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    • 专利摘要:
    summary combinations of active substances; cosmetic or dermatological preparations; non-therapeutic cosmetic use of preparations or combinations of active substances; and combinations of active substances and preparations combinations of active substances of alkylamidothiazoles and one or more preservatives cosmetically or dermatologically harmless. 1/1
    公开号:BR112015022148B1
    申请号:R112015022148-3
    申请日:2014-02-14
    公开日:2020-03-24
    发明作者:Tobias Mann；Cathrin Scherner；Ludger Kolbe；Jan Batzer
    申请人:Beiersdorf Ag；
    IPC主号:
    专利说明:

    COMBINATIONS OF ACTIVE SUBSTANCES, COSMETIC OR DERMATOLOGICAL PREPARATIONS AND COSMETIC USE
    DESCRIPTION [001] The present invention relates to combinations of active substances of alkylaminothiazoles and one or more preservatives cosmetically or dermatologically harmless. In addition, the present invention relates to cosmetic or dermatological preparations with a content of that combination of active substances, as well as their use to lighten human skin. Melanocytes are responsible for the pigmentation of the skin, which are found in the lower layer of the epidermis, the basal extract, in addition to the basal cells as - depending on the type of skin or isolated or, occurring more or less clustered - the cells that form pigment.
    [002] As characteristic cellular organelles, melanocytes contain melanosomes, in which melanin is formed. Among others, in stimulation through UV radiation more melanin is formed. This is transported through the live layers of the epidermis (keratinocytes), finally, to the horny layer (corneocytes) and causes a brownish to black-brown skin color more or less accentuated.
    [003] Melanin is formed as the final stage of an oxidative process, in which tyrosine, with the cooperation of the enzyme tyrosinase, is transformed through several intermediate steps, into brown to black-brown eumelanins (DHICA and DHI melanin) or with the participation of sulfur-containing compounds in the reddish pheomelanin. Melanins
    Petition 870190105153, of 10/17/2019, p. 5/16
    2/77
    DHICA and DHI are formed through all the intermediate steps dopaquinone and dopachrome. The latter, partially with the participation of other enzymes, is reacted either to indole-5,6-quinon-carboxylic acid or to indole-5,6quinone, from which the two mentioned eumelanins are formed.
    [004] The formation of pheomelanin occurs, among others, through the intermediate products dipaquinone and cysteinyl dopa. The expression of melanin-synthesizing enzymes is controlled by a specific transcription factor (microphthalmia-associated transcription factor, MITF). In addition to the enzymatic processes of melanin synthesis described, other proteins in melanosomes are still important for melanogenesis. An important role seems to be assumed here by the so-called p-protein, the exact function of which is not yet clear.
    [005] In addition to the process of melanin synthesis in melanocytes described above, in skin pigmentation the transfer of melanosomes, their permanence in the epidermis, as well as their degradation and melanin degradation, is also of decisive importance. It was possible to demonstrate that the PAR-2 receptor is important for the transport of melanosomes from melanocytes to keratinocytes (M. Seiberge collaborators, 2000, J. Cell. Sci., 113: 3093-101).
    [006] In addition, the size and shape of melanosomes have an influence on the light scattering properties and thus on the appearance of the skin color. Thus, in black Africans many large spheroidal melanosomes are found, isolated, while in Caucasians melanosomes are found
    3/77 quite small, which are present in groups.
    [007] Problems with hyperpigmentation of the skin have several causes or are concomitant to many biological processes, for example, UV radiation (for example, freckles, Ephelides), genetic disposition, abnormal skin pigmentation during healing or wound healing ( posinflammatory hyperpigmentation) or skin aging (for example, Lentigines seniles).
    [008] After inflammatory reactions, the skin's pigmentation system reacts with partially opposite reactions. Both hyper- and post-inflammatory hypopigmentations can occur. Postinflammatory hypomelanosis occurs, among others, often in association with atopy, lupus erythematosus and psoriasis. The different forms of reaction of the human skin pigmentation system as a result of inflammatory symptoms are only understood in a very incomplete way.
    [009] Problems with post-inflammatory hyperpigmentation often occur with darker skin types. In particular, in brown males the problem of Pseudofollikulitis barbae is known, which occurs with cosmetically unwanted or caused abnormal pigmentation. Also forms of melasma, which occur, in particular, in women of Asian affiliation on the face and in the neckline, as well as different forms of irregular skin pigmentation, are included in post-inflammatory hyperpigmentations. In addition, dark circles under the eyes are also considered as a form of post-inflammatory hyperpigmentation, with the inflammation of origin mostly occurring subclinically.
    4/77 [010] In many cases, such abnormal post-inflammatory pigments are still reinforced by the action of sunlight (UV light), without UV-induced inflammation (heat stroke) occurring.
    [011] Active substances and preparations are known to react against skin pigmentation. In practical use, there are essentially hydroquinone-based preparations, which, on the one hand, show their effect only after application for several weeks, the application of which is too long, on the other hand, is questionable for toxicological reasons. Albert Kligman and colleagues developed a so-called tri-formula, which represents a combination of 0.1% tretinoin, 5.0% hydroquinone, 0.1% dexamethasone (A. Kligman, 1975, Arch. Dermatol., 11 1: 40 -48). However, this formulation is also very controversial due to possible irreversible changes in the skin's pigmentation system.
    [012] In addition, skin peeling methods (chemical and mechanical peels) are applied, which can, however, frequently lead to inflammatory reactions and, due to post-inflammatory hyperpigmentations that have subsequently occurred, can even lead to stronger pigmentation instead of a weaker one. All of these frequent processes, which are also applied for the treatment of post-inflammatory hyperpigmentations, stand out for decisive side effects.
    [013] In addition, several other substances are known, which are described for a skin lightening efficacy. Among others, hexadecen-1,16-dicarboxylic acid, Kojic acid can be mentioned here
    5/77 derivatives, arbutin, ascorbic acid and derivatives, flavonoids, ellagic acid and derivatives, tranexamic acid and various resorcinol derivatives, such as, for example, 4-n-butylresorcinol, 4-n-hexyl-resorcinol and 4- (1-phenylethyl) benzene- 1,3-diol.
    [014] J.M. Ready describes in a publication (Bioorganic & Medicinal Chemistry Letter 17 (2007) 6871-6875 the effect of thiazole derivatives, among others, substituted for the inhibition of Mushroom tyrosinase.
    [015] In the patent application of the company Shiseido (WO 2009099195), thiazolamines or substituted hydrothiazolamines to lighten the skin are described.
    [016] The substances described in the state of the art mentioned above stand out for their moderate effectiveness.
    [017] Dark circles can also be formed as a consequence of a pigmentation disorder, and in addition, these also occur as a reaction to general stress, such as, for example, little sleep or simply due to excessive effort From the eyes. In younger people, the symptoms disappear again after a satisfactory night's rest, however, for prolonged periods the condition can become chronic and be very disturbing for the respective people. Also against such skin symptoms there is a lack of sufficiently promising active substances and treatment possibilities.
    • target of the following invention was, therefore, to remedy the disadvantageous state of the art.
    [018]
    This objective is solved by combinations
    6/11 of active substances of alkylamidothiazoles and by one or more preservatives cosmetically or dermatologically harmless.
    [019] Advantageous modalities of the present invention are also cosmetic or dermatological preparations with a content of this combination of active substances, as well as their use to lighten human skin.
    [020] Advantageously, the preparations according to the invention contain one or more preservatives, the total amount of preservatives being, for example, 0.00001% by weight to 10% by weight, preferably 0.001% by weight. 5% by weight, in particular, 0.005% by weight to 3% by weight, based on the total weight of the preparations, to make cosmetic preparations available.
    [021] Preservatives advantageous in the sense of the present invention are [022] ethylparaben (120-47-80), propylparaben (94-13-3), methylisothiazolinone (2682-20-4), methylpropanediol (2163-42-0), butylene glycol (107-88-0), propylene glycol (5755-6, 4254-14-2, 4254-15-3), ethylhexylglycerin (70445-339), sodium benzoate (532-32-1), 1, 2-hexanediol (6920-22-5), 1,3-butanediol (107-88-0), 1,2-octanediol (11 17-86-8), calcium sorbate (24634-61-5 / 590- 00-1), DMDM hydantoin (6440-58-0), benzyl alcohol (100-51 -6), phenoxyethanol (12299-6), dehydroacetic acid (520-45-6), pyroctone olamine (68890-66-4 ), methylparaben (99-76-3), alcohol (64-17-5), octanohydroxamic acid (7377-03-9), benzethonium chloride (121-54-0), glyceryl caprylate (26402-26-6 ), pentylene glycol (111-29-5), lauroethyl arginate (6037277-2), salicylic acid (69-72-7), benzoic acid (65-85-0),
    7/77 propionic acid (79-09-4), sorbic acid (110-44-1), with salicylic acid, benzoic acid and dehydracetic acid being preferred and it can also be advantageous to use hydrosoluble metal salts physiologically compatible with these acids.
    [023] Preferred preservatives are: methylisothiazolinone (2682-20-4), potassium sorbate (2463461-5 / 590-00-1), sodium benzoate (532-32-1), ethylhexylglycerone (70445-33-9) , benzyl alcohol (100-51 -6), benzethonium chloride (121-54-0), salicylic acid (69-72-7), benzoic acid (65-85-0), propionic acid (79-09-4 ), sorbic acid (110-44-1).
    [024] The preparations according to the invention preferably contain 0.0001 to 10% by weight, of one or more preservatives, preferably 0.001 to 5% by weight, of one or more preservatives, in particular, preferably 0.005 to 3% in weight, of one or more preservatives.
    [025] Advantageously, in particular, the preparations according to the invention or uses are distinguished by the fact that the preparations contain 0.000001 to 10% by weight, in particular, 0.0001 to 3% by weight, more particularly 0.001 to 1% by weight, of one or more alkylamidothiazoles, based on the total weight of the preparation.
    [026] Alkylamidothiazoles advantageous in the sense of the present invention are substances of the general formula
    Rj [027] in which
    8/77 [028] R 1 , R 2 , X and Y can be different, partially equal or completely the same and independently of each other can represent:
    [029] R 1 = -C 1 -C 24 -alkyl (linear and branched), -C 1 -C 24 -alkenyl (linear and branched), -C 1 -C 8 cycloalkyl, -C 1 -C 8 -cycloalkyl -alkylhydroxy, -C 1 -C 24 alkylhydroxy (linear and branched), -C1-C24 alkylamine (linear and branched), -C1-C24-alkylaryl (linear and branched), -C1-C24-alkyl- aryl-alkyl-hydroxy (straight and branched), -C1-C24-alkyl-heteroaryl (linear and branched), C1-C24-alkyl-O-C1-C24-alkyl (linear and branched), -C1-C24alkyl-morpholino , -C1-C24-alkyl-piperidine, -C1-C24-alkylpiperazine, -C1-C24-alkyl-piperazine-N-alkyl, [030] R 2 = H, -C 1 -C 24 -alkyl (linear and branched) ), -C1-C24-alkenyl (linear and branched), -C1-C8cycloalkyl, -C1-C24-hydroxyalkyl (linear and branched), C1-C24-alkylaryl (linear and branched), -C1-C24-alkyletheroaryl (linear and branched), [031] X = -H, -C1-C24-alkyl (linear and branched), -C1-C24-alkenyl (linear and branched), -C1-C8cycloalkyl, -C1-C24-aryl (optionally substituted one or more times with -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN), -C1C24-heteroaryl (optionally substituted one or more times with -OH, -F, -Cl, -Br , -I, -OMe, -NH 2 , -CN), -C 1 -C 24 Alkylaryl (linear and branched), -C1-C24-alkyl-heteroaryl (linear and branched), -aryl (optionally substituted one or more times with -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN), phenyl, -2,4-dihydroxyphenyl, -2,3-dihydroxyphenyl, -2,4dimethoxyphenyl, -2 , 3-dimethoxyphenyl, [032]
    H,
    -C1-C24-alkyl (linear
    Branched 9/11), -C 1 -C 24 -alkenyl (linear and branched), -Ci-C 8 cycloalkyl, -C 1 -C 24 -aryl, -C 1 -C 24 -heteroaryl, -C 1 -C 24 alkylaryl (linear and branched), -C 1 -C 24 -alkyl-heteroaryl (linear and branched), -aryl, -phenyl, -2,4-dihydroxyphenyl, -2,3-dihydroxyphenyl, -2,4-dimethoxyphenyl , -2,3dimethoxyphenyl, -COO-alkyl, -COO-alkenyl, -COOcycloalkyl, -COO-Aryl, -COO-Heteroaryl, [033] and X, Y can optionally also represent condensed aromatic compound, [034] where X and Y can form homo or heterocyclic, aliphatic or aromatic ring systems with up to n ring forming atoms and the number n can take values from 5 to 8 and the respective ring systems, in turn, can be substituted with up to 1 alkyl groups, hydroxyl groups, carboxyl groups, amino groups, nitrile functions, sulfur-containing substituents, ester groups and / or ether groups.
    [035] The mentioned thiazoles can be present both as free bases and also as salt: for example, as fluoride, chloride, bromide, iodide, sulfate, carbonate, ascorbate, acetate or phosphate. In particular, as halogen salts, such as, for example, chloride and bromide.
    [036] In addition, an advantageous embodiment of the present invention in cosmetic or dermatological preparations consists of an effective content of one or more of the alkylamidothiazoles mentioned above.
    [037] According to the invention, moreover, it is the use of the alkylamidothiazoles mentioned above for the treatment and / or prophylaxis of unwanted skin pigmentation.
    10/77 [038]
    In this case, the prophylaxis treatment of unwanted skin pigmentation can be carried out both in the cosmetic and pharmaceutical fields.
    [039]
    In this case, the pathological pharmaceutical treatment (or is understood, in the first line, in dermatological states) of the skin, while the cosmetic treatment and / or the prophylaxis of unwanted skin pigmentation refers, in the first line, to healthy skin.
    [040]
    Advantageously, it is selected from the group of substituted phenyls, where the substituents can be selected from the group -H,
    -OH, -F,
    -Cl, -Br, -I,
    OMe, -NH 2 , acetyl and may be the same or different.
    -CN,
    [041]
    Particularly advantageously, X is selected from the group of phenyl groups substituted with one or more hydroxy groups, where the substituent can be selected from the group -H, -OH,
    -F, -Cl, -Br, -I, -OMe, -NH 2 ,
    CN, acetyl and the following generic structure is preferred, in which Y, RI and R2 can have the properties defined above.
    R 1 [042] Particularly advantageous are those compounds, in which
    11 / ΊΊ
    HO j ' 1
    XY = H [043] Ri represents -Ci-C 24 -Alkyl (linear and branched), -Ci-C 2 4-alkenyl (linear and branched), -Ci_C 8 cycloalkyl, -Ci_C 8 -cycloalkyl-alkylhydroxy, -Ci-C 24 alkylhydroxy (linear and branched), -Ci-C 24 alkylamine (linear and branched), -Ci-C 24 -alkylaryl (linear and branched), -Ci-C 24 -alkyl-aryl-alkyl -hydroxy (linear and branched), -Ci-C 24 -alkyl-heteroaryl (linear and branched), -Ci-C 24 -alkyl-O-Ci-C 24 -alkyl (linear and branched), -Ci-C 24 alkyl-morpholino, -Ci-C 24 -alkyl-piperidine, -Ci-C 24 -alkipiperazine, -Ci_C 24 -alkyl-piperazine-N-alkyl, [044] R 2 represents H, -Ci-C 24 -alkyl ( linear and branched).
    [045] Z represents -H, -OH, -F, -Cl, -Br, -I, OMe, -NH 2 , -CN, acetyl.
    [046] Particularly preferred are those compounds, in which
    HCk
    Li x = [047] Y represents H [048] Ri represents -Ci-C 24 -alkyl (linear and branched), -Ci-C 24 -alkenyl (linear and branched), -Ci-C 8 cycloalkyl, -Ci- C 8 -cycloalkyl-alkylhydroxy, -Ci-C 24 alkylhydroxy (linear and branched), -Ci-C 24 -alkylamine (linear and branched), -Ci-C 24 -alkylaryl (linear and branched), - Ci-C 24 -alkyl-aryl-alkylhydroxy (straight and branched), -Ci-C 24 -alkyl-heteroaryl (linear and branched),
    12/77
    -Ci C 24 -Alkyl-O-C1-C 24 -alkyl (straight and branched), -C1-C24 alkyl-morpholine, -Ci-C 24 -alkyl-piperidine, -Ci-C 24 -alkylpiperazine, -Ci- C 24 -alkyl-piperazine-N-alkyl, [049] R 2 represents H.
    [050] The compounds
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) pivalamide

    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) isobutyramide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide
    13/77
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) heptanamide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -6hydroxyhexanamide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -3hydroxypropanamide
    14/77
    Ν- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -2methoxyacetamide
    -amino-N- (4- (2,4-dihydroxyphenyl) thiazol-2yl) propanamide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) acetamide
    15/77
    (hydroxymethyl) cyclohexanecarboxamide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2yl) cyclohexanecarboxamide
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -2- (4 (hydroxymethyl) phenyl) acetamide [051] are preferred according to the invention.
    16/77 [052] It was surprisingly possible to demonstrate that the alkylamidothiazoles according to the invention in combination with the UV filters according to the invention have an increased efficiency.
    DESCRIPTION OF THE EFFECTIVENESS RESEARCH METHOD:
    [053] The effectiveness of thiazoles was confirmed with an enzyme test, in which the conversion of L-DOPA to Ldopaquinone was measured by human tyrosinase. In this method known from the literature (Winder, AJ and Harris, H., New assays for the tyrosine hydroxylase and dopa oxydase activities of tyrosinase. Eur. J. Biochem. (1991), 198, 31726) the reaction product L-dopaquinone is reacted with MBTH (3-methyl-2-benzothiazoline hydrazone) to form a pink substance, whose increase over time is measured by absorption at 490 nm. The table shows, by way of examples, the efficacy data for some of the claimed substances. Of these it can be concluded, that the substances according to the invention are extremely effective substances that inhibit pigmentation.
    Table: Inhibition of tyrosinase activity by combining N-(4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide with variouspreservatives Substance Inhibition(% of control) Concentration N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 38.2 0.4 pg / mL Sodium benzoate 43.6 200 g / mL N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide + sodium benzoate 58.0 200.4 pg / mL
    17/77
    N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) isobutyramide 38.2 0.4 pg / mL Potassium sorbate 42.0 200 g / mL N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) isobutyramide + potassium sorbate 62.7 200.4 pg / mL
    ALKYLAMIDOTIAZOL SYNTHESIS PROCEDURES
    SELECTED EXAMPLE:
    2-BROMO-2,4'-BIS-METOXICARBONYLOXI-ACETOPHENONE:
    PG = COOCH 3 [054] Mitchell, David; Doecke, Christopher W .; Hay, Lynne A.; Koenig, Thomas M.; Wirth, David D. Tetra hedron Letters, 1995 [055] A solution of 60 g (369 mmol) of 2,4-dihydroxyacetophenone and 186 ml triethylamine in 900 ml tetrahydrofuran was cooled to 0 ° C and 93 ml of chloroformic acid methyl ester in 400 ml of tetrahydrofuran was added slowly to the drops. A white precipitate forms. After stirring for 3 hours at room temperature, the reaction is complete (DC control). The precipitate was aspirated and washed with plenty of tetrahydrofuran. The filtrate was centrifuged to dryness, recovered in ethyl acetate, washed with HCl and 1N NaCl solution (saturated) and dried over magnesium sulfate, filtered over magnesium sulfate and the ethyl acetate was concentrated on the rotary evaporator. 105 g of 2,4-bis-methoxycarbonyloxy-acetophenone were obtained. 1 H NMR (DMSO-D6): 8.05
    18/77 (d, 1 Η), 7.38 (d, 1 Η), 7.36 (s, 1 Η), 3.86 (d, 6H). The product was used without further purification. To the solution of 105 g of 2,4-bis-methoxycarbonyloxy-acetophenone in chloroform (1,000 ml), 63 g (392 mmol) of bromine in 450 ml of chloroform were added to the drops within 3 hours. Then, the reaction was stirred for another 15 minutes at room temperature. The solvent was centrifuged. The residue was mixed in ethyl acetate / n-hexane, the precipitate formed was aspirated. Recrystallization from ethyl acetate / n-hexane provided 100 g of 2-bromo-2 ', 4'-bis-methoxycarbonyloxyacetophenone. NMR- 1 !! (DMSO-D 6 ): 8.11 (d, 1 H), 7.42 (m, 2H), 4.87 (s, 2H), 3.87 (s, 3H), 3.85 (s, 3H) ppm; melting point: 73 to 74 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) PIVALAMIDE:
    previously introduced in toluene (1,000 ml) and 100 g (829 mmol) of pivaloyl chloride were added to the drops. The reaction solution was boiled at reflux for 3 hours, forming two phases. The upper phase was decanted and cooled. The precipitated colorless needles were aspirated and washed with cyclohexane and dried in vacuo. Yield: 64 g. X H NMR (DMSO-d6): 10.27 (s, 1H), 9.74 (s, 1H), 9.40 (s, 1 H), 1.19 (s, 9H) ppm.
    [057] 107.7 g (310 mmol) of 2-bromo-24'-bis
    19/77 methoxycarbonyloxy-acetophenone was boiled at reflux for 0.5 hour with 49.7 g (13.6 mmol) of N-pivaloiltiourea and 39.2 g (466 mmol) of NaHCO 3 in 1.21 ethanol. The reaction solution was cooled and mixed with 50.6 g (1.27 mol) of NaOH in 250 ml of water. After stirring for 30 minutes at room temperature, the reaction solution was recovered with 300 ml of water and neutralized with 2N HCl. The resulting precipitate was filtered and recrystallized from ethanol / water. 80 g of thiazole were obtained. X H NMR (DMSO-D 6 ): 11.77 (s 1, 1 H), 11.02 (s 1, 1 H), 9.47 (s 1, 2H), 7.65 (d, 1 H ), 7.39 (s, 1 H), 6.30 (s, 1 H), 6.28 (d, 1 H), 1.27 (s, 9H) ppm; melting point: 257 to 259 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) ISOBUTYRAMID:
    TcilBl 'NH.
    (1.5
    114
    HO.
    .OH [058] mol) of thiourea were previously introduced in toluene (800 ml) and 80 g (0.75 mol) of isobutyryl chloride were added to the drops, resulting in two phases. The upper phase was decanted and cooled. The precipitated white crystals were aspirated and washed with toluene and dried in vacuo. Yield: 62 g. NMR 1 (DMSO-D 6 ): 11.03 (s 1, 1 H), 9.66 (s 1, 1 H), 9.35 (s 1, 1 H), 2.72 (m, 1 H ), 1.03 (2.6H) ppm;
    [059] g (260 mmol) of 2-bromo-2 ', 4'-bismethoxycarbonyloxy-acetophenone were boiled at reflux for
    0.5 hour with 37.5 g (260 mmol) of N-isobutyrylthiourea and 32 g
    20/77 (3 80 mmol) of NaHCO 3 in 1,000 ml of ethanol. The reaction solution was cooled and mixed with 41 g (0.93 mol) of NaOH in 250 ml of water. After stirring for 30 minutes at room temperature, the reaction solution was recovered with 300 ml of water and adjusted to pH = 3 with 2N NCI. The resulting precipitate was filtered and recrystallized from ethanol / water.
    56 were obtained g thiazole. NMR 1 H (DMSO-D 6 ): 12.16 (s 1, 1 H), 10.88 (s 1, 1 H), 9.47 (s 1, 1 H), 7.65 (m, 1 H) , 7.41 (s, 1 H), 6.32 (m , 2H), 2.75 (m, 1 H), 1.14 (d, 6H) ppm. Fusion point: 243 at 245 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) -BUTYRAMID:

    thiourea were [060] 143 g (1.88 mol) of previously introduced in toluene (1,000 ml) and 100 g (0.93 mol) of n-butyryl chloride were added to the drops, resulting in two phases. The upper phase was decanted and cooled. The slightly yellowish precipitated crystals were aspirated and washed with toluene and dried in vacuo. Yield: 88 g. Y-NMR (DMSO-D s ): 11.03 (s 1, 1 H), 9.65 (s 1, 1 H), 9.33 (s 1, 1 H), 2.33 (t, 2H) , 1.53 (m, 2H), 0.86 (t, 3H) ppm; melting point: 115 to 188 ° C [061] 92 g (265 mmol) of 2-bromo-2 ', 4' -bismethoxycarbonyloxy-acetophenone were boiled at reflux for 0.5 hour with 38.75 g (265 mmol) of N-butyrylthiourea and 34 g (3 97 mmol) of NaHCO 3 in 900 ml ethanol. The reaction solution was cooled and mixed with 37 g (0.93 mol) of NaOH in 300
    21/77 ml of water. After stirring for 30 minutes at room temperature, the reaction solution was recovered with 300 ml of water and neutralized with 2N HCl. The resulting precipitate was filtered and recrystallized from ethanol / water. 67 g of thiazole were obtained. 1 H NMR (DMSO-D 6 ): 12.18 (s 1, 1 H), 10.89 (s 1, 1 H), 9.48 (s 1, 1 H), 7.65 (1 arom, H), 7.40 (s, 1 H), 6.31 (2 arom, H), 2.43 (t, 2H), 1.64 (m, 2H), 0.91 (t, 3H) ppm . Melting point: 227 to 229 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) -ACETAMIDE:
    THE
    HO.
    OH [062]
    4.71 g (13.6 mmol) of bis-methoxycarbonyloxy-acetophenone were boiled for 0.5 h at reflux with 1.61 g (13.6 mmol) of N-acetylthiourea and 1.72 g (20.4 mmol) of NaHCO 3 in 45 ml of ethanol. The reaction solution was cooled and mixed with 2.0 g (50 mmol) of NaOH in 20 ml of water. After stirring for 20 minutes at 0 ° C, the reaction solution was recovered with 30 ml of water and neutralized with semi-concentrated HCl. The resulting precipitate was filtered and recrystallized from ethanol / water. 2.73 g of product were obtained. 1 H NMR (DMSO-Ds): 12.20 (b, 1 H), 10.85 (s, 1 H), 9.46 (s, 1 H), 7.64 (m, 1 H), 7 , 38 (s, 1 H), 6.28 (m, 2H), 2.15 (s, 3H) ppm; melting point: 264 to 264 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) -4 (HYDROXIMETH) CYCLEEXANOCARBOXAMIDE:
    HD.
    The [063]
    Execution analogous to literature.
    22/77 [064] BANYU Pharmaceutical Co., Ltd., EP2072519
    Al, 2009 [065] Yield: 96%, NMR X H (DMSO-D 6 ): 12.03 (s 1, 1 H), 3.85, 3.82 (2 xd, 2H), 2.50, 2.47 (2 xm, 1 H), 2.00 (s, 3H), 0.95 to 1.90 (m, 9H) ppm;

    [066] 95 g (0.47 mol) of 4acetoxymethylcyclohexanecarboxylic acid were heated to reflux for 2 hours in 350 ml of thionyl chloride. After removing excess thionyl chloride in a vacuum, the residue is recovered in 1 liter of toluene and 71 g (0.94 mol) of thiourea are added. The reaction solution was boiled at reflux for 3 hours and then filtered hot. After cooling the mother liquor, the resulting white crystals were aspirated, washed with toluene and dried in a vacuum.
    Yield: 59 g. X H NMR (DMSO-D 6 ): 11.03, 10.97 (2 xs, 1
    H), 9.64 (s 1, 1 H), 9.35 (s 1, 1 H), 3.93, 3.82 (2 x d, 2H),
    2.61, 2.42 (2 x m, 1 H), 2.00 (s, 3H), 1.60 (m, 8H), 1.35,
    0.94 (2 x m, 1 H) ppm.
    [067] 79 g (228 mmol) of 2-bromo-2 ', 4'-bismethoxycarbonyloxy-acetophenone were boiled at reflux for
    0.5 hour with 59 g (228 mmol) of N- (4acetoxymethylcyclohexylcarbonyl) thiourea and 29 g (340 mmol) of NaHCO 3 in 1,000 ml of ethanol. The reaction solution was
    28 / ΊΊ cooled and mixed with 73 g (1.8 mol) of NaOH in 300 ml of water. After stirring for 30 minutes at room temperature, the reaction solution was recovered with 300 ml of water and adjusted to pH 3 with 2N HCl. The resulting precipitate was filtered and recrystallized from ethanol / water. 47 g of thiazole were obtained. 1 H NMR NMR (DMSO-D s ): 12.15, 12.10 (2 xs, 1 H), 10.96 (2 xs, 1 H), 9.47 (br, 2H), 7.64 ( d, 1 H), 7.39 (s, 1 H), 6.29 (m, 2H), 4.40 (br, 1 H), 3.32, 3.23 (2 xd, 2H), 2 , 65, 2.44 (2 xm, 1 H), 1.90 (m, 1 H), 1.78 (m, 2H), 1.50 (m, 5H), 0.94 (m, 1 H ) ppm. Melting point: 152 to 160 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) CYCLEEXANOCARBOXAMIDE

    previously introduced in toluene (500 ml) and 50 g (0.34 mol) of cyclohexanoyl chloride were added to the drops. The reaction solution was boiled at reflux for 3 hours, resulting in two phases. The upper phase was decanted and cooled. The precipitated crystals were aspirated, washed with toluene and recrystallized from methanol. Yield: 35 g. X H NMR (DMSO-Ds): 10.98 (s 1, 1 H), 9.65 (s 1, 1 H), 9.32 (s 1, 1 H), 2.49 (t, 1 H ), 1.75 (m, 4H), 1.61 (m, 1 H), 1.18 (m, 5H) ppm.
    [069] 92 g (265 mmol) of 2-bromo-2 ', 4' -bismethoxycarbonyloxy-acetophenone were boiled at reflux for 0.5 hour with 49.4 g (265 mmol) of N-cyclohexaneylthiourea and 34
    24/77 g (3 97 mmol) of NaHCO 3 in 900 ml ethanol. The reaction solution was cooled and mixed with 37 g (930 mmol) of NaOH in 300 ml of water. After stirring for 30 minutes at room temperature, the reaction solution was recovered with 300 ml of water and neutralized with 2N HCI. The ethanol was largely removed on the rotary evaporator. The resulting precipitate was filtered and recrystallized from ethanol / water. 70 g of thiazole were obtained. NMR '''H (DMSO-D s ): 12.14 (s 1, 1 H), 11.00 (s 1, 1
    H), 9.48 (s 1, 1 H), 7.64 (1 arom, H) , 7.39 (s, 1 H), 6.30 (2 arom, H) , 2 , 49 (m, 1 H) , 1 84 (m, 2H), 1.76 (m, 2H), 1, 65 (m, 1 H), 1, 42 (m, 2H), 1, 25 (m, 3H) ppm. bridge > from Fusion: 262 a
    266 ° C.
    N- (4- (2,4-DIHYDROXYphenyl) THIAZOL-2-IL) -2- (4 (HYDROXIMETHYL) PHENYL) ACETAMIDE
    2. HjO, 1ΰ0 · ϋ
    Action Fyrkin CHCIj, ffl'C
    [070] Execution similar to the literature.
    [071] BANYU Pharmaceutical Co., Ltd., EP2072519
    Al, 2009 [072] Yield: 76%, X H NMR (DMSO-D 6 ): 12.31 (s 1, 1 H), 7.26 (m, 4H), 5.05 (s, 2H), 3.57 (s, 2H), 2.05 (s, 3H) ppm;

    [073] 3.7 g (18 mmol) of 425/11 acetoxymethylphenylacetic acid were heated for 2 hours at reflux in 40 ml of thionyl chloride. After removing excess thionyl chloride in vacuo, the residue was taken up in 70 ml of toluene and 2.7 g (36 mmol) of thiourea was added. The reaction solution was boiled for 3 hours at reflux and then the solvent was removed in vacuo. Purification was performed by column chromatography with cyclohexane / acetic ester 1/1 on silica gel. Yield: 2.7 g. 1H NMR (DMSO-D s ): 11.29 (ls, 1 H), 9.55 (ls, 1 H), 9.40 (ls, 1 H), 7.30 (m, 4H), 5, 04 (s, 2H), 3.71 (s, 2H), 2.05 (s, 3H) ppm;
    [074] 3.5 g (10 mmol) of 2-bromo-2 ', 4'-bismethoxycarbonyloxy-acetophenone were boiled at reflux for 0.5 hour with 2.7 g (10 mmol) of N- [2- ( 4acetoxymethylphenyl) acetyl] thiourea and 1.3 g (15 mmol) of NaHCO3 in 50 ml of ethanol. The reaction solution was cooled and mixed with 4.0 g (0.1 mol) of NaOH in 20 ml of water. After stirring for 2 hours at 60 o C, the reaction solution was recovered in 100 ml of water and adjusted to pH = 3 with 2N HCl. The resulting precipitate was filtered and recrystallized from ethanol / water. 1.3 g of thiazole were obtained. 1 H NMR (DMSO-D6): 12.44 (s, 1 H), 10.80 (s, 1 H), 9.48 (s, 1 H), 7.66 (d, 1 H), 7 , 41 (s, 1 H), 7.29 (m, 4H), 6.32 (m, 2H), 5.13 (t, 1 H), 4.47 (d, 2H), 3.77 ( s, 2H) ppm. Melting point: 254 to 256 ° C.
    [075] Cosmetic or dermatological preparations with an alkylamidothiazole content or their use for the treatment and / or prophylaxis of unwanted skin pigmentation are likewise embodiments of the present invention.
    [076] It is advantageous, in particular, if such preparations contain 0.000001 to 10% by weight, in particular
    26/77
    0.0001 to 3% by weight, most particularly 0.001 to 1% by weight, of one or more of the alkylamidothiazoles used according to the invention, based on the total weight of the preparation.
    [077] Cosmetic and dermatological preparations according to the invention can be present in various forms. Thus, they can represent, for example, a solution, an anhydrous preparation, an emulsion or microemulsion of the water in oil type (W / O / W) or of the oil in water type (O / W), a multiple emulsion, for example , of the water in oil in water (W / O / W) type, a gel, a solid stick, an ointment or also an aerosol. According to the invention it is also advantageous to administer the substances used according to the invention and / or their derivatives in encapsulated form, for example, in collagen matrices and other conventional encapsulation materials, for example, with cellulose encapsulations, in gelatin or liposomally encapsulated.
    [078] It is also possible and advantageous in the sense of the present invention, to introduce the substances used according to the invention and / or their derivatives into aqueous systems
    or in preparations surfactants for cleaning of the skin and the hair. [079] At cosmetic preparations and dermatological wake up with the invention can to contain cosmetic substances auxiliaries such how are conventionally used in these preparations, for example,
    preservatives, bactericides, perfumes, substances to prevent defoaming, dyes, pigments, which have a coloring effect, thickeners, surfactants, emulsifiers, substances that provide softness, moisturizers and / or moisture maintenance, fats, oils, waxes or others
    27/77 conventional components of a cosmetic or dermatological formulation, such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
    [080] The lipid phase can be selected, in advantageously, from following group of substances:[081] - mineral oils, mineral waxes[082] - oils, such as triglycerides of capric acid or caprylic acid, in addition, oils natural resources such as , for example, castor;
    [083] - natural and synthetic fats, waxes and other fatty bodies, preferably fatty acid esters with low carbon alcohols, for example, with isopropanol, propylene glycol or glycerin or fatty alcohol esters with low carbon number alkanes or with fatty acids;
    [084] - alkyl benzoates;
    [085] - silicone oils, such as dimethylpolysiloxanes, diethylpolysiloxanes, diphenylpolysiloxanes, as well as mixed forms thereof.
    [086] The oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the sense of the present invention is advantageously selected from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanocarboxylic acids with a chain length from 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols with a chain length of 3 to 30 carbon atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated alcohols branched
    28/77 and / or unbranched with a chain length of 3 to 30 carbon atoms. Such ester oils can then be selected advantageously from the group of isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexyldecyl stearate, 2-octyldodecyl palmitate, oleyl oleate, oleyl oleate, oleyl oleate erucila, erucila erucato, as well as synthetic, semi-synthetic and natural mixtures of such esters, for example, jojoba oil.
    [087] The aqueous phase of the preparations according to the invention optionally contains, advantageously, moisture-maintaining agents, such as, for example, propylene glycol, panthenol or hyaluronic acid, as well as, in particular, one or more thickeners, which can or can be selected advantageously from the group silicon dioxide, aluminum silicates, hydroxypropylmethylcellulose, particularly advantageously a polyacrylate, such as, for example, Carbopole type 980, in each case individually or in combination.
    [088] In particular, mixtures of the solvents mentioned above are used. In alcoholic solvents, water can be another component.
    [089] Emulsions according to the invention are advantageous and contain, for example, the fats, oils, waxes and other fatty bodies mentioned above, as well as water and an emulsifier, such as this is conventionally used
    29/77 for such a formulation.
    [090] Gels according to the invention conventionally contain low carbon alcohols, for example, ethanol, propylene glycol and water or an oil mentioned above, in the presence of a thickener, which in oily alcohol alcohols is preferably a silicon dioxide or a aluminum silicate, in aqueous-alcoholic or alcoholic gels this is preferably a polyacrylate.
    [091] As blowing agents for preparations according to the invention sprayable from aerosol bottles suitable conventional liquefied, volatile blowing agents, for example, hydrocarbons (propane, butane, isobutane), which can be used alone or in combination, are suitable. mix with each other. Compressed air can also be used to advantage.
    [092] Advantageously, the preparations according to the invention may, in addition, contain substances, which absorb UV radiation in the IVB range, the total amount of filter substances being, for example, 0.1% in weight to 30% by weight, preferably 0.5 to 10% by weight, in particular 1.0 to 6.0% by weight, based on the total weight of the preparations, to make cosmetic preparations available, which protect the hair or the skin against the entire range of ultraviolet radiation. These can also serve as sunscreen for hair or skin.
    [093] In addition, the preparations according to the invention can advantageously contain additional substances, which cover the disturbing odor of the remaining raw materials used, the total amount of the constituent substances of perfume making up, for example,
    30/77 example, 0.001% by weight to 30% by weight, preferably 0.05 to 10% by weight, in particular 0.1 to 5.0% by weight, based on the total weight of the preparations, for placing cosmetic preparations available.
    [094] The following examples should illustrate the present invention, without restricting it. All specifications of quantity, proportions and percentages refer, unless otherwise specified, to the weight and quantity of weight or the total weight of the preparations.
    EXAMPLES OF REVENUE [095] Oil / water emulsions (O / W)
    Recipe example 1 2 3 4 Chemical name / INCI % inWeight % inWeight % inWeight % inWeight Stearic acid 2.50 2.00 2.00 2.50 Glyceryl stearate 1.00 1.00 1.00 1.00 C12-15 alkyl benzoate 3.00 500 3.00 2.00 Caprylic / capric acid triglyceride 2.50 2.50 2.00 2.50 Isopropyl palmitate 2.00 - - 2.00 Cetylstearyl alcohol 3.00 - 2.00 3.00 Cetyl alcohol - 2.00 - - Stearyl alcohol - 2.00 1.00 - C13-16 isoparaffin - - - 1.00 Dibutyladioate -1.50Cyclomethicone 1.00 1.00 0.50 -
    11/31
    Recipe example 1 2 3 4 Dicaprilil carbonate 2.00 2.00 2.00 2.00 Dimethicone 1.00 - 0.50 1.00 Glycerin 5.00 7.00 5.00 9.00 Ethylhexyl cocoate - - 1.00 - Methylparaben 0.20 - - - Phenoxyethanol 0.40 0.50 0.50 0.40 Propylparaben 0.10- 0.10 1,2-hexanediol - - 0.10 0.10 Ethylhexylglycerine - - 0.20 - Methylisothiazolinone - 0.05 - - Butylene glycol - - 2.0 - Carbomer 0.15 0.10 0.15 0.10 Carrageenan 0.10 - 0.10 - Xanthan gum - - 0.10 - Acrylate Crospolymer / C10-30 alkyl acrylate0.10 - 0.10 Trisodium EDTA 0.20 0.20 0.20 0.20 Tapioca starch 1.50 1.00 -Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,1-dione) - 0.20 - 0.50 Polymethylsilsesquioxane - 1.00 1.00 - Aluminum octenyl succinate starch - - 1.00 - Diamide Phosphate 1.00 1.00 - 1.00
    32/77
    Recipe example 1 2 3 4 Butyl methoxydibenzoylmethane 1.00 2.00 1.00 1.00 Phenylbenzimidazole sulfonic acid 1.00 1.00 2.00 2.00 Octocylene 2.00 2.00 1.00 2.00 Ethylhexyl salicylate 1.00 1.00 2.00 1.00 Sodium benzoate 0.01 0.05 0.10 0.15 Dehydroacetic acid 0.10 0.05 0.20 0.03 Hydroxypropyl tetrahydropyranotriol 1.00 0.50 - - Liponic acid - 0.50 0.20 - Potassium methoxysalicylate 0.30 - 0.10 0.05 Vitamin B6 HCI 0.10 0.05 - 0.30 Tranexamic acid - 0.01 0.25 - Pyrus Malus Stem Extract 1.00 0.25 0.50 0.75 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.20 0.10 0.05 0.30 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.01 0.25 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.25 0.15 0.30 0.35 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.10 0.10 0.15 0.20 Sodium hydroxide q.s. q.s. q.s. q.s. Hydroxy-isohexyl 3-cyclohexenocarboxaldehyde 0.10 - - 0.05 Citronelol 0.05 0.10 - 0.05
    33/77
    Recipe example 1 2 3 4 Linalol - 0.05 0.10 - perfume 0.30 0.20 0.20 0.20 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe example 5 6 7 8 Chemical name % inWeight % inWeight % inWeight % inWeight Glyceryl citrate stearate 2.00 1.50 2.00 2.00 Behenyl alcohol 1.50 1.00 1.00 1.00 C12-15 alkyl benzoate 2.00 2.50 2.00 2.50 Acid triglyceridecaprylic / capric 2.00 2.00 2.50 2.50 Cetyl alcohol 2.00 2.00 - 2.00 Cetearyl alcohol - - 2.00 - Cyclopentasiloxane - - - 1.00 Cyclomethicone 1.00 1.00 2.00 2.00 Dicaprilil carbonate - 2.00 2.50 2.50 Liquid paraffin (mineral oil) - - 0.50 - Octyldodecanol - 2.00 - - Isopropyl palmitate 1.50 -- Dimethicone 0.50 1.00 1.00 - Glycerin 3.00 5.00 7.00 9.00
    34/77
    Recipe example 5 6 7 8 Methylparaben 0.20 0.15 - - phenoxyethanol 0.40 0.60 0.50 0.50 Propylparaben 0.10 - - - Methylisothiazolinone - - 0.05 - Pyroctone olaminaa - - - 0.15 Sodium benzoate 0.10 0.10 0.10 0.10 Glyceryl caprylate - - - 0.20 Ethylparaben 0.10 - - - Carbomer 0.20 - 0.15 0.15 Sodium polyacrylate - 0.40 - - Xanthan gum 0.10 - 0.10 - Acrylate / acrylate crospolymerC10-30 alkyl - 0.10 - 0.10 Tapioca starch 0.50 - 0.50 - Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,7-dione) 1.00 - - 1.00 Polymethylsilsesquioxane - 1.00 1.00 - Aluminum octenyl succinate starch - 1.00 - 1.00 N- (4- (2,4-dihydroxyphenii) thiazol-2-il) -isobutyramide 0.25 0.15 0.30 0.35 N- (4- (2.4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.10 0.10 0.15 0.20 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) butyramide 0.01 0.25 0.15 0.10
    35/77
    Recipe example 5 6 7 8 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) cyclohexanecarboxamide 0.20 0.10 0.05 0.30 Glycyrrhiza root extractInflata 0.03 0.05 0.05 0.03 Titanium dioxide - 1.00 - - Octocylene 1.00 2.00 1.00 1.00 Bis-ethylhexyloxyphenol methoxyphenyl triazine 1.00 1.00 2.00 2.00 2-ethylhexyl methoxycinnamate 2.00 2.00 1.00 2.00 Homosalate (3.3.5-trimethylcyclohexylsalicylate) 1.00 1.00 2.00 1.00 Sodium hydroxide q.s. q.s. q.s. q.s. Trisodium EDTA 0.15 - 0.15 - 1- (1,2,3,4,5,6,7,8-octahydro-2,3,8,8, -tetramethyl-2-naphthyl) ethan-1-ona 0.1 - q.s. q.s. Geraniol0.05 - - Hexylcinamal 0.05perfume 0.10 0.20 0.30 0.20 Water ad 100 ad 100 ad 100 ad 100
    Examples of recipe 9 10 11 12 Name chemistry % inWeight % inWeight % inWeight % inWeight Diestearate polyglyceryl-3 2.00 2.50 2.50 2.50
    36/77
    Recipe examples 9 10 11 12 methylglucose Sorbitan stearate 1.50 3.00 1.50 3.00 C12-15 alkyl benzoate 2.50 2.50 2.50 2.50 Acid triglyceridescaprylic / capric 2.50 2.50 2.50 2.50 Stearyl alcohol 1.00 1.50 1.00 1.50 Cyclomethicone 3.00 1.00 2.00 1.00 Isopropyl myristate - 2.50 2.00 2.50 Isopropyl palmitate 2.00 - 1.00 - Hexyl ethyl stearate - 1.50 - - Dimethicone - 1.00 - 1.00 Decyl oleate -1.50 - Glycerin 5.00 7.50 3.00 7.50 Butirospermum Parkii butter 2.00 - - - Squalane 0.50 - -Sodium benzoate 0.10 0.10 0.10 0.10 Methylparaben 0.20 0.20 - 0.10 Phenoxyethanol 0.40 0.40 0.40 0.40 Propylparaben 0.10 - - - Benzethonium chloride - - 0.10 - Caprylglycol - 0.20 -Ethylhexylglycerine - 0.20 - 0.2 Pentylene glycol0.10 0.05 0.5
    37/77
    Recipe examples 9 10 11 12 Carbomer 0.15 0.10 0.15 0.10 Ammonium acryloyldimethyltaurate copolymer / VP - 0.20 - 0.20 Carrageenan 0.10 - 0.15 - Trisodium EDTA - 1.00 - 1.00 Tapioca starch - 1.00 1.00 - Diamide Phosphate - 1.00 - 1.00 Copolymer of acrylonitrilemethacrylonitrile-methyl methacrylate + isopentane + magnesium hydroxide - - 1.00 1.00 N- (4- (2,4-dihydroxyphenyl) thiazole-2- 0.01 0.25 0.15 0.10 il) -isobutyramide N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.20 0.10 0.05 0.30 N- (4- (2,4-dihydroxyphenyl) thiazoi-2-il) -butiramide 0.25 0.15 0.30 0.35 N- (4 - (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.10 0.10 0.15 0.20 Diethylamino benzoatehydroxybenzoyl hexyl 1.00 2.00 1.00 1.00 Butyl methoxycinnamate 1.00 1.00 2.00 2.00 Butyl methoxydibenzoylmethane 2.00 2.00 1.00 2.00 Octocylene 1.00 1.00 2.00 1.00 Titanium dioxide - - 1.00 -
    38/77
    Recipe examples 9 10 11 12 Sodium hydroxide q.s. q.s. q.s. q.s. Ubiquinona 0.10 - - - Sodium metabisulphite - 0.15 - - BHT (tert-butylhydroxytoluene) - - 0.05 - Linali acetate 0.05 - - - Hexyl salicylate - 0.05 - - Benzyl salicylate - - 0.01 - perfume q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 13 14 15 16 Chemical name % inWeight % inWeight % inWeight % inWeight PEG-40 stearate 0.80 1.00 1.00 1.00 Glyceryl stearate 2.50 3.00 3.00 3.00 C12-15 alkyl benzoate 2.00 2.50 2.00 2.00 Caprylic acid triglyceride / capric acid 2.00 2.50 2.50 2.00 Cetylstearyl alcohol 3.00 3.00 3.00 3.00 Cyclomethicone 2.00 2.00 2.00 2.00 Dicaprilil carbonateZOO 2.50 2.50 Octyldodecanol 1.00 -1.50 Tri-isostearin - 0.50 - 1.00
    39/77
    Recipe examples 13 14 15 16 Butirospermum Parkii butter 2.00 - - - Octyldodecyl myristate 1.00 - 1.50 1.00 Dimethicone 1.00 1.00 1.00 1.00 Glycerin 7.50 5.00 9.0 7.50 Methylparaben 0.20 - 0.10Phenoxyethanol 0.40 0.50 0.40 0.40 Propylparaben 0.10-Glyceryl caprylate - 0.25 - - Pentylene glycol - 0.50 - - Butylene glycol- 3.00Laurylethyl arginate 0.10 0.05 0.20 - Potassium sorbate 0.10 0.05 0.15 0.01 Sodium salicylate 0.01 0.02 0.01 0.05 Carbomer 0.15 0.10 0.10 0.15 Sodium polyacrylate0.20 0.20Xanthan gum 0, 1 0 - - - Acrylate / acrylate crospolymerC10-30 alkyl- - 0.1 Trisodium EDTA + water (20% aqueous solution) - 1.00 1.00 1.00 Tapioca starch - 1.00 1.00 1.00 Diamide Phosphate - 1.00 1.00 1.00 Aluminum octenyl succinate starch 2.00 - - -
    40/77
    Recipe examples 13 14 15 16 Copolymer of acrylonitrilemethacrylonitrile-methyl methacrylate + isopentane + magnesium hydroxide 1.00 - - - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.15 0.10 0.01 Ethylhexyl methoxycinnamate 1.00 2.00 1.00 1.00 Diethylamino benzoatehydroxybenzoyl hexyl 0.50 I 1.00 2.00 1.00 Homosalate (salicylate of 3.3.5-trimethylcyclohexyl) 2.00 2.00 1.00 2.00 Phenylbenzimidazolsulfonic acid 1.00 1.00 2.00 1.00 Titanium dioxide -1.00Glyceryl glycoside 3.00 - - - Short-chain hyaluronic acid0.10 Long-chain hyaluronic acid - - 0.10 - 4-butyl-resorcinol - - - 0.30 Magnolia bark extract 0.10 - - - Octadecenedioic acid - 0.05 - - Folic acid - - 0.01 - Carnitine - - - 0.50 Creatine 0.10 - - - Alpha-glycosylrutine0.01 - - Taurine- 0.10 -
    41/77
    Recipe examples 13 14 15 16 Blackberry Root Extract - - - 0.20 Sodium metabisulphite 0.10 - - - Diethylhexyl syringylidene malonate 0.13 0.13 Sodium hydroxide q.s. q.s. q.s. q.s. 3-methyl-5-phenyl-1-pentanol 0.10 - -Coumarina0.05 - - Ethinyl-linalool- 0.10 - Ascorbyl palmitate 0.10 - - - perfume q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 17 18 19 20 Chemical name % inWeight % inWeight % inWeight % inWeight Glyceryl citrate stearate 2.00 2.00 2.00 2.00 Isopropyl palmitate 3.00 2.00 3.00 1.00 Cetylstearyl alcohol 4.00 3.00 3.00 - Cetyl alcohol - - - 4.00 Caprylic acid triglyceride / capric acid 3.00 2.50 2.00 3.00 C12-15-alkyl benzoate 3.00 2.50 2.00 2.00 Cyclomethicone 1.00 - 1.00 - Dicaprilil carbonate- 2.50
    42/77
    Recipe examples 17 18 19 20 Dimethicone - 0.50 - - Octyldodecyl myristate - 1.00 - - Glycerin 4.00 6.00 5.00 6.00 Methylparaben 0.20 - 0.10 - Phenoxyethanol 0.40 0.40 0.40 0.40 Pyroctone olamine -- 0.10 Ethylhexyl glycerin - 0.30 - - Glyceryl caprylate - 0.30 - - 2-methyl-1,3-propanediol - 2.00 - 2.00 Sodium benzoate 0.01 - 0.20 0.10 Sodium salt of dehydracetic acid 0.01 0.05 0.10 0.02 Carbomer 0.20 0.10 0.15 - Sodium polyacrylate - 0.40 -Xanthan gum 0.10- 0.15 Acrylate / acrylate crospolymerC10-30 alkyl -0.10 0.20 Copolymer of acrylonitrile-methacrylonitrile-methyl methacrylate + isopentane + magnesium hydroxide 0.50 - 0.50 - Aluminum octenyl succinate starch - 1.00 - 1.00 Methyl methacrylate crospolymer 1.00 1.00 Glycyrrhiza root extract 0.03 - - -
    43/77
    Recipe examples 17 18 19 20 Inflata Vitamin C / ascorbic acid - 3.00 - - Glycine from soy germ extract - - 0.50 - Arctium Lappa root extract - - - 0.30 Pimpinella fruit extractAnisum 4.00 - - - Glycyrritinic acid - 0.10 - - N-acetylhydroxyproline - - 0.10 - Niacinamide - - - 0.20 Magnesium ascorbyl phosphate 0.10 - - - Ellagic acid - 0.01 - - Glycyrrhiza root extract - - 0.10 - Sea salt - - - 0.05 Isoserinol 1.00 - - - Dihydroxypropyltrimony chloride - 0.80 - - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.25 0.30 0.01 0.05 Titanium dioxide - 1.00 - 1.00 Bis-ethylhexyloxyphenol methoxyphenyl triazine 1.00 2.00 1.00 1.00 Octocylene 1.00 1.00 2.00 2.00 Butyl methoxydibenzoylmethane 2.00 2.00 1.00 2.00 Ethylhexyl salicylate 1.00 1.00 2.00 1.00
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    Recipe examples 17 18 19 20 Citronelol 0.05 - 0.05 - Coumarina 0.05 0.05 - 0.05 Triethyl citrate - - 0.05 0.05 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 21 22 23 24 Chemical name % inWeight % inWeight % inWeight % inWeight Sucrose polystearate + hydrogenated polyisobutene 1.00 1.00 2.00 2.00 Sodium stearoyl glutamate 0.20 0.20 0.30 0.30 C12-15-alkyl benzoate 1.50 1.50 - - Cetyl alcohol 0.50 0.50- Cyclomethicone 10.00 10.00 5.00 5.00 Dimethicone 3.00 3.00 2.50 2.50 Glycerin 7.50 7.50 5.00 5.00 Isopropyl stearate 1.00 1.00 2.00 2.00 Liquid paraffin (mineral oil) 3.00 3.00 1.00 1.00 Methylparaben 0.10 - - 0.10 Ethylhexylglycerine- 0.30 0.10 Propylparaben 0.10 - - - Methylisothiazolinone - 0.05 - -
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    Recipe examples 21 22 23 24 Phenoxyethanol 0.40 0.50 0.40 0.40 Potassium sorbate 0.10 0.05 0.20 0.01 Ascorbyl glycoside 0.10 - - - Undecenoylphenylalanine - 0.50 - - Kogic acid - - 0.10 - Arbutin - - - 0.01 Betaine 0.20 - - - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.10 0.25 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.15 0.15 0.01 0.06 Ethylhexyl methoxycinnamate 1.00 2.00 1.00 1.00 Butyl methoxydibenzoylmethane 1.00 1.00 2.00 2.00 Phenylbenzimidazole sulfonic acid 2.00 2.00 1.00 2.00 Copolymer ofacrylate / octylacrylamide - 1.00 - - Butylene glycol - - 3.00 - Polymethylsilsesquioxane - - 11.00 1.00 Prunus Amygdalus Dulcis Oil - - 1.00 - Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,7-dione) - 1.00 1.00 - Diamide Phosphate - 1.00 - 1.00
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    Recipe examples 21 22 23 24 Methyl methacrylate crospolymer 1.00 - - - Aluminum octenyl succinate starch 1.00 - - - Ammonium acryloyldimethyltaurate / VP copolymer- 0.25 0.25 Xanthan gum 0.10 - - 0.10 Acrylate / acrylate crospolymerC10-30 alkyl 0.25 0.10 - - Carbomer0.10 0.10 - Hexylcinamal 0.05 0.10 - 0.10 1- (1,2,3,4,5,6,7,8-octahydro-2,3,8,8, -tetramethyl-2-naphthyl) ethan-1-ona - 0.10 0.10 - Linalol - - 0.05 0.05 perfume 0.20 0.20 0.20 0.20 Sodium hydroxide q, s, q, s, q, s, q, s, Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 25 26 27 28 Chemical name % inWeight % inWeight % inWeight % inWeight Sodium cetearyl sulfate 0.15 0.15 - 0.15 Glyceryl stearate SE 2.00 2.00 - 1.50 Sodium stearoyl glutamate - - 0.30
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    Recipe examples 25 26 27 28 C12-15-alkyl benzoate 2.50 2.50 2.50 2.50 Octyldodecanol 1.00 1.00 - - Caprylic acid triglyceride / capric acid 2.00 2.00 2.00 2.00 Cetylstearyl alcohol 2.00 2.00 3.00 1.00 Cyclomethicone 1.50 1.50 2.50 2.50 Glyceryl stearate - - 2.00 - Dimethicone 0.50 0.50 0.50 0.50 Glycerin 5.00 5.00 7.50 7.50 Cetearyl alcohol 1.00 1.50 1.00 1.00 Isopropyl stearate 3.00 3.00 2.00 2.00 Liquid paraffin (mineral oil) 2.00 2.00 1.00 1.00 Methylisothiazolinone - - - 0.05 Phenoxyethanol 0.40 0.50 0.40 0.30 Methylparaben 0.15 - - - Propylparaben 0.10 - - - Pyroctone Olamine - 0.15 - - Benzethonium chloride - - 0.10 - Octane-hydroxamic acid 0.10 0.10 - 0.50 Sodium benzoate 0.05 0.20 0.10 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2- 0.25 0.30 0.01 0.05
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    Recipe examples 25 26 27 28 il) -pivalamide N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.15 0.15 0.01 0.06 Ethylhexyl methoxycinnamate 1.00 2.00 1.00 1.00 Butyl methoxydibenzoylmethane 1.00 1.00 2.00 2.00 Pentylene glycol - 1.00 1.00 - Butylene glycol 1.00 1.50 3.00 3.00 Dipropylene glycol 0.50 1.00 0.80 0.10 2-methyl-1,3-propanediol - - - - 1,2-hexanediol - - - 1.00 Nylon-12 (1,8 diazacyclotetradecan-2,7-dione homopolymer) 1.00 1.00 1.00 1.00 Carbomer - - 0.10 0.15 Ammonium acryloyldimethyltaurate / VP copolymer 0.20 - - - Chondrus Crispus 0.10 0.10 - - Xanthan gum - - 0.10 - Acrylate / acrylate crospolymerC10-30 alkyl - 0.20 0.10 0.10 Coumarina 0.10 - 0.05 0.05 Hydroxy-isohexyl 3-cyclohexenocarboxaldehyde 0.05 0.05 0.05 0.10
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    Recipe examples 25 26 27 28 1- (1,2,3,4,5,6,7,8-octahydro 2,3,8,8-tetramethyl-2-naphthyl) ethan-1-one - 0.05 0.10 - perfume 0.20 0.30 0.40 0.20 Sodium hydroxide q, s, q, s, q, s, q, s, Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 29 30 31 32 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Sodium cetearyl sulfate 0.15 0.15 020 0.20 Glyceryl stearate, self-emulsifying 2.00 2.00 1.50 1.50 C12-15-alkyl benzoate 2.00 2.00 2.00 2.00 Octyldodecanol 1.00 1.00 - - Caprylic acid triglyceride / capric acid 2.00 2.00 2.00 2.00 Cetylstearyl alcohol 2.00 2.00 1.00 1.00 Cyclomethicone 1.00 1.00 2.00 2.00 Dimethicone 0.50 0.50 1.00 1.00 Glycerin 5.00 5.00 7.50 7.50 Isopropyl palmitate 2.50 2.50 2.00 2.00 DMDM hydantoin 0.05 0.05 0.05 0.05 Phenoxyethanol 0.35 0.25 0.30 0.30 Ethanol - - 3.00 2.00
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    Recipe examples 29 30 31 32 Pentylene glycol 1.001.00 1.50 Potassium sorbate 0.10 0.30 - 0.05 Zingerona 0.10 - - - Dihydromyricetin - 0.03 - - White tea extract - - 1.004-hexyl-resorcinol- - 0.30 Phenylethyl resorcinol 0.50 - - - Ubiquinone - 0.10 - - Cyanomethylphenyl menthane carboxamide - - 0.10 - Mentoxipropanediol- - 0.10 Mentan carboxamide ethylpyridine 0.10 - - - Hydroxyethylurea - 0.50 - - Urea - - 1.00 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 Carbomer 0.20 0.20 0.20 0.20 Carrageenan 0.10 0.10 - - Xanthan gum - - 0.20 0.20 Acrylate / acrylate crospolymerC10-30 alkyl - - - 0.15 Sodium polyacrylate - 0.20 - - 2,6-diethylhexyl naphthalate - - 1.00 - Phenylbenzimidazolsulfonic acid 1.00 2.00 1.00 1.00
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    Recipe examples 29 30 31 32 Titanium dioxide 1.00 1.00 2.00 2.00 Diethylamino benzoatehydroxybenzoyl hexyl 2.00 2.00 1.00 2.00 Octocylene 1.00 1.00 2.00 1.00 3.3.5- Salicylatetrimethylcyclohexyl1.00 - - Diamide Phosphate - 1.00 1.00 - Methyl methacrylate crospolymer 1.00 -1.00 Polymethylsilsesquioxane - - 1.00 1.00 Copolymer of acrylonitrile-methacrylonitrile-methyl methacrylate + isopentane + magnesium hydroxide 1.00 1.00 - - 1- (1,2,3,4,5,6,7,8-octahydro 2,3,8,8-tetramethyl-2-naphthyl) ethan-1-one - 0.10 0.10 0.05 Hydroxy-isohexyl 3-cyclohexenocarboxaldehyde 0.05 0.05 0.10 - Linalyl acetate 0.10 - 0.05 0.05 perfume 0.15 0.15 0.30 0.30 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 33 34 35 36 INCI / chemical name % in % in % in % in
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    Recipe examples 33 34 35 36Weight Weight Weight Weight Sodium cetearyl sulfate 0.15 0.15 0.15 0.15 Glyceryl stearate, self-emulsifying 1.00 1.00 1.00 1.00 C12-15-alkyl benzoate 2.00 2.50 2.00 2.00 Isopropyl palmitate 3.50 3.00 2.50 '3.50 Dimethicone 1.00 1.00 1.00 1.0 Cetylstearyl alcohol 1.00 1.00 1.00 1.00 Octyldodecyl myristate - - - 1.00 Butirospermum Parkil butter - - 1.00 - Glycerin 7.00 3.00 9.00 5.00 Carbomer 0.10 0.15 0.10 0.10 Acrylate / acrylate crospolymerC10-30 alkyl 0.15 0.10 0.10 0.15 Xanthan gum 0.15 0.15 0.15 0.15 Phenylbenzimidazolsulfonic acid 1.00 1.00 0.50 1.00 Butyl methoxydibenzoylmethane 1.50 1.50 1.50 1.50 Ethylhexyl salicylate 2.00 2.50 2.50 2.50 Octocylene 1.50 1.50 2.50 1.50 Trisodium dioxide + trimethoxyprilylsilane 1.00 - 1.00 - Aluminum octenyl succinate starch - 1.00 - 0.50 Methyl methacrylate crospolymer 0.50 - 0.50 -
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    Recipe examples 33 34 35 36 Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,7-dione) 0.50 - 1.00 - Tapioca starch 0.50 0.50 - 1.00 Phenoxyethanol 0.50 0.50 0.50 0.40 Ethylhexylglycerine 0.25 - 0.251,2-hexanediol - 1.00 - 3.00 Caprylglycol - 0.30 0.302-methyl-1,2-propanediol 2.00 2.00 2.001,3-butanediol 0.01 - 0.20 - Sodium benzoate - 0.10 - 0.20 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 0.01 0.05 Ethyl-linalool 0.05 - 0.05 - 3-methyl-5-phenyl-1-pentanol - 0.05 - 0.05 Geraniol 0.05 - 0.05 - Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Examples of recipe 37 38 39 40 Name INCI / chemistry % inWeight % inWeight % inWeight % inWeight Stearate polyglyceryl-10 0.20 0.20 0.20 0.20
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    Recipe examples 37 38 39 40 Glyceryl stearate 3.00 0.50 0.50 0.50 C12-15-alkyl benzoate 4.00 2.00 1.50 2.50 Isopropyl palmitate 4.00 1.00 2.00 2.50 Caprylic acid triglyceride / capric acid 4.00 3.00 2.00 2.50 Hydrogenated coconut glyceride 3.00 - - 2.00 Butirospermum Parkii butter 3.00 - 2.50 - Cetylstearyl alcohol 5.00 3.50 4.00 3.00 Liquid paraffin (mineral oil) - - - 1.00 Glycerin 5.00 3.00 7.00 9.00 Acrylate / acrylate crospolymerC10-30 alkyl 0.30 0.20 0.15 0.20 Methylisothiazolinone 0.05 - - 0.05 Phenoxyethanol 0.50 0.40 0.40 0.40 Carbomer 0.10 0.15 0.10 0.10 Methylparaben - 0.10 0.10 i - Propylparaben - 0.10 - - Benzilic alcohol 0.10 0.10 0.05 0.15 Sodium benzoate 0.50 0.40 0.40 0.40 Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,7-dione) 1.00 0.50 - - Polymethylsilsesquioxane - 1.00 0.50 - Methyl methacrylate crospolymer - - 1.00 0.50
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    Recipe examples 37 38 39 40 Tapioca starch 0.50 - - 0.50 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 0.01 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.01 0.60 1.00 0.20 Benzophenone-4 1.00 2.00 1.50 0.50 Ethylhexyl triazone 2.00 0.50 1.00 2.00 Ethanol 100 - 2.00 - Geraniol 0.05 0.05 - - Benzyl salicylate - 0.05 0.05 - Ethyl-linalool - - 0.05 0.05 perfume 0.20 0.15 0.30 0.30 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Examples of recipe 41 42 43 44 % in % in % in % in Name INCI / chemistry Weight Weight Weight Weight Stearate polyglyceryl-10 0.20 0.20 0.15 0.15 Benzoate C12-15-alkyl 2.50 2.50 2.00 3.00
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    Recipe examples 41 42 43 44 Isopropyl palmitate 2.50 2.50 2.00 2.00 Caprylic acid triglyceride / capric acid 2.00 2.50 1.00 2.00 Glyceryl stearate 1.00 1.00 0.50 0.50 Octyldodecanol 0.50 - - 1.00 Cyclomethicone - - 0.50 0.50 Butyl methoxydibenzoylmethane 1.00 2.00 2.00 1.00 Octocylene 0.50 2.00 3.00 2.00 Ethylhexyl salicylate 2.00 1.00 1.00 1.50 Phenylbenzimidazole sulfonic acid 1.00 1.00 0.50 1.50 Titanium dioxide - 1.00 - 1.00 3.3.5- Salicylatetrimethylcyclohexyl - - 1.00 1.00 Glycerin 9.00 5.00 7.00 7.00 Tapioca starch 1.00 1.00 - - Copolymer of acrylonitrile-methacrylonitrile-methyl methacrylate + isopentane + magnesium hydroxide - 1.00 0.50 - Aluminum octenyl succinate starch - - 1.00 1.00 Diamide Phosphate - - - 1.00 Methylisothiazolinone 0.05 0.05 - - Phenoxyethanol 0.50 0.50 0.40 0.40 Benzethonium chloride - - 0.10 -
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    Recipe examples 41 42 43 44 Ethylhexylglycerine - - 0.10 - Methylparaben - - - 0.20 Salicylic acid 0.01 0.05 0.10 0.02 Potassium sorbate 0.10 0.05 0.20 0.30 Carbomer 0.25 0.20 0.20 0.20 Acrylate / acrylate crospolymerC10-30 alkyl 0.20 - - 0.15 Ammonium acryloyldimethyltaurate / VP copolymer - 0.25 - - Sodium polyacrylate - - 0.30 - Xanthan gum - - - 0.15 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 Ethanol 3.00 3.00 - - Butylene glycol - - ZOO 2.00 Cumarin - 0.05 0.05 - Hexylcinamal 0.05 0.05 - 0.05 Hexyl salicylate - - 0.05 0.05 perfume 0.15 0.20 0.25 0.30 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 45 46 47 48 INCI / chemical name % in % in % in % in
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    Recipe examples 45 46 47 48Weight Weight Weight Weight Potassium cetylphosphate 0.20 0.20 0.20 0.20 Dicaprilil carbonate - 1.00 - - C12-15-alkyl benzoate 2.50 2.00 1.00 3.00 Isopropyl palmitate 2.50 2.00 3.00 1.00 Caprylic acid triglyceride / capric acid 2.50 2.00 1.50 2.00 Microcrystalline wax - - - 0.50 Cyclocomethicone 0.25 - 0.50 0.50 2,6-diethylhexyl naphthalate - 0.50 - 1.00 Diethylamino benzoatehexidohydroxybenzoyl - 1.00 - 1.00 Ethylhexyl salicylate 1.00 0.50 2.00 1.00 Octocylene 2.00 1.00 3.00 2.00 Glycerin 5.00 7.00 9.00 7.00 Acrylate / acrylate crospolymerC10-30 alkyl 0.10 0.30 - 0.10 Sodium polyacrylate 0.30 - - - Carbomer - 0.10 0.15 0.15 Ammonium acryloyldimethyltaurate / VP copolymer - - 0.25 - Chondrus Crispus Extract(carrageenan) - - - 0.10 Methylisothiazolinone 0.05 0.05 - -
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    Recipe examples 45 46 47 48 Phenoxyethanol 0.50 0.50 0.40 0.40 Pyroctone Olamine - - - 0.20 Salicylic acid 0.05 0.10 0.01 0.20 Benzoic acid 0.20 0.05 0.10 0.01 Nylon-12 (homopolymer of 1.8-diazacyclotetradecan-2,7-dione) 0.50 - 0.50 0.50 Diamide Phosphate - 1.00 - 0.50 Methyl methacrylate crospolymer - 0.50 0.50 - Caprylglycol - - 0.301,2-hexanediol - - - 0.50 Butylene glycol - - 2.00 2.00 Hydantoin DMDM - - 0.15 - Glycyrrhiza root extractInflata - - 0.05 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 0.01 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.01 0.60 1.00 020 Hydroxy-isohexyl 3-cyclohexenocarboxaldehyde 0.05 0.05 0.05 -
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    Recipe examples 45 46 47 48 Citronelol - 0.05 - 0.05 Benzyl salicylate - - 0.05 0.05 perfume 0.20 0.20 0.20 0.20 Sodium hydroxide q.s. q.s. q.s. q.s. Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 49 50 51 52 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Potassium cetylphosphate 0.20 0.20 0.25 0.20 C12-15-alkyl benzoate 2.50 2.50 2.00 2.00 Isopropyl palmitate 2.50 2.50 - 3.00 Isopropyl stearate - - 2.00 - Caprylic acid triglyceride / capric acid 2.50 2.50 1.50 2.00 Glyceryl stearate 1.00 1.00 1.25 1.50 Octyldodecanol - - 1.50 - Liquid paraffin (mineral oil) - - - 1.00 Glycerin 5.00 7.00 9.00 6.00 Bis-ethylhexyloxyphenol methoxyphenyl triazine - 1.00 - 1.00 Titanium dioxide + trimethoxyprilylsilane - - 1.00 1.00 Phenylbenzimidazolsulfonic acid 1.00 2.00 1.00 1.00
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    Recipe examples 49 50 51 52 Butyl methoxydibenzoylmethane 1.00 1.00 2.00 2.00 Disodium phenyl dibenzimidazole tetrasulfonate 2.00 2.00 1.00 2.00 Ethylhexyltriazone 1.00 1.00 2.00 1.00 Ethylhexyl methoxycinnamate + BHT 0.50 1.00 0.50 1.00 Carbomer0.15 0.20 0.30 Acrylate / acrylate crospolymerC10-30 alkyl 0.30 0.10 0.15 - Xanthan gum 0.15 0.10 Methylisothiazolinone 0.05 - - - Phenoxyethanol 0.50 0.50 0.40 0.40 Methylparaben - 0.10 - - Ethylhexyl salicylate - - 0.30 - Butylene glycol - - 3.00 3.00 Benzethonium chloride - - - 0.10 Sodium benzoate - 0.20 0.05 0.10 Propionic acid 0.10 0.20 0.05 0.02 Octane-hydroxamic acid 0.20 0.05 0.01 0.30 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide - 0.30 - 0.05 N- (4- (2,4-dihydroxyphenyl) thiazo1-2-il) -butiramide - - 0.15 0.10
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    Recipe examples 49 50 51 52 N- (4- (2,4-dihydroxyphenyl) thiazo1-2-il) -cyclohexanecarboxamide - 0.60 1.00 0.20 Coumarina - 0.05 - 0.05 Linanol 0.05 - - 0.05 Hexylcinamal 0.05 0.05 - - 1- (1,2,3,4,5,6,7,8-octahydro 2,3,8,8-tetramethyl-2-naphthyl) ethan-1-one - - 0.10 - perfume 0.10 0.30 0.20 0.30 BHT (tert-butylhydroxytoluene) 0.05 - - - Tocopheryl acetate - 0.10 - - Sodium hydroxide q. s . q. s . q. s . q. s . Water ad 100 ad 100 ad 100 ad 100
    Recipe examples 53 54 INCI / chemical name % by weight % by weight Polyglyceryl-3-isostearate 1.50 1.50 PEG-40 sorbitan periso stearate 2.50 2.50 Lanolin alcohol 0.50 0.50 Liquid paraffin (mineral oil) 8.00 8.00 Microcrystalline wax 2.50 2.50 Cyclomethicone 4.00 4.00 Isohexadecane 2.00 2.00 Isopropyl palmitate 5.00 5.00
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    Recipe examples 53 54 slodopropynyl butylcarbamate - 0.10 Magnesium sulfate 0.5 0.50 Potassium sorbate 0.10 0.05 Benzyl salicylate 0.10 0.01 1,2-Octanodiol 0.01 0.05 Sodium benzoate 0.10 0.01 Homosalate 0.50 1.00 Benzophenone-4 2.00 0.50 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 0.10 0.10 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) pivalamide 0.25 0.05 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide 0.10 0.15 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.01 0.02 Glycerin 7 7 perfume q.s. q.s. Water ad 100 ad 100
    Recipe examples 55 56 57 58 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Polyethylene glycol (21) stearic ether 2.50 2.50 1.50 1.50
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    Recipe examples 55 56 57 58 Polyethylene glycol (2) stearic ether 1.50 1.50 2.50 2.50 Etherpolypropylene glycol (15) stearic 3.00 3.00 4.00 4.00 Trisodium salt of ethylenediaminetetra — skeptic acid (20% aqueous solution) 1.50 1.50 1.50 1.50 Persea Gratissima Oil 01 (Avocado Oil) 0.10 0.10 0.15 0.15 perfume q.s. q.s. q.s. q.s. 1- (1,2,3,4,5,6,7,8-octahydro-2,3,8,13, -tetramethyl-2-naphthyl) ethan-1-one 0.10 0.05 - 0.05 Linayl acetate - 0.05 0.05 - Citronelol - - 0.05 - Triethyl citrate - - - 0.05 Sodium benzoate 0.10 0.02 - - Potassium sorbate - - 0.10 0.01 Silver citrate 0.10 - - - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 - - 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 - 0.15 0.10 N- (4- (2,4-dihydroxyphenyl) thiazole-2- 0.01 - - -
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    Recipe examples 55 56 57 58 il) -cyclohexanecarboxamide Water, ad ad 100 ad 100 ad 100 ad 100
    Recipe examples 59 60 61 62 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Isoceteth-20 3.50 3.00 4.00 4.00 Glyceryl isostearate 2.00 2.00 2.00 2.50 Tipprylic Ether - 0.50 2.00 2.50 Capryl-capric acid ester 2.00 1.50 - - Chlorine-aluminum hydrate 5.00 5.00 - 3.00 Persea Gratissima Oil (Avocado Oil) - - 0.20 - Diestearatepolyethylene glycol (150) 0.50 0.50 1.00 1.00 Glycerin 4.00 2.00 - 2.00 Butylene glycol - 3.00 1.00 2.00 Propylene glycol 3.00 - 3.004 - [(cyclopentyl-) bromidehydroxyphenylacetyl) oxy] -1,1-dimethyl-piperidinium 0.05 0.10 - - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4 (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide - - - 0.05
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    Recipe examples 59 60 61 62 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide - - 0.15 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide - - 1.00 0.20 Sodium benzoate 0.10 0.02 - - Potassium sorbate - - 0.10 0.01 Geraniol - 0.05 - - Ethyl-linalool - - 0.05 - Linalol - - - 0.10 perfume 0.25 0.50 0.50 0.75 Water, ad ad 100 ad 100 ad 100 ad 100
    Recipe examples 63 64 65 66 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Etherpolyoxyethylene (20) cetylstearic 3.00 3.00 4.00 4.00 Etherpolyoxyethylene (12) cetylstearic 0.50 0.50 - - Glycerin stearate 3.00 3.00 3.00 3.00 Cetylstearyl alcohol 0.50 0.50 - - Cetyl palmitate 0.50 0.50 - - Capryl-capric acid ester 4.00 4.00 3.50 3.50 Di-n-octyl ether 5.00 5.00 5.00 5.00
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    Recipe examples 63 64 65 66 Diestearatepolyethylene glycol (150) - - 1.00 1.00 Glycerin 4.00 4.00 2.00 2.00 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,41-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 0.01 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 0.15 - N- (4- (2,4-dihydroxiferryl) thiazole-2-il) -cyclohexanecarboxamide 0.01 0.60 1.00 - 1,3-butanediol 0.10 - 0.10Sorbic acid 0.20 0.01 0.02 0.02 hexylcinamal 0.05 0.10 1- (1,2,3,4,5,6,7,8-octahydro-2,3,8,8, -tetramethyl-2-naphthyl) ethan-1-ona0.05 0.103-methyl-5-phenyl-1-pentanol 0.05 0.05 perfume 0.30 0.30 0.50 0.50 Water, ad ad100.00 ad100.00 ad100.00 ad100.00
    Examples of recipe 67 68 69 70 Name INCI / chemistry % inWeight % inWeight % inWeight % inWeight
    68/77
    Recipe examples 67 68 69 70 Steareth-100 1.00 1.00 1.00 1.00 polyglyceryl-3-isostearate 1.60 1.60 1.60 1.60 PEG-45 / dodecylglycol copolymer 0.80 0.80 0.80 0.80 C20-40-alkyl stearate 10.00 10.00 10.00 10.00 Acid triglyceridecaprylic / capric 3.00 3.00 3.00 3.00 Octyldodecanol 3.00 3.00 3.00 3.00 Tipprylic Ether 4.00 4.00 4.00 4.00 Potassium sorbate 0.10 0.10 0.10 0.10 Ethylhexylglycerine 0.10 0.10 0.10 0.10 Butylene glycol 4.00 4.00 4.00 4.00 N- (4 - (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 - 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 - 0.10 N- (4 - (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.01 0.60 - 0.20 Hydroxy-isohexyl 3-cyclohexenocarboxaldehyde 0.05 0.05 0.05 0.05 perfume 0.35 0.30 0.25 0.15 Water, ad ad100.00 ad100.00 ad100.00 ad100.00
    69/77
    EXAMPLE RECIPES
    Recipe examples 71 72 73 74 INCI / chemical name % inWeight % inWeight % inWeight % inWeight Denatured alcohol 20.0 20.0 30.0 30.0 hydroxyethylcellulose 0.40 0.40 0.30 0.30 Polyethylene glycol 400 3.00 3.00 2.00 ZOO Polyethylene glycol (2000) hydrogenated castor oil 2.00 2.00 3.00 3.00 Persea Gratissima Oil (Avocado Oil) 0.50 0.50 0.10 0.10 4 - [(cyclopentylhydroxyphenylacetyl) oxy] -1,1-dimethylpiperidinium bromide 0.10 0.30 - - Sodium benzoate 0.01 0.02 0.01 0.02 Hydantoin DMDM 0.02 0.01 0.02 0.01 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 0.10 0.05 0.01 N- (4 (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 - 0.01 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 - 0.15 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.01 - 1.00 0.20 Coumarina - - 0.05 - Benzyl salicylate - 0.05 - -
    70/77
    Recipe examples 71 72 73 74 Butylphenylmethylpropional 0.05 - - - perfume 0.25 0.30 0.50 0.30 Water, ad ad 100 ad 100 ad 100 ad 100
    Recipe examples 75 76 77 78 INCI / chemical name % inWeight % inWeight % inWeight % inWeight 2-Octyldodecanol 0.50 0.50 0.50 0.50 1,2-propylene glycol 1.00 1.00 1.00 1.00 2-butyloctanoic acid 0.25 - 0.25 - Chlorine-aluminum hydrate 2.00 3.00 - 3.00 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -isobutyramide 0.10 - 0.10 0.05 N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -pivalamide 0.25 0.30 0.01 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -butiramide 0.10 0.25 0.15 - N- (4- (2,4-dihydroxyphenyl) thiazole-2-il) -cyclohexanecarboxamide 0.01 0.60 1.00 - Sorbic acid 0.10 0.10 0.10 0.10 Sodium benzoate 0.10 0.10 0.10 0.10 Linalol 0.05 - 0.05 0.05 Cumarin - - 0.05 - Benzyl salicylate 0.05 0.05 - 0.05
    71/77
    Recipe examples 75 76 77 78 perfume 0.10 0.20 0.40 0.20 Ethanol ad 100 ad 100 ad 100 ad 100
    [096] The liquid phase obtained by mixing the respective components is filled in aerosol flasks with a mixture of propane-butane (2.7) in the proportion of
    39:61.
    Recipe examples 79 80 81 Chemical name % inWeight % inWeight % inWeight Denatured alcohol 20.0 30.0 20.0 Hydroxyethylcellulose 0.40 0.30 0.40 Polyethylene glycol 400 3.00 2.00 3.00 Polyethylene glycol (2000) hydrogenated castor oil 2.00 3.00 2.00 Amazing Persea Oil (Avocado Oil) 0.50 0.10 0.50 4 - [(cyclopentyl-) bromidehydroxyphenylacetyl) oxy] -1,1-dimethyl-piperidinium 0.05 - - N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 0.10 0.10 0.05 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) pivalamide - 0.30 0.01 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide - 0.25 0.15
    72/77
    Recipe examples 79 80 81 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide0.60 1.00 Potassium sorbate 0.20 0.10 0.01 Octane-hydroxamic acid 0.01 0.20 0.10 2-Butyloctanoic acid - 0.10 - Geraniol - 0.05 - Citronelol 0.05 - - ethylinalol - - 0.05 perfume 0.30 0.40 0.20 Water, ad ad 100 ad 100 ad 100
    Recipe examples 82 83 84 INCI / chemical name % inWeight % inWeight % inWeight Glycerin monostearate 5.00 5.00 5.00 Polyethylene glycol monostearate (2000) 2.00 2.00 2.00 Stearyl alcohol 3.00 3 .00 3 .00 Cyclomethicone 4.00 4.00 4.00 Paraffin oil 6.00 6.00 6.00 Trisodium EDTA 0.20 0.20 0.20 Chlorine-aluminum hydrate 2.50 2.50 2.50 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 0.10 0.10 0.05 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -pivalamide 0.25 - 0.01
    73/77
    Recipe examples 82 83 84 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide 0.10 - 0.15 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.01 - 1.00 Sodium benzoate 0.20 0.10 0.10 Methylpropanediol 0.01 0.50 0.60 2-methylpropanediol 3.00 3.00 3.00 2-ethylhexylglyceric ether 0.50 0.50 0.50 Benzyl salicylate - - 0.05 Triethyl citrate - 0. 05 - Hexalcininamal 0.05 - - perfume 0.40 0.30 0.20 Water, ad 100 100 100
    HAIR SHAMPOO
    Example recipe 85 86 Chemical name % by weight % by weight Cocamidopropyl betaine 2.50 230 Sodium Laureth Sulfate 9.00 9.00 PEG-40 hydrogenated castor oil 0.50 0.50 Polyquaternium-10 0.20 0.20 PEG-8 0.50 0.10 Sodium benzoate 0.05 0.45 Laureth-9 2.20 2.20
    74/77
    Example recipe 85 86 Sodium salicylate 0.20 0.20 Epsilon-poly-L-lysine - 0.25 Climbazole 0.45 0.45 Pearly brightness 1.50 1.50 Butyl acrylate / ethyltrimony chloride / styrene copolymer 2.50 1.00 N- (4- (2.4-dihydroxyphenyl) thiazole-2-l) -isobutyramide 0.10 0.10 N- (4- (2.4-dihydroxyphenyl) thiazol-2-l) -pivalamide 025 - N- (4- (2.4-dihydroxyphenyl) thiazol-2-l) -butyramide 0.10 - N- (4- (2.4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.01 - Sodium benzoate 0.10 0.15 perfume 0.30 0.30 Citric acid q.s. q.s Sodium chloride q.s. q.s. Water Ad. 100 Ad 100
    ANTICASPA SHAMPOO
    Example recipe 87 88 Chemical name % by weight % by weight Sodium Laureth Sulfate 9.00 10.00 Cocamidopropyl betaine 4.00 3.00 PEG-5 lauryl citrate sulfosuccinate - 1.00
    75/77
    Example recipe 87 88 disodium Thickener 0.20 0.40 Polyquaternium-10 0.30 0.10 Hydroxypropyl trimonium guar chloride 0.20 - Potassium sorbate 0.10 0.20 Climbazole - 0.50 Epsilon-poly-L-lysine 1.00 0.20 Laureth-9 - 2.00 Pyroctone olamine 1.00 0.50 Selenium sulfide 0.20 - Zinc pyrithione 1.00 1.00 Pearly brightness - 2.50 Clouding agent - 0.50 PEG-40 hydrogenated castor oil 0.50 0.20 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 0.10 0.10 N- (4- (2,4-Dihydroxyphenyl) thiazol-2-yl) pivalamide 0.25 - N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide 0.10 - N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.01 - Sodium salicylate 0.30 0.20
    76/77
    Example recipe 87 88 Sodium benzoate 0.25 0.30 Sodium chloride q.s. q.s. Citric acid q.s. q.s. perfume q. s . q. s . Water ad 100 ad 100
    CAPILLARY TONIC
    Example recipe 89 90 Chemical name % by weight % by weight Ethanol 30.00 40.00 Panthenol 0.20 0.10 Tocopheryl acetate 0.20 - pentylene glycol 0.10 0.15 C12-13-alkyl lactate 0.20 0.10 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) -isobutyramide 0.10 0.10 N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) pivalamide 0.25 - N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) butyramide 0.10 - N- (4- (2,4-dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.01 - Climbazole 0.1 0.1 PEG-40 hydrogenated castor oil - 0.3
    77/77
    Example recipe 89 90 Perfume, preservative q.s. q.s. Water ad 100 ad 100
    1/8
    权利要求:
    Claims (8)
    [1]
    1. COMBINATIONS OF ACTIVE SUBSTANCES, characterized by comprising one or more alkylamidothiazoles and one or more cosmetically or dermatologically acceptable preservatives, selected from the group ethylparaben (120-47-80), propylparaben (94-13-3), methylisothiazolinone (2682 -20-4), methylpropanediol (2163-42-0), butylene glycol (107-88-0), propylene glycol (57-55-6, 4254-142, 4254-15-3), ethylhexylglycerine (70445-33 -9), sodium benzoate (532-32-1), 1,2-hexandiol (6920-22-5), 1,3-butanediol (107-88-0), 1,2-octanediol (11 17- 86-8), potassium sorbate (24634-61-5 / 590-00-1), DMDM hydantoin (6440-58-0), benzyl alcohol (100-51-6), phenoxyethanol (122-99-6) , dehydracetic acid (520-45-6), pyroctone olamine (68890-66-4), methylparaben (99-76-3), alcohol (64-17-5), octanohydroxamic acid (7377-03-9), chloride benzethonium (121-540), glyceryl caprylate (26402-26-6), pentylene glycol (11 1-29-5), lauroethyl arginate (60372-77-2), salicylic acid (69-72-7),benzoic acid (65-85-0), propionic acid (79-09-4), sorbic acid (110-44-1), with salicylic acid, benzoic acid and dehydracetic acid being preferred and where it can also be advantageous to use salts physiologically compatible hydrosoluble metals from these
    Petition 870190105153, of 10/17/2019, p. 6/16
    [2]
    2/8 acids in which the alkylamidothiazole or alkylamidothiazoles have the following structure:

    [3]
    3/8

    [4]
    4/8

    [5]
    5/8

    [6]
    6/8
    thiazol-2-yl) -butyramide Behenyl alcohol 1, 20 1.20 1, 20 Cetyl alcohol 2.00 2.00 2.00 Caprylic acid triglyceride / capric acid 2.50 2.50 2.50 Carbonatetipprilila 2.50 2.50 2.50 Dimethicone 0.35 0.35 0.35 C12- Benzoate15 alkyl 2.50 2.50 2.50 Cyclomethicone 2, 15 2, 15 2, 15 Stearateglyceryl citrate 2.00 2.00 2.00 Glycerin 8.70 8.70 8.70 Butylene glycol 3.00 3.00 3.00 Water + Sodium hydroxide 0.03 0.03 0.03 Methylparaben 0, 20 0, 20 0, 20 Propylparaben 0.10 0.10 0.10 Phenoxyethanol 0.40 0.40 0.40 Carbomer 0.10 0.10 0.10 Sodium polyacrylate 0, 20 0.20 0, 20 Water Ad 100.00
    INCI / Substance Formula 7 Formula 9 N- (4- (2,4dihydroxyphenyl) thiazol-2-yl) cyclohexanecarboxamide 0.10 N- (4- (2,4dihydroxyphenyl) thiazol-2-yl) heptanamide0.10 Behenyl alcohol 1, 20 1, 20 Cetyl alcohol 2.00 2.00 Triglyceride 2.50 2.50
    Petition 870190105153, of 10/17/2019, p. 11/16
    [7]
    7/8
    caprylic acid / capric acidCarbonatetipprilila 2.50 2.50 Dimethicone 0.35 0.35 C12-15 alkyl benzoate 2.50 2.50 Cyclomethicone 2, 15 2, 15 Stearateglyceryl citrate 2.00 2.00 Glycerin 8.70 8.70 Butylene glycol 3.00 3.00 Water + Sodium hydroxide 0.03 0.03 Methylparaben 0, 20 0, 20 Propylparaben 0.10 0.10 Phenoxyethanol 0.40 0.40 Carbomer 0.10 0.10 Polyacrylatesodium 0, 20 0, 20 Water Ad 100.00
    2. COMBINATIONS OF ACTIVE SUBSTANCES, according to claim 1, characterized by the fact that the alkylamidothiazole (s) can be present as halide, carbonate, ascorbate, sulfate, acetate and / or phosphate.
    3. COSMETIC OR DERMATOLOGICAL PREPARATIONS, characterized in that they comprise a content of combinations of active substances, as defined in any of claims 1 or 2.
    PREPARATIONS, according to claim 3, characterized in that they contain 0, 000001 to 10% by weight, in particular, 0.001 to 3% by weight, most preferably
    Petition 870190105153, of 10/17/2019, p. 12/16
    [8]
    8/8
    0.001 to 1% by weight of one or more alkylamidothiazoles, based on the total weight of the preparation.
    5. PREPARATIONS, according to claim 3, characterized in that the total amount of preservatives is 0.00001% by weight to 10% by weight, preferably 0.001% by weight to 5% by weight, in particular, 0.005% by weight to 3 % by weight, based on the total weight of the preparations.
    6. COSMETIC, non-therapeutic use of preparations, as defined in any of claims 3 to 5, or of combinations of active substances, as defined in any of claims 1 or 2, characterized in that it is to lighten human skin.
    7. COMBINATIONS OF ACTIVE SUBSTANCES, as defined in any of claims 1 or 2, and preparations, as defined in any of claims 3 to 5, characterized in that they are for the therapeutic lightening of human skin.
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    同族专利:
    公开号 | 公开日
    MX2015011990A|2015-12-01|
    CN105050575A|2015-11-11|
    EP2968100A1|2016-01-20|
    ES2729374T3|2019-11-04|
    MX362140B|2018-12-24|
    WO2014139757A1|2014-09-18|
    CN105050575B|2019-10-01|
    PL2968100T3|2019-08-30|
    US9610234B2|2017-04-04|
    BR112015022148A2|2017-07-18|
    JP2016510775A|2016-04-11|
    DE102013204081A1|2014-09-11|
    KR20150130358A|2015-11-23|
    JP6444324B2|2018-12-26|
    US20160015615A1|2016-01-21|
    EP2968100B1|2019-04-10|
    KR102143561B1|2020-08-11|
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    法律状态:
    2019-07-23| B06U| Preliminary requirement: requests with searches performed by other patent offices: suspension of the patent application procedure|
    2020-03-03| B09A| Decision: intention to grant|
    2020-03-24| B16A| Patent or certificate of addition of invention granted|Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 14/02/2014, OBSERVADAS AS CONDICOES LEGAIS. |
    优先权:
    申请号 | 申请日 | 专利标题
    DE102013204081.4|2013-03-11|
    DE102013204081.4A|DE102013204081A1|2013-03-11|2013-03-11|Active ingredient combinations of alkylamidothiazoles and one or more cosmetically or dermatologically acceptable preservatives|
    PCT/EP2014/052968|WO2014139757A1|2013-03-11|2014-02-14|Combinations of alkylamidothiazoles and preservatives|
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