)
    [5582] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5583]
    [5584] TLC: Rf 0.16 (ethyl acetate: methanol = 9: 1);
    [5585] NMR (CD 3 OD): δ 7.83 (ddd, J = 7.8, 1.5, 1.2 Hz, 1H), 7.60 (dd, J = 2.4, 1.5 Hz, 1H), 7.57 (d, J = 8.7 Hz, 2H), 7.51 (t, J = 7.8 Hz, 1H), 7.29 (ddd, J = 7.8, 2.4, 1.2 Hz, 1H), 7.12 (d, J = 8.7 Hz, 2H), 4.35 (s, 2H), 4.04 (dd , J = 7.5, 4.5 Hz, 1H), 3.90-3.74 (m, 2H), 3.58-3.35 (m, 4H), 2.49-2.34 (m, 2H), 2.28-2.09 (m, 2H), 1.93-1.10 (m, 15 H), 1.07-0.85 (m, 5 H).
    [5586] Example 40 (67)
    [5587] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (piperidin-1-ylmethyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [5588]
    [5589] TLC: Rf 0.56 (CHCl 3: MeOH = 9: 1);
    [5590] NMR (CD 3 OD): δ 7.75 (d, J = 8.4 Hz, 2H), 7.64 (d, J = 8.4 Hz, 2H), 4.40 (s, 2H), 4.34 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.90-3.72 (m, 2H), 3.53-3.38 (m, 6H), 3.05-2.91 (m, 2H), 2.66-2.49 (m, 2H), 2.24-2.04 ( m, 2H), 2.00-1.13 (m, 21H), 1.04-0.86 (m, 5H).
    [5591] Example 40 (68)
    [5592] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (pyrrolidin-1-ylsulfonyl) phenyl) pyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5593]
    [5594] TLC: Rf 0.40 (ethyl acetate: methanol = 9: 1);
    [5595] NMR (CD 3 OD): δ 8.01 (d, J = 8.7 Hz, 2H), 7.76 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.75 (m, 2H), 3.66-3.56 (m, 2H), 3.49-3.41 (m, 2H), 3.32-3.25 (m, 4H), 2.60-2.46 (m, 2H), 2.48 ( s, 3H), 2.40 (s, 3H), 2.30-2.11 (m, 2H), 1.83-1.14 (m, 19H), 1.05-0.87 (m, 5H).
    [5596] Example 40 (69)
    [5597] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,3-dihydrobenzofuran-5-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Hydrochloride
    [5598]
    [5599] TLC: Rf 0.61 (ethyl acetate: methanol = 9: 1);
    [5600] NMR (CD 3 OD): δ 7.39 (d, J = 1.8 Hz, 1H), 7.26 (dd, J = 8.4, 1.8 Hz, 1H), 6.81 (d, J = 8.4 Hz, 1H), 4.59 (t, J = 8.7 Hz, 2H), 4.26 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.67 (m, 2H), 3.54-3.34 (m, 4H), 3.25 (t , J = 8.7 Hz, 2H), 2.48-2.31 (m, 2H), 2.26-2.07 (m, 2H), 1.83-1.14 (m, 15H), 1.04-0.87 (m, 5H).
    [5601] Example 40 (70)
    [5602] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5603]
    [5604] TLC: Rf 0.55 (ethyl acetate: methanol = 9: 1);
    [5605] NMR (CD 3 OD): δ 8.04 (d, J = 8.7 Hz, 2H), 7.61 (d, J = 8.7 Hz, 2H), 7.18 (d, J = 8.7 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 4.38 (s, 2H), 4.05 (dd, J = 7.8, 4.8 Hz, 1H), 3.91-3.74 (m, 2H), 3.57-3.35 (m, 4H), 2.50-2.33 (m , 2H), 2.29-2.09 (m, 2H), 1.84-1.14 (m, 15H), 1.05-0.86 (m, 5H).
    [5606] Example 40 (71)
    [5607] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (2-hydroxyethylaminosulfonyl) phenyl) pyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5608]
    [5609] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [5610] NMR (CD 3 OD): δ 8.03 (d, J = 8.7 Hz, 2H), 7.72 (d, J = 8.7 Hz, 2H), 4.31 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.94-3.74 (m, 2H), 3.66-3.56 (m, 2H), 3.56 (t, J = 5.7 Hz, 2H), 3.51-3.41 (m, 2H), 3.01 (t, J = 5.7 Hz , 2H), 2.63-2.43 (m, 2H), 2.47 (s, 3H), 2.40 (s, 3H), 2.32-2.10 (m, 2H), 1.93-1.10 (m, 15H), 1.06-0.93 (m , 2H), 0.96 (t, J = 7.2 Hz, 3H).
    [5611] Example 40 (72)
    [5612] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (2-dimethylaminoethylaminosulfonyl) phenyl) pyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane trihydrochloride
    [5613]
    [5614] TLC: Rf 0.13 (CHCl 3: MeOH = 10: 1);
    [5615] NMR (CD 3 OD): δ 8.07 (d, J = 8.7 Hz, 2H), 7.79 (d, J = 8.7 Hz, 2H), 4.31 (s, 2H), 4.04 (dd, J = 7.5, 4.2 Hz, 1H), 3.82-3.76 (m, 2H), 3.68-3.48 (m, 4H), 3.34-3.24 (m, 4H), 2.95 (s, 6H), 2.76-2.52 (m, 2H), 2.50 (s, 3H), 2.43 (s, 3H), 2.25-2.08 (m, 2H), 1.82-1.14 (m, 15H), 1.02-0.88 (m, 5H).
    [5616] Example 40 (73)
    [5617] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (1-hydroxy-1-phenylmethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5618]
    [5619] TLC: Rf 0.30 (CHCl 3: MeOH = 10: 1);
    [5620] NMR (CD 3 OD): δ 7.62-7.18 (m, 9H), 5.82 (s, 1H), 4.34 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.88-3.72 (m , 2H), 3.58-3.30 (m, 4H), 2.42-2.04 (m, 4H), 1.82-1.24 (m, 15H), 0.94 (t, J = 7.2 Hz, 3H), 0.94 (m, 2H).
    [5621] Example 40 (74)
    [5622] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (carboxymethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5623]
    [5624] TLC: Rf 0.30 (CHCl 3: MeOH = 10: 1);
    [5625] NMR (CD 3 OD): δ 7.47 (d, J = 8.7 Hz, 2H), 7.04 (d, J = 8.7 Hz, 2H), 4.70 (s, 2H), 4.29 (s, 2H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.69 (m, 2H), 3.54-3.33 (m, 4H), 2.44-2.28 (m, 2H), 2.26-2.06 (m, 2H), 1.83-1.12 ( m, 15H), 1.04-0.85 (m, 5H).
    [5626] Example 40 (75)
    [5627] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-hydroxypiperidin-1-ylmethyl) phenylmethyl) -1,4,9- Triaza spiro [5.5] undecane dihydrochloride
    [5628]
    [5629] TLC: Rf 0.17 (CHCl 3: MeOH = 10: 1);
    [5630] NMR (CD 3 OD): δ 7.76 (d, J = 7.8 Hz, 2H), 7.70-7.61 (m, 2H), 4.40 (s, 2H), 4.38-4.32 (m, 2H), 4.10-4.05 (m , 1H), 4.03 (dd, J = 7.5, 4.5 Hz, 1H), 3.90-3.68 (m, 2H), 3.56-3.40 (m, 4H), 3.18-3.00 (m, 1H), 2.70-2.48 (m , 2H), 2.23-1.82 (m, 5H), 1.82-1.10 (m, 19H), 1.06-0.83 (m, 2H), 0.94 (t, J = 7.2 Hz, 3H).
    [5631] Example 40 (76)
    [5632] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-carboxyphenylmethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5633]
    [5634] TLC: Rf 0.57 (CHCl 3: MeOH = 5: 1);
    [5635] NMR (CD 3 OD): δ 8.10 (s, 1H), 7.98 (d, J = 7.8 Hz, 1H), 7.68 (d, J = 7.8 Hz, 1H), 7.50 (t, J = 7.8 Hz, 1H) , 7.46 (d, J = 8.7 Hz, 2H), 7.13 (d, J = 8.7 Hz, 2H), 5.22 (s, 2H), 4.28 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.84-3.68 (m, 2H), 3.52-3.32 (m, 4H), 2.42-2.08 (m, 4H), 1.82-1.16 (m, 15H), 0.95 (t, J = 7.8 Hz, 3H) , 0.95 (m, 2 H).
    [5636] Example 40 (77)
    [5637] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (1,4-benzodioxane-6-yloxy) phenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [5638]
    [5639] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [5640] NMR (CD 3 OD): δ 7.48 (d, J = 9.0 Hz, 2H), 7.02 (d, J = 9.0 Hz, 2H), 6.86 (m, 1H), 6.55-6.51 (m, 2H), 4.31 ( s, 2H), 4.24 (s, 4H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.70 (m, 2H), 3.58-3.36 (m, 4H), 2.42-2.08 (m, 4H), 1.82-1.12 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5641] Example 40 (78)
    [5642] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (3-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5643]
    [5644] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [5645] NMR (CD 3 OD): δ 7.81 (s, 1H), 7.74 (m, 1H), 7.60-7.50 (m, 2H), 7.28 (m, 1H), 7.15-7.08 (m, 2H), 6.82 (m , 1H), 4.43 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.78 (m, 2H), 3.58-3.34 (m, 4H), 2.48-2.08 (m, 4H ), 1.84-1.12 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [5646] Example 40 (79)
    [5647] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (methylsulfonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5648]
    [5649] TLC: Rf 0.40 (CHCl 3: MeOH = 10: 1);
    [5650] NMR (CD 3 OD): δ 7.53 (d, J = 8.4 Hz, 2H), 7.34 (d, J = 8.4 Hz, 2H), 4.32 (s, 2H), 4.03 (dd, J = 7.8, 4.8 Hz, 1H), 3.86-3.72 (m, 2H), 3.52-3.34 (m, 4H), 3.01 (s, 3H), 2.50-2.32 (m, 2H), 2.24-2.06 (m, 2H), 1.82-1.10 ( m, 15H), 1.02-0.86 (m, 5H).
    [5651] Example 40 (80)
    [5652] (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6- (4-methoxyphenyl) pyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5653]
    [5654] TLC: Rf 0.67 (CHCl 3: MeOH = 10: 1);
    [5655] NMR (CD 3 OD): δ 8.26 (m, 1H), 8.02 (m, 1H), 7.08-6.84 (m, 5H), 4.38 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H ), 3.90-3.72 (m, 2H), 3.81 (s, 3H), 3.56-3.44 (m, 2H), 3.42-3.32 (m, 2H), 2.50-2.30 (m, 2H), 2.30-2.08 (m) , 2H), 1.82-1.14 (m, 15H), 1.02-0.88 (m, 5H).
    [5656] Example 40 (81)
    [5657] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylaminocarbonylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5658]
    [5659] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [5660] NMR (CD 3 OD): δ 8.39 (br d, J = 4.5 Hz, 1H), 7.84 (d, J = 9.0 Hz, 2H), 7.58 (d, J = 8.4 Hz, 2H), 7.15 (d, J = 8.4 Hz, 2H), 7.07 (d, J = 9.0 Hz, 2H), 4.35 (s, 2H), 4.04 (m, 1H), 3.85-3.74 (m, 2H), 3.53-3.38 (m, 4H) , 2.91 (d, J = 4.5 Hz, 3H), 2.55-2.30 (m, 2H), 2.30-2.10 (m, 2H), 1.80-1.10 (m, 15H), 1.10-0.90 (m, 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5661] Example 40 (82)
    [5662] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-chlorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5663]
    [5664] TLC: Rf 0.76 (CHCl 3: MeOH = 10: 1);
    [5665] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.38 (d, J = 9.0 Hz, 2H), 7.09 (d, J = 9.0 Hz, 2H), 7.02 (d, J = 9.0 Hz, 2H), 4.32 (s, 2H), 4.04 (m, 1H), 3.90-3.70 (m, 2H), 3.60-3.30 (m, 4H), 2.50-2.10 (m, 4H), 1.90-1 . 10 (m, 15H), 1.10-0.90 (m, 2H), 0.95 (t, J = 7.5 Hz, 3H).
    [5666] Example 40 (83)
    [5667] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-bis (methylsulfonyl) aminophenylmethyl) -1,4,9-triazaspiro [5.5] Can hydrochloride
    [5668]
    [5669] TLC: Rf 0.60 (CHCl 3: MeOH = 5: 1);
    [5670] NMR (CD 3 OD): δ 7.69 (d, J = 8.4 Hz, 2H), 7.60 (d, J = 8.4 Hz, 2H), 4.41 (s, 2H), 4.05 (dd, J = 7.8, 4.8 Hz, 1H), 3.92-3.70 (m, 2H), 3.56-3.36 (m, 4H), 3.47 (s, 6H), 2.46-2.08 (m, 4H), 1.84-1.16 (m, 15H), 0.96 (t, J = 7.5 Hz, 3H), 0.96 (m, 2H).
    [5671] Example 40 (84)
    [5672] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (4-carboxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5673]
    [5674] TLC: Rf 0.60 (CHCl 3: MeOH = 5: 1);
    [5675] NMR (CD 3 OD): δ 8.13 (d, J = 9.0 Hz, 2H), 7.95 (s, 1H), 7.84 (m, 1H), 7.82 (d, J = 9.0 Hz, 2H), 7.66-7.61 ( m, 2H), 4.46 (s, 2H), 4.04 (dd, J = 7.5, 4.5 Hz, 1H), 3.96-3.78 (m, 2H), 3.62-3.36 (m, 4H), 2.54-2.32 (m, 2H), 2.28-2.08 (m, 2H), 1.82-1.08 (m, 15H), 0.95 (t, J = 7.2 Hz, 3H), 0.95 (m, 2H).
    [5676] Example 40 (85)
    [5677] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylaminocarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5678]
    [5679] TLC: Rf 0.25 (chloroform: methanol = 10: 1);
    [5680] NMR (CD 3 OD): δ 8.07 (d, J = 8.1 Hz, 2H), 7.73-7.67 (m, 2H), 7.71 (d, J = 8.1 Hz, 2H), 7.38 (t, J = 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 4.45 (s, 2H), 4.05 (dd, J = 7.8, 4.8 Hz, 1H), 3.92-3.72 (m, 2H), 3.58-3.36 (m , 4H), 2.50-2.08 (m, 4H), 1.84-1.08 (m, 15H), 0.96 (t, J = 7.8 Hz, 3H), 0.96 (m, 2H).
    [5681] Example 40 (86)
    [5682] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylthiophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecane hydrochloride
    [5683]
    [5684] TLC: Rf 0.48 (CHCl 3: MeOH = 10: 1);
    [5685] NMR (CD 3 OD): δ 7.54 (d, J = 8.7 Hz, 2H), 7.33 (d, J = 8.7 Hz, 2H), 7.06 (d, J = 8.7 Hz, 2H), 7.00 (d, J = 8.7 Hz, 2H), 4.34 (s, 2H), 4.05 (dd, J = 7.5, 4.5 Hz, 1H), 3.86-3.70 (m, 2H), 3.56-3.36 (m, 4H), 2.48 (s, 3H ), 2.48-2.32 (m, 2H), 2.28-2.08 (m, 2H), 1.82-1.14 (m, 15H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5686] Example 40 (87)
    [5687] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4- (2-dimethylaminoethylaminocarbonyl) phenyloxy) phenylmethyl) -1,4, 9-triazaspiro [5.5] undecane hydrochloride
    [5688]
    [5689] TLC: Rf 0.11 (CHCl 3: MeOH = 10: 1);
    [5690] NMR (CD 3 OD): δ 7.94 (d, J = 9.0 Hz, 2H), 7.64 (d, J = 8.7 Hz, 2H), 7.15 (d, J = 8.7 Hz, 2H), 7.10 (d, J = 9.0 Hz, 2H), 4.36 (s, 2H), 4.04 (dd, J = 7.8, 4.8 Hz, 1H), 3.88-3.72 (m, 4H), 3.52-3.36 (m, 6H), 2.98 (s, 6H ), 2.62-2.44 (m, 2H), 2.24-2.08 (m, 2H), 1.80-1.10 (m, 15H), 1.00-0.88 (m, 5H).
    [5691] Example 40 (88)
    [5692] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-aminocarbonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5693]
    [5694] TLC: Rf 0.19 (CHCl 3: MeOH = 10: 1);
    [5695] NMR (CD 3 OD): δ 7.98 (d, J = 8.4 Hz, 2H), 7.68 (d, J = 8.4 Hz, 2H), 4.43 (s, 2H), 4.03 (dd, J = 7.5, 4.8 Hz, 1H), 3.92-3.76 (m, 2H), 3.54-3.28 (m, 4H), 2.52-2.36 (m, 2H), 2.24-2.08 (m, 2H), 1.82-1.10 (m, 15H), 1.02- 0.88 (m, 5 H).
    [5696] Example 40 (89)
    [5697] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylaminocarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5698]
    [5699] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5700] NMR (CD 3 OD): δ 7.67 (d, J = 8.1 Hz, 2H), 7.54 (d, J = 8.1 Hz, 2H), 4.41 (s, 2H), 4.04 (dd, J = 7.5, 4.2 Hz, 1H), 3.92-3.76 (m, 2H), 3.54-3.32 (m, 4H), 3.11 (s, 3H), 2.99 (s, 3H), 2.52-2.32 (m, 2H), 2.26-2.08 (m, 2H), 1.82-1.10 (m, 15 H), 1.02-0.86 (m, 5H).
    [5701] Example 40 (90)
    [5702] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [5703]
    [5704] TLC: Rf 0.73 (CHCl 3: MeOH = 10: 1);
    [5705] NMR (CDCl 3 ): δ 7.37-7.25 (m, 4H), 7.10 (m, 1H), 7.04-6.98 (m, 2H), 6.96 (d, J = 8.7 Hz, 2H), 5.81 (brs, 1H) , 3.99 (m, 1H), 3.52 (s, 2H), 3.52-3.32 (m, 2H), 2.92-2.74 (m, 3H), 2.57 (dt, J = 12.0, 3.0 Hz, 1H), 2.18-1.88 (m, 5H), 1.76-1.13 (m, 14H), 1.07-0.88 (m, 2H), 0.93 (t, J = 7.5 Hz, 3H).
    [5706] Example 41
    [5707] Resin (3), N-allyloxycarbonyl-4-piperidone, n-butylamine and (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino prepared in Reference Example 2 The same procedure as in Reference Example 3-Reference Example 4 using -3-hydroxy-4-methylpentanoic acid, and Reference Example 5-> Reference Example 6 using 1,4-benzodioxane-6-carboxyaldehyde → The same operations as in Example 1 were carried out to obtain the following compounds (1) and (2) of the present invention, respectively.
    [5708] Example 41 (1)
    [5709] 1-butyl-2,5-dioxo-3- (1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5710]
    [5711] In the above formula, * indicates that the syn and anti bodies are mixed in a ratio of 2: 3.
    [5712] TLC: Rf 0.47 (CHCl 3: MeOH = 10: 1);
    [5713] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.4, 2.1 Hz, 1H), 6.93 (d, J = 8.4 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.13 (d, J = 2.1 Hz, 0.6H), 4.08 (d, J = 1.2 Hz, 0.4H), 4.05-3.90 (m, 1H), 3.76-3.63 (m , 1H), 3.62-3.35 (m, 3.4H), 3.19 (dd, J = 9.6, 2.1 Hz, 0.6H), 3.20-3.10 (m, 1H), 2.55-2.33 (m, 2H), 2.30-1.95 (m, 3H), 1.80-1.60 (m, 1H), 1.55-1.25 (m, 3H), 1.05-0.89 (m, 9H).
    [5714] Example 41 (2)
    [5715] (Z) -1-Butyl-2,5-dioxo-3- (2-methylpropylidene) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triaza Spiro [5.5] undecane hydrochloride
    [5716]
    [5717] TLC: Rf 0.52 (CHCl 3: MeOH = 20: 1);
    [5718] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.4, 2.1 Hz, 1H), 6.93 (d, J = 8.4 Hz, 1H), 5.84 (d, J = 10.5 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 3.72-3.55 (m, 2H), 3.53-3.35 (m, 4H), 2.80-2.60 (m, 1H), 2.43 -2.26 (m, 2H), 2.25-2.15 (m, 2H), 1.62-1.48 (m, 2H), 1.45-1.30 (m, 2H), 1.04 (d, J = 6.6 Hz, 6H), 0.95 (t , J = 7.5 Hz, 3H).
    [5719] Example 41 (3) -41 (5)
    [5720] Compound corresponding to instead of (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid is 1,4-benzodioxane-6- The compound of the present invention was obtained in the same manner as in Example 41 using the compound corresponding to carboxyaldehyde.
    [5721] Example 41 (3)
    [5722] (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxyethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] undecane hydrochloride
    [5723]
    [5724] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [5725] NMR (CD 3 OD): δ 7.54 (d, J = 8.7 Hz, 2H), 7.43-7.35 (m, 2H), 7.21-7.14 (m, 1H), 7.08-7.00 (m, 4H), 4.32 (s , 2H), 4.19 (dq, J = 1.5, 6.9 Hz, 1H), 4.10-3.97 (m, 1H), 3.78 (d, J = 1.5 Hz, 1H), 3.72-3.51 (m, 2H), 3.51- 3.40 (m, 2H), 3.28-3.14 (m, 1H), 2.57-2.42 (m, 2H), 2.40-2.25 (m, 1H), 2.21-2.10 (m, 1H), 1.81-1.60 (m, 1H ), 1.50-1.30 (m, 3H), 1.22 (d, J = 6.9 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [5726] Example 41 (4)
    [5727] (Z) -1-butyl-2,5-dioxo-3-ethylidene-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5728]
    [5729] TLC: Rf 0.29 (CHCl 3: MeOH = 20: 1);
    [5730] NMR (CD 3 OD): δ 7.53 (d, J = 9.0 Hz, 2H), 7.43-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.09-7.00 (m, 4H), 6.08 (q, J = 7.5 Hz, 1H), 4.33 (s, 2H), 3.76-3.61 (m, 2H), 3.57-3.40 (m, 4H), 2.45-2.30 (m, 2H), 2.28-2.15 ( m, 2H), 1.77 (d, J = 7.5 Hz, 3H), 1.62-1.46 (m, 2H), 1.44-1.28 (m, 2H), 0.96 (t, J = 7.5 Hz, 3H).
    [5731] Example 41 (5)
    [5732] (Z) -1-butyl-2,5-dioxo-3- (2-methylpropylidene) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5733]
    [5734] TLC: Rf 0.42 (CHCl 3: MeOH = 20: 1);
    [5735] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.43-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.06 (d, J = 8.7 Hz, 2H), 7.08-7.01 (m, 2H), 5.85 (d, J = 10.5 Hz, 1H), 4.34 (s, 2H), 3.78-3.64 (m, 2H), 3.57-3.40 (m, 4H), 2.78 -2.62 (m, 1H), 2.43-2.18 (m, 4H), 1.62-1.48 (m, 2H), 1.46-1.30 (m, 2H), 1.04 (d, J = 6.6 Hz, 6H), 0.96 (t , J = 7.5 Hz, 3H).
    [5736] Example 42
    [5737] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [5738]
    [5739] (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid instead of N- (t-butyloxycarbonyl) -L-leucine Using the same operation as in Example 35, the compound of the present invention having the following physical properties was obtained.
    [5740] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5741] NMR (CD 3 OD): δ 7.39-7.30 (m, 5H), 5.13 (br, 2H), 4.12 (d, J = 2.5 Hz, 1H), 4.10-4.00 (m, 2H), 3.76-3.50 (m , 2H), 3.39-3.25 (m, 2H), 3.10-2.94 (m, 1H), 2.18 (m, 1H), 2.08-1.83 (m, 4H), 1.70-1.56 (m, 1H), 1.45-1.15 (m, 3 H), 1.01-0.89 (m, 9 H).
    [5742] Example 43
    [5743] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5744]
    [5745] Using the compound prepared in Example 42, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [5746] TLC: Rf 0.08 (CHCl 3: MeOH = 10: 1);
    [5747] NMR (CD 3 OD): δ 4.15 (d, J = 2.0 Hz, 1H), 3.96 (dt, J = 13.0, 4.0 Hz, 1H), 3.71 (dt, J = 13.0, 4.0 Hz, 1H), 3.57- 3.47 (m, 1H), 3.40-3.34 (m, 2H), 3.23-3.12 (m, 2H), 2.47-2.30 (m, 2H), 2.25-1.98 (m, 3H), 1.79-1.66 (m, 1H ), 1.52-1.28 (m, 3H), 1.07-0.94 (m, 9H).
    [5748] Example 44 (1) -44 (13)
    [5749] Using the compound prepared in Example 43 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5750] Example 44 (1)
    [5751] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5752]
    [5753] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [5754] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.44-7.35 (m, 2H), 7.18 (t, J = 7.5 Hz, 1H), 7.10-7.00 (m, 4H), 4.33 (s, 2H), 4.14 (d, J = 2.1 Hz, 1H), 4.06-3.93 (m, 1H), 3.80-3.67 (m, 1H), 3.56-3.40 (m, 3H), 3.19 (dd, J = 9.3, 2.1 Hz, 1H), 3.20-3.10 (m, 1H), 2.53-2.35 (m, 2H), 2.35-2.20 (m, 1H), 2.19-2.08 (m, 1H), 2.07-1.91 ( m, 1H), 1.80-1.70 (m, 1H), 1.50-1.25 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t , J = 7.2 Hz, 3H).
    [5755] Example 44 (2)
    [5756] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5757]
    [5758] TLC: Rf 0.38 (CHCl 3: MeOH = 10: 1);
    [5759] NMR (CD 3 OD): δ 7.60-7.45 (m, 5H), 4.30 (s, 2H), 4.15 (d, J = 2.4 Hz, 1H), 4.05 (m, 1H), 3.79 (m, 1H), 3.62-3.48 (m, 3H), 3.29-3.16 (m, 2H), 2.60-2.45 (m, 2H), 2.44-2.30 (m, 7H), 2.17 (m, 1H), 2.01 (m, 1H), 1.70 (m, 1 H), 1.51-1.31 (m, 3H), 1.03-0.91 (m, 9H).
    [5760] Example 44 (3)
    [5761] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (6-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5762]
    [5763] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [5764] NMR (CD 3 OD): δ 8.39 (d, J = 2.1 Hz, 1H), 8.16 (dd, J = 8.4, 2.1 Hz, 1H), 7.46 (t, J = 7.8 Hz, 2H), 7.29 (t, J = 7.8Hz, 1H), 7.17 (d, J = 7.8Hz, 2H), 7.08 (d, J = 8.4Hz, 1H), 4.40 (s, 2H), 4.13 (d, J = 2.1 Hz, 1H) , 4.07-3.94 (m, 1H), 3.83-3.69 (m, 1H), 3.60-3.42 (m, 3H), 3.29-3.22 (m, 1H), 3.19 (dd, J = 9.6, 2.1 Hz, 1H) , 2.62-2.32 (m, 3H), 2.18-2.07 (m, 1H), 2.06-1.94 (m, 1H), 1.78-1.60 (m, 1H), 1.50-1.31 (m, 3H), 1.07-0.87 ( m, 9H).
    [5765] Example 44 (4)
    [5766] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5767]
    [5768] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [5769] NMR (CD 3 OD): δ 7.47 (d, J = 8.7 Hz, 2H), 7.20 (d, J = 8.7 Hz, 2H), 7.02 (d, J = 8.7 Hz, 2H), 6.92 (d, J = 8.7 Hz, 2H), 4.29 (s, 2H), 4.14 (d, J = 2.1 Hz, 1H), 3.97 (m, 1H), 3.72 (m, 1H), 3.56-3.39 (m, 2H), 3.25- 3.09 (m, 3H), 2.53-2.08 (m, 7H), 2.01 (m, 1H), 1.70 (m, 1H), 1.48-1.28 (m, 3H), 1.05-0.88 (m, 9H).
    [5770] Example 44 (5)
    [5771] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4-cyclohexyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5772]
    [5773] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5774] NMR (CD 3 OD): δ 7.40 (d, J = 8.7 Hz, 2H), 7.00 (d, J = 8.7 Hz, 2H), 4.37 (m, 1H), 4.24 (brs, 2H), 4.13 (d, J = 2.1 Hz, 1H), 3.94 (m, 1H), 3.68 (m, 1H), 3.52-3.34 (m, 2H), 3.29-3.07 (m, 3H), 2.52-1.92 (m, 7H), 1.8 5-1.27 (m, 12 H), 1.04-0.89 (m, 9 H).
    [5775] Example 44 (6)
    [5776] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5777]
    [5778] TLC: Rf 0.20 (ethyl acetate: methanol = 10: 1);
    [5779] NMR (CD 3 OD): δ 7.45 (d, J = 8.7 Hz, 2H), 7.06 (d, J = 8.7 Hz, 2H), 4.67-4.59 (m, 1H), 4.28 (s, 2H), 4.13 ( d, J = 2.5 Hz, 1H), 4.00-3.90 (m, 3H), 3.75-3.67 (m, 1H), 3.63-3.53 (m, 2H), 3.50-3.41 (m, 3H), 3.18 (dd, J = 9.0, 2.0 Hz, 1H), 3.18 (m, 1H), 2.49-1.96 (m, 7H), 1.77-1.65 (m, 3H), 1.44-1.30 (m, 3H), 0.98 (d, J = 6.5 Hz, 3H), 0.96 (d, J = 6.5 Hz, 3H), 0.94 (t, J = 7.2 Hz, 3H).
    [5780] Example 44 (7)
    [5781] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4- (pyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5782]
    [5783] TLC: Rf 0.22 (ethyl acetate: methanol = 10: 1);
    [5784] NMR (CD 3 OD): δ 8.76 (d, J = 2.5 Hz, 1H), 8.63 (d, J = 6.0 Hz, 1H), 8.29 (dd, J = 9.0, 2.5 Hz, 1H), 8.08 (dd, J = 9.0, 6.0 Hz, 1H), 7.77 (d, J = 9.0 Hz, 2H), 7.35 (d, J = 9.0 Hz, 2H), 4.41 (s, 2H), 4.14 (d, J = 2.0 Hz , 1H), 4.00 (m, 1H), 3.76 (m, 1H), 3.61-3.47 (m, 3H), 3.20 (dd, J = 9.5, 2.0 Hz, 1H), 3.20 (m, 1H), 2.62 ( m, 1H), 2.46 (m, 2H), 2.10 (m, 1H), 2.05-1.95 (m, 1H), 1.69 (m, 1H), 1.41-1.35 (m, 3H), 0.99 (d, J = 6.5 Hz, 3H), 0.97 (d, J = 6.5 Hz, 3H), 0.95 (t, J = 7.5 Hz, 3H).
    [5785] Example 44 (8)
    [5786] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5787]
    [5788] TLC: Rf 0.55 (CHCl 3: MeOH = 10: 1);
    [5789] NMR (CD 3 OD): δ 7.47 (d, J = 8.1 Hz, 2H), 7.37 (d, J = 8.1 Hz, 2H), 4.31 (s, 2H), 4.13 (d, J = 2.1 Hz, 1H) , 4.05-3.91 (m, 1H), 3.80-3.65 (m, 1H), 3.57-3.38 (m, 3H), 3.26-3.13 (m, 1H), 3.19 (dd, J = 9.3, 2.1 Hz, 1H) , 3.03-2.86 (m, 1H), 2.53-2.38 (m, 2H), 2.38-2.23 (m, 1H), 2.16-2.05 (m, 1H), 2.06-1.92 (m, 1H), 1.77-1.56 ( m, 1H), 1.49-1.26 (m, 3H), 1.25 (d, J = 6.9 Hz, 6H), 0.98 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.94 (t, J = 7.2 Hz, 3H).
    [5790] Example 44 (9)
    [5791] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5792]
    [5793] TLC: Rf 0.49 (CHCl 3: MeOH = 10: 1);
    [5794] NMR (CD 3 OD): δ 7.40 (s, 4H), 4.33 (s, 2H), 4.15 (d, J = 2.1 Hz, 1H), 4.11-3.97 (m, 1H), 3.86-3.72 (m, 1H ), 3.64-3.50 (m, 3H), 3.39-3.30 (m, 1H), 3.21 (dd, J = 9.3, 2.1 Hz, 1H), 2.72-2.55 (m, 1H), 2.53-2.40 (m, 2H) ), 2.46 (s, 3H), 2.44 (s, 3H), 2.40 (s, 3H), 2.18-2.07 (m, 1H), 2.07-1.96 (m, 1H), 1.78-1.60 (m, 1H), 1.50-1.30 (m, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [5795] Example 44 (10)
    [5796] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3-methyl-5-chloro-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5797]
    [5798] TLC: Rf 0.56 (CHCl 3: MeOH = 10: 1);
    [5799] NMR (CD 3 OD): δ 7.58-7.47 (m, 5H), 4.33 (s, 2H), 4.15 (d, J = 2.1 Hz, 1H), 4.15-4.02 (m, 1H), 3.89-3.75 (m , 1H), 3.65-3.48 (m, 3H), 3.30-3.20 (m, 1H), 3.20 (dd, J = 9.6, 2.1 Hz, 1H), 2.64-2.46 (m, 2H), 2.44 (s, 3H ), 2.44-2.32 (m, 1H), 2.21-2.10 (m, 1H), 2.08-1.93 (m, 1H), 1.80-1.60 (m, 1H), 1.52-1.30 (m, 3H), 0.99 (d , J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 7.2 Hz, 3H).
    [5800] Example 44 (11)
    [5801] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4- (4-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5802]
    [5803] TLC: Rf 0.29 (CHCl 3: MeOH = 10: 1);
    [5804] NMR (CD 3 OD): δ 8.04 (d, J = 9.0 Hz, 2H), 7.60 (d, J = 8.7 Hz, 2H), 7.18 (d, J = 8.7 Hz, 2H), 7.07 (d, J = 9.0 Hz, 2H), 4.37 (s, 2H), 4.14 (d, J = 2.1 Hz, 1H), 4.10-3.94 (m, 1H), 3.83-3.69 (m, 1H), 3.59-3.40 (m, 3H ), 3.25-3.12 (m, 1H), 3.19 (dd, J = 9.3, 2.1 Hz, 1H), 2.55-2.37 (m, 2H), 2.37-2.22 (m, 1H), 2.19-2.08 (m, 1H) ), 2.08-1.94 (m, 1H), 1.79-1.60 (m, 1H), 1.52-1.26 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [5805] Example 44 (12)
    [5806] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- (pyridin-2-yl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [ 5.5] undecane dihydrochloride
    [5807]
    [5808] TLC: Rf 0.28 (CHCl 3: MeOH = 10: 1);
    [5809] NMR (CD 3 OD): δ 8.53 (d, J = 5.1 Hz, 1H), 8.05 (t, J = 7.8 Hz, 1H), 7.81 (d, J = 7.8 Hz, 1H), 7.44 (dd, J = 7.8, 5.1 Hz, 1H), 4.33 (s, 2H), 4.16 (d, J = 2.1 Hz, 1H), 4.06 (m, 1H), 3.78 (m, 1H), 3.62-3.44 (m, 3H), 3.26 (m, 1H), 3.21 (dd, J = 9.6, 2.1 Hz, 1H), 2.68 (s, 3H), 2.60-2.30 (m, 3H), 2.42 (s, 3H), 2.16 (m, 1H) , 2.02 (m, 1H), 1.72 (m, 1H), 1.50-1.26 (m, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.96 ( t, J = 7.2 Hz, 3H).
    [5810] Example 44 (13)
    [5811] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- (4-carboxyphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Dihydrochloride
    [5812]
    [5813] TLC: Rf 0.25 (chloroform: methanol: acetic acid = 20: 2: 1);
    [5814] NMR (CD 3 OD): δ 8.19 (d, J = 8.7 Hz, 2H), 7.62 (d, J = 8.7 Hz, 2H), 4.32 (s, 2H), 4.16 (d, J = 2.1 Hz, 1H) , 4.12-3.98 (m, 1H), 3.87-3.74 (m, 1H), 3.63-3.45 (m, 3H), 3.30-3.10 (m, 1H), 3.20 (dd, J = 9.3, 2.1 Hz, 1H) , 2.59-2.48 (m, 2H), 2.44 (s, 3H), 2.40-2.23 (m, 1H), 2.39 (s, 3H), 2.23-2.10 (m, 1H), 2.10-1.96 (m, 1H) , 1.80-1.62 (m, 1H), 1.52-1.24 (m, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 7.2 Hz, 3H).
    [5815] Example 45
    [5816] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [5817]
    [5818] (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-3-cyclohexylpropanoic acid instead of N- (t-butyloxycarbonyl) -L-leucine Using the same operation as in Example 35, the compound of the present invention having the following physical property values was obtained.
    [5819] TLC: Rf 0.53 (CHCl 3: MeOH = 10: 1);
    [5820] NMR (CD 3 OD): δ 7.39-7.27 (m, 5H), 5.13 (m, 2H), 4.13 (d, J = 2.5 Hz, 1H), 4.06-4.02 (m, 2H), 3.78-3.48 (m , 2H), 3.36-3.29 (m, 2H), 3.02 (br, 1H), 2.17 (m, 1H), 2.03-1.58 (m, 10H), 1.47-1.13 (m, 6H), 1.02-0.89 (m , 5H).
    [5821] Example 46
    [5822] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [5823]
    [5824] Using the compound prepared in Example 45, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [5825] TLC: Rf 0.33 (CHCl 3: MeOH: Acetic Acid = 20: 6: 1);
    [5826] NMR (CD 3 OD): δ 4.13 (d, J = 2.5 Hz, 1H), 3.48-3.22 (m, 5H), 2.97-2.89 (m, 2H), 2.12-1.65 (m, 10H), 1.56-1.16 (m, 7 H), 1.03-0.85 (m, 5 H).
    [5827] Example 47 (1) -47 (8)
    [5828] Using the compound prepared in Example 46 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5829] Example 47 (1)
    [5830] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5831]
    [5832] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [5833] NMR (CD 3 OD): δ 7.55-7.51 (m, 2H), 7.42-7.36 (m, 2H), 7.18 (tt, J = 7.5, 1.0 Hz, 1H), 7.08-7.01 (m, 4H), 4.32 (s, 2H), 4.15 (d, J = 2.0 Hz, 1H), 3.98 (dt, J = 3.5, 12.5 Hz, 1H), 3.73 (dt, J = 3.5, 12.5 Hz, 1H), 3. 57-3.39 (m, 3H), 3.26 (d, J = 2.0 Hz, 1H), 3.20 (m, 1H), 2.52-2.39 (m, 2H), 2.30 (m, 1H), 2.12 (d, J = 15.5 Hz, 1H), 2.04-1.92 (m, 2H), 1.80-1.62 (m, 5H), 1.48-1.11 (m, 6H), 1.01-0.82 (m, 5H).
    [5834] Example 47 (2)
    [5835] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5836]
    [5837] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [5838] NMR (CD 3 OD): δ 7.60-7.50 (m, 5H), 4.33 (s, 2H), 4.17 (d, J = 2.5 Hz, 1H), 4.04 (m, 1H), 3.85-3.75 (m, 1H ), 3.61-3.51 (m, 3H), 3.35-3.27 (m, 2H), 2.62 (m, 1H), 2.49-2.44 (m, 5H), 2.41 (s, 3H), 2.15 (m, 1H), 2.05-1.92 (m, 2H), 1.77-1.65 (m, 5H), 1.44-1.15 (m, 6H), 1.01-0.85 (m, 5H).
    [5839] Example 47 (3)
    [5840] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5841]
    [5842] TLC: Rf 0.69 (CHCl 3: MeOH = 10: 1);
    [5843] NMR (CD 3 OD): δ 7.48 (d, J = 8.4 Hz, 2H), 7.36 (d, J = 8.4 Hz, 2H), 4.31 (s, 2H), 4.14 (d, J = 2.1 Hz, 1H) , 3.98 (m, 1H), 3.72 (m, 1H), 3.55-3.40 (m, 3H), 3.29-3.16 (m, 2H), 2.95 (m, 1H), 2.52-2.24 (m, 3H), 2.15 -1.86 (m, 3H), 1.80-1.60 (m, 5H), 1.48-1.10 (m, 6H), 1.25 (d, J = 6.9 Hz, 6H), 1.02-0.82 (m, 5H).
    [5844] Example 47 (4)
    [5845] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4- (6-methylpyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane Hydrochloride
    [5846]
    [5847] TLC: Rf 0.51 (ethyl acetate: methanol = 10: 1);
    [5848] NMR (CD 3 OD): δ 8.59 (d, J = 2.7 Hz, 1H), 8.19 (dd, J = 9.0, 2.7 Hz, 1H), 7.91 (d, J = 9.0 Hz, 1H), 7.75 (d, J = 8.4 Hz, 2H), 7.30 (d, J = 8.4 Hz, 2H), 4.39 (s, 2H), 4.15 (d, J = 2.0 Hz, 1H), 3.99 (m, 1H), 3.73 (m, 1H), 3.61-3.46 (m, 3H), 3.37-3.26 (m, 2H), 2.77 (s, 3H), 2.62 (m, 1H), 2.45 (m, 1H), 2.13-1.92 (m, 3H) , 1.73 (m, 4H), 1.40-1.14 (m, 8H), 1.01-0.86 (m, 2H), 0.95 (t, J = 7.0 Hz, 3H).
    [5849] Example 47 (5)
    [5850] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5851]
    [5852] TLC: Rf 0.49 (ethyl acetate: methanol = 10: 1);
    [5853] NMR (CD 3 OD): δ 7.57 (m, 2H), 7.37-7.31 (m, 2H), 4.32 (s, 2H), 4.16 (d, J = 2.0 Hz, 1H), 4.08-4.00 (m, 1H ), 3.79 (m, 1H), 3.63-3.52 (m, 3H), 3.37-3.27 (m, 2H), 2.65 (m, 1H), 2.48 (m, 1H), 2.45 (s, 3H), 2.39 ( s, 3H), 2.16-1.92 (m, 3H), 1.73 (m, 4H), 1.42-1.15 (m, 8H), 1.01-0.88 (m, 2H), 0.95 (t, J = 7.0 Hz, 3H) .
    [5854] Example 47 (6)
    [5855] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5856]
    [5857] TLC: Rf 0.25 (chloroform: methanol = 10: 1);
    [5858] NMR (CD 3 OD): δ 7.47 (d, J = 9.0 Hz, 2H), 7.00 (d, J = 9.0 Hz, 2H), 6.99-6.92 (m, 4H), 4.30 (s, 2H), 4.16 ( d, J = 2.1 Hz, 1H), 3.98 (m, 1H), 3.80 (s, 3H), 3.72 (m, 1H), 3.58-3.38 (m, 3H), 3.30-3.08 (m, 2H), 2.54 -1.88 (m, 6H), 1.82-1.60 (m, 5H), 1.50-1.10 (m, 6H), 0.96 (t, J = 7.5 Hz, 3H), 0.96 (m, 2H).
    [5859] Example 47 (7)
    [5860] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-fluorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5861]
    [5862] TLC: Rf 0.28 (CHCl 3: MeOH = 10: 1);
    [5863] NMR (CD 3 OD): δ 7.51 (d, J = 8.7 Hz, 2H), 7.13 (d, J = 8.7 Hz, 2H), 7.10-7.04 (m, 4H), 4.33 (s, 2H), 4.16 ( d, J = 2.1 Hz, 1H), 4.00 (m, 1H), 3.72 (m, 1H), 3.58-3.40 (m, 3H), 3.30-3.08 (m, 2H), 2.56-1.88 (m, 6H) , 1.82-1.60 (m, 5H), 1.54-1.10 (m, 6H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5864] Example 47 (8)
    [5865] (3R * ) -1-butyl-2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5866]
    [5867] TLC: Rf 0.52 (ethyl acetate: methanol = 10: 1);
    [5868] NMR (CD 3 OD): δ 7.53 (d, J = 8.1 Hz, 2H), 7.30 (d, J = 9.0 Hz, 2H), 7.08 (d, J = 8.1 Hz, 2H), 7.04 (d, J = 9.0 Hz, 2H), 4.34 (s, 2H), 4.16 (d, J = 2.1 Hz, 1H), 4.00 (m, 1H), 3.76 (m, 1H), 3.58-3.42 (m, 3H), 3.30- 3.08 (m, 2H), 2.96 (s, 3H), 2.54-1.88 (m, 6H), 1.82-1.62 (m, 5H), 1.50-1.14 (m, 6H), 0.96 (t, J = 7.2 Hz, 3H), 0.96 (m, 2H).
    [5869] Example 48
    [5870] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9-allyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane
    [5871]
    [5872] Resin (3) prepared in Reference Example 2, N-allyloxycarbonyl-4-piperidone, 2-butynylamine, (2R * , 3R * )-N- (t-butyloxycarbonyl) -2- In the same manner as in Reference Example 3-Reference Example 6-Example 1 using amino-3-hydroxy-3-cyclohexylpropanoic acid, the compound of the present invention having the following physical properties was obtained.
    [5873] TLC: Rf 0.32 (CHCl 3: MeOH = 15: 1);
    [5874] NMR (CD 3 OD): δ 6.04-5.91 (m, 1H), 5.35-5.27 (m, 1H), 5.23-5.19 (m, 1H), 4.60-4.58 (m, 2H), 4.27 (dq, J = 17.5, 2.5 Hz, 1H), 4.19 (d, J = 2.5 Hz, 1H), 4.07-4.01 (m, 2H), 3.89 (dq, J = 17.5, 2.5 Hz, 1H), 3.75-3.50 (m, 2H ), 3.38 (dd, J = 9.0, 2.5 Hz, 1H), 2.32-2.17 (m, 2H), 2.07-1.70 (m, 11H), 1.33-1.14 (m, 3H), 1.00-0.85 (m, 2H) ).
    [5875] Example 49
    [5876] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [5877]
    [5878] Using the compound prepared in Example 48, the same operation as in Reference Example 4 was carried out to obtain a compound of the present invention having the following physical properties.
    [5879] TLC: Rf 0.33 (CHCl 3: MeOH: Acetic Acid = 20: 6: 1);
    [5880] NMR (CD 3 OD): δ 4.28 (dq, J = 17.5, 2.5 Hz, 1H), 4.18 (d, J = 2.5 Hz, 1H), 4.03 (dq, J = 17.5, 2.5 Hz, 1H), 3.48- 3.29 (m, 3H), 2.99-2.90 (m, 2H), 2.26-1.73 (m, 14H), 1.32-1.18 (m, 3H), 1.01-0.91 (m, 2H).
    [5881] Example 50 (1)-50 (6)
    [5882] Using the compound prepared in Example 49 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5883] Example 50 (1)
    [5884] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5885]
    [5886] TLC: Rf 0.37 (CHCl 3: MeOH = 10: 1);
    [5887] NMR (CD 3 OD): δ 7.60-7.50 (m, 5H), 4.42-4.33 (m, 3H), 4.21 (d, J = 2.5 Hz, 1H), 4.08-3.99 (m, 2H), 3.85-3.75 (m, 1H), 3.65-3.57 (m, 2H), 3.32 (m, 1H), 2.79 (m, 1H), 2.48-2.43 (m, 5H), 2.40 (s, 3H), 2.22 (m, 1H ), 2.05-1.93 (m, 2H), 1.80-1.64 (m, 7H), 1.39-1.11 (m, 3H), 1.03-0.84 (m, 2H).
    [5888] Example 50 (2)
    [5889] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5 Undecane Dihydrochloride
    [5890]
    [5891] TLC: Rf 0.35 (CHCl 3: MeOH = 10: 1);
    [5892] NMR (CD 3 OD): δ 7.40 (s, 4H), 4.45-4.30 (m, 3H), 4.20 (m, 1H), 4.16-3.98 (m, 2H), 3.78 (m, 1H), 3.68-3.56 (m, 2H), 3.30 (m, 1H), 2.82 (m, 1H), 2.56-2.42 (m, 8H), 2.39 (s, 3H), 2.28-1.88 (m, 3H), 1.80-1.60 (m , 7H), 1.40-1.10 (m, 3H), 1.12-0.82 (m, 2H).
    [5893] Example 50 (3)
    [5894] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5895]
    [5896] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5897] NMR (CD 3 OD): δ 7.47 (d, J = 8.1 Hz, 2H), 7.36 (d, J = 8.1 Hz, 2H), 4.38-4.28 (m, 3H), 4.17 (m, 1H), 4.04- 3.88 (m, 2H), 3.74 (m, 1H), 3.50-3.40 (m, 2H), 3.28 (m, 1H), 2.92 (m, 1H), 2.64 (m, 1H), 2.50-1.86 (m, 5H), 1.80-1.62 (m, 7H), 1.36-1.04 (m, 3H), 1.25 (d, J = 7.2 Hz, 6H), 1.00-0.82 (m, 2H).
    [5898] Example 50 (4)
    [5899] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5900]
    [5901] TLC: Rf 0.39 (CHCl 3: MeOH = 10: 1);
    [5902] NMR (CD 3 OD): δ 7.53 (d, J = 9.0 Hz, 2H), 7.42-7.37 (m, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.06-7.02 (m, 4H), 4.40-4.30 (m, 3H), 4.18 (m, 1H), 4.04-3.90 (m, 2H), 3.72 (m, 1H), 3.30-3.20 (m, 2H), 3.28 (m, 1H), 2.68 ( m, 1H), 2.52-1.86 (m, 5H), 1.80-1.60 (m, 7H), 1.38-1.10 (m, 3H), 1.02-0.82 (m, 2H).
    [5903] Example 50 (5)
    [5904] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5905]
    [5906] TLC: Rf 0.45 (CHCl 3: MeOH = 10: 1);
    [5907] NMR (CD 3 OD): δ 7.50 (d, J = 8.4 Hz, 2H), 7.20 (d, J = 8.7 Hz, 2H), 7.01 (d, J = 8.7 Hz, 2H), 6.92 (d, J = 8.4 Hz, 2H), 4.40-4.28 (m, 3H), 4.18 (m, 1H), 4.04-3.88 (m, 2H), 3.74 (m, 1H), 3.52-3.40 (m, 2H), 3.26 (m , 1H), 2.64 (m, 1H), 2.54-1.86 (m, 5H), 2.33 (s, 3H), 1.80-1.62 (m, 7H), 1.38-1.10 (m, 3H), 1.02-0.82 (m , 2H).
    [5908] Example 50 (6)
    [5909] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-1-cyclohexylmethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5910]
    [5911] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5912] NMR (CD 3 OD): δ 7.04 (s, 1H), 6.99-6.91 (m, 2H), 4.35 (m, 1H), 4.27 (s, 4H), 4.24 (s, 2H), 4.18 (m, 1H ), 4.04-3.84 (m, 2H), 3.70 (m, 1H), 3.56-3.38 (m, 2H), 3.28 (m, 1H), 2.68-1.88 (m, 6H), 1.80-1.60 (m, 7H) ), 1.4 0-1.10 (m, 3H), 1.02-0.80 (m, 2H).
    [5913] Example 51
    [5914] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane acetate
    [5915]
    [5916] (2R * , 3R * )-N- (t-butyl instead of (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-3-cyclohexylpropanoic acid Using the oxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid, the same procedure as in Example 48-49 was carried out to obtain the compound of the present invention having the following physical properties.
    [5917] TLC: Rf 0.22 (CHCl 3: MeOH: Acetic Acid = 20: 6: 1);
    [5918] NMR (CD 3 OD): δ 4.36 (dq, J = 17.0, 2.5 Hz, 1H), 4.19 (d, J = 2.0 Hz, 1H), 3.95-3.79 (m, 2H), 3.62 (dt, J = 3.5 , 13.0 Hz, 1H), 3.34-3.26 (m, 2H), 3.22 (dd, J = 9.5, 2.0 Hz, 1H), 2.54-2.43 (m, 1H), 2.37 (m, 1H), 2.20-1.98 ( m, 3H), 1.91 (s, 3H), 1.75 (t, J = 2.5 Hz, 3H), 1.01-0.97 (m, 6H).
    [5919] Example 52 (1) -52 (5)
    [5920] Using the compound prepared in Example 51 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5921] Example 52 (1)
    [5922] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecane dihydrochloride
    [5923]
    [5924] TLC: Rf 0.28 (CHCl 3: MeOH = 10: 1);
    [5925] NMR (CD 3 OD): δ 7.38 (d, J = 3.9 Hz, 2H), 7.35 (d, J = 3.9 Hz, 2H), 4.33 (s, 2H), 4.20 (d, J = 2.1 Hz, 1H) , 4.10-3.90 (m, 2H), 3.78 (m, 1H), 3.68-3.52 (m, 2H), 3.22 (dd, J = 9.3, 2.1 Hz, 1H), 2.74 (m, 1H), 2.54-2.20 (m, 3H), 2.44 (s, 3H), 2.40 (s, 3H), 2.36 (s, 3H), 1.98 (m, 1H), 1.75 (t, J = 2.1 Hz, 3H), 1.01 (d, J = 6.6 Hz, 3H), 0.99 (d, J = 6.6 Hz, 3H).
    [5926] Example 52 (2)
    [5927] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5928]
    [5929] TLC: Rf 0.26 (CHCl 3: MeOH = 10: 1);
    [5930] NMR (CD 3 OD): δ 7.49 (d, J = 9.0 Hz, 2H), 7.21 (d, J = 8.4 Hz, 2H), 7.04 (d, J = 9.0 Hz, 2H), 6.93 (d, J = 8.4 Hz, 2H), 4.40 (m, 1H), 4.34 (s, 2H), 4.19 (d, J = 2.1 Hz, 1H), 4.08-3.82 (m, 2H), 3.76 (m, 1H), 3.58- 3.40 (m, 2H), 3.20 (dd, J = 9.6, 2.1 Hz, 1H), 2.72-2.42 (m, 2H), 2.35 (s, 3H), 2.35-2.18 (m, 2H), 2.00 (m, 1H), 1.74 (t, J = 2.1 Hz, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H).
    [5931] Example 52 (3)
    [5932] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5933]
    [5934] TLC: Rf 0.34 (CHCl 3: MeOH = 10: 1);
    [5935] NMR (CD 3 OD): δ 7.06-6.92 (m, 3H), 4.38 (m, 1H), 4.28 (s, 4H), 4.25 (s, 2H), 4.19 (d, J = 2.1 Hz, 1H), 4.02-3.84 (m, 2H), 3.70 (m, 1H), 3.52-3.36 (m, 2H), 3.20 (dd, J = 9.6, 2.1 Hz, 1H), 2.60 (m, 1H), 2.48 (m, 1H), 2.32-2.16 (m, 2H), 2.00 (m, 1H), 1.74 (t, J = 2.1 Hz, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H).
    [5936] Example 52 (4)
    [5937] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5938]
    [5939] TLC: Rf 0.29 (CHCl 3: MeOH = 10: 1);
    [5940] NMR (CD 3 OD): δ 7.47 (d, J = 8.1 Hz, 2H), 7.38 (d, J = 8.1 Hz, 2H), 4.40 (m, 1H), 4.33 (s, 2H), 4.19 (d, J = 2.1 Hz, 1H), 4.08-3.84 (m, 2H), 3.76 (m, 1H), 3.52-3.40 (m, 2H), 3.20 (dd, J = 9.6, 2.1 Hz, 1H), 2.96 (m , 1H), 2.62 (m, 1H), 2.48 (m, 1H), 2.36-2.12 (m, 2H), 2.00 (m, 1H), 1.74 (t, J = 2.1 Hz, 3H), 1.24 (d, J = 7.2 Hz, 6H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H).
    [5941] Example 52 (5)
    [5942] (3R * ) -1- (2-butynyl) -2,5-dioxo-3-((1R * ) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5943]
    [5944] TLC: Rf 0.24 (CHCl 3: MeOH = 10: 1);
    [5945] NMR (CD 3 OD): δ 7.52 (d, J = 9.0 Hz, 2H), 7.41 (t, J = 7.2 Hz, 2H), 7.19 (t, J = 7.2 Hz, 1H), 7.09-7.03 (m, 4H), 4.40 (m, 1H), 4.35 (s, 2H), 4.19 (d, J = 2.1 Hz, 1H), 4.08-3.84 (m, 2H), 3.78 (m, 1H), 3.58-3.42 (m , 2H), 3.21 (dd, J = 9.6, 2.1 Hz, 1H), 2.72-2.42 (m, 2H), 2.38-2.18 (m, 2H), 2.00 (m, 1H), 1.74 (t, J = 2.1 Hz, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H).
    [5946] Example 53
    [5947] (3R * ) -1-butyl-2,5-dioxo-3-((1S * ) -1-hydroxy-1-cyclohexylmethyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane
    [5948]
    [5949] Resin (3) prepared in Reference Example 2, N-benzyl-4-piperidone, n-butylamine, (2R * , 3S * )-N- (t-butyloxycarbonyl) -2-amino-3- The compound of the present invention having the following physical properties was obtained in the same manner as in Reference Example 3-Reference Example 6-Example 1 using hydroxy-3-cyclohexylpropanoic acid.
    [5950] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [5951] NMR (CD 3 OD): δ 7.40-7.20 (m, 5H), 4.04 (d, J = 1.5 Hz, 1H), 3.65-3.45 (m, 2H), 3.57 (s, 2H), 3.30 (m, 1H ), 3.05 (m, 1H), 2.86-2.77 (m, 3H), 2.30-2.00 (m, 4H), 1.90-1.60 (m, 6H), 1.60-1.10 (m, 9H), 1.10-0.90 (m) , 2H), 0.95 (t, J = 7.2 Hz, 3H).
    [5952] Example 54
    [5953] (3R * ) -1-butyl-2,5-dioxo-3-((1S * ) -1-hydroxy-1-cyclohexylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5954]
    [5955] Using the compound prepared in Example 53, the same operation as in Example 9 was carried out to obtain a compound of the present invention having the following physical properties.
    [5956] TLC: Rf 0.59 (CHCl 3: MeOH: Acetic Acid = 10: 2: 1);
    [5957] NMR (CD 3 OD): δ 4.08 (d, J = 1.5 Hz, 1H), 4.03 (m, 1H), 3.70-3.12 (m, 7H), 2.50-2.02 (m, 5H), 1.85-1.66 (m , 5H), 1.55-1.10 (m, 7H), 1.10-0.85 (m, 2H), 0.97 (t, J = 6.9 Hz, 3H).
    [5958] Examples 55 (1) to 55 (3)
    [5959] Using the compound prepared in Example 54 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5960] Example 55 (1)
    [5961] (3R * ) -1-butyl-2,5-dioxo-3-((1S * ) -1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5962]
    [5963] TLC: Rf 0.46 (CHCl 3: MeOH = 10: 1);
    [5964] NMR (CD 3 OD): δ 7.50 (d, J = 8.7 Hz, 2H), 7.39 (dd, J = 8.7, 7.5 Hz, 2H), 7.17 (t, J = 7.5 Hz, 1H), 7.09-7.00 ( m, 4H), 4.30 (brs, 2H), 4.08 (d, J = 1.2 Hz, 1H), 4.04 (m, 1H), 3.74-3.36 (m, 5H), 3.16 (m, 1H), 2.55-2.33 (m, 2H), 2.32-2.09 (m, 2H), 2.04 (m, 1H), 1.84-1.61 (m, 5H), 1.53-1.12 (m, 7H), 1.04-0.86 (m, 5H).
    [5965] Example 55 (2)
    [5966] (3R * ) -1-butyl-2,5-dioxo-3-((1S * ) -1-hydroxy-1-cyclohexylmethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5967]
    [5968] TLC: Rf 0.41 (CHCl 3: MeOH = 10: 1);
    [5969] NMR (CD 3 OD): δ 7.04 (d, J = 2.1 Hz, 1H), 6.97 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.21 (s, 2H), 4.07 (d, J = 1.2 Hz, 1H), 4.01 (m, 1H), 3.70-3.34 (m, 5H), 3.16 (m, 1H), 2.53-2.32 (m , 2H), 2.31-2.08 (m, 2H), 2.03 (m, 1H), 1.84-1.60 (m, 5H), 1.52-1.12 (m, 7H), 1.04-0.85 (m, 5H).
    [5970] Example 55 (3)
    [5971] (3R * ) -1-butyl-2,5-dioxo-3-((1S * ) -1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane Dihydrochloride
    [5972]
    [5973] TLC: Rf 0.31 (CHCl 3: MeOH = 10: 1);
    [5974] NMR (CD 3 OD): δ 7.61-7.44 (m, 5H), 4.31 (s, 2H), 4.19-4.06 (m, 2H), 3.73 (m, 1H), 3.66-3.52 (m, 4H), 3.26 (m, 1H), 2.62-2.48 (m, 2H), 2.45-2.30 (m, 7H), 2.19 (m, 1H), 2.04 (m, 1H), 1.84-1.63 (m, 5H), 1.54-1.12 (m, 7 H), 1.05-0.86 (m, 5 H).
    [5975] Example 56
    [5976] (3S) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5977]
    [5978] (2S, 3S) -N- (t-butyloxycarbonyl instead of (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid The compound of the present invention having the following physical properties was obtained in the same manner as in Example 42-> 43 using) -2-amino-3-hydroxy-4-methylpentanoic acid.
    [5979] TLC: Rf 0.08 (CHCl 3: MeOH = 10: 1);
    [5980] NMR (CD 3 OD): δ 4.15 (d, J = 2.0 Hz, 1H), 3.96 (dt, J = 13.0, 4.0 Hz, 1H), 3.71 (dt, J = 13.0, 4.0 Hz, 1H), 3.57- 3.47 (m, 1H), 3.40-3.34 (m, 2H), 3.23-3.12 (m, 2H), 2.47-2.30 (m, 2H), 2.25-1.98 (m, 3H), 1.79-1.66 (m, 1H ), 1.52-1.28 (m, 3H), 1.07-0.94 (m, 9H);
    [5981] Specific light intensity: [α] D -13.8 (c 1.00, methanol).
    [5982] Examples 57 (1) to 57 (4)
    [5983] Using the compound prepared in Example 56 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [5984] Example 57 (1)
    [5985] (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [5986]
    [5987] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5988] NMR (CD 3 OD): δ 7.61-7.43 (m, 5H), 4.32 (s, 2H), 4.16 (d, J = 2.1 Hz, 1H), 4.12-3.99 (m, 1H), 3.90-3.72 (m , 1H), 3.64-3.44 (m, 3H), 3.30-3.12 (m, 1H), 3.20 (dd, J = 9.3, 2.1 Hz, 1H), 2.60-2.30 (m, 9H), 2.24-2.10 (m , 1H), 2.10-1.95 (m, 1H), 1.78-1.60 (m, 1H), 1.54-1.30 (m, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 6.9 Hz, 3H).
    [5989] Example 57 (2)
    [5990] (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [5991]
    [5992] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [5993] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.43-7.36 (m, 2H), 7.21-7.14 (m, 1H), 7.10-7.00 (m, 4H), 4.33 (s , 2H), 4.14 (d, J = 2.1 Hz, 1H), 4.06-3.92 (m, 1H), 3.81-3.66 (m, 1H), 3.58-3.40 (m, 3H), 3.30-3.10 (m, 1H ), 3.19 (dd, J = 9.6, 2.1 Hz, 1H), 2.53-2.37 (m, 2H), 2.37-2.18 (m, 1H), 2.18-2.08 (m, 1H), 2.06-1.95 (m, 1H) ), 1.78-1.60 (m, 1H), 1.50-1.26 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [5994] Example 57 (3)
    [5995] (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane hydrochloride
    [5996]
    [5997] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [5998] NMR (CD 3 OD): δ 7.06 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.13 (d, J = 2.4 Hz, 1H), 4.02-3.87 (m, 1H), 3.77-3.62 (m, 1H), 3.57-3.35 (m, 3H), 3.28 -3.08 (m, 1H), 3.19 (dd, J = 9.6, 2.4 Hz, 1H), 2.51-2.35 (m, 2H), 2.35-2.18 (m, 1H), 2.17-2.05 (m, 1H), 2.05 -1.90 (m, 1H), 1.80-1.58 (m, 1H), 1.50-1.26 (m, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [5999] Example 57 (4)
    [6000] (3S) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6001]
    [6002] TLC: Rf 0.35 (CHCl 3: MeOH = 10: 1);
    [6003] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.29 (d, J = 9.0 Hz, 2H), 7.10-7.00 (m, 4H), 4.33 (s, 2H), 4.14 ( d, J = 2.1 Hz, 1H), 4.06-3.92 (m, 1H), 3.81-3.66 (m, 1H), 3.58-3.40 (m, 3H), 3.25-3.10 (m, 1H), 3.19 (dd, J = 9.6, 2.1 Hz, 1H), 2.95 (s, 3H), 2.54-2.37 (m, 2H), 2.37-2.22 (m, 1H), 2.18-2.08 (m, 1H), 2.08-1.92 (m, 1H), 1.78-1.60 (m, 1H), 1.50-1.28 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.5 Hz, 3H).
    [6004] Example 58
    [6005] (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6006]
    [6007] (2R, 3R) -N- (t-butyloxycarbonyl instead of (2R * , 3R * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid The compound of the present invention having the following physical properties was obtained in the same manner as in Example 42-> 43 using) -2-amino-3-hydroxy-4-methylpentanoic acid.
    [6008] TLC: Rf 0.08 (CHCl 3: MeOH = 10: 1);
    [6009] NMR (CD 3 OD): δ 4.15 (d, J = 2.0 Hz, 1H), 3.96 (dt, J = 13.0, 4.0 Hz, 1H), 3.71 (dt, J = 13.0, 4.0 Hz, 1H), 3.57- 3.47 (m, 1H), 3.40-3.34 (m, 2H), 3.23-3.12 (m, 2H), 2.47-2.30 (m, 2H), 2.25-1.98 (m, 3H), 1.79-1.66 (m, 1H ), 1.52-1.28 (m, 3H), 1.07-0.94 (m, 9H);
    [6010] Specific light intensity: [α] D +13.9 (c 1.00, methanol).
    [6011] Example 59 (1)-59 (4)
    [6012] Using the compound prepared in Example 58 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [6013] Example 59 (1)
    [6014] (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [6015]
    [6016] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [6017] NMR (CD 3 OD): δ 7.61-7.43 (m, 5H), 4.32 (s, 2H), 4.16 (d, J = 2.1 Hz, 1H), 4.12-3.99 (m, 1H), 3.90-3.72 (m , 1H), 3.64-3.44 (m, 3H), 3.30-3.12 (m, 1H), 3.20 (dd, J = 9.3, 2.1 Hz, 1H), 2.60-2.30 (m, 9H), 2.24-2.10 (m , 1H), 2.10-1.95 (m, 1H), 1.78-1.60 (m, 1H), 1.54-1.30 (m, 3H), 1.00 (d, J = 6.6 Hz, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 6.9 Hz, 3H).
    [6018] Example 59 (2)
    [6019] (3R) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza spiro [5.5] Undecane hydrochloride
    [6020]
    [6021] TLC: Rf 0.51 (CHCl 3: MeOH = 10: 1);
    [6022] NMR (CD 3 OD): δ 7.52 (d, J = 8.7 Hz, 2H), 7.43-7.36 (m, 2H), 7.21-7.14 (m, 1H), 7.10-7.00 (m, 4H), 4.33 (s , 2H), 4.14 (d, J = 2.1 Hz, 1H), 4.06-3.92 (m, 1H), 3.81-3.66 (m, 1H), 3.58-3.40 (m, 3H), 3.30-3.10 (m, 1H ), 3.19 (dd, J = 9.6, 2.1 Hz, 1H), 2.53-2.37 (m, 2H), 2.37-2.18 (m, 1H), 2.18-2.08 (m, 1H), 2.06-1.95 (m, 1H) ), 1.78-1.60 (m, 1H), 1.50-1.26 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [6023] Example 59 (3)
    [6024] (3R) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6025]
    [6026] TLC: Rf 0.43 (CHCl 3: MeOH = 10: 1);
    [6027] NMR (CD 3 OD): δ 7.06 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.13 (d, J = 2.4 Hz, 1H), 4.02-3.87 (m, 1H), 3.77-3.62 (m, 1H), 3.57-3.35 (m, 3H), 3.28 -3.08 (m, 1H), 3.19 (dd, J = 9.6, 2.4 Hz, 1H), 2.51-2.35 (m, 2H), 2.35-2.18 (m, 1H), 2.17-2.05 (m, 1H), 2.05 -1.90 (m, 1H), 1.80-1.58 (m, 1H), 1.50-1.26 (m, 3H), 0.98 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H).
    [6028] Example 59 (4)
    [6029] (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6030]
    [6031] TLC: Rf 0.35 (CHCl 3: MeOH = 10: 1);
    [6032] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.29 (d, J = 9.0 Hz, 2H), 7.10-7.00 (m, 4H), 4.33 (s, 2H), 4.14 ( d, J = 2.1 Hz, 1H), 4.06-3.92 (m, 1H), 3.81-3.66 (m, 1H), 3.58-3.40 (m, 3H), 3.25-3.10 (m, 1H), 3.19 (dd, J = 9.6, 2.1 Hz, 1H), 2.95 (s, 3H), 2.54-2.37 (m, 2H), 2.37-2.22 (m, 1H), 2.18-2.08 (m, 1H), 2.08-1.92 (m, 1H), 1.78-1.60 (m, 1H), 1.50-1.28 (m, 3H), 0.99 (d, J = 6.6 Hz, 3H), 0.97 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.5 Hz, 3H).
    [6033] Example 60
    [6034] (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6035]
    [6036] In lieu of (2R * , 3S * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-3-cyclohexylpropanoic acid, (2R, 3S) -N- (t-butyl The compound of the present invention having the following physical properties was obtained in the same manner as in Example 53-54 using oxycarbonyl) -2-amino-3-hydroxy-4-methylpentanoic acid.
    [6037] TLC: Rf 0.51 (CHCl 3: MeOH: Acetic Acid = 10: 2: 1);
    [6038] NMR (CD 3 OD): δ 4.08 (d, J = 1.5 Hz, 1H), 4.02 (dt, J = 12.6, 3.9 Hz, 1H), 3.70-3.00 (m, 6H), 2.50-2.10 (m, 4H ), 1.80-1.60 (m, 2H), 1.55-1.35 (m, 3H), 1.02 (d, J = 6.6 Hz, 3H), 0.99 (t, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H);
    [6039] Specific light intensity: [α] D +21.2 (c 1.00, methanol).
    [6040] Examples 61 (1) to 61 (3)
    [6041] Using the compound prepared in Example 60 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [6042] Example 61 (1)
    [6043] (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [6044]
    [6045] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [6046] NMR (CD 3 OD): δ 7.64-7.46 (m, 5H), 4.32 (s, 2H), 4.19-4.06 (m, 1H), 4.10 (d, J = 1.5 Hz, 1H), 3.80-3.53 (m , 4H), 3.51 (dd, J = 10.2, 1.5 Hz, 1H), 3.40-3.20 (m, 1H), 2.70-2.30 (m, 9H), 2.23-2.10 (m, 1H), 1.83-1.60 (m , 2H), 1.53-1.30 (m, 3H), 1.02 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 7.2 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [6047] Example 61 (2)
    [6048] (3R) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxan-6-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6049]
    [6050] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [6051] NMR (CD 3 OD): δ 7.06 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.08 (d, J = 1.5 Hz, 1H), 4.08-3.96 (m, 1H), 3.72-3.35 (m, 4H), 3.49 (dd, J = 10.2, 1.5 Hz , 1H), 3.28-3.08 (m, 1H), 2.55-2.35 (m, 2H), 2.35-2.18 (m, 1H), 2.18-2.08 (m, 1H), 1.82-1.62 (m, 2H), 1.52 -1.25 (m, 3H), 1.01 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H), 0.92 (d, J = 6.6 Hz, 3H).
    [6052] Example 61 (3)
    [6053] (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6054]
    [6055] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [6056] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.29 (d, J = 9.0 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 7.03 (d, J = 9.0 Hz, 2H), 4.33 (s, 2H), 4.13-4.00 (m, 1H), 4.09 (d, J = 1.5 Hz, 1H), 3.75-3.62 (m, 1H), 3.62-3.39 (m, 3H ), 3.49 (dd, J = 10.5, 1.5 Hz, 1H), 3.26-3.12 (m, 1H), 2.95 (s, 3H), 2.56-2.37 (m, 2H), 2.37-2.20 (m, 1H), 2.20-2.10 (m, 1H), 1.82-1.63 (m, 2H), 1.50-1.30 (m, 3H), 1.01 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H) , 0.92 (d, J = 6.6 Hz, 3H).
    [6057] Example 62
    [6058] (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6059]
    [6060] (2S, 3R) -N- (t-butyloxycarthyl, instead of (2R * , 3S * )-N- (t-butyloxycarbonyl) -2-amino-3-hydroxy-3-cyclohexylpropanoic acid The compound of the present invention having the following physical properties was obtained in the same manner as in Example 53-54 using Bonyl) -2-amino-3-hydroxy-4-methylpentanoic acid.
    [6061] TLC: Rf 0.51 (CHCl 3: MeOH: Acetic Acid = 10: 2: 1);
    [6062] NMR (CD 3 OD): δ 4.08 (d, J = 1.5 Hz, 1H), 4.02 (dt, J = 12.6, 3.9 Hz, 1H), 3.70-3.00 (m, 6H), 2.50-2.10 (m, 4H ), 1.80-1.60 (m, 2H), 1.55-1.35 (m, 3H), 1.02 (d, J = 6.6 Hz, 3H), 0.99 (t, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H);
    [6063] Specific light intensity: [α] D -23.4 (c 1.00, methanol).
    [6064] Examples 63 (1) to 63 (3)
    [6065] Using the compound prepared in Example 62 and the corresponding aldehyde compound, the same operation as in Example 10 was carried out to obtain a compound of the present invention shown below.
    [6066] Example 63 (1)
    [6067] (3S) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole-4- Monomethyl) -1,4,9-triazaspiro [5.5] undecane dihydrochloride
    [6068]
    [6069] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [6070] NMR (CD 3 OD): δ 7.64-7.46 (m, 5H), 4.32 (s, 2H), 4.19-4.06 (m, 1H), 4.10 (d, J = 1.5 Hz, 1H), 3.80-3.53 (m , 4H), 3.51 (dd, J = 10.2, 1.5 Hz, 1H), 3.40-3.20 (m, 1H), 2.70-2.30 (m, 9H), 2.23-2.10 (m, 1H), 1.83-1.60 (m , 2H), 1.53-1.30 (m, 3H), 1.02 (d, J = 6.6 Hz, 3H), 0.96 (t, J = 7.2 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H).
    [6071] Example 63 (2)
    [6072] (3S) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6073]
    [6074] TLC: Rf 0.44 (CHCl 3: MeOH = 10: 1);
    [6075] NMR (CD 3 OD): δ 7.06 (d, J = 2.1 Hz, 1H), 6.98 (dd, J = 8.1, 2.1 Hz, 1H), 6.92 (d, J = 8.1 Hz, 1H), 4.26 (s, 4H), 4.23 (s, 2H), 4.08 (d, J = 1.5 Hz, 1H), 4.08-3.96 (m, 1H), 3.72-3.35 (m, 4H), 3.49 (dd, J = 10.2, 1.5 Hz , 1H), 3.28-3.08 (m, 1H), 2.55-2.35 (m, 2H), 2.35-2.18 (m, 1H), 2.18-2.08 (m, 1H), 1.82-1.62 (m, 2H), 1.52 -1.25 (m, 3H), 1.01 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H), 0.92 (d, J = 6.6 Hz, 3H).
    [6076] Example 63 (3)
    [6077] (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6078]
    [6079] TLC: Rf 0.42 (CHCl 3: MeOH = 10: 1);
    [6080] NMR (CD 3 OD): δ 7.53 (d, J = 8.7 Hz, 2H), 7.29 (d, J = 9.0 Hz, 2H), 7.07 (d, J = 8.7 Hz, 2H), 7.03 (d, J = 9.0 Hz, 2H), 4.33 (s, 2H), 4.13-4.00 (m, 1H), 4.09 (d, J = 1.5 Hz, 1H), 3.75-3.62 (m, 1H), 3.62-3.39 (m, 3H ), 3.49 (dd, J = 10.5, 1.5 Hz, 1H), 3.26-3.12 (m, 1H), 2.95 (s, 3H), 2.56-2.37 (m, 2H), 2.37-2.20 (m, 1H), 2.20-2.10 (m, 1H), 1.82-1.63 (m, 2H), 1.50-1.30 (m, 3H), 1.01 (d, J = 6.6 Hz, 3H), 0.95 (t, J = 7.2 Hz, 3H) , 0.92 (d, J = 6.6 Hz, 3H).
    [6081] Example 64
    [6082] (3S) -2,5-dioxo-3- (3-benzyloxycarbonylaminopropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane hydrochloride
    [6083]
    [6084] Resin (3) synthesized in Reference Example 2, N- (2-phenylethyl) -4-piperidone, 2,4,6-trimethoxybenzylamine and N α- (t-butyloxycarbonyl) -N The compound of the present invention having the following physical properties was obtained in the same manner as in Reference Example 9-Reference Example 10-Example 1 using δ-(benzyloxycarbonyl) -L-ornithine.
    [6085] TLC: Rf 0.33 (CHCl 3: MeOH = 10: 1);
    [6086] NMR (DMSO-d 6 ): δ 10.80-10.00 (m, 1H), 8.65-8.45 (m, 1H), 8.33 (s, 1H), 7.50-7.20 (m, 10H), 5.01 (s, 2H), 4.01 (m, 1H), 3.70-3.45 (m, 3H), 3.45-3.20 (m, 3H), 3.15-2.90 (m, 4H), 2.50-2.30 (m, 2H), 2.10-1.90 (m, 1H ), 1.87-1.60 (m, 3H), 1.60-1.35 (m, 2H).
    [6087] Example 65
    [6088] (3S) -1-methyl-2,5-dioxo-3- (3-benzyloxycarbonylaminopropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Canned acetate
    [6089]
    [6090] Resin (3) synthesized in Reference Example 2, N- (2-phenylethyl) -4-piperidone, methylamine and N α- (t-butyloxycarbonyl) -N δ- (benzyloxycarbonyl)- The compound of the present invention having the following physical properties was obtained in the same manner as in Example 19 using L-ornithine.
    [6091] TLC: Rf 0.36 (CHCl 3: MeOH = 10: 1);
    [6092] MS (ESI, Pos., 40 V): 493 (M + H) &lt; + &gt;;
    [6093] HPLC conditions: F;
    [6094] HPLC retention time: 3.36 minutes.
    [6095] Example 66
    [6096] (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenyloxyphenylmethyl) -9-oxide-1,4,9-triazaspiro [5.5] undecane
    [6097]
    [6098] To a solution of acetone (4 ml) of the compound (104 mg) prepared in Example 40 (90) was added water (1 ml), sodium bicarbonate (210 mg) and oxone (615 mg) (trade name). The reaction mixture was stirred at rt for 1 h. The reaction mixture was diluted with ethyl acetate, washed with saturated aqueous sodium hydrogen carbonate solution and saturated aqueous sodium chloride solution, dried over anhydrous magnesium sulfate and concentrated. The residue was purified by preparative thin layer chromatography (chloroform: methanol = 30: 1,20: 1) to give a compound of the present invention (73 mg) having the following physical properties.
    [6099] TLC: Rf 0.50 (CHCl 3: MeOH = 9: 1);
    [6100] NMR (CDCl 3 ): δ 7.49 (dt, J = 8.7, 2.1 Hz, 2H), 7.36 (ddt, J = 8.7, 7.2, 2.1 Hz, 2H), 7.14 (tt, J = 7.2, 1.2 Hz, 1H) , 7.04 (dq, J = 8.7, 1.2 Hz, 2H), 7.01 (dt, J = 8.7, 2.1 Hz, 2H), 5.82 (brs, 1H), 4.32 (s, 2H), 4.07-3.85 (m, 3H ), 3.55-3.46 (m, 2H), 3.19-2.97 (m, 4H), 2.02-1.49 (m, 11H), 1.48-1.12 (m, 6H), 1.08-0.90 (m, 2H), 0.90 (t , J = 7.2 Hz, 3H).
    [6101] Example 67 (H32-1)-67 (H34-15)
    [6102] The same procedure as in Example 23 was carried out using the resin (3) prepared in Reference Example 2, the corresponding 4-piperidone derivative, the corresponding amine derivative, the corresponding amino acid derivative, and the corresponding aldehyde derivative, and the following Table 32A-1 The compound of this invention which showed the compound name in -34A-2 and showed the structural formula in Table 32B-1-34B-3 was obtained. In addition, the physical properties of these compounds of the present invention are shown in Tables 32C-1 to 34C-1 below.
    [6103] Table 32A-1
    [6104] Example number Compound name
    [6105] 67 (H32-1) 1-Butyl-2,5-dioxo-3-benzyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6106] 67 (H32-2) 1-Butyl-2,5-dioxo-3-benzyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6107] 67 (H32-3) 1-Butyl-2,5-dioxo-3-benzyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6108] 67 (H32-4) 1-Butyl-2,5-dioxo-3-benzyl-9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6109] 67 (H32-5) 1-Butyl-2,5-dioxo-3-benzyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6110] 67 (H32-6) 1-butyl-2,5-dioxo-3-benzyl-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [6111] 67 (H32-7) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6112] 67 (H32-8) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6113] 67 (H32-9) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6114] Table 32A-2
    [6115] Example number Compound name
    [6116] 67 (H32-10) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6117] 67 (H32-11) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [6118] 67 (H32-12) 1- (2-methoxyethyl) -2,5-dioxo-3-benzyl-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6119] 67 (H32-13) 1-benzyl-2,5-dioxo-3-benzyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6120] 67 (H32-14) 1-benzyl-2,5-dioxo-3-benzyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6121] 67 (H32-15) 1-benzyl-2,5-dioxo-3-benzyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6122] 67 (H32-16) 1-benzyl-2,5-dioxo-3-benzyl-9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6123] 67 (H32-17) 1-benzyl-2,5-dioxo-3-benzyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6124] 67 (H32-18) 1-benzyl-2,5-dioxo-3-benzyl-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [6125] Table 32A-3
    [6126] Example number Compound name
    [6127] 67 (H32-19) (3S) -1-Butyl-2,5-dioxo-3- (4-methoxybenzyl) -9-cyclohexylmethyl-1,4,9-triazaspiro [5.5] Cannes
    [6128] 67 (H32-20) (3S) -1-Butyl-2,5-dioxo-3- (4-methoxybenzyl) -9- (2-methylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [6129] 67 (H32-21) (3R) -1-butyl-2,5-dioxo-3- (4-methoxybenzyl) -9-cyclohexylmethyl-1,4,9-triazaspiro [5.5] Cannes
    [6130] 67 (H32-22) (3R) -1-Butyl-2,5-dioxo-3- (4-methoxybenzyl) -9- (2-methylpropyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [6131] 67 (H32-23) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-chlorophenyl) thiophen-2-ylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6132] 67 (H32-24) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (4-methoxyphenyl) thiophen-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6133] TABLE 33A-1
    [6134] Example number Compound name
    [6135] 67 (H33-1) 1- (2-Chlorophenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6136] 67 (H33-2) 1- (2-fluorophenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6137] 67 (H33-3) 1- (2-trifluoromethylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6138] 67 (H33-4) 1-cyclopropylmethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [6139] 67 (H33-5) 1- (2,2-dimethylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6140] 67 (H33-6) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6141] 67 (H33-7) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6142] 67 (H33-8) 1-((2E) -2-butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6143] TABLE 33A-2
    [6144] Example number Compound name
    [6145] 67 (H33-9) 1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (5-ethylthiophen-2-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6146] 67 (H33-10) 1- (2-phenyloxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6147] 67 (H33-11) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-hydroxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6148] 67 (H33-12) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6149] 67 (H33-13) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-hydroxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6150] 67 (H33-14) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6151] 67 (H33-15) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-hydroxyphenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6152] 67 (H33-16) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6153] TABLE 33A-3
    [6154] Example number Compound name
    [6155] 67 (H33-17) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-hydroxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6156] 67 (H33-18) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-hydroxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [6157] TABLE 34A-1
    [6158] Example number Compound name
    [6159] 67 (H34-1) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6160] 67 (H34-2) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6161] 67 (H34-3) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3-((1S) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6162] 67 (H34-4) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3-((1S) -1-methylpropyl) -9- (1,4-benzodioxane -6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6163] 67 (H34-5) (3S) -1-Butyl-2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6164] 67 (H34-6) (3S) -1-Butyl-2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [6165] 67 (H34-7) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (4-phenyloxyphenylmethyl) -1, 4,9-Triaza spiro [5.5] Undecan
    [6166] TABLE 34A-2
    [6167] Example number Compound name
    [6168] 67 (H34-8) (3S) -1- (2-methoxyethyl) -2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (1,4-benzodioxane-6- Monomethyl) -1,4,9-triazaspiro [5.5] undecane
    [6169] 67 (H34-9) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-chloro-1,3-benzodioxolan-5-ylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6170] 67 (H34-10) 1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-chloro-1,3-benzodioxolan-5-yl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [6171] 67 (H34-11) 1- (3-methyl-2-butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6172] 67 (H34-12) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9-((2E) -3-phenyl-2-propenyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6173] 67 (H34-13) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9-((2E) -3-phenyl-2-propenyl) -1,4,9-triazaspiro [ 5.5] Undecan
    [6174] 67 (H34-14) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (quinolin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6175] 67 (H34-15) 1- (3-methyl-2-butenyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6176] Table 32B-1
    [6177]
    [6178] Table 32B-2
    [6179]
    [6180] Table 32B-3
    [6181]
    [6182] Table 32B-4
    [6183]
    [6184] TABLE 33B-1
    [6185]
    [6186] TABLE 33B-2
    [6187]
    [6188] Table 33B-3
    [6189]
    [6190] TABLE 34B-1
    [6191]
    [6192] TABLE 34B-2
    [6193]
    [6194] TABLE 34B-3
    [6195]
    [6196] Table 32C-1
    [6197]
    [6198] TABLE 33C-1
    [6199]
    [6200] TABLE 34C-1
    [6201]
    [6202] Example 68 (H35-1)-68 (H35-61)
    [6203] The same procedure as in Reference Example 11 was carried out using the resin (3) prepared in Reference Example 2, the corresponding 4-piperidone derivative, the corresponding amine derivative, and the corresponding amino acid derivative, and the Reference Example 12 using the corresponding alcohol derivative. → The same operation as in Example 33 was carried out, and the present invention was extracted from the resin, and the compound names are shown in the following Tables 35A-1 to 35A-8, and the structural formulas are shown in Tables 35B-1 to 35B-13. The compound was obtained. In addition, the physical properties of these compounds of the present invention are shown in Tables 35C-1 to 35C-3 below.
    [6204] TABLE 35A-1
    [6205] Example number Compound name
    [6206] 68 (H35-1) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4- (2- (N, N-diethylamino) ethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6207] 68 (H35-2) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4- (2- (N, N-diethylamino) ethyloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6208] 68 (H35-3) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2- (N, N-diethylamino) ethyloxy) phenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6209] 68 (H35-4) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4- (2- (N, N -Diethylamino) ethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6210] 68 (H35-5) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4- (2- (N, N-diethylamino) ethyloxy) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6211] 68 (H35-6) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4- (2- (N, N-diethylamino ) Ethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6212] 68 (H35-7) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2- (N, N-diethylamino) ethyloxy) phenylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [6213] TABLE 35A-2
    [6214] Example number Compound name
    [6215] 68 (H35-8) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-methoxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6216] 68 (H35-9) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6217] 68 (H35-10) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6218] 68 (H35-11) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6219] 68 (H35-12) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-methoxyphenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6220] 68 (H35-13) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6221] 68 (H35-14) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [6222] 68 (H35-15) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-ethoxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6223] TABLE 35A-3
    [6224] Example number Compound name
    [6225] 68 (H35-16) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-ethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6226] 68 (H35-17) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-ethoxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6227] 68 (H35-18) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-ethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6228] 68 (H35-19) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-ethoxyphenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6229] 68 (H35-20) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-ethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6230] 68 (H35-21) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-ethoxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6231] 68 (H35-22) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-ethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes
    [6232] 68 (H35-23) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-propyloxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6233] TABLE 35A-4
    [6234] Example number Compound name
    [6235] 68 (H35-24) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-propyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6236] 68 (H35-25) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-propyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6237] 68 (H35-26) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-propyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6238] 68 (H35-27) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-propyloxyphenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6239] 68 (H35-28) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-propyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6240] 68 (H35-29) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-propyloxyphenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6241] 68 (H35-30) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-isopropyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6242] 68 (H35-31) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-isopropyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [6243] Table 35A-5
    [6244] Example number Compound name
    [6245] 68 (H35-32) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-isopropyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6246] 68 (H35-33) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-isopropyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6247] 68 (H35-34) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-isopropyloxyphenylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [6248] 68 (H35-35) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-isopropyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6249] 68 (H35-36) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-isopropyloxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6250] 68 (H35-37) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-isopropyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6251] 68 (H35-38) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4- (cyclopropylmethyloxy) phenylmethyl)- 1,4,9-triaza spiro [5.5] Undecan
    [6252] Table 35A-6
    [6253] Example number Compound name
    [6254] 68 (H35-39) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4- (cyclopropylmethyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6255] 68 (H35-40) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4- (cyclopropylmethyloxy) phenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6256] 68 (H35-41) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (cyclopropylmethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6257] 68 (H35-42) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4- (cyclopropylmethyloxy) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane
    [6258] 68 (H35-43) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4- (cyclopropylmethyloxy) phenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6259] 68 (H35-44) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4- (cyclopropylmethyloxy) phenylmethyl) -1 , 4,9-triazaspiro [5.5] Undecan
    [6260] 68 (H35-45) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (cyclopropylmethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6261] Table 35A-7
    [6262] Example number Compound name
    [6263] 68 (H35-46) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-cyclobutyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6264] 68 (H35-47) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-cyclobutyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [6265] 68 (H35-48) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclobutyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6266] 68 (H35-49) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-cyclopentyloxyphenylmethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6267] 68 (H35-50) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4-cyclopentyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    [6268] 68 (H35-51) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopentyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan
    [6269] 68 (H35-52) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopentyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6270] 68 (H35-53) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-cyclopentyloxyphenylmethyl)- 1,4,9-triazaspiro [5.5] Undecan
    [6271] Table 35A-8
    [6272] Example number Compound name
    [6273] 68 (H35-54) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4-cyclopentyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan
    [6274] 68 (H35-55) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopentyloxyphenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6275] 68 (H35-56) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopentyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6276] 68 (H35-57) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4- (tetrahydropyran-4-yloxy) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6277] 68 (H35-58) 1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chloro-4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6278] 68 (H35-59) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (2-chloro-4- (tetrahydropyran-4- Yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane
    [6279] 68 (H35-60) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclobutyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan
    [6280] 68 (H35-61) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6281] TABLE 35B-1
    [6282]
    [6283] TABLE 35B-2
    [6284]
    [6285] TABLE 35B-3
    [6286]
    [6287] TABLE 35B-4
    [6288]
    [6289] Table 35B-5
    [6290]
    [6291] Table 35B-6
    [6292]
    [6293] Table 35B-7
    [6294]
    [6295] Table 35B-8
    [6296]
    [6297] Table 35B-9
    [6298]
    [6299] Table 35B-10
    [6300]
    [6301] TABLE 35B-11
    [6302]
    [6303] TABLE 35B-12
    [6304]
    [6305] TABLE 35B-13
    [6306]
    [6307] TABLE 35C-1
    [6308]
    [6309] TABLE 35C-2
    [6310]
    [6311] Table 35C-3
    [6312]
    [6313] Example 69 (H36-1)-69 (H36-24)
    [6314] Using the same amine derivative and the corresponding acid chloride derivative as in place of the compound prepared in Example 14, the compound names are shown in Tables 36A-1 to 36A-4 below, and Table 36B-1. The compound of this invention which showed a structural formula in -36B-5 was obtained. In addition, the physical properties of these compounds of the present invention are shown in Table 36C-1 below.
    [6315] TABLE 36A-1
    [6316] Example number Compound name
    [6317] 69 (H36-1) (3S) -1-propyl-2,5-dioxo-3-((2-phenylphenyl) carbonylaminomethyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6318] 69 (H36-2) (3S) -1-propyl-2,5-dioxo-3-((3-phenylphenyl) carbonylaminomethyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6319] 69 (H36-3) (3S) -1-propyl-2,5-dioxo-3-((4-phenylphenyl) carbonylaminomethyl) -9- (2-phenylethyl) -1,4,9 -Triaza Spiro [5.5] Undecan
    [6320] 69 (H36-4) (3S) -1-propyl-2,5-dioxo-3-((2-phenylphenyl) acetylaminomethyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6321] 69 (H36-5) (3S) -1-propyl-2,5-dioxo-3-((3-phenylphenyl) acetylaminomethyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    [6322] 69 (H36-6) (3S) -1-propyl-2,5-dioxo-3-((4-phenylphenyl) acetylaminomethyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan
    [6323] 69 (H36-7) (3S) -1-propyl-2,5-dioxo-3- (2- (2-phenylphenyl) carbonylaminoethyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6324] TABLE 36A-2
    [6325] Example number Compound name
    [6326] 69 (H36-8) (3S) -1-propyl-2,5-dioxo-3- (2- (3-phenylphenyl) carbonylaminoethyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6327] 69 (H36-9) (3S) -1-propyl-2,5-dioxo-3- (2- (4-phenylphenyl) carbonylaminoethyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6328] 69 (H36-10) (3S) -1-propyl-2,5-dioxo-3- (2- (2-phenylphenyl) acetylaminoethyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6329] 69 (H36-11) (3S) -1-propyl-2,5-dioxo-3- (2- (3-phenylphenyl) acetylaminoethyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6330] 69 (H36-12) (3S) -1-propyl-2,5-dioxo-3- (2- (4-phenylphenyl) acetylaminoethyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6331] 69 (H36-13) (3S) -1-propyl-2,5-dioxo-3- (3- (2-phenylphenyl) carbonylaminopropyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6332] 69 (H36-14) (3S) -1-propyl-2,5-dioxo-3- (3- (3-phenylphenyl) carbonylaminopropyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6333] TABLE 36A-3
    [6334] Example number Compound name
    [6335] 69 (H36-I5) (3S) -1-propyl-2,5-dioxo-3- (3- (4-phenylphenyl) carbonylaminopropyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6336] 69 (H36-16) (3S) -1-propyl-2,5-dioxo-3- (3- (2-phenylphenyl) acetylaminopropyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6337] 69 (H36-17) (3S) -1-propyl-2,5-dioxo-3- (3- (3-phenylphenyl) acetylaminopropyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6338] 69 (H36-18) (3S) -1-propyl-2,5-dioxo-3- (3- (4-phenylphenyl) acetylaminopropyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6339] 69 (H36-19) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenylphenyl) carbonylaminobutyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6340] 69 (H36-20) (3S) -1-propyl-2,5-dioxo-3- (4- (3-phenylphenyl) carbonylaminobutyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6341] 69 (H36-21) (3S) -1-propyl-2,5-dioxo-3- (4- (4-phenylphenyl) carbonylaminobutyl) -9- (2-phenylethyl) -1,4 , 9-triazaspiro [5.5] Undecan
    [6342] TABLE 36A-4
    [6343] Example Number Compound Name
    [6344] 69 (H36-22) (3S) -1-propyl-2,5-dioxo-3- (4- (2-phenylphenyl) acetylaminobutyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6345] 69 (H36-23) (3S) -1-propyl-2,5-dioxo-3- (4- (3-phenylphenyl) acetylaminobutyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6346] 69 (H36-24) (3S) -1-propyl-2,5-dioxo-3- (4- (4-phenylphenyl) acetylaminobutyl) -9- (2-phenylethyl) -1,4, 9-Triaza spiro [5.5] Undecan
    [6347] TABLE 36B-1
    [6348]
    [6349] TABLE 36B-2
    [6350]
    [6351] Table 36B-3
    [6352]
    [6353] TABLE 36B-4
    [6354]
    [6355] TABLE 36B-5
    [6356]
    [6357] TABLE 36C-1
    [6358]
    [6359] [Example]
    [6360] Formulation Example 1
    [6361] Each of the following components were mixed by a conventional method, followed by tableting to obtain 100 tablets containing 50 mg of the active ingredient in one tablet.
    [6362] 9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1-propyl-1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [6363] ‥‥‥ 5.0 g
    [6364] Carboxymethyl cellulose calcium (disintegrant) 0.2 g
    [6365] Magnesium stearate (lubricant) 0.1 g
    [6366] Microcrystalline cellulose ‥‥‥ 4.7 g
    [6367] Formulation Example 2
    [6368] After mixing each of the following components by a conventional method, the solution was sterilized by the conventional method and filled in the ampoules by 5 ml, and lyophilized by the conventional method to contain 20 mg of the active ingredient in 1 ampoule. 100 ampoules were obtained.
    [6369] 9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1-propyl-1,4 , 9-triazaspiro [5.5] undecane, dihydrochloride
    [6370] ‥‥‥ 2.0 g
    [6371] 20 g of mannitol
    [6372] Distilled water 500 ml
    [443] [Application to Drugs]
    [444] In animals, including humans, in particular humans, the compounds of the present invention represented by the formula (I) control the action of chemokine / chemokine receptors, and therefore, various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases (allergic bronchial pulmonary asper) Gillus, allergic eosinophilic gastroenteritis, etc.), nephritis, nephritis, hepatitis, arthritis, chronic joint rheumatism, psoriasis, rhinitis, conjunctivitis, suppression of ischemic reperfusion injury, multiple sclerosis, ulcerative colitis, acute respiratory distress syndrome, bacteria It is useful for the treatment of shock, diabetes, autoimmune diseases following infection, transplant rejection, immune suppression, cancer metastasis prevention, prevention and / or treatment of acquired immunodeficiency syndrome.
    [445] In order to use the compound of the present invention represented by the formula (I), its non-toxic salt, acid addition salt, or hydrate thereof for the above-mentioned purposes, it is usually administered systemically or topically in oral or parenteral form.
    [446] Dosages vary depending on age, weight, symptoms, therapeutic effect, method of administration, treatment time, and the like, but are usually orally administered once to several times per day, ranging from 1 mg to 1000 mg per adult, per adult Multiple parenteral administration (preferably intravenously) once a day, in the range of 1 mg to 100 mg per person, per person or continuously administered intravenously in the range of 1 hour to 24 hours per day .
    [447] Of course, as mentioned above, since a dosage varies with various conditions, an amount smaller than the said dosage may be sufficient, and it may be necessary beyond the range.
    [448] When administering the compound of the present invention, it is used as an oral solid preparation for oral administration, an oral solution preparation, and an injection, external preparation, suppository, etc. for parenteral administration.
    [449] Internal solids for oral administration include tablets, pills, capsules, powders, granules and the like. Capsules include hard capsules and soft capsules.
    [450] In such internal solids, one or more active substances may be used as such or as excipients (lactose, mannitol, glucose, microcrystalline cellulose, starch, etc.), binders (hydroxypropylcellulose, polyvinylpyrrolidone, metasilicate aluminic acid). Magnesium, etc.), disintegrating agents (such as calcium cellulose glycolate), lubricants (such as magnesium stearate), stabilizers, dissolving aids (glutamic acid, aspartic acid, etc.), and the like, and are formulated and used by conventional methods. Moreover, it may be coat | covered with a coating agent (white sugar, gelatin, hydroxypropyl cellulose, hydroxypropyl methylcellulose phthalate etc.) as needed, and may be coat | covered with two or more layers. Also included are capsules of absorbable materials, such as gelatin.
    [451] Oral solution for oral administration includes pharmaceutically acceptable homemade, suspension, emulsion, syrup, elixirs and the like. In such liquids, one or more active substances are dissolved, suspended or emulsified in commonly used diluents (purified water, ethanol or a mixture thereof). This liquid may also contain a humectant, a suspending agent, an emulsifier, a sweetener, a flavoring agent, a fragrance, a preservative, a buffer, and the like.
    [452] Injections for parenteral administration include solutions, suspensions, emulsions and solid injections used by dissolving or suspending in solvents in use. Injections are used by dissolving, suspending or emulsifying one or more active substances in a solvent. As the solvent, for example, distilled water for injection, physiological saline, vegetable oil, propylene glycol, polyethylene glycol, alcohols such as ethanol and the like and combinations thereof are used. The injection may also contain a stabilizer, a dissolution aid (glutamic acid, aspartic acid, polysorbate 80, etc.), a suspending agent, an emulsifying agent, a painless agent, a buffer, a preservative, and the like. They are either sterilized in the final process or prepared and prepared by aseptic manipulation. Aseptic solids, such as lyophilized products, may also be prepared and dissolved in sterile or sterile distilled water or other solvents prior to their use.
    [453] Other preparations for parenteral administration include external preparations, ointments, coatings, inhalants, sprays, suppositories, and pessaries for vaginal administration, which include one or more active substances, and are prescribed by conventional methods.
    [454] Sprays may contain, in addition to the diluents generally used, stabilizers such as sodium hydrogen sulfite and buffers which impart isotonicity, such as isotonic agents such as sodium chloride, sodium citrate or citric acid. Methods of making sprays are described in detail, for example, in US Pat. Nos. 2,868,691 and 3,095,355.
    权利要求:
    Claims (9)
    [1" claim-type="Currently amended] Triazaspiro represented by the following formula (I) [5. 5] undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof,
    Formula I

    In which R 1 is
    (1) a hydrogen atom,
    (2) a C1-18 alkyl group,
    (3) a C2-18 alkenyl group,
    (4) a C2-18 alkynyl group,
    (5) -COR 6 ,
    (6) -CONR 7 R 8 ,
    (7) -COOR 9 ,
    (8) -SO 2 R 10 ,
    (9) -COCOOR 11 ,
    (10) -CONR 12 COR 13 ,
    (11) Cyc1, or
    (12) optionally selected 1 to 5 (a) halogen atoms, (b) -CONR 7 R 8 , (c) -COOR 9 , (d) -OR 14 , (e) -SR 15 , (f) -NR 16 R 17 , (g) -NR 18 COR 19 , (h) -SO 2 NR 20 R 21 , (i) -OCOR 22 , (j) -NR 23 SO 2 R 24 , (k) -NR 25 COOR 26 , (l) -NR 27 CONR 28 R 29 , (m) Cyc 1, (n) keto group, (o) C 1-18 alkyl group substituted by -N (SO 2 R 24 ) 2 , C 2-18 alkenyl group, Or a C2-18 alkynyl group,
    (In the group, R 6 to R 9 , R 11 to R 21 , R 23 , R 25, and R 27 to R 29 are each independently.
    (1) a hydrogen atom,
    (2) a C1-8 alkyl group,
    (3) a C2-8 alkenyl group,
    (4) a C2-8 alkynyl group,
    (5) Cyc1, or
    (6) 1 to 5 optionally selected (a) Cyc1, (b) halogen atoms, (c) -OR 30 , (d) -SR 31 , (e) -NR 32 R 33 , (f) -COOR 34 , (g) a C1-8 alkyl group substituted by -CONR 35 R 36 , (h) -NR 37 COR 38 , (i) -NR 39 SO 2 R 40 , (j) -N (SO 2 R 40 ) 2 , C2-8 alkenyl group, or C2-8 alkynyl group, or
    R 7 and R 8 , R 20 and R 21 , R 28 and R 29 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 195 - (C2~6 alkylene) - represents the (in which R 195 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    R 10 , R 22 , R 24 and R 26 are each independently
    (1) a C1-8 alkyl group,
    (2) a C2-8 alkenyl group,
    (3) a C2-8 alkynyl group,
    (4) Cyc1, or
    (5) 1-5 optionally selected (a) Cyc1, (b) halogen atom, (c) -OR 30 , (d) -SR 31 , (e) -NR 32 R 33 , (f) -COOR 34 , (g) a C1-8 alkyl group substituted by -CONR 35 R 36 , (h) -NR 37 COR 38 , (i) -NR 39 SO 2 R 40 , (j) -N (SO 2 R 40 ) 2 , C2-8 alkenyl group, or C2-8 alkynyl group,
    (In the group, R 30 to R 37 and R 39 each independently represent a hydrogen atom, a C 1-8 alkyl group, Cyc 1, or a C 1-8 alkyl group substituted with Cyc 1, or
    R 35 and R 36 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene group) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 196 - (C2~6 alkylene) - a represents (in which, R 196 is hydrogen, C1~8 alkyl group, a phenyl group Or a C1-8 alkyl group substituted with a phenyl group),
    R 38 and R 40 each independently represent a C1-8 alkyl group, Cyc1, or a C1-8 alkyl group substituted by Cyc1)
    Cyc1 is C3-15 monocyclic, cyclic, or tricyclic (condensed or spiro) carbon ring, or 3 to 3 containing 1 to 4 nitrogen atoms, 1 to 3 oxygen atoms and / or 1 to 3 sulfur atoms 15-membered monocyclic, cyclic or tricyclic (condensed or spiro) heterocyclic rings are shown.
    However, Cyc1 may be substituted by 1 to 5 R 51 s ,
    R 51 is
    (1) a C1-8 alkyl group,
    (2) a C2-8 alkenyl group,
    (3) a C2-8 alkynyl group,
    (4) halogen atoms,
    (5) nitro groups,
    (6) trifluoromethyl group
    (7) trifluoromethoxy group,
    (8) nitrile group,
    (9) ketogi,
    (10) Cyc2
    (11) -OR 52 ,
    (12) -SR 53 ,
    (13) -NR 54 R 55 ,
    (14) -COOR 56 ,
    (15) -CONR 57 R 58 ,
    (16) -NR 59 COR 60 ,
    (17) -SO 2 NR 61 R 62 ,
    (18) -OCOR 63 ,
    (19) -NR 64 SO 2 R 65 ,
    (20) -NR 66 COOR 67 ,
    (21) -NR 68 CONR 69 R 70 ,
    (22) -B (OR 71 ) 2 ,
    (23) -SO 2 R 72 ,
    (24) -N (SO 2 R 72 ) 2 , or
    (25) 1-5 optionally selected (a) halogen atoms, (b) Cyc2, (c) -OR 52 , (d) -SR 53 , (e) -NR 54 R 55 , (f) -COOR 56 , (g) -CONR 57 R 58 , (h) -NR 59 COR 60 , (i) -SO 2 NR 61 R 62 , (j) -OCOR 63 , (k) -NR 64 SO 2 R 65 , (l) -NR 66 COOR 67 , (m) -NR 68 CONR 69 R 70 , (n) -B (OR 71 ) 2 , (o) -SO 2 R 72 , (p) -N (SO 2 R 72 ) 2 Substituted C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group)
    (In the group, R 52 to R 62 , R 64 , R 66 and R 68 to R 71 are each independently.
    1) hydrogen atom, 2) C1-8 alkyl group, 3) C2-8 alkenyl group, 4) C2-8 alkynyl group, 5) Cyc2, or 6) Cyc2, -OR 73 , -COOR 74 , -NR 75 R 76 C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by
    R 57 and R 58 , R 61 and R 62 , R 69 and R 70 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 197 - (C2~6 alkylene) - represents the (in which R 197 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    R 63 , R 65 , R 67 and R 72 are each independently 1) C1-8 alkyl group, 2) C2-8 alkenyl group, 3) C2-8 alkynyl group, 4) Cyc2, or 5) Cyc2, -OR 73 , -COOR 74 , C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by -NR 75 R 76 ,
    (In the group, R 73 to R 76 each independently represent a hydrogen atom, a C1-8 alkyl group, Cyc2, or a C1-8 alkyl group substituted with Cyc2.)
    Cyc2 has the same meaning as Cyc1.
    However, Cyc2 may be substituted by 1 to 5 R 77 ,
    R 77 is
    1) a C1-8 alkyl group,
    2) halogen atoms,
    3) nitro group,
    4) trifluoromethyl group,
    5) trifluoromethoxy group,
    6) nitrile group,
    7) -OR 78 ,
    8) -NR 79 R 80 ,
    9) -COOR 81 ,
    10) -SR 82 ,
    11) -CONR 83 R 84 ,
    12) a C2-8 alkenyl group,
    13) a C2-8 alkynyl group,
    14) ketogi,
    15) Cyc6,
    16) -NR 161 COR 162 ,
    17) -SO 2 NR 163 R 164 ,
    18) -OCOR 165 ,
    19) -NR 166 SO 2 R 167 ,
    20) -NR 168 COOR 169 ,
    21) -NR 170 CONR 171 R 172 ,
    22) -SO 2 R 173 ,
    23) -N (SO 2 R 167 ) 2 ,
    24) optionally selected 1 to 5 (a) halogen atoms, (b) -OR 78 , (c) -NR 79 R 80 , (d) -COOR 81 , (e) -SR 82 , (f) -CONR 83 R 84 , (g) keto group, (h) Cyc6, (i) -NR 161 COR 162 , (j) -SO 2 NR 163 R 164 , (k) -OCOR 165 , (l) -NR 166 SO 2 R 167 , (m) -NR 168 COOR 169 , (n) -NR 170 CONR 171 R 172 , (o) -SO 2 R 173 , (p) -N (SO 2 R 167 ) 2 substituted by C 1-8 Alkyl group, C2-8 alkenyl group, C2-8 alkynyl group)
    (In the group, R 78 to R 84 , R 161 to R 164 , R 166 , R 168 and R 170 to R 172 each independently represent (a) a hydrogen atom, (b) a C1-8 alkyl group, and (c) C2 to 8 alkenyl group, (d) C2-8 alkynyl group, (e) Cyc6, (f) Cyc6, -OR 174 , -COOR 175 , -NR 176 R 177 , -CONR 178 R 179 substituted by C1-8 alkyl group , C2-8 alkenyl group, C2-8 alkynyl group, or
    R 83 and R 84 , R 163 and R 164 , R 171 and R 172 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 198 - (C2~6 alkylene) - represents the (in which R 198 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted by a phenyl group),
    R 165 , R 167 , R 169 and R 173 each independently represent (a) a C1-8 alkyl group, (b) a C2-8 alkenyl group, (c) a C2-8 alkynyl group, (d) Cyc6, or (e) C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by Cyc6, -OR 174 , -COOR 175 , -NR 176 R 177 , -CONR 178 R 179 )
    (Wherein, R 174 to R 177 each independently represent 1) a hydrogen atom, 2) a C 1-8 alkyl group, 3) Cyc 6, or 4) a C 1-8 alkyl group substituted by Cyc 6, or
    R 178 and R 179 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene group) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 199 - (C2~6 alkylene) - a represents (in which, R 199 is hydrogen, C1~8 alkyl group, a phenyl group Or a C1-8 alkyl group substituted with a phenyl group),
    Cyc6 represents a C3-8 monocyclic carbon ring or a 3-8 membered monocyclic ring containing 1-4 nitrogen atoms, 1-2 oxygen atoms and / or 1-2 sulfur atoms.
    However, Cyc6 may be substituted by 1 to 5 R 180 ,
    R 180 is
    (1) a C1-8 alkyl group,
    (2) a halogen atom,
    (3) nitro groups,
    (4) trifluoromethyl group,
    (5) trifluoromethoxy group,
    (6) nitrile group,
    (7) -OR 181 ,
    (8) -NR 182 R 183 ,
    (9) -COOR 184 ,
    (10) -SR 185 , or
    (11) represents -CONR 186 R 187
    (In the group, R 181 to R 187 each independently represent 1) a hydrogen atom, 2) a C1-8 alkyl group, 3) a phenyl group, or 4) a C1-8 alkyl group substituted with a phenyl group,
    R 182 and R 183 , R 186 and R 187 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3)-(C 2-6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 200 - (C2~6 alkylene) - represents the (in which, R 200 represents a hydrogen atom, C1-8 alkyl group substituted by C1-8 alkyl group, phenyl group, phenyl group)),
    R 2 is
    (1) a hydrogen atom,
    (2) a C1-8 alkyl group,
    (3) a C2-8 alkenyl group,
    (4) a C2-8 alkynyl group,
    (5) -OR 90 ,
    (6) Cyc3, or
    (7) 1-5 optionally selected (a) halogen atoms, (b) -OR 90 , (c) -SR 91 , (d) -NR 92 R 93 , (e) -COOR 94 , (f) -CONR 95 R 96 , (g) -NR 97 COR 98 , (h) -SO 2 NR 99 R 100 , (i) -OCOR 101 , (j) -NR 102 SO 2 R 103 , (k) -NR 104 COOR 105 , (l) -NR 106 CONR 107 R 108 , (m) Cyc3, (n) keto group, (o) C1-8 alkyl group substituted by -N (SO 2 R 103 ) 2 , C2-8 alkenyl group or A C2-8 alkynyl group,
    (In the group, R 90 to R 100 , R 102 , R 104 and R 106 to R 108 are each independently 1) a hydrogen atom, 2) a C1-8 alkyl group, 3) a C2-8 alkenyl group, 4) C2-8 An alkynyl group, 5) Cyc3, or 6) a C1-8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group substituted by Cyc3, or
    R 95 and R 96 , R 99 and R 100 , R 107 and R 108 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 )-(C2-6 alkylene group) -S- (C2-6 alkylene group)-or 4)-(C2-6 alkylene group) -NR 201- (C2-6 alkylene group)- R 201 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, or a C1-8 alkyl group substituted with a phenyl group),
    R 101 , R 103 and R 105 are each independently 1) a C1-8 alkyl group, 2) a C2-8 alkenyl group, 3) a C2-8 alkynyl group, or 4) a C1-8 alkyl group substituted by Cyc3 or Cyc3, C2-8 alkenyl group, C2-8 alkynyl group,
    Cyc3 has the same meaning as Cyc1.
    However, Cyc3 may be substituted by 1 to 5 R 109 ,
    R 109 has the same meaning as R 51 )
    R 3 and R 4 are each independently
    (1) a hydrogen atom,
    (2) a C1-8 alkyl group,
    (3) a C2-8 alkenyl group,
    (4) a C2-8 alkynyl group,
    (5) -COOR 120 ,
    (6) -CONR 121 R 122 ,
    (7) Cyc4, or
    (8) 1-5 optionally selected (a) halogen atoms, (b) nitrile groups, (c) Cyc4, (d) -COOR 120 , (e) -CONR 121 R 122 , (f) -OR 123 , ( g) -SR 124 , (h) -NR 125 R 126 , (i) -NR 127 COR 128 , (j) -SO 2 NR 129 R 130 , (k) -OCOR 131 , (l) -NR 132 SO 2 R 133 , (m) -NR 134 COOR 135 , (n) -NR 136 CONR 137 R 138 , (o) -S-SR 139 , (p) -NHC (= NH) NHR 140 , (q) keto group, (r) C1-8 alkyl group, C2-8 alkenyl group, or C2-8 alkynyl group substituted with -NR 145 CONR 146 COR 147 , (s) -N (SO 2 R 133 ) 2 ,
    (In the group, R 120 to R 130 , R 132 , R 134 , R 136 to R 138 , R 145 and R 146 are each independently 1) a hydrogen atom, 2) a C1-8 alkyl group, and 3) a C2-8 alkenyl group. 4) C2-8 alkynyl group, 5) Cyc4, or 6) Cyc4, a halogen atom, C1-8 alkyl group substituted by -OR 148 , -SR 149 , -COOR 150 , or -NHCOR 141 , C2-8 alkenes Or a C2-8 alkynyl group,
    R 121 and R 122 , R 129 and R 130 , R 137 and R 138 together are 1) C 2-6 alkylene group, 2)-(C 2-6 alkylene group) -O- (C 2-6 alkylene group)-, 3 ) - (C2~6 alkylene) -S- (C2~6 alkylene) - or 4) - (C2~6 alkylene) -NR 202 - (C2~6 alkylene) - represents the (in which R 202 represents a hydrogen atom, a C1-8 alkyl group, a phenyl group, a C1-8 alkyl group substituted with a phenyl group),
    R 131 , R 133 , R 135 , R 139 and R 147 are each independently 1) C1-8 alkyl group, 2) C2-8 alkenyl group, 3) C2-8 alkynyl group, 4) Cyc4, or 5) Cyc4, C1-8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group substituted by a halogen atom, -OR 148 , -SR 149 , -COOR 150 , or -NHCOR 141 ,
    R 140 represents a hydrogen atom, -COOR 142 , or -SO 2 R 143 ,
    (In the group, R 141 to R 143 are each independently 1) C 1-8 alkyl group, 2) C 2-8 alkenyl group, 3) C 2-8 alkynyl group, 4) Cyc 4, or 5) C 1 -substituted by Cyc 4. 8 alkyl group, C2-8 alkenyl group, C2-8 alkynyl group,
    R 148 to R 150 are each independently 1) hydrogen atom, 2) C1-8 alkyl group, 3) C2-8 alkenyl group, 4) C2-8 alkynyl group, 5) Cyc4, or 6) C1 substituted by Cyc4 It represents a -8 alkyl group, a C2-8 alkenyl group, a C2-8 alkynyl group,
    Cyc4 has the same meaning as Cyc1.
    Provided that Cyc4 may be substituted with 1 to 5 R 144 , and R 144 has the same meaning as R 51;
    R 3 and R 4 together

    In which R 190 and R 191 each independently represent the same meaning as R 3 or R 4, and
    R 5 is
    (1) a hydrogen atom,
    (2) a C1-8 alkyl group,
    (3) Cyc5, or
    (4) C1-8 alkyl group substituted by Cyc5.
    (In the group, Cyc5 has the same meaning as Cyc1.
    However, Cyc5 may be substituted by 1 to 5 R 160 , and R 160 has the same meaning as R 51. )
    [2" claim-type="Currently amended] The compound according to claim 1, wherein in the formula (I) described in claim 1, R 3 and R 4 are hydrogen atoms.
    [3" claim-type="Currently amended] The compound according to claim 1, wherein in the formula (I) described in claim 1, R 3 is a hydrogen atom,
    R 4 is
    (1) a C1-8 alkyl group,
    (2) a C2-8 alkenyl group,
    (3) a C2-8 alkynyl group,
    (4) -COOR 120 ,
    (5) -CONR 121 R 122 ,
    (6) Cyc4, or
    (7) 1-5 optionally selected (a) halogen atoms, (b) nitrile groups, (c) Cyc4, (d) -COOR 120 , (e) -CONR 121 R 122 , (f) -OR 123 , ( g) -SR 124 , (h) -NR 125 R 126 , (i) -NR 127 COR 128 , (j) -SO 2 NR 129 R 130 , (k) -OCOR 131 , (l) -NR 132 SO 2 R 133 , (m) -NR 134 COOR 135 , (n) -NR 136 CONR 137 R 138 , (o) -S-SR 139 , (p) -NHC (= NH) NHR 140 , (q) keto group, (r) a compound which is a C1-8 alkyl group, C2-8 alkenyl group, or C2-8 alkynyl group substituted with -NR 145 CONR 146 COR 147 , (s) -N (SO 2 R 133 ) 2 .
    (All symbols represent the same meaning as described in claim 1).
    [4" claim-type="Currently amended] The compound of claim 1, wherein in Formula (I) described in claim 1, R 3 and R 4 are each independently,
    (1) a C1-8 alkyl group,
    (2) a C2-8 alkenyl group,
    (3) a C2-8 alkynyl group,
    (4) -COOR 120 ,
    (5) -CONR 121 R 122 ,
    (6) Cyc4, or
    (7) 1-5 optionally selected (a) halogen atoms, (b) nitrile groups, (c) Cyc4, (d) -COOR 120 , (e) -CONR 121 R 122 , (f) -OR 123 , ( g) -SR 124 , (h) -NR 125 R1 126 , (i) -NR 127 COR 128 , (j) -SO 2 NR 129 R 130 , (k) -OCOR 131 , (l) -NR 132 SO 2 R 133 , (m) -NR 134 COOR 135 , (n) -NR 136 CONR 137 R 138 , (o) -S-SR 139 , (p) -NHC (= NH) NHR 140 , (q) keto group, (r) a compound which is a C1-8 alkyl group, C2-8 alkenyl group, or C2-8 alkynyl group substituted with -NR 145 CONR 146 COR 147 , (s) -N (SO 2 R 133 ) 2 .
    (All symbols represent the same meaning as described in claim 1).
    [5" claim-type="Currently amended] A compound according to claim 1, wherein R 3 and R 4 together in Formula (I) Attributable compound.
    (In this, all the symbols show the same meaning as described in Claim 1.)
    [6" claim-type="Currently amended] The compound of claim 1 wherein the compound is
    (1) 9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1-propyl-1,4 9-triazaspiro [5.5], Undecan,
    (2) 9- (1,4-benzodioxane-6-ylmethyl) -1-butyl-3-cyclohexylmethyl-2,5-dioxo-1,4,9-triazaspiro [5.5] Cannes,
    (3) 1-Butyl-3-cyclohexylmethyl-2,5-dioxo-9- (2-phenylimidazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (4) 1-butyl-3- (2-methyl-1-propyl) -2,5-dioxo-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (5) (3S) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1-propyl-1,4,9-triazaspiro [5.5] undecane ,
    (6) (3R) -2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1-propyl-1,4,9-triazaspiro [5.5] undecane ,
    (7) 1-butyl-9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) methyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (8) 1-butyl-3-cyclohexylmethyl-2,5-dioxo-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (9) 9- (1,4-benzodioxane-6-ylmethyl) -1-butyl-3- (2-methyl-1-propyl) -2,5-dioxo-1,4,9-tri Azaspiro [5.5] Undecan,
    (10) 9- (4-benzyloxyphenylmethyl) -1-butyl-2,5-dioxo-3- (2-methyl-1-propyl) -1,4,9-triazaspiro [5.5] Cannes,
    (11) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylhexyl) -1,4,9-triazaspiro [5.5] undecane,
    (12) (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (13) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (14) (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (15) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (3-phenylpropyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (16) (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (3-phenylpropyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (17) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (18) (3R) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-phenylbutyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (19) (3S) -1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane,
    (20) (3R) -1-Benzyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyl-1,4,9-triazaspiro [5.5] undecane,
    (21) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2- (2-phenyl-5-methyloxazole -4-yl) ethyl) -1,4,9-triazaspiro [5.5] undecane,
    (22) (3S) -1-propyl-2,5-dioxo-3- (4- (N- (2-chlorophenylmethyl) oxycarbonyl) aminobutyl) -9- (2-phenylethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (23) (3S) -1-propyl-2,5-dioxo-3- [3- (3- (2,4,6-trimethylphenylsulfonyl) guanidino) propyl] -9- (2- Phenylethyl) -1,4,9-triazaspiro [5.5] undecane,
    (24) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (25) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (26) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-allyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (27) (3S) -1-propyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1,4,9-triazaspiro [5.5] undecane,
    (28) (3R) -1-propyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -2,5-dioxo-3- (2-methyl-1-propyl) -1,4,9-triazaspiro [5.5] undecane,
    (29) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9-phenylmethyl-1,4,9-triazaspiro [5.5] undecane,
    (30) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (31) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (32) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (33) 1-butyl-2,5-dioxo-3-propyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (34) 1-butyl-2,5-dioxo-3-methoxymethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (35) 1- (1-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (36) 1- (2-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (37) 1- (2-methylpropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (38) 1- (2-Dimethylaminoethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (39) 1- (2-methoxyethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (40) 1- (2-methylthioethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (41) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [ 5.5] (42) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-benzyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (43) 1-benzyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (44) 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (45) 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (46) 1- (1-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (47) 1- (3-methylbutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (48) 1- (2-methoxyphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (49) 1- (3-methoxyphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9-((3,5-dimethyl-1-phenyl) -4-pyrazolyl) Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (50) 1- (2-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (51) 1- (3-methylphenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (52) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (53) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-ethylfuran-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (54) (3S) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (55) (3R) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (56) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9-allyloxycarbonyl-1,4,9-triaza Spiro [5.5] Undecan,
    (57) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -1,4,9-triazaspiro [5.5] undecane,
    (58) 1-propyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane,
    (59) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane,
    (60) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane,
    (61) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (4-dihydroxyboranephenylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (62) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (1,3-benzodioxalan-4-ylmethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (63) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (1,4-benzodioxan-6-yl) ethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (64) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (4-phenyloxyphenyl) ethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (65) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1- (1,4-benzodioxan-6-yl) ethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (66) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9-allyl-1,4,9-triazaspiro [5.5 ] Undecan,
    (67) (3S) -1-propyl-2,5-dioxo-3- (4-aminobutyl) -9-phenylethyl-1,4,9-triazaspiro [5.5] undecane,
    (68) (3S) -1-propyl-2,5-dioxo-3- (4- (N- (4-phenyl) phenylcarbonyl) aminobutyl) -9-phenylethyl-1,4,9- Triaza Spiro [5.5] Undecan,
    (69) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-methyl-9- (1- (1,4-benzodioxan-6-yl) ethyl iodide) -1,4, Diaza-9-Azonia Spiro [5.5] Undecan,
    (70) (3S) -3- (4- (N-benzyloxycarbonyl) aminobutyl) -2,5-dioxo-9- (2-hydroxy-2-phenylethyl) -1-propyl-1 , 4,9-triazaspiro [5,5] undecane,
    (71) (3S) -3- (4- (N-benzyloxycarbonyl) aminobutyl) -2,5-dioxo-9- (2-oxo-2-phenylethyl) -1-propyl-1, 4,9-triazaspiro [5,5] undecane,
    (72) (3S) -1- (2-methylpropyl) -2,5-dioxo-3-methyl-9-allyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (73) (3S) -1- (2-methylpropyl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (74) (3S) -1- (2-methylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (75) (3S) -1- (1-benzylpiperidin-4-yl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (76) (3S) -1- (1-benzylpiperidin-4-yl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2 -Phenylethyl) -1,4,9-triazaspiro [5.5] undecane,
    (77) (3S) -1- (2,2-diphenylpropyl) -2,5-dioxo-3-methyl-9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (78) (3S) -1- (2,2-diphenylpropyl) -2,5-dioxo-3- (4- (N-benzyloxycarbonyl) aminobutyl) -9- (2-phenylethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (79) (3S) -1-propyl-2,5-dioxo-3- (4-benzyloxyphenylmethyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (80) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (2,4,6-trimethoxybenzyl) -1,4 9-triazaspiro [5.5], Undecan,
    (81) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (2,2-dimethylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (82) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9- (3-phenylpropanoyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (83) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9-benzenesulfonyl-1,4,9-triazaspiro [5.5] Undecan,
    (84) (3S) -1-propyl-2,5-dioxo-3- (4- (benzylcarbonylamino) butyl) -9-benzylaminocarbonyl-1,4,9-triazaspiro [5.5 ] Undecan,
    (85) (3S) -1-propyl-2,5-dioxo-3- (4- (3-phenylpropanoyl) aminobutyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (86) (3S) -1-propyl-2,5-dioxo-3- (4-benzenesulfonylaminobutyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (87) (3S) -1-propyl-2,5-dioxo-3- (4- (N-benzylcarbamoyl) aminobutyl) -9- (2-phenylethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (88) (3S) -1-butyl-2,5-dioxo-3- (4-methoxyphenylmethyl) -9-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane,
    (89) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-chlorophenyl) thiophen-5-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (90) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (4-methoxyphenyl) thiophen-5-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (91) 1-((2E) -butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (92) 1- (furan-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (93) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (94) 1-cyclopropylmethyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (95) 1- (2-fluorophenylmethyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (96) 1- (3-methyl-2-butenyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (97) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (quinolin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (98) 1-butyl-2,5-dioxo-3- (benzyloxycarbonylmethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (99) 1- (3-methyl-2-butenyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (100) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-((2E) -3-phenyl-2-propenyl) -1,4,9-triazaspiro [5.5] Cannes,
    (101) (3S) -1-Butyl-2,5-dioxo-3- (1,1-dimethylethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (102) (3S) -1-Butyl-2,5-dioxo-3- (1,1-dimethylethyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (103) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (104) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (105) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (106) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-methylthiazol-2-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (107) (3R) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (108) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (109) (3R) -1-Butyl-2,5-dioxo-3-((1R) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (110) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (111) 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (112) 1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (113) 1-pentyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (114) 1- (3-methoxyphenylmethyl) -2,5-dioxo-3- (benzyloxymethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (115) (3R) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (116) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (117) 1-butyl-2,5-dioxo-3-cyclopentylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (118) 1-propyl-2,5-dioxo-3- (cyclohexylmethyloxymethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (119) (3S) -1-Butyl-2,5-dioxo-3- (1-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (120) (3R) -1-Butyl-2,5-dioxo-3- (1-methylpropyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (121) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5-phenylmethylthiophen-2-ylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (122) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenylmethylthiophen-5-ylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (123) (3R) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (124) (3S) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (125) (3R) -1- (2-butynyl) -2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (126) (3S) -1- (2-butynyl) -2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (127) 1-butyl-2,5-dioxo-3-cycloheptylmethyl-9- (1,4-benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (128) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,4,6-trimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (129) 1-butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (130) 1-butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (131) 1-butyl-2,5-dioxo-3- (3-cyclohexylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (132) 1-butyl-2,5-dioxo-3- (2-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (133) 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (134) 1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (135) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (136) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (137) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (138) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylbenzomorpholin-7-ylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (139) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylbenzomorpholin-7-ylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (140) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (N-methyl-N-phenylamino) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (141) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (N-methyl-N-phenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (142) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (3,5-dimethylpyrazol-1-yl) -5-methoxyphenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (143) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2- (3,5-dimethylpyrazol-1-yl) -5-methoxyphenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (144) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-diethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (145) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-diethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (146) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (147) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-phenyloxypyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (148) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,3-benzodioxolan-5-ylmethyl) -1,4,9-triazaspiro [ 5.5] (149) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,3-benzodioxolan-5-ylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (150) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-hydroxy-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (151) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylthiophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (152) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (N, N-diphenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (153) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (N, N-diphenylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (154) (3S) -1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (155) (3S) -1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (156) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (157) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (158) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (159) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (160) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-chlorophenyl) pyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (161) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-trifluoromethylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (162) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-trifluoromethylphenyl) pyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (163) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-diethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (164) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-diethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (165) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-phenylthiazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (166) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenylthiazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (167) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (1,4-benzodioxan-2-yl) thiazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (168) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-trifluoromethyl-2- (morpholin-1-yl) thiazol-5-ylmethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (169) 1-butyl-2,5-dioxo-3- (tetrahydropyran-4-ylmethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (170) 1-butyl-2,5-dioxo-3- (tetrahydropyran-4-ylmethyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (171) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-carboxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (172) 1-butyl-2,5-dioxo-3- (2-cyclohexylethyl) -9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (173) 1-butyl-2,5-dioxo-3- (2-cyclohexylethyl) -9- (1,4-benzodioxan-6-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (174) (3R) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (175) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methyl-2-phenylthiazol-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (176) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (thiophen-1-yl) thiazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (177) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2- (pyridin-4-yl) thiazol-4-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (178) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,4-dimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (179) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (180) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-2-yl) furan-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (181) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-3-yl) furan-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (182) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3,5-dimethylpyrazol-1-yl) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (183) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-chloropyridin-3-yloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (184) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrimidin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (185) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (186) 1- (2-butynyl) -2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylphenyl) pyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (187) (3R) -1- (2-butynyl) -2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (188) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-hydroxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (189) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-2-yl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (190) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-3-yl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (191) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-carboxyphenyl) pyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (192) 1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrazin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (193) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-carboxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (194) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-4-yl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (195) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyridin-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (196) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (naphthalen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (197) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-methoxynaphthalen-2-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (198) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (199) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (pyridin-4-yl) furan-2-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (200) 1-butyl-2,5-dioxo-3-cyclopentylmethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (201) (3R) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (202) (3S) -1-Butyl-2,5-dioxo-3- (2,2-dimethylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (203) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-nitrophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (204) (3R) -1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan,
    (205) (3S) -1- (tetrahydrofuran-2-ylmethyl) -2,5-dioxo-3-phenylmethyl-9- (4-phenylbutyl) -1,4,9-triazaspiro [5.5] Undecan,
    (206) (3S) -1-propyl-2,5-dioxo-3- (3- (benzyloxycarbonylamino) propyl) -9- (2-phenylethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (207) 1-butyl-2,5-dioxo-3- (carboxymethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (208) 1- (3-hydroxybutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (209) 1- (3-hydroxypropyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (210) 1- (2-hydroxybutyl) -2,5-dioxo-3- (2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (211) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-aminophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (212) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylcarbonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (213) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-((4-methylphenyl) sulfonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (214) (3S) -1-butyl-2,5-dioxo-3-benzyloxymethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (215) (3S) -1-butyl-2,5-dioxo-3-hydroxymethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (216) (3S) -1-butyl-2,5-dioxo-3-hydroxymethyl-1,4,9-triazaspiro [5.5] undecane,
    (217) (3S) -1-Butyl-2,5-dioxo-3-hydroxymethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (218) (3S) -1-Butyl-2,5-dioxo-3-hydroxymethyl-9- (3,5-dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (219) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopentyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (220) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-diethylaminoethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (221) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-dimethylaminoethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (222) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-propyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (223) 1- (thiophen-2-ylmethyl) -2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (224) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (225) 1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclopropylmethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (226) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (227) 1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (diethylamino) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (228) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (229) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane,
    (230) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (5- (3-methyl-4-chlorophenyl) -1- (4-methylphenylmethyl ) Pyrazol-3-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (231) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dimethylaminophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (232) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-diethylaminophenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (233) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-cyclohexyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (234) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (235) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methoxyphenyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (236) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-butylphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (237) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-methylpropyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (238) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-fluorophenyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (239) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-hydroxy-4-methoxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (240) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (241) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (242) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (243) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (244) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (245) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (246) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methyl-4-methoxyphenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (247) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (7-methoxy-1,3-benzodioxolan-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (248) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylthiophenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (249) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (250) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (251) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (252) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1-methylethyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (253) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-fluoro-4-methoxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (254) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-hydroxyethyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (255) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-hydroxy-3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (256) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-trifluoromethyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (257) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3-methyl-5-chloro-1-phenylpyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (258) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6-phenylpyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (259) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (260) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-methylsulfonylaminophenyl) pyrazole- 4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (261) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-methylpyridin-2-yloxy) phenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (262) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (6-methylpyridin-1-oxide-3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (263) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1- (2-methylpropyloxycarbonyl) indol-5-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (264) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2-phenyl-5-methyloxazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (265) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (266) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (6-methylpyridin-3-yloxy) phenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (267) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazole-4- Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (268) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (pyridin-2-yl) pyrazole-4- Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (269) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4-hydroxyphenyl) pyrazole-4- Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (270) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-carboxyethyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (271) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (dimethylaminosulfonyl) phenyl) pyra Zol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (272) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (5-methylpyridin-1-oxide-2-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (273) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (2-carboxy-1-ethenyl) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (274) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4- (2-carboxy-1-ethenyl) phenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (275) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-aminocarbonylphenyloxy) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (276) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-aminosulfonylphenyloxy) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (277) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-benzylpyrazol-4-ylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (278) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (2,4-difluorophenyl) pyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (279) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (pyrrolidin-1-ylmethyl) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (280) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (morpholin-4-ylsulfonyl) Phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (281) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (methylaminosulfonyl) phenyl) pyra Zol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (282) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-cyanophenyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (283) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (dimethylaminomethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (284) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (2-dimethylaminoethylaminosulfonyl ) Phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, 3
    (285) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (4-hydroxyphenyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (286) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-methoxyphenyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (287) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (quinoxalin-2-yl) pyrazole-4 -Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (288) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylcarbonylphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (289) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (N- (2-hydroxyethyl ) -N-methylaminosulfonyl) phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (290) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (2-phenylethyl) pyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (291) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (1,3,5-trimethylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (292) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (morpholin-4-ylmethyl) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (293) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylpiperazin-1-ylmethyl) phenylmethyl) -1, 4,9-triazaspiro [5.5] Undecan, 3
    (294) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-phenylsulfonylphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (295) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1-cyclohexylpyrazol-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (296) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-carboxyphenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (297) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (piperidin-1-ylmethyl) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (298) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (pyrrolidin-1-ylsulfonyl ) Phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (299) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (2,3-dihydrobenzofuran-5-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (300) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3,5-dimethyl-1- (4- (2-hydroxyethylaminosulfonyl ) Phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (301) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (carboxymethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (302) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1-phenyl-1-hydroxymethyl) phenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (303) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-hydroxypiperidin-1-ylmethyl) phenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (304) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (3-carboxyphenylmethyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (305) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (bis (methylsulfonyl) amino) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (306) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (1,4-benzodioxan-6-yloxy) phenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (307) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (3-hydroxyphenyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (308) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (methylsulfonylamino) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (309) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (6- (4-methoxyphenyloxy) pyridin-3-ylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (310) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylaminocarbonylphenyloxy) phenylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (311) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-chlorophenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (312) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (3- (4-carboxyphenyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (313) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (phenylaminocarbonyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (314) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4-methylthiophenyloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (315) (3S) -1-butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4- (4- (2-dimethylaminoethylaminocarbonyl) phenyloxy) phenylmethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (316) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-aminocarbonylphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (317) (3S) -1-Butyl-2,5-dioxo-3- (2-methylpropyl) -9- (4-dimethylaminocarbonylphenylmethyl) -1,4,9-triazaspiro [ 5.5] (318) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9-benzyloxycarbonyl-1,4,9-triazaspiro [5.5] undecane,
    (319) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-1,4,9-triazaspiro [5.5] undecane,
    (320) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (321) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (322) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (323) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (324) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-fluorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (325) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (326) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-cyclohexyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (327) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxy-3-hydroxyphenylmethyl) -1,4,9-triazaspiro [ 5.5] (328) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (329) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (330) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (331) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (332) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenylthiophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (333) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (2-methylpropyl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (334) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-butylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (335) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-isopropylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (336) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-methoxy-3-fluorophenylmethyl) -1,4,9-triazaspiro [ 5.5] (337) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-hydroxyethoxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (338) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2-hydroxy-3-methylphenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (339) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-chlorophenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (340) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (7-methoxy-1,3-benzodioxolan-5-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (341) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methyl-4-methoxyphenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (342) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-fluorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (343) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-trifluoromethoxyphenylmethyl) -1,4,9-triazaspiro [5.5] Cannes,
    (344) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3-methyl-5-chloro-1-phenylpyrazol-4-ylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (345) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,3-dimethyl-5-oxo-1-phenylpyrazolin-4-ylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (346) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1- (2-methylpropyloxycarbonyl) indol-5-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (347) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (5-methyl-2-phenyloxazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (348) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylsulfonylaminophenyl) pyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (349) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylsulfonylaminophenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (350) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (6-methylpyridin-3-yloxy) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (351) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (6-methylpyridin-1-oxide-3-yloxy) phenylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (352) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (tetrahydropyran-4-yloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (353) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6-phenylpyridin-3-ylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (354) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (355) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (pyridin-2-yl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (356) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-hydroxyphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (357) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-carboxyethyl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (358) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-hydroxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (359) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-carboxyphenyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (360) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (dimethylaminosulfonyl) phenyl) pyrazole-4 -Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (361) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (5-methylpyridin-1-oxide-2-yloxy) phenylmethyl) -1, 4,9-triazaspiro [5.5] Undecan,
    (362) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (2-carboxy-1-ethynyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (363) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-((1E) -2-carboxy-1-ethynyl) phenyloxy) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (364) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-aminocarbonylphenyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (365) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-aminosulfonylphenyloxy) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (366) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-benzylpyrazol-4-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (367) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (2,4-difluorophenyl) pyrazole-4- Ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (368) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (pyrrolidin-1-ylmethyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (369) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (morphon-4-ylsulfonyl) phenyl) pyra Zol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (370) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-cyanophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (371) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (N- (2-hydroxyethyl) -N -Methylaminosulfonyl) phenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (372) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (2-phenylethyl) pyrazol-4-ylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (373) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylaminomethyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (374) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (4-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (375) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (quinoxalin-2-yl) pyrazol-4-ylmethyl ) -1,4,9-triazaspiro [5.5] undecane,
    (376) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylcarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (377) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4-methylaminosulfonylphenyl) pyrazol-4-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (378) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (1,3,5-trimethylpyrazol-4-ylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (379) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (morpholin-4-ylmethyl) phenylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (380) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-methoxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (381) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylpiperazin-1-ylmethyl) phenylmethyl) -1,4,9 Triza spiro [5.5] Undecan, 3
    (382) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (pyridine-1-oxide-3-yloxy) phenylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (383) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenylsulfonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (384) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1-cyclohexylpyrazol-4-ylmethyl) -1,4, 9-triazaspiro [5.5] Undecan,
    (385) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (386) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (piperidin-1-ylmethyl) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (387) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (pyrrolidin-1-ylsulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (388) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (2,3-dihydrobenzofuran-5-ylmethyl) -1,4,9-triaza Spiro [5.5] Undecan,
    (389) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-carboxyphenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (390) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (2-hydroxyethylaminosulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (391) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3,5-dimethyl-1- (4- (2-dimethylaminoethylaminosulfonyl) phenyl) Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane, 3
    (392) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (1-hydroxy-1-phenylmethyl) phenylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (393) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (carboxymethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (394) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-hydroxypiperidin-1-ylmethyl) phenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (395) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (3-carboxyphenylmethyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (396) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (1,4-benzodioxane-6-yloxy) phenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (397) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (3-hydroxyphenyl) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (398) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (methylsulfonylamino) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (399) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (6- (4-methoxyphenyl) pyridin-3-ylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (400) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylaminocarbonylphenyloxy) phenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (401) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-chlorophenyloxy) phenylmethyl) -1,4,9-triazaspiro [ 5.5] (402) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-bis (methylsulfonyl) aminophenylmethyl) -1,4,9-triazaspiro [ 5.5] (403) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (3- (4-carboxyphenyl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (404) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (phenylaminocarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (405) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4-methylthiophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] Undecan,
    (406) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (4- (2-dimethylaminoethylaminocarbonyl) phenyloxy) phenylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (407) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-aminocarbonylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (408) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4- (dimethylaminocarbonyl) phenylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (409) (3S) -1-butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (410) 1-butyl-2,5-dioxo-3- (1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (411) (Z) -1-butyl-2,5-dioxo-3- (2-methylpropylidene) -9- (1,4-benzodioxane-6-ylmethyl) -1,4,9 -Triaza spiro [5.5] Undecan,
    (412) (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxyethyl) -9- (4-phenyloxyphenylmethyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (413) (Z) -1-butyl-2,5-dioxo-3-ethylidene-9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (414) (Z) -1-butyl-2,5-dioxo-3- (2-methylpropylidene) -9- (4-phenyloxyphenylmethyl) -1,4,9-triazaspiro [5.5 Undecan
    (415) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9-benzyloxycarbonyl-1,4,9 -Triaza spiro [5.5] Undecan,
    (416) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] Undecan,
    (417) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (418) (3R * )-1-butyl-2,5-dioxo-3-((1R *)-1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenyl Pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (419) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (6-phenyloxypyridin-3-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (420) (3R * )-1-butyl-2,5-dioxo-3-((1R *)-1-hydroxy-2-methylpropyl) -9- (4- (4-methylphenyloxy) phenyl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (421) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4-cyclohexyloxyphenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (422) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4- (tetrahydropyran-4- Yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (423) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4- (pyridin-3-yloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (424) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4-isopropylphenylmethyl) -1 , 4,9-triazaspiro [5.5] undecane,
    (425) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- ( 4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (426) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (3-methyl-5-chloro-1 -Phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (427) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4- (4-carboxyphenyloxy) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (428) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- ( Pyridin-2-yl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (429) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1- ( 4-carboxyphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (430) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9-benzyloxycarbonyl-1,4, 9-triazaspiro [5.5] Undecan,
    (431) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (432) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyloxyphenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (433) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1- Phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (434) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4-isopropylphenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (435) (3R * )-1-Butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4- (6-methylpyridine- 3-yloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (436) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1- (4-fluorophenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (437) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-methoxyphenyl Oxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (438) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-fluorophenyl Oxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (439) (3R * )-1-butyl-2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4- (4-methylsulfonyl Aminophenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (440) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9-allyloxycarbonyl -1,4,9-triazaspiro [5.5] undecane,
    (441) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -1,4,9- Triaza Spiro [5.5] Undecan,
    (442) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (3,5 -Dimethyl-1-phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (443) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (3,5 -Dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (444) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4-iso Propylphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (445) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyl Oxyphenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (446) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (4- ( 4-methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (447) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-1-cyclohexylmethyl) -9- (1,4 -Benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (448) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -1,4,9-tri Azaspiro [5.5] Undecan,
    (449) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (3,5- Dimethyl-1- (4-methylphenyl) pyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (450) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4- (4 -Methylphenyloxy) phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (451) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (1,4- Benzodioxane-6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (452) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4-isopropyl Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (453) (3R * )-1- (2-butynyl) -2,5-dioxo-3-((1R * )-1-hydroxy-2-methylpropyl) -9- (4-phenyloxy Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (454) (3R * )-1-butyl-2,5-dioxo-3-((1S * )-1-hydroxy-1-cyclohexylmethyl) -9-benzyl-1,4,9-tri Azaspiro [5.5] Undecan,
    (455) (3R * )-1-Butyl-2,5-dioxo-3-((1S * )-1-hydroxy-1-cyclohexylmethyl) -1,4,9-triazaspiro [5.5 ] Undecan,
    (456) (3R * )-1-butyl-2,5-dioxo-3-((1S * )-1-hydroxy-1-cyclohexylmethyl) -9- (4-phenyloxyphenylmethyl)- 1,4,9-triazaspiro [5.5] undecane,
    (457) (3R * )-1-Butyl-2,5-dioxo-3-((1S * )-1-hydroxy-1-cyclohexylmethyl) -9- (1,4-benzodioxane- 6-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (458) (3R * )-1-butyl-2,5-dioxo-3-((1S * )-1-hydroxy-1-cyclohexylmethyl) -9- (3,5-dimethyl-1- Phenylpyrazol-4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (459) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane ,
    (460) (3S) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (461) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (462) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxan-6-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (463) (3S) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (464) (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane ,
    (465) (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (466) (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4-phenyloxyphenylmethyl) -1,4 9-triazaspiro [5.5], Undecan,
    (467) (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxan-6-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (468) (3R) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (469) (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane ,
    (470) (3R) -1-Butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (471) (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxan-6-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (472) (3R) -1-butyl-2,5-dioxo-3-((1S) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (473) (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -1,4,9-triazaspiro [5.5] undecane ,
    (474) (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (3,5-dimethyl-1-phenylpyrazole -4-ylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (475) (3S) -1-Butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (1,4-benzodioxan-6-yl Methyl) -1,4,9-triazaspiro [5.5] undecane,
    (476) (3S) -1-butyl-2,5-dioxo-3-((1R) -1-hydroxy-2-methylpropyl) -9- (4- (4-methylsulfonylaminophenyloxy ) Phenylmethyl) -1,4,9-triazaspiro [5.5] undecane,
    (477) (3S) -2,5-dioxo-3- (3-benzyloxycarbonylaminopropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [5.5] undecane ,
    (478) (3S) -1-Methyl-2,5-dioxo-3- (3-benzyloxycarbonylaminopropyl) -9- (2-phenylethyl) -1,4,9-triazaspiro [ 5.5] undecane, or
    (479) (3S) -1-Butyl-2,5-dioxo-3-cyclohexylmethyl-9- (4-phenyloxyphenylmethyl) -9-oxide-1,4,9-triazaspiro [5.5 ] Undecane, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof.
    [7" claim-type="Currently amended] A pharmaceutical composition comprising the triazaspiro [5.5] undecane derivative represented by the general formula (I) according to claim 1, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof as an active ingredient.
    [8" claim-type="Currently amended] Agents of chemokine / chemokine receptors containing triazaspiro [5.5] undecane derivatives represented by the formula (I) as described in claim 1, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof as an active ingredient yesterday.
    [9" claim-type="Currently amended] Asthma, atopic dermatitis, urticaria containing triazaspiro [5.5] undecane derivatives represented by the formula (I) as described in claim 1, quaternary ammonium salts thereof, N-oxides thereof or non-toxic salts thereof as an active ingredient , Allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, nephritis, nephritis, hepatitis, arthritis, chronic joint rheumatism, psoriasis, rhinitis, conjunctivitis, suppression of ischemic reperfusion injury, multiple sclerosis, ulcerative colitis, acute Respiratory bowel syndrome, shock following bacterial infection, treatment of diabetes, autoimmune disease, transplant rejection, immune suppression, cancer metastasis prevention, prophylaxis and / or treatment of acquired immunodeficiency syndrome.
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    同族专利:
    公开号 | 公开日
    EP1236726A1|2002-09-04|
    EP1236726B1|2004-12-01|
    CA2394679A1|2001-06-07|
    CN1433419A|2003-07-30|
    NZ519183A|2005-02-25|
    NO20022609D0|2002-05-31|
    DE60016454T2|2005-08-04|
    CN1246321C|2006-03-22|
    JP4721087B2|2011-07-13|
    HU0300641A2|2003-06-28|
    ES2233479T3|2005-06-16|
    BR0016111A|2003-03-25|
    AU780419B2|2005-03-17|
    AT283854T|2004-12-15|
    AU1650601A|2001-06-12|
    PT1236726E|2005-04-29|
    MXPA02005465A|2003-10-15|
    US7119091B2|2006-10-10|
    KR100613176B1|2006-08-17|
    EP1236726A4|2003-01-15|
    NO20022609L|2002-07-26|
    AU780419C|2005-09-29|
    DE60016454D1|2005-01-05|
    WO2001040227A1|2001-06-07|
    TWI224597B|2004-12-01|
    US20040097511A1|2004-05-20|
    NO323631B1|2007-06-18|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    法律状态:
    1999-12-03|Priority to JP34496799
    1999-12-03|Priority to JPJP-P-1999-00344967
    2000-01-27|Priority to JPJP-P-2000-00018673
    2000-01-27|Priority to JP2000018673
    2000-02-04|Priority to JP2000027968
    2000-02-04|Priority to JPJP-P-2000-00027968
    2000-05-19|Priority to JPJP-P-2000-00147882
    2000-05-19|Priority to JP2000147882
    2000-12-01|Application filed by 오노 야꾸힝 고교 가부시키가이샤
    2000-12-01|Priority to PCT/JP2000/008517
    2003-01-09|Publication of KR20030003218A
    2006-08-17|Application granted
    2006-08-17|Publication of KR100613176B1
    优先权:
    申请号 | 申请日 | 专利标题
    JP34496799|1999-12-03|
    JPJP-P-1999-00344967|1999-12-03|
    JPJP-P-2000-00018673|2000-01-27|
    JP2000018673|2000-01-27|
    JP2000027968|2000-02-04|
    JPJP-P-2000-00027968|2000-02-04|
    JPJP-P-2000-00147882|2000-05-19|
    JP2000147882|2000-05-19|
    PCT/JP2000/008517|WO2001040227A1|1999-12-03|2000-12-01|Triazaspiro[5.5]undecane derivatives and drugs containing the same as the active ingredient|
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