• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    1450287 Pharmaceutical compositions BOBHRINGER INGELHElM GmbH 27 Feb 1974 [28 Feb 1973 26 Jan 1974] 8949/74 Heading A5B [Also in Division C2] Pharmaceutical compositions comprise a compound of the general formula R 1 = H, halogen, NO 2 , C 1-5 alkyl, C 1-4 alkoxy, C 2-5 alkenyl or alkynyl, C 1-6 alkylamino, di(C 1-6 alkyl)amino, C 1-6 alkoxy-(C 1-6 alkyl), C 1-6 alkyl- or di(C 1-6 alkyl)-amino- (C 1-6 alkyl), (CH 2 ) 0-3 -(CN, NH 2 or OH), COOH C 2-5 alkoxycarbonyl, C 3-6 alkenyloxy or alkylnyloxy, optionally substituted aliphatic or araliphatic acyl, acyloxy or acrylamino wherein each aliphatic moiety contains 1-6 carbon atoms, aromatic acyl, acyloxy or acylamino, C 3-7 cycloalkyl, QCONR 7 R 8 : Q = single bond, O, NH, CH 2 , CH 2 NH: R 7 , # =H, C 1-6 alkyl, aryl or aryloxy optionally bearing one or more substituents selected from halogen, alkyl, alkoxy, NO 2 ,CN, COOH, or NR 7 R 8 = heterocyclic group; R 2 = H, halogen, CN, NH 2 , NO 2 , C 1-4 alkyl or alkoxy, C 2-4 acyl or alkenyl, or R 1+2 = 3. 4-methylenedioxy: R 3 = H, halogen, C 1-4 alkyl or alkoxy. or R 2 +3 (bonded to adjacent carbon atoms) = (CH 2 ) 3-5 or -CH=CH-CH=CH-: R 4 = H, C 1-3 alkyl; R = C 1-3 alkyl, or R 4+5 = (CH 2 ) 4-6 or acid addition salt thereof, with or without a further active ingredient, e.g. coronary detectors, sympathicomimetics, cardiac glycosides, tranquilisers), in association with a carrier. The primary active ingredients are adrelytics and hypotensive agents.
    公开号:SU793381A3
    申请号:SU752100046
    申请日:1975-01-29
    公开日:1980-12-30
    发明作者:Кеппе Герберт；Куммер Вернер；Штэле Гельмут；Муацевиц Гайко
    申请人:К.Х.Берингер Зон (Фирма)；
    IPC主号:
    专利说明:

    active 1-aryloxy-2-hydroxy-3-alkynyl aminopropanes of the general formula D) OCHg- СНОН- СНг-NH-d -С CR, R, where Rj means a hydrogen or halogen atom, a nitro group, an alkyl group with atoms / alkoxy group with atoms C, 4) alkenyl or alkynyl group with C2-5 atoms, lower alkyl (or dialkyl) amino group, lower alkoxyalkyl or lower alkyl (or dialkyl) -aminoalkyl group, radical of the formula - (sleep-СМ, - (CHuk NH2, - ( CHa), where the host.-Starts O or an integer from 1 to 3, -COOH-COORQ and Rg means an alkyl radical with Cf-v atoms, alkenyloxy or alkynyl syrad Cal with atoms, lower aliphatic, araliphatic or aromatic acyl-acyloxy or acylamino radical, cycloalkyl radical with Cj automata -Q.-CO-NHR.Rg group, and C means a simple bond, oxygen atoms, NH-, СН2 - or an AND group and R-, and Rg are hydrogen, lower alkyl, or a heterocycle together with an N-atom, such as a pyrrolidino, pi, peridino or morFolyno radical, or substituted, if necessary, with a halo gene, alkyl, alkoxy, nitro, cyano or kAE) with a boxing group, aryl or aryloxy (preferably phenyl or phenoxy) radical; Rj. hydrogen or halogen atom, alkyl or alkoxy group with 0.4 atoms of acyl or alkenyl group e with Su cyano, amino or nitro group, or together with R 3, 4-methylenedioxy group R - hydrogen or halogen alkyl or alkoxy group with C atoms, .. together with R2, the group —CH — CH — CH — CH — or - (CH 2) n (n is an integer of 3 to 5), is a valence bond in ortho position; R (. Is a hydrogen atom or an alkyl radical with C atoms; Rg is an alkyl radical with Ct atoms, or together with R the group is (CH2) p, and p means one of the integers 4-6, or acid addition salts. Method lies in the fact that the oxazolidine derivative of the general formula // OCHO-CH-CH, p II g o N-C-C CH, y / I where K (have the values indicated in the formula T and X means -CO-, -CH .- or -CH-lower alkyl group, is subjected to hydrolysis in an aqueous-alcoholic medium, for example, using sodium hydroxide or a solution of potassium hydroxide, followed by separation of the target product in free form, in the form of a salt, a racemate of diastereomers B or optically active antipodes. The resulting 1-phenoxy-2-hydroxy-3-alkynylaminopropanes of the general formula I can be converted into their physiologically tolerable acid addition salts. Suitable acids are, for example, salt on, hydrobromide, sulfuric, methanesulfomeleic, acetic, oxalic, lactic, tartaric acid, or 3-chlorofeophyllin. 1- (2-cyanophenoxy) -3- (2-methylbutin-3-amine-2) -2-propanol hydrochloride. 2.84 g of Co, 02 mol) 3- (2-methylbutin-3-yl-2) -5- (2-cyanophenoxymethyl) -oxazolidin-2-one in 20 ml of ethanol after adding 3 g of KOH in b ml of HjO B The mixture is heated to reflux for 3 hours. After distilling off the solvent, the residue is taken up with HjO and extracted; chloroform. The chloroform solution is then removed by shaking with diluted HCf and the separated aqueous phase is made alkaline with sodium hydroxide, the base is taken up in chloroform, the organic phase is washed with HjO and dried over NaG.S04. After filtration, the CH2NOe is distilled off, and, by adding petroleum ether, the residue is recrystallized from ethyl acetate. Vkod 1.3 g; m.p. 84-8bS (base); m.p. mixtures with an identical substance of 83-85 ° C. In the same way as in the above example, compounds of the formula i are obtained, shown in the table.
    Table continuation
    权利要求:
    Claims (2)
    [1]
    K ^ - lower alkyl- (or dialkyl) -amino group, lower alkoxyalkyl or lower alkyl (or dialkyl) «- aminoalkyl group;
    0 — simple bond, oxygen atom, ΝΗ-, СН ^, СН ^ -ΝΗ-;
    K 7 and Κθ - substituted or unsubstituted aryl radical, '
    K2 ~ acyl group.
    Sources of information taken into account in the examination
    1. The patent of Switzerland to »4 356 59, cl. From 07 to 93/06, 1970.
    [2]
    2. USSR patent by request
    No. 1705730/04, cl. C 07 C 93/06,
    1969.
    2.7)
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    同族专利:
    公开号 | 公开日
    GB1450287A|1976-09-22|
    JPS5024232A|1975-03-15|
    SE411897B|1980-02-11|
    ES436315A1|1977-01-01|
    ATA104774A|1975-09-15|
    CH605690A5|1978-10-13|
    NL169733C|1982-08-16|
    BG20566A3|1975-12-05|
    ES423466A1|1977-01-16|
    BG20564A3|1975-12-05|
    ES436311A1|1977-01-01|
    PL91560B1|1977-03-31|
    DD110652A5|1975-01-05|
    BG21394A3|1976-05-20|
    CA1062717A|1979-09-18|
    CH605637A5|1978-10-13|
    BG20565A3|1975-12-05|
    HU168598B|1976-06-28|
    NO740670L|1974-08-29|
    CH605689A5|1978-10-13|
    NO138062C|1978-06-21|
    IE39482L|1974-08-28|
    BG21208A3|1976-03-20|
    CH605691A5|1978-10-13|
    CH605636A5|1978-10-13|
    YU109580A|1982-06-30|
    MX4588E|1982-06-25|
    AU6606574A|1975-08-28|
    FR2218900B1|1978-01-06|
    CS186263B2|1978-11-30|
    ES436314A1|1977-01-01|
    BG20335A3|1975-11-05|
    PL93591B1|1977-06-30|
    NL169733B|1982-03-16|
    BG20334A3|1975-11-05|
    FI62054B|1982-07-30|
    IE39482B1|1978-10-25|
    ES436312A1|1977-01-01|
    FI62054C|1982-11-10|
    FR2218900A1|1974-09-20|
    CH605638A5|1978-10-13|
    MX4592E|1982-06-25|
    YU50074A|1982-06-30|
    CH605639A5|1978-10-13|
    DK143128C|1981-11-16|
    JPS594417B2|1984-01-30|
    AT330150B|1976-06-10|
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    PH9722A|1976-02-27|
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    引用文献:
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    US3541130A|1967-02-06|1970-11-17|Boehringer Sohn Ingelheim|1--2-hydroxy-3-tert.-butylamine propanes|
    GB1199037A|1967-09-27|1970-07-15|Ici Ltd|Alkanolamine Derivatives|US4038313A|1970-01-08|1977-07-26|Ciba-Geigy Corporation|Cycloalkylureido phenoxy propanolamines|
    US4078146A|1972-07-06|1978-03-07|Aktiebolaget Hassle|Phenoxy propanolamines|
    US4035420A|1972-07-06|1977-07-12|Aktiebolaget Hassle|Substituted ureido alkylene phenoxy propanolamines|
    GB1374366A|1972-07-21|1974-11-20|Science Union & Cie|Propanol derivatives and a process for their preparation|
    AT334385B|1973-12-20|1976-01-10|Chemie Linz Ag|PROCESS FOR THE PREPARATION OF NEW PHENOXYPROPYLAMINE DERIVATIVES AND THEIR SALTS|
    US4243681B1|1977-10-11|1985-09-10|
    DE2805404A1|1978-02-09|1979-08-16|Merck Patent Gmbh|1-ARYLOXY-3-NITRATOALKYLAMINO-2-PROPANOLS AND METHOD FOR THE PRODUCTION THEREOF|
    DE3009036A1|1980-03-08|1981-09-24|C.H. Boehringer Sohn, 6507 Ingelheim|NEW L-2-HYDROXY-3-ALKINYLAMINOPROPANES AND METHOD FOR THEIR PRODUCTION|
    DE3009047A1|1980-03-08|1981-09-24|C.H. Boehringer Sohn, 6507 Ingelheim|NEW L-2-HYDROXY-3-ALKINYLAMINOPROPANES AND METHOD FOR THEIR PRODUCTION|
    US4387103A|1980-11-28|1983-06-07|American Hospital Supply Corporation|Method for treatment or prophylaxis of cardiac disorders|
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    DE3133719A1|1981-08-26|1983-03-10|Boehringer Ingelheim KG, 6507 Ingelheim|NEW 1-ARYLOXY-3-ALKINYLAMINO-2-PROPANOLS AND METHOD FOR THE PRODUCTION THEREOF|
    JPH02130007U|1989-03-31|1990-10-26|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    DE2309887A|DE2309887C2|1973-02-28|1973-02-28|1-aryloxy-2-hydroxy-3-alkynylaminopropane derivatives and their physiologically acceptable acid addition salts, pharmaceutical preparations and manufacturing processes for the compounds|
    DE19742403809|DE2403809C2|1974-01-26|1974-01-26|1-Aryloxy-2-hydroxy-3-alkynylaminopropanes and processes for their manufacture and pharmaceutical preparations|
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