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    • 1. 发明授权
    • Use of substituted vinyltetrahydronaphthalenes and vinyl-benzotetrahydropyrans as light protection agents
    • 使用取代的乙烯基四氢萘和乙烯基 - 苯并四氢吡喃作为防光剂
    • US06524560B1
    • 2003-02-25
    • US09583760
    • 2000-05-31
    • Frank PrechtlThorsten HabeckHorst WestenfelderThomas Wünsch
    • Frank PrechtlThorsten HabeckHorst WestenfelderThomas Wünsch
    • A61K742
    • A61K8/40A61K8/368A61K8/37A61K8/498A61K2800/52A61Q17/04
    • The invention relates to the use of compounds of the formula I in which X is the divalent radical of oxygen, a carbonyl radical, optionally aliphatically substituted imino or the radical ═CR9R10, Y is a carbonyl group or the radical ═CR9R10, R1 and R2 are identical or different electron-withdrawing radicals, chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl, optionally substituted aminocarbonyl, alkyl- or arylsulfinyl, alkyl- or arylsulfonyl and optionally substituted aminosulfonyl, R3 is a hydrogen atom, a cyano, hydroxyl, carboxyl or aminocarbonyl group or a C5-C20-aryl radical or C1-C20-alkylradical optionally bonded via an oxygen bridge, an aminocarbonyl bridge or oxycarbonyl bridge, R4 is a hydrogen atom, a hydroxyl group, an amino group, or a C5-C20-aryl radical or C1-C20-alkyl radical optionally bonded via an oxygen bridge, and R5 to R10 independently of one another are hydrogen or C1-C20-alkyl radicals and where in addition R7 and R8 together with the chain carbon atom are a carbonyl group, as photostable UV filters in cosmetic and pharmaceutical preparations for protecting human skin and human hair from solar rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    • 本发明涉及式Iin化合物的用途,其中X是氧的二价基团,羰基,任选地是脂族取代的亚氨基或基团= CR 9 R 10,Y是羰基或基团= CR 9 R 10,R 1和R 2相同 或不同的吸电子基团,其选自氰基,烷基 - 或芳基羰基,烷氧基 - 或芳氧基羰基,任选取代的氨基羰基,烷基 - 或芳基亚磺酰基,烷基 - 或芳基磺酰基和任选取代的氨基磺酰基,R 3是氢原子, 氰基,羟基,羧基或氨基羰基或C 5 -C 20 - 芳基或任选经由氧桥,氨基羰基桥或氧羰基桥键合的C 1 -C 20烷基取代基,R 4是氢原子,羟基,氨基, 或通过氧桥任选键合的C 5 -C 20芳基或C 1 -C 20烷基,R 5至R 10彼此独立地为氢或C 1 -C 20 - 烷基,并且其中R 7和R 8为 具有链状碳原子的碳原子是羰基,作为用于保护人类皮肤和人类头发免受太阳光线影响的化妆品和药物制剂中的光稳定性紫外线过滤器,单独或与在UV区域吸收的化合物一起,并且本身已被用于化妆品和 药物制剂。
    • 4. 发明授权
    • Photo-stable cosmetic and pharmaceutical formulations containing UV-filters
    • 光稳定的化妆品和药物配方含有紫外线过滤器
    • US06407247B1
    • 2002-06-18
    • US09494474
    • 2000-01-31
    • Thorsten HabeckAlexander AumüllerVolker SchehlmannHorst WestenfelderThomas Wünsch
    • Thorsten HabeckAlexander AumüllerVolker SchehlmannHorst WestenfelderThomas Wünsch
    • C07D22102
    • C07D275/03A61K8/411A61K8/42A61K8/466A61K8/49A61K8/498A61K8/4986A61Q1/04A61Q17/04C07C229/56C07C229/60C07C255/30C07C255/58C07C309/46C07D319/06C07D333/38
    • A method of using compounds of formula I in which the C═C double bond is present in E and/or Z configuration and the variables have the following meanings: R1 denotes COOR5, COR5, CONR5R6, CN, O═S(—R5)═O, O═S(═OR5)═O, R7O—P(—OR8)═O; R2 denotes COOR6, COR6, CONR5R6, CN, O═S(—R6)═O, O═S(═OR6)═O, R7O—P(—OR8)═O; R3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms; R4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms; R5 to R8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms, where the variables R3 to R8 may also form, together with the carbon atoms to which they are attached, a 5-membered or 6-membered ring, which may be anellated if desired, as UV filters, particularly UV-A filters, in cosmetic and pharmaceutical formulations for the protection of the human skin or human hair from solar radiation, alone or together with compounds known per se in cosmetic and pharmaceutical formulations and capable of absorbing radiation in the UV range.
    • 在E和/或Z构型中使用存在C = C双键的式Iin化合物的方法,并且变量具有以下含义:R 1表示COOR 5,COR 5,CONR 5 R 6,CN,O = S(-R 5)= O = S(= OR5)= O,R7O-P(-OR8)= O; R2表示COOR6,COR6,CONR5R6,CN,O = S(-R6)= O,O = S(= OR6)= O,R7O-P(-OR8)= O; R3表示氢,任选取代的脂族,脂环族,芳脂族或芳族基团,其中每种情况下最多可达18个碳原子; R4表示任选取代的芳族或杂芳族基团, 12个环原子; R5至R8独立地表示氢,开链或支链脂族,芳脂族,脂环族或任选取代的芳族基团,其中每种情况最多可包含18个碳原子,其中变量R3至R8也可以形成, 它们所连接的碳原子,5元或6元环,如果需要,可以将其作为UV滤光器,特别是UV-A滤光器,在化妆品和药物中 用于保护人类皮肤或人类头发免受太阳辐射,单独或与化妆品和药物制剂中本身已知的化合物一起并且能够吸收UV范围内的辐射。
    • 6. 发明授权
    • Use of cyclic enamines as light protection agents
    • 使用环状烯胺作为防晒剂
    • US06603014B1
    • 2003-08-05
    • US10053323
    • 2002-01-23
    • Thorsten HabeckFrank PrechtlThomas WünschHorst Westenfelder
    • Thorsten HabeckFrank PrechtlThomas WünschHorst Westenfelder
    • C07D27764
    • A61K8/4946A61K8/49A61K8/494A61K2800/52A61Q1/04A61Q17/04
    • The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2—CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical where R3 is as defined above, is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation, as photostable UV filters in cosmetic and pharmaceutical preparations to protect human skin and human hair against solar rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    • 使用其中R 1和R 2相同或不同的式Iin化合物,选自氰基,烷基 - 或芳基羰基,烷氧基 - 或芳氧基羰基和任选取代的氨基羰基的吸电子基,R 3是氢原子,C 1 -C 20 - 烷基或C 3 -C 20环烷基或式-CH 2 -CH 2 -SO 3 -M +的基团,其中M +是阳离子,X是氧,硫或基团的二价基团,其中R3如所定义 是式II或III的二价基团,其与式I的基团形成稠合体系,其中R 4可以与亚苄基环I或亚萘基环II键合一次或多次,并且是氢,烷基,环烷基 ,烷氧基,环烷氧基,烷氧基羰基,单或二烷基氨基羰基,烷基氨基,二烷基氨基,各自具有至多20个碳原子,以及氰基,氨基和SO3-M +,其中M +是阳离子,作为化妆品和药物制剂中的光稳定性UV过滤剂 保护人体皮肤a 将人类头发抵抗太阳光线,单独或与在UV区域吸收的化合物一起,并且本身已知用于化妆品和药物制剂。
    • 8. 发明授权
    • Cosmetic and pharmaceutical preparations containing photostable UV filters
    • 含有光稳定紫外线过滤器的化妆品和药物制剂
    • US06545174B2
    • 2003-04-08
    • US09765624
    • 2001-01-22
    • Thorsten HabeckSylke HaremzaVolker SchehlmannHorst WestenfelderThomas WünschMichael DrögemüllerVolker Bomm
    • Thorsten HabeckSylke HaremzaVolker SchehlmannHorst WestenfelderThomas WünschMichael DrögemüllerVolker Bomm
    • C07C6976
    • C07C235/34A61K8/35A61K8/37A61K8/40A61K8/42A61K31/12A61K31/122A61K31/216A61K31/277A61K2800/52A61Q1/04A61Q17/04C07C69/618C07C233/11
    • 4,4-Diarylbutadienes of the formula I, where the diene system has the Z,Z; Z,E; E,Z or E,E configuration or a mixture thereof, and where the variables independently of one another have the following meanings: R1 and R2 are hydrogen, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C3-C10-cycloalkenyl, C1-C12-alkoxy, C1-C20-alkoxycarbonyl, C1-C12-alkylamino, C1-C12-dialkylamino, aryl, hetaryl, unsubstituted or substituted, substituents which confer solubility in water and are selected from the group consisting of carboxylate, sulfonate, or ammonium residues; R3 is COOR5, CONR5R6; R4 is COOR6, CONR5R6; R5 and R6 are hydrogen, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C7-C10-bicycloalkyl, C3-C10-cycloalkenyl, C7-C10-bicycloalkenyl, aryl, hetaryl, unsubstituted or substituted; n is 1 to 3; and R3 and R4 are not COOCH3 when R1 and R2 are hydrogen, are used as photostable UV filters in cosmetic and pharmaceutical preparations to protect the human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    • 式I的4,4-二芳基丁二烯,其中二烯体系具有Z,Z; Z,E; E,Z或E,E构型或其混合物,其中彼此独立的变量具有以下含义:R 1和R 2为氢,C 1 -C 20 - 烷基,C 2 -C 10 - 烯基,C 3 -C 10 - 环烷基, C 3 -C 10 - 环烯基,C 1 -C 12 - 烷氧基,C 1 -C 20烷氧基羰基,C 1 -C 12 - 烷基氨基,C 1 -C 12 - 二烷基氨基,芳基,杂芳基,未取代或取代的取代基,其赋予在水中的溶解性并且选自 由羧酸盐,磺酸盐或铵残基组成; R3为COOR5,CONR5R6; R4是COOR6,CONR5R6; R 5和R 6是氢,C 1 -C 20烷基,C 2 -C 10 - 烯基,C 3 -C 10 - 环烷基,C 7 -C 10 - 双环烷基,C 3 -C 10 - 环烯基,C 7 -C 10 - 双环烯基,芳基,杂芳基,未取代或取代的; n为1〜3; 当R 1和R 2为氢时,R 3和R 4不是COOCH 3,用作化妆品和药物制剂中的光稳定性UV过滤剂,以保护人皮肤或人类头发免受太阳光线的影响,单独或与在UV区域吸收的化合物一起, 本身就是化妆品和药物制剂。
    • 9. 发明授权
    • Oligomeric diarylbutadienes
    • 低聚二芳基丁二烯
    • US06436373B1
    • 2002-08-20
    • US09455484
    • 1999-12-06
    • Thorsten HabeckThomas WünschHorst Westenfelder
    • Thorsten HabeckThomas WünschHorst Westenfelder
    • A61K742
    • A61Q17/04A61K8/40C07C69/618C07C255/41
    • Oligomeric 4,4-diarylbutadienecarboxylates and -carboxamides of the formula I in which R1 and R2 independently of one another are hydrogen, an aliphatic, cycloaliphatic, aromatic, araliphatic or heterocyclic radical or substituents which confer solubility in water, chosen from the group consisting of carboxylate, sulfonate or ammonium radicals; R3 is an aliphatic, cycloaliphatic, aromatic, araliphatic or heterocyclic radical or a radical which is bonded by a carbonyl, sulfonyl or a phosphonyl group, or is a carboxylate or a cyano group; Y is the group; in which R4 is hydrogen, an aliphatic, cycloaliphatic, aromatic, araliphatic or heterocyclic radical and m is from 2 to 10, n is from 1 to 3, and x is the m-valent radical of a polyol having from 2 to 10 hydroxyl groups.
    • 式Iin的低聚4,4'-二芳基丁二羧酸酯和羧酰胺,其中R 1和R 2彼此独立地是氢,脂族,脂环族,芳族,芳脂族或杂环基或其在水中赋予溶解性的取代基,其选自羧酸酯, 磺酰基或铵基; R 3是脂族,脂环族,芳族,芳脂族或杂环基或通过羰基,磺酰基或膦酰基键合或者是羧酸酯或氰基键合的基团; Y是基团;其中R 4 是氢,脂族,脂环族,芳族,芳脂族或杂环基团,且m为2至10,n为1至3,x为具有2至10个羟基的多元醇的m价基团。
    • 10. 发明授权
    • Use of cyclic enamines as light protection agents
    • 使用环状烯胺作为防晒剂
    • US06413503B1
    • 2002-07-02
    • US09583288
    • 2000-05-31
    • Thorsten HabeckFrank PrechtlThomas WünschHorst Westenfelder
    • Thorsten HabeckFrank PrechtlThomas WünschHorst Westenfelder
    • A61K742
    • A61K8/4946A61K8/49A61K8/494A61K2800/52A61Q1/04A61Q17/04
    • The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2-CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical  where R3 is as defined above, Z is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I  where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation,  as photostable UV filters in cosmetic and pharmaceutical preparations to protect human skin and human hair against solar rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    • 使用其中R 1和R 2相同或不同的式Iin化合物,选自氰基,烷基 - 或芳基羰基,烷氧基 - 或芳氧基羰基和任选取代的氨基羰基的吸电子基,R 3是氢原子,C 1 -C 20 - 烷基或C 3 -C 20环烷基或式-CH 2 -CH 2 -SO 3 -M +的基团,其中M +是阳离子,X是氧,硫或R3的二价基团,其中R 3为 Z是式II或III的二价基团,其与式I基团形成稠合体系,其中R4可以与亚苄基环I或亚萘基环II键合一次或多次,并且是氢, 烷基,环烷基,烷氧基,环烷氧基,烷氧基羰基,单或二烷基氨基羰基,烷基氨基,二烷基氨基,各自具有至多20个碳原子,以及氰基,氨基和SO3-M +,其中M +是阳离子,作为化妆品中的光稳定性紫外线过滤器 药物制剂保护人类 亲和人类头发对抗太阳光线,单独或与在UV区域吸收的化合物一起,并且本身已知用于化妆品和药物制剂。