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    • 3. 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。
    • 4. 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。
    • 5. 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。
    • 6. 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。
    • 7. 发明授权
    • Use of isoindolinone derivatives as stabilizers for organic materials
    • 异吲哚啉酮衍生物作为有机材料的稳定剂的使用
    • US06210657B1
    • 2001-04-03
    • US09207624
    • 1998-12-09
    • Thorsten HabeckSylke HaremzaHubert TrauthVolker SchehlmannHorst Westenfelder
    • Thorsten HabeckSylke HaremzaHubert TrauthVolker SchehlmannHorst Westenfelder
    • A61K742
    • A61K31/4035C08K5/3417C09D7/48C09K15/30Y10S514/844Y10S514/97Y10S514/972
    • Isoindolinone derivatives of the formula I, in which the variables have the following meanings: R1 is hydrogen, COOR4, COR4, CONR4R5, CN, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C3-C10-cycloalkenyl, aryl or heteroaryl, substituted or unsubstituted; R1 and R2 together are C7-C10-bicycloalkyl or C7-C10-bicycloalkenyl; R3 is 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 or heteroaryl, substituted or unsubstituted, substituents which confer solubility in water, selected from the group consisting of carboxylate, sulfonate or ammonium radicals; R4 and R5 independently of one another are hydrogen, C1-C20-alkyl, C2-C10-alkenyl, C3-C10-cycloalkyl, C3-C10-cycloalkenyl; aryl or heteroaryl, substituted or unsubstituted; are used as stabilizers for organic materials.
    • 式I的异吲哚啉酮衍生物,其中变量具有以下含义:R1是氢,COOR4,COR4,CONR4R5,CN,C1-C20-烷基,C2-C10-烯基,C3-C10-环烷基,C3-C10- 环烯基,芳基或杂芳基,取代或未取代的; R1和R2一起是C7-C10-双环烷基或C7-C10-双环烯基; R3是氢,C1-C20-烷基,C2-C10-烯基,C3-C10-环烷基,C3 -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,芳基或杂芳基,取代或未取代的赋予水溶性的取代基, 羧酸酯,磺酸酯或铵基; R 4和R 5彼此独立地是氢,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; 芳基或杂芳基,取代或未取代的;被用作有机材料的稳定剂。
    • 8. 发明授权
    • Cosmetic and pharmaceutical preparations comprising photostable UV
filters
    • 包含光稳定型紫外线过滤器的化妆品和药物制剂
    • US6090374A
    • 2000-07-18
    • US172672
    • 1998-10-15
    • Thorsten HabeckSylke HaremzaVolker SchehlmannHorst WestenfelderThomas Wunsch
    • Thorsten HabeckSylke HaremzaVolker SchehlmannHorst WestenfelderThomas Wunsch
    • A61K8/00A61K8/40A61K31/00A61P17/00A61P17/16A61Q1/04A61Q17/04A61K7/42A61K7/00A61K7/44
    • A61Q17/04A61K8/40A61Q1/04A61K2800/52
    • The use of substituted .alpha.-methylstyrene derivatives of the formula I, ##STR1## where the variables have the following meanings: R.sup.1 C.sub.4 -C.sub.10 -alkoxy, C.sub.1 -C.sub.12 -alkylamino, C.sub.1 -C.sub.12 -dialkylamino, substituents which confer solubility in water and which are selected from the group consisting of carboxylate, sulfonate or ammonium residues;R.sup.2 hydrogen, C.sub.2 -C.sub.10 -alkyl, C.sub.1 -C.sub.12 -alkoxy;R.sup.3 COOR.sup.5, COR.sup.5, CONR.sup.5 R.sup.6, CN;R.sup.4 COOR.sup.5, COR.sup.5, CONR.sup.5 R.sup.6, CN; where the substituents R.sup.3 and R.sup.4 are identical in each case;R.sup.5 andR.sup.6 independently of one another hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkenyl, aryl, hetaryl, unsubstituted or substituted;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 UV-absorbing compounds known per se for cosmetic and pharmaceutical preparations.
    • 使用式I的取代的α-甲基苯乙烯衍生物,其中变量具有以下含义:R 1 C 4 -C 10 - 烷氧基,C 1 -C 12 - 烷基氨基,C 1 -C 12 - 二烷基氨基,赋予在水中溶解度并且被选择的取代基 由羧酸盐,磺酸盐或铵残基组成的组; R2氢,C2-C10-烷基,C1-C12-烷氧基; R3 COOR5,COR5,CONR5R6,CN; R4 COOR5,COR5,CONR5R6,CN; 其中取代基R 3和R 4在每种情况下相同; R 5和R 6彼此独立地为氢,C 1 -C 12 - 烷基,C 2 -C 10 - 烯基,C 3 -C 10 - 环烷基,C 3 -C 10 - 环烯基,芳基,杂芳基,未取代或取代的; 作为化妆品和药物制剂中的光稳定紫外线过滤器,用于保护人体皮肤或人体毛发免受太阳光线的照射,或者与本身已知的用于化妆品和药物制剂的紫外线吸收化合物一起使用。