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    • 2. 发明申请
    • DIMERIC BENZYLIDENE MALONATES
    • 二甲苯胆碱
    • US20110038815A1
    • 2011-02-17
    • US12867777
    • 2009-03-04
    • Markus HanschThomas EhlisBarbara Wagner
    • Markus HanschThomas EhlisBarbara Wagner
    • A61K8/37C07C67/31A61Q17/04
    • A61Q17/04A61K8/37A61K8/585C07C67/03C07C67/31C07C67/343C07C69/734C07C2601/14C07F7/0889C07C69/732
    • Disclosed is the use of benzylidene malonates of formula (1), wherein R1 and R2, independently from each other are hydrogen; OH; C1-C12alkyl; C1-C12alkoxy; C1-C12alkylamino; C1-C12dialkylamino; water-solubilizing groups, selected from carboxylate, sulfonates or ammonium radicals; R3 is COOR5; COR5; CONR5R6; CN; or SO2R7, R4 is COOR8; COR9; CONR8R9; CN; or SO2R10; R5, R6, R7, R8, R9 and R10 independently from each other are C1-C18alkyl; unsubstituted or by one or more than one C1-C4alkyl substituted C3-C12-cycloalkyl; unsubstituted or C1-C6alkyl-substituted C6-C20aryl; organosilanyl, or organosiloxanyl; A is —C1-C20alkylene-, —CH2CH(OH)CH2—, —C5-C20cycloalkylene, —C2-C20alkenylene-, —C5-C10arylene-, or —C5-C10arylene-(C1-C10alkylene)- which are unsubstituted or substituted, straight-chain or branched, optionally interrupted by one or more than one heteroatoms selected from —O, —S— or —NH—; for the protection of human and animal hair and skin against UV radiation.
    • 公开了式(1)的亚苄基丙二酸酯的用途,其中R 1和R 2彼此独立地为氢; 哦; C 1 -C 12烷基; C1-C12烷氧基; C 1 -C 12烷基氨基; C1-C12二烷基氨基; 选自羧酸盐,磺酸盐或铵基的水溶性基团; R3为COOR5; COR5; CONR5R6; CN; 或SO 2 R 7,R 4为COOR 8; COR9; CONR8R9; CN; 或SO2R10; R 5,R 6,R 7,R 8,R 9和R 10彼此独立地为C 1 -C 18烷基; 未取代或被一个或多个C 1 -C 4烷基取代的C 3 -C 12 - 环烷基取代; 未取代的或C 1 -C 6烷基取代的C 6 -C 20芳基; 有机硅烷基或有机硅氧烷基; A是未取代或取代的-C 1 -C 20亚烷基 - , - CH 2 CH(OH)CH 2 - , - C 5 -C 20亚环烷基,-C 2 -C 20亚烯基,-C 5 -C 10亚芳基或-C 5 -C 10亚芳基 - (C 1 -C 10亚烷基) 直链或支链,任选被一个或多于一个选自-O,-S-或-NH-的杂原子中断; 用于保护人和动物的头发和皮肤免受紫外线辐射。
    • 3. 发明申请
    • UV FILTER COMBINATIONS COMPRISING BENZYLIDENE MALONATES
    • 紫外线过滤器组合包含苄基胆碱酯
    • US20120128611A1
    • 2012-05-24
    • US13381965
    • 2010-06-29
    • Julie GrumelardThomas EhlisPaul Adriaan Van Der SchaafMarkus HanschMyriam Sohn
    • Julie GrumelardThomas EhlisPaul Adriaan Van Der SchaafMarkus HanschMyriam Sohn
    • A61K8/37A61K8/49A61K8/58A61Q17/04
    • A61Q17/04A61K8/37
    • Disclosed is the use of a UV filter combination, comprising (a) a first UV filter selected from benzylidene malonates of formula (1), wherein R1 methyl; ethyl; propyl; or n-butyl; if R1 is methyl, then R is tert. butyl; formula (II); formula (III); a radical of formula (1a); or a radical of formula (1b); wherein R2 and R3, independently from each other are hydrogen; or methyl; R4 is methyl; ethyl; or n-propyl; R5 and R6 independently from each other are hydrogen; or C1-C3alkyl; if R1 is ethyl; propyl; or n-butyl, then R is isopropyl; and (b) a second UV filter selected from (b1) Bis-Ethylhexyloxyphenol Methoxyphenyl Triazine; (b2) Butyl Methoxydibenzoylmethane; (b3)Diethylhexyl Butamido Triazone; (b4) Ethylhexyl Triazone; (b5) Diethylamino Hydroxy Benzoyl Hexyl Benzoate; (b6) Ethylhexyl Methoxycinnamate; (b7) Ethylhexyl Salicylate; (b8) Homosalate; (b9) Octocrylene; (b10) micronized Methylene Bis-Benzotriazolyl Tetramethylbutylphenol; (b11) Phenylbenzimidazole Sulfonic Acid; (b12) Titanium Dioxide; (b13) micronized Tris-Biphenyl Triazine; and (b14) micronized (2-{4-[2-(4-Diethylamino-2-hydroxy-benzoyl)-benzoyl]-piperazine-1-carbonyl}-phenyl)-(4-diethylamino-2-hydroxy-phenyl)-methanone; (b15) benzoicacid,4,4-[[3-[1,3,3,3-tetramethyl-1-[trimethylsilyl)oxy]-1-disiloxanyl]propyl]amino]-1,3,5-triazine-2,4-diyl]diimino]bis-, dibutyl ester wherein the UV filter combination comprises at least 2 UV filters of component (b1)-(b14); for the protection of human and animal hair and skin against UV radiation.
    • 公开了使用UV过滤器组合,其包含(a)选自式(1)的亚苄基丙二酸酯的第一UV过滤器,其中R 1甲基; 乙基; 丙基; 或正丁基; 如果R1是甲基,那么R是叔丁基。 丁基; 式(II); 式(III); 式(1a)的基团; 或式(1b)的基团; 其中R2和R3彼此独立地是氢; 或甲基; R4是甲基; 乙基; 或正丙基​​; R5和R6彼此独立地是氢; 或C 1 -C 3烷基; 如果R1是乙基; 丙基; 或正丁基,那么R是异丙基; 和(b)选自(b1)双 - 乙基己氧基苯酚甲氧基苯基三嗪的第二UV过滤器; (b2)丁基甲氧基二苯甲酰甲烷; (b3)丁酰己二酸二乙基己酯; (b4)乙基己基三嗪酮; (b5)二乙基氨基羟基苯甲酰己基苯甲酸酯; (b6)甲氧基肉桂酸乙基己酯; (b7)水杨酸乙基己酯; (b8)均质酸; (b9) (b10)微米亚甲基双苯并三唑基四甲基丁基苯酚; (b11)苯基苯并咪唑磺酸; (b12)二氧化钛; (b13)微粉化的三联苯三嗪; 和(b14)微粉化(2- {4- [2-(4-二乙基氨基-2-羟基 - 苯甲酰基) - 苯甲酰基] - 哌嗪-1-羰基} - 苯基) - (4-二乙基氨基-2-羟基 - 苯基) 甲酮 (b15)苯甲酸,4,4 - [[3- [1,3,3,3-四甲基-1- [三甲基甲硅烷基]氧基] -1-二硅氧烷基]丙基]氨基] -1,3,5-三嗪-2 ,4-二基]二亚氨基]双 - 二丁酯,其中UV滤光器组合包含至少2个组分(b1) - (b14)的UV滤光剂; 用于保护人和动物的头发和皮肤免受紫外线辐射。
    • 4. 发明授权
    • UV filter combinations comprising benzylidene malonates
    • US09764169B2
    • 2017-09-19
    • US13381965
    • 2010-06-29
    • Julie GrumelardThomas EhlisMarkus HanschMyriam Sohn
    • Julie GrumelardThomas EhlisMarkus HanschMyriam Sohn
    • A61Q17/04A61K8/37
    • A61Q17/04A61K8/37
    • Disclosed is the use of a UV filter combination, comprising (a) a first UV filter selected from benzylidene malonates of formula (1), wherein R1 methyl; ethyl; propyl; or n-butyl; if R1 is methyl, then R is tert. butyl; formula (II); formula (III); a radical of formula (1a); or a radical of formula (1b); wherein R2 and R3, independently from each other are hydrogen; or methyl; R4 is methyl; ethyl; or n-propyl; R5 and R6 independently from each other are hydrogen; or C1-C3alkyl; if R1 is ethyl; propyl; or n-butyl, then R is isopropyl; and (b) a second UV filter selected from (b1) Bis-Ethylhexyloxyphenol Methoxyphenyl Triazine; (b2) Butyl Methoxydibenzoylmethane; (b3)Diethylhexyl Butamido Triazone; (b4) Ethylhexyl Triazone; (b5) Diethylamino Hydroxy Benzoyl Hexyl Benzoate; (b6) Ethylhexyl Methoxycinnamate; (b7) Ethylhexyl Salicylate; (b8) Homosalate; (b9) Octocrylene; (b10) micronized Methylene Bis-Benzotriazolyl Tetramethylbutylphenol; (b11) Phenylbenzimidazole Sulfonic Acid; (b12) Titanium Dioxide; (b13) micronized Tris-Biphenyl Triazine; and (b14) micronized (2-{4-[2-(4-Diethylamino-2-hydroxy-benzoyl)-benzoyl]-piperazine-1-carbonyl}-phenyl)-(4-diethylamino-2-hydroxy-phenyl)-methanone;(b15) benzoicacid,4,4-[[3-[1,3,3,3-tetramethyl-1-[trimethylsilyl)oxy]-1-disiloxanyl]propyl]amino]-1,3,5-triazine-2,4-diyl]diimino]bis-, dibutyl ester wherein the UV filter combination comprises at least 2 UV filters of component (b1)-(b14); for the protection of human and animal hair and skin against UV radiation.
    • 7. 发明授权
    • Merocyanine derivatives for cosmetic use
    • 用于化妆品使用的花青衍生物
    • US07893292B2
    • 2011-02-22
    • US12378566
    • 2009-02-17
    • Barbara WagnerThomas EhlisStefan Müller
    • Barbara WagnerThomas EhlisStefan Müller
    • C07C255/00A61K8/00A61K8/18A61K8/49A61K31/13A61K31/16A61Q17/04A01N33/00A01N33/02
    • C07D295/116A61K8/41A61K8/44A61K8/46A61K8/494A61K8/81A61Q17/00A61Q17/02C07C225/20C07C229/46C07C255/31C07C317/48C07C2601/14C07C2601/16C07D295/155
    • Described are merocyanine derivatives of formula wherein R2 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; a cyano group; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is optionally interrupted by —O— or by —NR7—; R4 is a cyano group; or -Q1-R5; Q1 is —COO—; —CONH—; —CO—; —SO2—; or —CONR6—; R5 is C1-C22alkyl; cyclo-C3-C8alkyl; or unsubstituted or C1-C6alkyl-substituted C6-C20aryl; R6 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; R7 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; the cyclohexene radical C is not substituted or substituted by one or more C1-C5alkyl; m is from 3 to 7; n is from 2 to 4; and o is from 2 to 4. Said merocyanine derivatives are useful in protecting human and animal hair and skin from UV radiation and to cosmetic compositions comprising said derivatives.
    • 描述的是下式的部花青衍生物其中R2是氢; C 1 -C 22烷基; 环-C 3 -C 8烷基; 未取代的或C 1 -C 6烷基 - 或C 1 -C 6烷氧基取代的C 6 -C 20芳基; 氰基; 或R 1和R 2与连接它们的氮原子一起形成 - (CH 2)m - 环,其任选被-O-或-NR 7 - 间隔; R4是氰基; 或-Q1-R5; Q1是-COO-; -CONH-; -CO-; -SO2-; 或-CONR6-; R5是C1-C22烷基; 环C 3 -C 8烷基; 或未取代的或C 1 -C 6烷基取代的C 6 -C 20芳基; R6是氢; C 1 -C 22烷基; 环-C 3 -C 8烷基; 未取代的或C 1 -C 6烷基 - 或C 1 -C 6烷氧基取代的C 6 -C 20芳基; R7是氢; C 1 -C 22烷基; 环-C 3 -C 8烷基; 未取代的或C 1 -C 6烷基 - 或C 1 -C 6烷氧基取代的C 6 -C 20芳基; 环己烯基C不被一个或多个C 1 -C 5烷基取代或取代; m为3〜7; n为2〜4; 和o为2至4.所述的部花青衍生物可用于保护人和动物毛发和皮肤免受紫外线辐射和包含所述衍生物的化妆品组合物。
    • 8. 发明授权
    • Merocyanine derivatives
    • US07772242B2
    • 2010-08-10
    • US11630489
    • 2005-06-20
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • A61K31/519A61K31/445A61K31/16A61K31/165
    • A61K8/498A61K8/4913A61K8/494A61Q17/04
    • Disclosed is the use of the compounds of formula  wherein Q is —OH; —OR7; —NH2; —NHR7; —NR7R8; or —N═R9; T is —COR5; —CN; or —SO2—(C6-C12)aryl; R1 is hydrogen; —OR7, —SR7; —NHR7; —NR7R8; C1-C22alkyl; C2-C12Alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R2 and R3 independently from each other are C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl, C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C3-C12cycloheteroalkyl; C2-C11heteroaralkyl, C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; CONH2; CONHR7; CONR7R8; SO2(C6-C12)aryl, C2-C12alk-1 -enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl, C3-C5heterocycloalkyl, C6-C10aryl; or C1-C9heteroaryl; R5 is —COR7; —COOR7; —OR7; —SR7, —NHR7, —NR7R8; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12alkylphenyl; C1-C12alkoxy-C6-C10aryl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C3-C12cycloheteroalkyl; C6-C10aryl; C1-C12alkoxy-C6-C10aryl or C1-C9heteroaryl; R6, R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; o-C6-C10aryl; or C1-C9heteroaryl; R9 is a (C1-C6)alkylidene radical; or R1 and R2, R1 and Q, R1 and R4, R1 and R6, R2 and R3, R3 and Q, R6 and Q, T and Q, each independently, are linked together, so that 1, 2, 3 or 4 carbocyclic or N, O and/or S-heterocyclic rings are formed, wherein each of them, independently from each other, may be condensed with an aromatic or heteroaromatic ring, and/or more N-, O- and/or S-heterocycic rings, and each N atom in a N-heterocyclic ring may be substituted by C1-C22alkyl; and n is a number from 1 to 4; for protecting of human hair and skin against the damaging effect of UV radiation.