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    • 1. 发明申请
    • NAPHTHALENE AMIDINE IMIDES
    • 萘胺类胺
    • WO2007012611A1
    • 2007-02-01
    • PCT/EP2006/064531
    • 2006-07-21
    • CIBA SPECIALTY CHEMICALS HOLDING INC.LANGHALS, HeinzJASCHKE, HaraldEHLIS, ThomasWALLQUIST, Olof
    • LANGHALS, HeinzJASCHKE, HaraldEHLIS, ThomasWALLQUIST, Olof
    • C09B57/00C09B57/08C09K11/06C07D471/08
    • C09B5/62C07D471/04
    • Disclosed are naphthalinamidinimide of formula (I), wherein R 1 R 2 , R 3 , R 4 , R 5 and R6 independently from each other are hydrogen; or C 1 -C 37 alkyl; wherein - one to 10 of the CH 2 units of C 1 -C 37 alkyl independently from each may be substituted by carbonyl groups; oxygen atoms; sulphur atoms; selenium atoms; tellurium atoms; cis- or trans-CH=CH-groups; acetylenic C≡C- groups; 1 ,2-, 1 ,3- or 1 ,4-substituted phenyl radicals; 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5-disubstituted pyridine radicals; 2,3- , 2,4-, 2,5- or 3,4-disubstituted thiophene radicals; 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 2,3-, 2,6- or 2,7-disubstituted 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 1 ,9-, 1 ,10-, 2,3-, 2,6-, 2,7-, 2,9-, 2,10- or 9,10-disubstituted anthracene radicals; wherein one or 2 CH-groups of the CH=CH- groups, the naphthalene radicals and the anthracene radicals may be substituted by nitrogen atoms; - up to 12 single hydrogen atoms of the CH 2 -groups independently from each other may be substituted at the same carbon atoms by fluorine; chlorine; bromine; or iodine; the cyano group; a linear alkyl chain with up to 18 carbon atoms; cis- or frans-CH=CH-groups; acetylenic C≡C-groups; 1 ,2-, 1 ,3- or 1 ,4-substituted phenyl radicals; 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5- disubstituted pyridine radicals; 2,3-, 2,4-, 2,5- or 3,4-disubstituted thiophene radicals; 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 2,3-, 2,6- or 2,7-disubstituted naphthalene radicals; 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 1 ,9-, 1 ,10-, 2,3-, 2,6-, 2,7-, 2,9-, 2,10- or 9,10-disubstituted anthracene radicals; wherein up to 6 CH 2 - units in the alkyl chain independently from each other may be substituted by carbonyl groups, oxygen atoms, sulphur atoms, selenium atoms, tellurium atoms and up to 12 single hydrogen atoms of the CH 2 -groups of the alkyl radicals each independently from each other may also be substituted at the same C-atoms by fluorine, chlorine, bromine or iodine or cyano groups or linear alkyl chains with up to 18 carbon atoms, wherein one to 6 CH 2 -units independently from each other may be substituted by carbonyl groups, oxygen atoms, sulphur atoms, selenium atoms, tellurium atoms, cis- or frans-CH=CH-groups, wherein one CH-unit may also be substituted by a nitrogen atom, by acetylenic C≡C-groups, 1 ,2-, 1 ,3- or 1 ,4-substituted phenyl radicals, 2,3-, 2,4-, 2,5-, 2,6-, 3,4- or 3,5-disubstituted pyridine radicals, 2,3-, 2,4-, 2,5- or 3,4-disubstituted thiophene radicals, 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 2,3-, 2,6- or 2,7-disubstituierte naphthalene radicals, wherein one or two carbon atoms may be substituted by nitrogen atoms, by 1 ,2-, 1 ,3-, 1 ,4-, 1 ,5-, 1 ,6-, 1 ,7-, 1 ,8-, 1 ,9-, 1 ,10-, 2,3-, 2,6-, 2,7-, 2,9-, 2,10- or 9,10-di- substituierte anthracene radicals, wherein one or two carbon atoms may be substituted by nitrogen atoms; or instead of substituents the free valencies of the methine- or quarternary carbon atoms may be linked pairwise forming rings like cyclohexane rings; or are an amino radical, if R 1 and R 2 together with the carbon atoms C 1 and C 2 or R 3 and R 4 together with the carbon atoms C 3 and C 4 form a 6-membered radical; R 7 and R 8 , independently from each other are =0; or =NH-, if =NH- together with the nitrogen atom N 1 (for R 6 ) or together with the nitrogen atom N 2 (for R 7 ) forms a five-membered radical. The compounds are useful for different purposes, preferably as UV absorbers for cosmetic applications.
    • 公开了式(I)的萘胺亚胺,其中R 1 R 2,R 3,R 4,R 5和R6彼此独立地是氢; 或C 1 -C 13烷基; 其中 - 独立地各自独立地具有1至10个C 1 -C 3 - 烷基的CH 2 - 2个单元可以被羰基取代; 氧原子; 硫原子 硒原子; 碲原子 顺式或反式-CH = CH-基团; 炔属C = C-基团; 1,2或1-3或1,4-取代的苯基; 2,3-,2,4-,2,5-,2,6-,3,4-或3,5-二取代的吡啶基; 2,3-,2,4-,2,5-或3,4-二取代噻吩基; 1,2,1-,1,3-,1,1-,4-,1,5-,1,6-,1,7-,1,8-,2,3,2,6-或2,7-二取代 1,2-,1,3-,1-,4-,1,5-,1,6-,1,7-,1,8-,1,9-,1,10-,2,3-, 2,6-,2,7-,2,9-,2,10-或9,10-二取代的蒽基; 其中CH = CH-基团,萘基和蒽基团的一个或两个CH-基团可以被氮原子取代; - CH 2 - 2个基团多达12个单个氢原子彼此独立地可以被相同的碳原子被氟取代; 氯; 溴; 或碘; 氰基; 具有至多18个碳原子的直链烷基链; 顺式或反式-CH = CH-基团; 炔属C = C - 基; 1,2或1-3或1,4-取代的苯基; 2,3-,2,4-,2,5-,2,6-,3,4-或3,5-二取代吡啶基; 2,3-,2,4-,2,5-或3,4-二取代噻吩基; 1,2,1-,1,3-,1,1-,4-,1,5-,1,6-,1,7-,1,8-,2,3,2,6-或2,7-二取代 萘基; 1,2-,1,3-,1-,4-,1,5-,1,6-,1,7-,1,8-,1,9-,1,10-,2,3-, 2,6-,2,7-,2,9-,2,10-或9,10-二取代的蒽基; 其中烷基链中多达6个CH 2 - 单元彼此独立地可被羰基,氧原子,硫原子,硒原子,碲原子和至多12个单氢原子取代 烷基的CH 2 - 2个基团各自独立地也可以在相同的C原子上被氟,氯,溴或碘或氰基或具有至多18个碳的直链烷基链取代 原子,其中一个至六个CH 2 - 彼此独立地可以被羰基,氧原子,硫原子,硒原子,碲原子,顺式或反式-CH = CH-基团取代 其中一个CH-单元也可以被氮原子取代,被炔基C = C - 基,1,2-,1,3-或1,4-取代的苯基,2,3-, ,2,5-,2,6-,3,4-或3,5-二取代的吡啶基,2,3-,2,4-,2,5-或3,4-二取代的噻吩基,1,2 - ,1,3 - ,1,4 - ,1,5 - ,1,6 - ,1-7 - ,1,8-,2,3 - ,2,6 - 或2,7-二枯基 其中一个或两个碳原子可以被氮原子取代,其中一个或两个碳原子可以被1,2 - ,1,3 - ,1,4 - ,1-5 - ,1-6 - ,1-7 - 8-,1,9-,1,10-,2,3-,2,6-,2,7-,2,9-,2,10-或9,10-二取代的蒽基,其中一个 或两个碳原子可以被氮原子取代; 或代替取代基,次甲基或季碳原子的自由价可以成对连接形成环如环己烷环; 或者如果R 1和R 2与碳原子C 1和C 2一起是氨基, 或R 3和R 4与碳原子C 3和C 4连接形成6元基团 ; R 7和R 8彼此独立地为= 0; 或= NH-,如果= NH-与氮原子N 1(对于R 6)或与氮原子N 2一起, (R 7 7)形成五元基团。 该化合物可用于不同的目的,优选用于化妆品应用的UV吸收剂。
    • 2. 发明申请
    • MEROCYANINE DERIVATIVES
    • WO2006003094A2
    • 2006-01-12
    • PCT/EP2005/052850
    • 2005-06-20
    • CIBA SPECIALTY CHEMICALS HOLDING INC.WAGNER, BarbaraBIENEWALD, FrankWOLLEB, HeinzWALLQUIST, OlofHERZOG, BerndEHLIS, ThomasHAASE, Jürg
    • WAGNER, BarbaraBIENEWALD, FrankWOLLEB, HeinzWALLQUIST, OlofHERZOG, BerndEHLIS, ThomasHAASE, Jürg
    • A61K7/42
    • A61K8/498A61K8/4913A61K8/494A61Q17/04
    • Disclosed is the use of merocyanine derivatives of formula (I), wherein Q is hydrogen; C 1 -C 22 alkyl; -OH; -OR 7 ; -NR 7 R 8 ; or -N=R 9 ; R 1 is hydrogen; C 1 -C 22 alkyl; -OR 7 , -SR 7 ; -NR 7 R 8 ; C 1 -C 22 alkyl; C 2 -C 12 alkenyl; C 2 -C 12 alkinyl; C 3 -C 12 cycloalkyl; C 3 -C 12 cycloalkenyl; C 7 -C 12 aralkyl; C 1 -C 12 heteroalkyl, C 2 -C 11 heteroaralkyl; C 6 -C 10 aryl; or C 1 -C 9 heteroaryl; R 4 is cyano; COR 7 , COOR 7 ; CONR 7 R 8 ; SO 2 (C 6 -C 12 )aryl; C 2 -C 12 alk-1-enyl; C 3 -C 12 cycloalk-1-enyl; C 2 -C 12 alk-1-inyl; C 2 -C 12 heteroalkyl; C 3 -C 5 heterocycloalkyl; C 6 -C 10 aryl; or C 1 -C 9 heteroaryl; R 5 is -COR 7 ; -COOR 7 ; -OR 7 ; -SR 7 , -NHR 7 , -NR 7 R 8 ; C 1 -C 22 alkyl; C 2 -C 12 alkenyl; C 2 -C 12 alkinyl; C 3 -C 12 cycloalkyl; C 3 -C 12 cycloalkenyl; C 7 -C 12 aralkyl; C 1 -C 12 alkylphenyl; C 1 -C 12 alkoxy-C 6 -C 10 aryl; C 1 -C 12 heteroalkyl; C 2 -C 11 heteroaralkyl; C 3 -C 12 cycloheteroalkyl; C 6 -C 10 aryl; C 1 - C 12 alkoxy-C 6 -C 10 aryl; or C 1 -C 9 heteroaryl; R 6 is hydrogen; C 1 -C 22 alkyl; C 1 -C 22 alkoxy; or COR 7 ; R 7 and R 8 independently from each other are hydrogen; C 1 -C 22 alkyl; C 2 -C 12 alkenyl; C 2 -C 12 alkinyl; C 3 -C 12 cycloalkyl; C 3 -C 12 cycloalkenyl; -(CH 2 ) t COOH; C 7 -C 12 aralkyl; C 1 -C 12 heteroalkyl; C 2 -C 11 heteroaralkyl; C 6 -C 10 aryl; C 1 -C 9 heteroaryl; Si-R 10 R 11 R 12 ; Si(OR 10 )(OR 11 )(OR 12 ); SiR 10 (OR 11 )(OR 12 ); SiR 10 R 11 (OR 12 ); -(CH 2 ) u -O-(CH 2 ) v -SiR 10 R 11 R 12 ; or a radical X-Sil; t, u and v, independently from each other are a number from 1 to 5; R 9 is a (C 1 -C 6 )alkylidene radical; R 10 , R 11 , R 12 independently form each other are C 1 -C 22 alkyl; X is a linker; Sil is a silane-, oligosiloxane- or polysiloxane radical; R 1 and R 2 , R 1 and Q, R 1 and R 6 , R 1 and T, R 2 and R 3 , R 2 and R 4 , R 2 and R 6 , R 2 and Q, R 4 and R 6 , R 4 and T, R 6 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-heterocyclic rings, and each N atom in a N-heterocyclic ring may be substituted by C 1 -C 22 alkyl; n is a number from 1 to 4; wherein at least one of the radicals R 1 , R 6 or Q is different from hydrogen; if n = 1 T is -COR 5 ; -CN; C 6 -C 10 aryl; -NHR 5 ; or -SO 2 -(C 6 -C 12 )aryl; R 2 and R 3 independently from each other are C 1 -C 22 alkyl; hydroxy-C 1 -C 22 alkyl; C 2 -C 12 alkenyl; C 2 -C 12 alkinyl; C 3 -C 12 cycloalkyl, C 3 -C 12 cycloalkenyl; C 7 -C 12 aralkyl; C 1 -C 12 heteroalkyl; C 3 -C 12 cycloheteroalkyl; C 6 -C 10 aryl; C 1 -C 9 heteroaryl; or a radical of formula (II); p is a number from 5 to 100; q is a number from 1 to 5; s is a number from 0 to 4; if n = 2 R 2 and R 3 are each C 1 -C 5 alkylene; and simultaneously T is defined as for n = 1; or T is a bivalent radical of formula -NR 7 -V-NR 7 -, wherin V is phenylene; or C 1 -C 5 alkylene; R 7 is hydrogen; or C 1 -C 5 alkyl; and R 2 and R 3 simultaneously are defined as for n = 1; if n = 3 one of R 2 , R 3 or T is a trivalent radical; if n = 4 one of R 2 , R 3 or T is a tetravalent radical; for protecting of human hair and skin against the damaging effect of UV radiation.
    • 5. 发明申请
    • MEROCYANINE DERIVATIVES FOR COSMETIC USE
    • 用于化妆品使用的MEROCANANINE衍生物
    • WO2004006878A1
    • 2004-01-22
    • PCT/EP2003/006955
    • 2003-07-01
    • CIBA SPECIALTY CHEMICALS HOLDING INC.WAGNER, BarbaraEHLIS, ThomasEICHIN, Kai
    • WAGNER, BarbaraEHLIS, ThomasEICHIN, Kai
    • A61K7/42
    • C07D239/54A61K8/4906A61Q17/04C07C255/30C07C255/31C07C2601/16C07D207/20C07D231/36C07D263/14C07D277/10C07D295/145C07D295/155C07D319/06
    • The use is described of merocyanine derivatives of formula (1), wherein R 1 and R 2 are each independently of the other hydrogen; C 1 -C 22 alkyl; cyclo-C 3 C 8 alkyl; or unsubstituted or C 1 -C 5 alkyl- or C 1 -C 5 alkoxy-substituted C 6 -C 20 aryl; orl; or R 1 and R 2 together with the nitrogen atom linking them form a -(CH 2 ) m - ring which is uninterrupted or. interrupted by -O- or by -NH-; R 3 is a cyano group; -COOR 5 ; -CONHR 5 ; -COR 5 ; or -SO 2 R 5 ; R 4 is a cyano group; -COOR 6 ; -CONHR 6 ; -COR 6 ; or -SO 2 R 6 ; R 5 and R 6 are each independently of the other C 1 -C 22 alkyl; or unsubstituted or C 1 -C 5 alkyl substituted C 6 -C 20 aryl; or R 3 and R 4 together or R 5 and R 6 together form a 5- to 7-membered, monocyclic, carbocyclic or heterocyclic ring; Z 1 , and Z 2 are each independently of the other a -(CH 2 ),- group which is uninterrupted or interrupted by -O-, -S-, or by -NR 7 -, and/or is unsubstituted or substituted by C, 1 -C 5 alkyl; R 7 is C 1 ­C 5 alkyl; I is from 1 to 4; m is from 1 to 7; n is from 1 to 4; when n = 2, R 1 , R 5 or R 6 is a bivalent alkyl group; or R 1 , and R 2 together with the 2 nitrogen atoms linking them form a -(CH 2 ) m - ring; when n = 3, R 1 , R 5 or R 6 is a trivalent alkyl group; when n = 4, R 1 , R 5 or R 6 is a tetravalent alkyl group; and R 1 , and R 2 in formula (1) are not simultaneously hydrogen, in protecting human and animal hair and skin from UV radiation.
    • 描述了式(1)的部花青衍生物,其中R 1和R 2各自独立地为氢; C1-C22烷基; 环C3C8alkyl; 或未取代的或C 1 -C 5烷基 - 或C 1 -C 5烷氧基取代的C 6 -C 20芳基; ORL; 或R 1和R 2与连接它们的氮原子一起形成不间断的 - (CH 2)m - 环。 被-O-或-NH-中断; R3是氰基; -COOR5; -CONHR5; -COR5; 或-SO 2 R 5; R4是氰基; -COOR6; -CONHR6; -COR 6; 或-SO 2 R 6; R 5和R 6各自独立地为C 1 -C 22烷基; 或未取代的或C 1 -C 5烷基取代的C 6 -C 20芳基; 或R 3和R 4一起或R 5和R 6一起形成5-至7-元单环,碳环或杂环; Z 1和Z 2各自独立地为不间断或被-O - , - S-或-NR 7 - 间隔的另一个 - (CH 2) - 基,和/或未取代或被C 1〜 C 5烷基; R7是C1C5烷基; 我是从1到4; m为1〜7; n为1至4; 当n = 2时,R 1,R 5或R 6为二价烷基; 或R 1和R 2与连接它们的2个氮原子一起形成 - (CH 2)m - 环; 当n = 3时,R 1,R 5或R 6为三价烷基; 当n = 4时,R 1,R 5或R 6为四价烷基; 式(1)中的R 1和R 2不同时为氢,以保护人和动物的头发和皮肤免受UV辐射。
    • 8. 发明申请
    • SYMMETRICAL TRIAZINE DERIVATIVES
    • 对称TRIAZINE衍生物
    • WO2004085412A2
    • 2004-10-07
    • PCT/EP2004/050331
    • 2004-03-19
    • CIBA SPECIALTY CHEMICALS HOLDING INC.EHLIS, ThomasMÜLLER, StefanHAYOZ, Pascal
    • EHLIS, ThomasMÜLLER, StefanHAYOZ, Pascal
    • C07D251/24
    • C07D251/24A61K8/4966A61Q17/04
    • Disclosed is the use of the compounds of formula wherein A is a radical of formula (1a) or (1b) R, R 1 and R 5 independently from each other are hydrogen; C 1 -C 18 alkyl; or C 6 -C 12 aryl; R 2 , R 3 and R 4 independently from each other are hydrogen; or a radical of formula wherein at least one of the radicals R 2 , R 3 and R 4 are a radical of formula (1c); R 6 , R 7 , R 8 , R 9 and R 10 independently from each other are hydrogen; hydroxy; C 1 -C 18 alkyl; C 1 -C 18 alkoxy;C 6 -C 12 aryl; C 6 -C 12 aryloxy; C 1 -C 18 alkylthio; carboxy; -COOM; C 1 -C 18 alkylcarboxyl; aminocarbonyl; or mono- or di-C 1 -C 18 alkylamino; M is an alkali metal ion; x is 1 or 2; and y is a number from 2 to 10; for the protection of human and animal hair and skin against the damaging effect of UV radiation. The compounds of formula (1) are high effective UV absorbers for cosmetic formulations aund can - depending on their physical properties - be used in micronized or soluble form.
    • 公开了下式化合物的用途其中A是式(1a)或(1b)的基团,R,R 1和R 5彼此独立地是氢; C1-C18烷基; 或C6-C12芳基; R2,R3和R4彼此独立地是氢; 或下式的基团,其中基团R 2,R 3和R 4中的至少一个为式(1c)的基团; R 6,R 7,R 8,R 9和R 10彼此独立地为氢; 羟基; C1-C18烷基; C1-C18烷氧基; C 6 -C 12芳基; C6-C12aryloxy; C1-C18alkylthio; 羧基; -COOM; C1-C18alkylcarboxyl; 羰基; 或单或二C1-C18烷基氨基; M是碱金属离子; x为1或2; y为2〜10的数; 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。 式(1)的化合物是用于化妆品制剂的高效紫外线吸收剂,可根据其物理性质 - 以微粉化或可溶形式使用。