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    • 2. 发明申请
    • USE OF BENZOTROPOLONE DERIVATIVES AS UV ABSORBERS AND ANTIOXIDANTS AND THEIR USE IN SUNSCREENS AND/OR COSMETIC COMPOSITIONS
    • 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
    • WO2009156324A3
    • 2012-06-21
    • PCT/EP2009057587
    • 2009-06-18
    • BASF SEWAGNER BARBARAOEHRLEIN REINHOLDHERZOG BERNDEICHIN KAIBAISCH GABRIELEPORTMANN STEPHANIE
    • WAGNER BARBARAOEHRLEIN REINHOLDHERZOG BERNDEICHIN KAIBAISCH GABRIELEPORTMANN STEPHANIE
    • A61Q17/00A61K8/35A61Q17/04C07C49/717C07C49/747C07C62/38C07C69/712C07C69/757C07C305/18C07D311/02C07F9/40C07H15/18C07H15/203C07H15/26
    • A61Q17/04A61K8/35A61Q19/08C07C49/747C07C62/38C07C69/712C07C69/757C07C305/18C07C2602/12C07F9/4006C07H15/18C07H15/203C07H15/26
    • 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.
    • 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。
    • 5. 发明申请
    • WATER BASED CONCENTRATED PRODUCT FORMS OF OIL-SOLUBLE ORGANIC UV ABSORBERS
    • 水溶性有机紫外线吸收剂的基于水的浓缩产品形式
    • WO2009007264A3
    • 2009-09-03
    • PCT/EP2008058356
    • 2008-06-30
    • BASF SEMUELLER STEFANLINDEMANN BRIGITTEHERZOG BERND
    • MUELLER STEFANLINDEMANN BRIGITTEHERZOG BERND
    • A61K8/11A61K8/35A61K8/37A61K8/44A61K8/49A61K8/81A61Q17/04
    • A61Q17/04A61K8/11A61K8/35A61K8/37A61K8/44A61K8/445A61K8/496A61K8/4966A61K8/585A61K8/8152A61K8/893A61K2800/413
    • The instant invention refers to the use of a concentrated aqueous polymer dispersion with an average particle size of less than 1000 nm comprising (a) a polymer carrier prepared by heterophase radical polymerization of at least one ethylenically unsaturated monomer in the presence of (b) an oil-soluble organic UV absorber selected from the class of p-aminobenzoic acid derivatives; salicylic acid derivatives; benzophenone derivatives; diphenyl acrylate derivatives; benzofuran derivatives; polymeric UV absorbers, comprising one or more organosilicon radicals; cinnamic acid derivatives; camphor derivatives; s-triazine derivatives; trianilino-s-triazine derivatives; menthyl anthranilates; and benzotriazole derivatives; wherein the weight ratio of the oil-soluble organic UV absorber (b) to polymer carrier (a) is greater than 50 parts UV absorber per 100 parts of carrier; for the protection of human and animal hair and skin against the damaging effect of UV radiation. The concentrated aqueous polymer dispersions show unexpectedly high sunscreen effects and a positive skin feeling.
    • 本发明涉及使用平均粒径小于1000nm的浓缩水性聚合物分散体,其包含(a)通过至少一种烯属不饱和单体的异相自由基聚合制备的聚合物载体,所述聚合物载体在(b) 选自对氨基苯甲酸衍生物类的油溶性有机UV吸收剂; 水杨酸衍生物; 二苯甲酮衍生物; 二苯基丙烯酸酯衍生物; 苯并呋喃衍生物; 包含一个或多个有机硅基团的聚合物UV吸收剂; 肉桂酸衍生物; 樟脑衍生物 三嗪衍生物; 三苯胺三嗪衍生物; 薄荷基邻氨基苯甲酸酯; 和苯并三唑衍生物; 其中油溶性有机UV吸收剂(b)与聚合物载体(a)的重量比相对于100份载体大于50份UV吸收剂; 用于保护人体和动物毛发和皮肤免受紫外线辐射的破坏作用。 浓缩的水性聚合物分散体表现出意想不到的高防晒效果和阳性皮肤感觉。
    • 9. 发明申请
    • STABILIZATION OF COSMETIC COMPOSITIONS
    • 化妆品组合物的稳定性
    • WO2009027390A2
    • 2009-03-05
    • PCT/EP2008061132
    • 2008-08-26
    • CIBA HOLDING INCHERZOG BERNDQUASS KATJAACKER STEPHANIE
    • HERZOG BERNDQUASS KATJAACKER STEPHANIE
    • A61K8/37A61K8/49A61Q17/04
    • A61K8/4973A61K8/35A61K8/368A61K8/37A61K8/40A61K8/4966A61K2800/592A61Q17/04
    • Disclosed is the use of UV absorbers selected from (a1) diphenylacrylates; (a2) hydroxyphenyl triazines of formula (1), in which R1, R2 and R3 independently of one another, are C1-C18alkyl; (a3) benzotriazole derivatives of formula (2), wherein R4 is a random statistical mixture of at least three isomeric branched secondary alkyl groups each having 8 to 30 carbon atoms and having the formula (2a); E1 is a straight-chain C1-C14alkyl; E2 is a straight-chain C4-C15alkyl; wherein the total number of carbon atoms in E1 plus E2 is from 7 to 29; and R5 is C1-C5alkyl; and (a4) dialkyl naphthalate; for stabilizing cosmetic compositions comprising (b) symmetrical triazine derivatives of formula (3), wherein A is a radical of formula (3a); or (3b) R6 and R10 independently from each other are hydrogen; C1-C18alkyl; or C6-C12aryl; R7, R8 and R9 independently from each other are hydrogen; or a radical of formula (3c), wherein, in formula (3a), at least one of the radicals R7, R8 and R9 are a radical of formula (3c); R11, R12, R13 and R14 independently from each other are hydrogen; hydroxy; halogen; C1-C18alkyl; C1-C18alkoxy; C6-C12aryl; biphenylyl; C6-C12aryloxy; C1-C18alkylthio; carboxy; -COOM; C1-C18-alkylcarboxyl; aminocarbonyl; mono- or di-C1-C18alkylamino; C1-C10acylamino; or -COOH; M is an alkali metal ion; x is 1 or 2; and y is a number from 2 to 10; and a UV-absorber selected from (c1) cinnamic acid derivatives; and (C2) dibenzoylmethane derivatives.
    • 公开了使用选自(a1)二苯基丙烯酸酯的UV吸收剂; (a2)式(1)的羟基苯基三嗪,其中R 1,R 2和R 3彼此独立地是C 1 -C 18烷基; (a3)式(2)的苯并三唑衍生物,其中R4是至少三个具有8至30个碳原子并具有式(2a)的异构支链仲烷基的随机统计混合物; E1是直链C1-C14烷基; E2是直链C4-C15烷基; 其中E1加E2的总碳原子数为7〜29; R5是C1-C5烷基; 和(a4)萘二甲酸二烷基酯; 用于稳定化妆品组合物,其包含(b)式(3)的对称三嗪衍生物,其中A是式(3a)的基团; 或(3b)R 6和R 10彼此独立地为氢; C1-C18烷基; 或C6-C12芳基; R 7,R 8和R 9彼此独立地为氢; 或式(3c)的基团,其中在式(3a)中,基团R7,R8和R9中的至少一个是式(3c)的基团; R 11,R 12,R 13和R 14彼此独立地为氢; 羟基; 卤素; C1-C18烷基; C1-C18烷氧基; C6-12芳基; 联苯基; C6-C12aryloxy; C1-C18alkylthio; 羧基; -COOM; C1-C18-烷羧基; 羰基; 单或二C1-C18烷基氨基; C1-C10acylamino; 或-COOH; M是碱金属离子; x为1或2; y为2〜10的数; 和选自(c1)肉桂酸衍生物的紫外线吸收剂; 和(C2)二苯甲酰甲烷衍生物。