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    USE OF BENZOTROPOLONE DERIVATIVES AS UV ABSORBERS AND ANTIOXIDANTS AND THEIR USE IN SUNSCREENS AND/OR COSMETIC COMPOSITIONS
    27.
    发明申请
    USE OF BENZOTROPOLONE DERIVATIVES AS UV ABSORBERS AND ANTIOXIDANTS AND THEIR USE IN SUNSCREENS AND/OR COSMETIC COMPOSITIONS 审中-公开
    作为紫外线吸收剂和抗氧化剂的苯并吡喃酮衍生物的使用及其在SUNSCREENS和/或化妆品组合物中的应用

    公开(公告)号：WO2009156324A3

    公开(公告)日：2012-06-21

    申请号：PCT/EP2009057587

    申请日：2009-06-18

    申请人： BASF SE ,  WAGNER BARBARA ,  OEHRLEIN REINHOLD ,  HERZOG BERND ,  EICHIN KAI ,  BAISCH GABRIELE ,  PORTMANN STEPHANIE

    发明人： WAGNER BARBARA ,  OEHRLEIN REINHOLD ,  HERZOG BERND ,  EICHIN KAI ,  BAISCH GABRIELE ,  PORTMANN STEPHANIE

    IPC分类号： A61Q17/00 ,  A61K8/35 ,  A61Q17/04 ,  C07C49/717 ,  C07C49/747 ,  C07C62/38 ,  C07C69/712 ,  C07C69/757 ,  C07C305/18 ,  C07D311/02 ,  C07F9/40 ,  C07H15/18 ,  C07H15/203 ,  C07H15/26

    CPC分类号： A61Q17/04 ,  A61K8/35 ,  A61Q19/08 ,  C07C49/747 ,  C07C62/38 ,  C07C69/712 ,  C07C69/757 ,  C07C305/18 ,  C07C2602/12 ,  C07F9/4006 ,  C07H15/18 ,  C07H15/203 ,  C07H15/26

    摘要： Described is the use of benzotropolone and their derivatives, especially the compounds of formula (1); wherein R2, R3, R4, R5 and R6 independently of one another are hydrogen; OH; C1-C30alkyl, C2-C30al- kenyl, C1-C30alkoxy, C3-C12cycloalkyl or C1C30hydroxyalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substitu¬ ted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2- C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, CN, or -CO-R17; C1-C30mono- or dialkylamino; COR9; COOR9; CONR9R10; CN; SO2R9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; *-(CO)-NH-(CH2)n1-(PO)-(OR11)2; -(CO)-O-(CH2)n1-(PO)-(OR11)2; sulphate; sulphonate; phosphate; phosphonate; -(CH2)n2-[O-(SO2)]n3-OR11; -O-(CH2)n4(CO)n5-R11; -(O)n6-(CH2)n7-(PO)-(OR9)2; -(O)n6-(CH2)n7-SO2-OR9; halogen; organosilanyl; organo- siloxanyl; or a sugar residue linked directly in an a- or ß-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar- (CH2)n-(X1)1 or 0 -benzotropolone system, wherein n = 1 -10 and X1 = -0-; -(CO)-; -0-C0-; -COO-, -NH-; -S-; -SO2-); R1, R7 and R8 independently of one another are hydrogen; C1C12alkyl or C3-C12-cycloalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6- C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, or COOR9; COR9; CONR9R10; SO3R9; SO2R9; PO3(R9)2; PO2(R9)2; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an a- or ß-mode via the anomeric oxygen to the benzotropolone system or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar-(CH2)n-(X2)1 or 0-*, wherein n = 1 -10 and X2 = -C(=0)-; -0-C0-*); R9 and R10 independently from each other are hydrogen; C1C18alkyl or C3-C12-cycloalkyl which may be substituted by one or more E and/or interrupted by one or more D; C6- C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an a- or ß-mode via the anomeric oxygen or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar- (CH2)n-*, wherein n = 1 -10); or R9 and R10 together form a five or six membered ring, R11 is hydrogen; or C1-C5alkyl; n1, n2, n4 and n7 independently from each other are a number from 1 to 5; n3, n5 and n6 independently from each other are a 0; or 1; D is -CO-; -COO-; -S-; -SO-; -SO2-; -O-; -NR14-; -S1R19R20-; -POR11-; -CR12=CR13-; or -C=C-; and E is -0R18; -SR18; -NR14R15; -NR14COR15; -C0R17; -COOR16; -CONR14R15; -CN; halogen; Or SO3R18; SO2R18; PO3(R18)2; PO2(R18)2; organosilanyl; organosiloxanyl; or a sugar residue linked directly in an a- or ß-mode via the anomeric oxygen or via a linear or branched alkylene, alkenylene, alkadiene or alkatriene spacer (sugar- (CH2)n-(X1)1 or 0-*, wherein n = 1 -10 and X1 = -0-; -C(=0)-; -0-C0-; -COO-; -NH-; -S-; -SO2-); G is E; C1-C18alkyl, which is optionally interrupted by D; C1-C18perfluoroalkyl; C1-C18alkoxy, which is optionally substituted by E and/or interrupted by D; wherein R12, R13, R14 and R15 independently of each other are hydrogen; C6-C18aryl which is optionally substituted by OH, C1-C18alkyl or C1-C18alkoxy; C1-C18alkyl, which is optionally interrupted by -O-; or Ri4 and Ri5 together form a five or six membered ring, Ri6 is hydrogen; C6-Ci8aryl which is optionally substituted by OH, C1-C18alkyl or d- C18alkoxy; C1-C18alkyl which is optionally interrupted by -O-; R17 is H; C6-C18aryl which is optionally substituted by OH, C1-C18alkyl or C1-C18alkoxy; or d- C18alkyl which is optionally interrupted by -O-; R18 is hydrogen; C6-C18aryl, which is optionally substituted by OH, C1-C18alkyl or d- C18alkoxy; C1-C18alkyl, which is optionally interrupted by -O-; R19 and R20 independently of each other are hydrogen; C1-C18alkyl; C6-C18aryl which is optionally substituted by C1-C18alkyl; and R21 is C1-C18alkyl; or C6-C18aryl, which is substituted by C1-C18alkyl; * means, that this radical is directed to the benzotropolone moiety; for the protection of human and animal hair and skin against UV radiation.

    摘要翻译： 描述了苯佐龙醇及其衍生物，特别是式（1）的化合物的用途; 其中R2，R3，R4，R5和R6彼此独立地是氢; 哦; C 1 -C 30烷基，C 2 -C 30亚烯基，C 1 -C 30烷氧基，C 3 -C 12环烷基或C 1 -C 30羟烷基，其可以被一个或多个E取代和/或被一个或多个D中断; 可以被一个或多个G取代的C 6 -C 20芳基; 可以被一个或多个G，C 2 -C 18烯基，C 2 -C 18炔基，C 7 -C 25芳烷基，CN或-CO-R 17取代的C 4 -C 20杂芳基; C 1 -C 30单 - 或二烷基氨基; COR 9; COOR9; CONR9R10; CN; SO 2 R 9; OCOOR9; OCOR9; NHCOOR9; NR9COR10; NH2; * - （CO）-NH-（CH 2）N 1 - （PO） - （OR 11）2; - （CO）-O-（CH 2）N 1 - （PO） - （OR 11）2; 硫酸盐; 磺酸盐; 磷酸盐; 膦酸盐; - （CH 2）N 2 - [O-（SO2）] N3-OR11; -O-（CH2）N4（CO）N5-R11; - （O）N 6 - （CH 2）N 7 - （PO） - （OR 9）2; - （O）N 6 - （CH 2）N7-SO2-OR 9; 卤素; organosilanyl; 有机硅氧烷基 或通过异头氧直接连接到苯佐洛酮系统或通过直链或支链亚烷基，亚烯基，链二烯或烷基三烯间隔物（糖 - （CH 2）n - （X1）1或O - 苯并异噻唑酮系统，其中n = 1-10且X1 = -0-; - （CO） - ; -O-C0-; -COO-，-NH-; -S-; -SO2-）; R 1，R 7和R 8彼此独立地是氢; C 1 -C 12烷基或C 3 -C 12环烷基，其可以被一个或多个E取代和/或被一个或多个D中断; C 6 -C 20芳基，其可以被一个或多个G取代; 可以被一个或多个G，C 2 -C 18烯基，C 2 -C 18炔基，C 7 -C 25芳烷基或COOR 9取代的C 1 -C 20杂芳基; COR 9; CONR9R10; SO3R9; SO 2 R 9; PO3（R 9）2; PO2（R 9）2; organosilanyl; 有机硅氧烷; 或直链或α-支链的亚烷基，链烯二烯或三亚胺间隔基（糖 - （CH 2）n - （X 2）1或O - *，其中n = 1-10，X2 = -C（= O） - ; - O-C0- *）; R9和R10彼此独立地是氢; 可以被一个或多个E取代和/或被一个或多个D中断的C 1 -C 18烷基或C 3 -C 12 - 环烷基; 可以被一个或多个G取代的C 6 -C 20芳基; 可以被一个或多个G取代的C 4 -C 20杂芳基; organosilanyl; 有机硅氧烷; 或通过端基异构体氧或经由直链或支链的亚烷基，亚烯基，链二烯或烷基三烯间隔物（糖 - （CH 2）n - ），其中n = 1-10）直接连接在α-或β-模式中的糖残基; 或R 9和R 10一起形成五元或六元环，R 11为氢; 或C 1 -C 5烷基; n1，n2，n4和n7彼此独立地为1至5的数; n3，n5和n6彼此独立地为0; 或1; D是-CO-; -COO-; -S-; -所以-; -SO2-; -O-; NR 14; -S1R19R20-; -POR11-; -CR12 = CR13-; 或-C = C-; E为-0R18; -SR18; -NR14R15; -NR14COR15; -C0R17; -COOR16; -CONR14R15; -CN; 卤素; 或SO3R18; SO2R18; PO3（R18）2; PO2（R18）2; organosilanyl; 有机硅氧烷; 或通过异头氧直接或通过直链或支链亚烷基，亚烯基，链二烯或烷三胺间隔基（糖 - （CH 2）n - （X1）1或0- *）直接连接在α-或β-模式上的糖残基，其中 n = 1-10且X1 = -0-; -C（= O） - ; - O-O-COO-; -NH-; -S-; -SO2-）; G是E 任选地被D中断的C 1 -C 18烷基; C1-C18perfluoroalkyl; C1-C18烷氧基，其任选地被E取代和/或被D中断; 其中R 12，R 13，R 14和R 15彼此独立地是氢; 任选被OH，C 1 -C 18烷基或C 1 -C 18烷氧基取代的C 6 -C 18芳基; 任选地被-O-间隔的C 1 -C 18烷基; 或R 14和R 15一起形成五元或六元环，R 6为氢; 任选被OH，C 1 -C 18烷基或C 1 -C 18烷氧基取代的C 6 -C 18芳基; 任选被-O-间隔的C 1 -C 18烷基; R17为H; 任选被OH，C 1 -C 18烷基或C 1 -C 18烷氧基取代的C 6 -C 18芳基; 或任选被-O-中断的C 1 -C 18烷基; R18是氢; 任选被OH，C 1 -C 18烷基或C 1 -C 18烷氧基取代的C 6 -C 18芳基; 任选地被-O-间隔的C 1 -C 18烷基; R 19和R 20彼此独立地是氢; C1-C18烷基; 任选被C 1 -C 18烷基取代的C 6 -C 18芳基; 和R 21是C 1 -C 18烷基; 或被C 1 -C 18烷基取代的C 6 -C 18芳基; *表示该基团针对苯佐洛尔酮部分; 用于保护人和动物的头发和皮肤免受紫外线辐射。