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    2,4-Pentadienoic acid derivatives having retinoid-like biological activity
    52.
    发明授权
    2,4-Pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-二戊烯酸衍生物

    公开(公告)号：US5780647A

    公开(公告)日：1998-07-14

    申请号：US805793

    申请日：1997-02-25

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31/35 ,  A61K31/20 ,  A61K31/23 ,  A61K31/38 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07C57/50 ,  C07C69/618 ,  C07C215/02 ,  C07C215/18 ,  C07C311/58 ,  C07C335/06 ,  C07C403/00 ,  C07D277/22 ,  C07D311/58 ,  C07D333/54 ,  C07D335/06 ,  C07D311/04 ,  C07D409/02

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译： 式1的化合物其中Z选自由式2和式3所示的基团组成的组。式3 Y是3至8个碳的环烷基或环烯基，任选地 被一个或两个R 4基取代，或Y选自苯基，吡啶基，噻吩基，呋喃基，吡咯基，哒嗪基，嘧啶基，吡嗪基，噻唑基，恶唑基和咪唑基，所述基团任选被一个或两个R 4基团取代，二价 Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R 5是H或低级烷基，B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基， 苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

    2,4-pentadienoic acid derivatives having retinoid-like biological activity
    53.
    发明授权
    2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-戊二烯酸衍生物

    公开(公告)号：US06313163B1

    公开(公告)日：2001-11-06

    申请号：US09640850

    申请日：2000-08-17

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31382

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of formula 1 wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, Y is cyclopropyl optionally substituted with one or two R4 groups, the divalent Y radical being substituted by the Z and —CR1═CR1—CR1═CR1 groups on adjacent carbons; X is S, O, or NR5; n is 1 or 2; R1 and R2 independently are H, lower alkyl or fluoroalkyl; R3 is hydrogen, lower alkyl, Cl or Br; R4 is lower alkyl, fluoroalkyl or halogen; R5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR8, CONR9R10, —CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, 13 COR7, CR7(OR12)2, CR7OR13O, or tri-lower alkylsilyl, where R7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R8 is phenyl or lower alkylphenyl, R9 and R10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R11 is lower alkyl, phenyl or lower alkylphenyl, R12 is lower alkyl, and R13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译： 式1化合物，其中Z选自式2和式3中所示的基团，Y是任选被一个或两个R 4基团取代的环丙基，二价Y基团被Z和-CR 1 = CR1- CR1 =相邻碳上的CR1基团; X是S，O或NR5; n为1或2; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，低级烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R5是H或低级烷基，B是氢，COOH或其药学上可接受的盐，COOR8，CONR9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，13 COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基， 苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

    Aryl substituted 3,4-dihydroanthracene derivatives having retinoid antagonist or retinoid inverse agonist type biological activity
    54.
    发明授权
    Aryl substituted 3,4-dihydroanthracene derivatives having retinoid antagonist or retinoid inverse agonist type biological activity 失效

    公开(公告)号：US07166726B2

    公开(公告)日：2007-01-23

    申请号：US10336344

    申请日：2003-01-02

    申请人： Vidyasagar Vuligonda ,  Alan T. Johnson ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Alan T. Johnson ,  Roshantha A. Chandraratna

    IPC分类号： C07D495/00 ,  C07D221/00 ,  C07D221/22

    CPC分类号： C07C69/76 ,  C07C45/00 ,  C07C47/548 ,  C07C2603/24 ,  C07D213/55 ,  C07D311/92 ,  C07D333/24 ,  C07D335/08 ,  C07D409/06

    摘要： Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; n is an integer of between 0 and 2; o is an integer between 0 and 3; R3 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br or I; R4 is heteroaryl or (R5)p-heteroaryl where the heteroaryl group is 5-membered or 6-membered and has 1 to 3 heteroatoms selected from the group consisting of O, S, and N; p is an integer having the values of 0–5; R5 is F, Cl, Br, I, NO2, N(R8)2, N(R8)CORO8, N(R8)CON(R8)2, OH, OCOR8, OR8, CN, COOH, COOR8, C1-10 alkyl, fluoro substituted C1-10 alkyl, C2-10 alkenyl having 1 to 3 double bonds, C2-10 alkynyl having 1 to 3 triple bonds, or a (trialkyl)silyl or (trialkyl)silyloxy group where the alkyl groups independently have 1 to 6 carbons; A is (CH2)q where q is 0–5, C3-6 branched alkyl, C3-6 cycloalkyl, C2-6 alkenyl having 1 or 2 double bonds, or C2-6 alkynyl having 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COORO8, CONR9R10, CH2OH, CH2OR11, CH2OCOR11, CHO, CH(OR12)2, CHOR13O, COR7, CR7(OR12)2, CR7OR13O, or Si(C1-6alkyl)3; R7 is C1-5 alkyl, C3-5 cycloalkyl, or C2-5 alkenyl; R8 is C1-10 alkyl, C1-10 (trimethylsilyl)alkyl, or C5-10 cycloalkyl; R9 and R10 are independently hydrogen, C1-10 alkyl, C5-10 cycloalkyl, phenyl or R12-phenyl; R11 is C1-6 alkyl, phenyl, or R12-phenyl; R12 is C1-6 alkyl; and R13 is divalent alkyl radical of 2–5 carbons.

    2,4-pentadienoic acid derivatives having retinoid-like biological activity
    57.
    发明授权
    2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-戊二烯酸衍生物

    公开(公告)号：US6034242A

    公开(公告)日：2000-03-07

    申请号：US165917

    申请日：1998-10-02

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31/35 ,  A61K31/20 ,  A61K31/23 ,  A61K31/38 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07C57/50 ,  C07C69/618 ,  C07C215/02 ,  C07C215/18 ,  C07C311/58 ,  C07C335/06 ,  C07C403/00 ,  C07D277/22 ,  C07D311/58 ,  C07D333/54 ,  C07D335/06 ,  C07D215/06 ,  C07D215/12

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CO.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译： 式1的化合物，其中Z选自式3中所示的基团，Y是任选被一个或两个R 4基团取代的碳原子数为3至8的环烷基或环烯基，所述基团任选被一个或两个R 4基团取代 ，二价Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是NR5; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，有情人烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R5是H或低级烷基，B是氢，COOH或其可药用盐，COOR8，CO9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基， 苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。