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    • 5. 发明授权
    • Amino substituted hydroxyphenyl benzophenone derivatives
    • 氨基取代羟苯基二苯甲酮衍生物
    • US07374749B2
    • 2008-05-20
    • US10537940
    • 2003-12-03
    • Jürg HaaseThomas EhlisElek BorsosStefan Müller
    • Jürg HaaseThomas EhlisElek BorsosStefan Müller
    • A61K8/44A61K8/49C07D277/66C07D313/12C07C233/73C07C233/69C07C233/78C07C229/52
    • C07D295/192A61K8/42A61K8/44A61K8/49A61K8/4973A61Q17/04C07C229/52C07C237/32C07C237/34C07C237/40C07C237/42C07D277/46C07D277/66C07D313/12
    • Described are amino substituted hydroxyphenyl benzophenone derivatives of formula (I), wherein R1, and R2 independently from each other are; C1-C20alkyl; C2-C20-alkenyl; C3-C10cycloalkyl; C3-C10cycloalkenyl; or R1, and R2 together with the linking nitrogen atom form a 5- or 6-membered heterocyclic ring; n1 is a number from 1 to 4; when n1=1, R3 is a saturated or unsaturated heterocyclic radical; hydroxy-C1-C5alkyl; cyclohexyl optionally substituted with one or more C1-C5alkyl; phenyl optionally substituted with a heterocyclic radical, aminocarbonyl or C1-C5alkylcarboxy; when n1 is 2, R3 is an alkylene-, cycloalkylene- or alkenylene radical which is optionally substituted by a carbonyl- or carboxy group; o R3 together with A forms a bivalent radical of the formula (Ia), wherein n2 is a number from 1 to 3; when n1 is 3, R3 is an alkanetriyl radical; when n1 is 4, R3 is an alkanetetrayl radical; A is —O—; or —N(R5)—; and R5 is hydrogen; C1-C5alkyl; or hydroxy-C1-C5alkyl. The compounds are useful as UV filters in sunscreen applications.
    • 描述了式(I)的氨基取代的羟基苯基二苯甲酮衍生物,其中R 1和R 2彼此独立地是; C 1 -C 20烷基; C 1 -C 20烷基; C 2 -C 20 - 烯基; C 3 -C 10环烷基; C 3 -C 10环烯基; 或R 1和R 2与连接氮原子一起形成5-或6-元杂环; n 1是1至4的数; 当n 1 = 1时,R 3 3是饱和或不饱和杂环基; 羟基-C 1 -C 5烷基; 任选被一个或多个C 1 -C 5烷基取代的环己基; 任选被杂环基取代的苯基,氨基羰基或C 1 -C 5烷基羧基; 当n 1是2时,R 3是任选被羰基或羧基取代的亚烷基 - 亚环烷基 - 或亚烯基; R 3与A一起形成式(Ia)的二价基团,其中n 2是1至3的数; 当n 1为3时,R 3为烷三基; 当n 1为4时,R 3为烷基乙酰基; A为-O- 或-N(R 5) - ; 并且R 5是氢; C 1 -C 5烷基; 或羟基-C 1 -C 5烷基。 这些化合物可用作防晒霜中的紫外线过滤器。
    • 6. 发明授权
    • Hydroxybenzophenone derivatives
    • 羟基二苯甲酮衍生物
    • US07999128B2
    • 2011-08-16
    • US12223686
    • 2007-02-06
    • Jürg HaaseStefan MüllerThomas Ehlis
    • Jürg HaaseStefan MüllerThomas Ehlis
    • C07F7/04
    • A61Q17/04A61K8/585C07F7/0838
    • Disclosed are hydroxyphenylbenzophenone derivatives of formula (1), wherein R1 and R2 independently from each other are hydrogen; C1-C20alkenyl; C3-C10cycloalkyl; or R1 and R2 together with the linking nitrogen atom form a 5- 6-membered heterocyclic ring; R3, R4 and R5 independently from each other are C1-C4alkyl; C1-C4alkoxy; or a radical of formula (1a) R6 is C1-C6alkyl; and A is a straight-chain or branched C3-C6alkylene, which is optionally interrupted by one or more *—O—*, or *—O—(CO)—* groups; and m is 0; or a number from 1 to 5. The compounds are useful as cosmetic UV filters with outstanding solubility properties in cosmetic oils.
    • 公开了式(1)的羟基苯基二苯甲酮衍生物,其中R 1和R 2彼此独立地是氢; C1-C20烯基; C 3 -C 10环烷基; 或R 1和R 2与连接氮原子一起形成5-6元杂环; R 3,R 4和R 5彼此独立地为C 1 -C 4烷基; C1-C4烷氧基; 或式(1a)的基团,R 6为C 1 -C 6烷基; 并且A是直链或支链C 3 -C 6亚烷基,其任选地被一个或多个* -O- *或* -O-(CO)*基团间隔; m为0; 或1至5的数字。该化合物可用作化妆品油中具有优异溶解性的化妆品UV滤光片。
    • 8. 发明授权
    • Merocyanine derivatives
    • 梅花菁衍生物
    • US08044058B2
    • 2011-10-25
    • US12715839
    • 2010-03-02
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • A61K31/517A61K31/445A61K31/16
    • A61K8/498A61K8/4913A61K8/494A61Q17/04
    • Disclosed is the use of merocyanine derivatives of formula Q is hydrogen; C1-C22alkyl; —OH; —OR7; —NR7R8; or —N═R9; R1 is hydrogen; C1-C22alkyl; —OR7, —SR7; —NR7R8; C1-C22alkyl; C2-C12 alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; 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 is hydrogen; C1-C22alkyl; C1-C22alkoxy; or COR7; R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl; Si—R10R11R12; Si(OR10)(OR11)(OR12); SiR10(OR11)(OR12); SiR10R11(OR12); —(CH2)u—O—(CH2)v—SiR10R11R12; or a radical X-Sil; t, u and v, independently from each other are a number from 1 to 5; R9 is a (C1-C6)alkylidene radical; R10, R11, R12 independently form each other are C1-C22alkyl; X is a linker; for protecting of human hair and skin against the damaging effect of UV radiation.
    • 披露式Q的部花青衍生物的用途是氢; C 1 -C 22烷基; -哦; -OR7; -NR7R8; 或-N = R9; R1是氢; C 1 -C 22烷基; -OR7,-SR7; -NR7R8; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; C7-C12芳烷基; C 1 -C 12杂烷基,C 2 -C 11杂芳烷基; C6-C10芳基; 或C 1 -C 9杂芳基; R4是氰基; COR7,COOR7; CONR7R8; SO2(C6-C12)芳基; C2-C12烷-1-烯基; C 3 -C 12环烯-1-烯基; C2-C12alk-1-inyl; C 2 -C 12杂烷基; C3-C5杂环烷基; C6-C10芳基; 或C 1 -C 9杂芳基; R5为-COR7; -COOR7; -OR7; -SR 7,-NHR 7,-NR 7 R 8; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; C7-C12芳烷基; C 1 -C 12烷基苯基; C 1 -C 12烷氧基-C 6 -C 10芳基; C 1 -C 12杂烷基; C 2 -C 11杂芳烷基; C 3 -C 12环杂烷基; C6-C10芳基; C 1 -C 12烷氧基-C 6 -C 10芳基; 或C 1 -C 9杂芳基; R6是氢; C 1 -C 22烷基; C1-C22烷氧基; 或COR7; R 7和R 8彼此独立地是氢; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; - (CH 2)t COOH; C7-C12芳烷基; C 1 -C 12杂烷基; C 2 -C 11杂芳烷基; C6-C10芳基; C1-C9杂芳基; Si-R10R11R12; Si(OR10)(OR11)(OR12); SiR10(OR11)(OR12); SiR10R11(OR12); - (CH 2)u -O-(CH 2)v -SiR 10 R 11 R 12; 或基团X-Sil; t,u和v彼此独立地为1至5的数; R9是(C1-C6)亚烷基; R 10,R 11,R 12彼此独立地为C 1 -C 22烷基; X是一个连接子; 用于保护人的头发和皮肤免受紫外线辐射的破坏作用。
    • 9. 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.
    • 10. 发明申请
    • MEROCYANINE DERIVATIVES
    • 月桂酰胺衍生物
    • US20100209466A1
    • 2010-08-19
    • US12715839
    • 2010-03-02
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • Barbara WagnerFrank BienewaldHeinz WollebOlof WallquistBernd HerzogThomas EhlisJürg Haase
    • A61K8/41A61Q17/04A61K8/49A61K8/42A61K8/46A61K8/58A61K8/898A61K8/02
    • A61K8/498A61K8/4913A61K8/494A61Q17/04
    • Disclosed is the use of merocyanine derivatives of formula Q is hydrogen; C1-C22alkyl; —OH; —OR7; —NR7R8; or —N═R9; R1 is hydrogen; C1-C22alkyl; —OR7, —SR7; —NR7R8; C1-C22alkyl; C2-C12 alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; C7-C12aralkyl; C1-C12heteroalkyl, C2-C11heteroaralkyl; C6-C10aryl; or C1-C9heteroaryl; R4 is cyano; COR7, COOR7; 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 is hydrogen; C1-C22alkyl; C1-C22alkoxy; or COR7; R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl; Si—R10R11R12; Si(OR10)(OR11)(OR12); SiR10(OR11)(OR12); SiR10R11(OR12); —(CH2)u—O—(CH2)v—SiR10R11R12; or a radical X-Sil; t, u and v, independently from each other are a number from 1 to 5; R9 is a (C1-C6)alkylidene radical; R10, R11, R12 independently form each other are C1-C22alkyl; X is a linker; for protecting of human hair and skin against the damaging effect of UV radiation.
    • 公开了使用式Q的部花青衍生物是氢; C 1 -C 22烷基; -哦; -OR7; -NR7R8; 或-N = R9; R1是氢; C 1 -C 22烷基; -OR7,-SR7; -NR7R8; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; C7-C12芳烷基; C 1 -C 12杂烷基,C 2 -C 11杂芳烷基; C6-C10芳基; 或C 1 -C 9杂芳基; R4是氰基; COR7,COOR7; CONR7R8; SO2(C6-C12)芳基; C2-C12烷-1-烯基; C 3 -C 12环烯-1-烯基; C2-C12alk-1-inyl; C 2 -C 12杂烷基; C3-C5杂环烷基; C6-C10芳基; 或C 1 -C 9杂芳基; R5是-COR7; -COOR7; -OR7; -SR 7,-NHR 7,-NR 7 R 8; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; C7-C12芳烷基; C 1 -C 12烷基苯基; C 1 -C 12烷氧基-C 6 -C 10芳基; C 1 -C 12杂烷基; C 2 -C 11杂芳烷基; C 3 -C 12环杂烷基; C6-C10芳基; C 1 -C 12烷氧基-C 6 -C 10芳基; 或C 1 -C 9杂芳基; R6是氢; C 1 -C 22烷基; C1-C22烷氧基; 或COR7; R 7和R 8彼此独立地是氢; C 1 -C 22烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 3 -C 12环烷基; C3-C12环烯基; - (CH 2)t COOH; C7-C12芳烷基; C 1 -C 12杂烷基; C 2 -C 11杂芳烷基; C6-C10芳基; C1-C9杂芳基; Si-R10R11R12; Si(OR10)(OR11)(OR12); SiR10(OR11)(OR12); SiR10R11(OR12); - (CH 2)u -O-(CH 2)v -SiR 10 R 11 R 12; 或X-Sil基团; t,u和v彼此独立地为1至5的数; R9是(C1-C6)亚烷基; R 10,R 11,R 12彼此独立地为C 1 -C 22烷基; X是一个连接子; 用于保护人的头发和皮肤免受紫外线辐射的破坏作用。