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    Tricyclic 5-HT.sub.3 receptor antagonists
    2.
    发明授权
    Tricyclic 5-HT.sub.3 receptor antagonists 失效
    三环5-HT 3受体拮抗剂

    公开(公告)号：US5202333A

    公开(公告)日：1993-04-13

    申请号：US704565

    申请日：1991-05-22

    申请人： Jacob Berger ,  Robin D. Clark ,  Richard M. Eglen ,  William L. Smith ,  Klaus K. Weinhardt

    发明人： Jacob Berger ,  Robin D. Clark ,  Richard M. Eglen ,  William L. Smith ,  Klaus K. Weinhardt

    IPC分类号： C07D487/08 ,  A61K31/47 ,  A61K31/55 ,  A61P1/00 ,  A61P1/08 ,  A61P1/14 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D205/12 ,  C07D209/52 ,  C07D221/22 ,  C07D401/04 ,  C07D403/04 ,  C07D451/02 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D471/06 ,  C07D471/08

    CPC分类号： C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D471/06 ,  C07D471/08 ,  Y10S514/872

    摘要： The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

    摘要翻译： 本发明涉及式I的5-HT 3受体拮抗剂化合物：其中虚线表示任选的双键; n为1,2或3; p为0,1,2或3; q是0,1或2; 每个R 1独立地选自卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; 每个R 2是低级烷基; （a），（b），（c）和（d）所示的基团：其中，（a），（c） 你是0或1; z为1,2或3; 和R 4是C 1-7烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基或基团（CH 2）t R 5，其中t是1或2，R 5是噻吩基，吡咯基或呋喃基， 选自C 1-6烷基，C 1-6烷氧基，三氟甲基或卤素的一个或两个取代基，或被任选被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基的取代基取代的苯基和 任选被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。

    Tricyclic compounds acting at serotonin receptor subtypes
    3.
    发明授权
    Tricyclic compounds acting at serotonin receptor subtypes 失效
    作用于血清素受体亚型的三环化合物

    公开(公告)号：US5202318A

    公开(公告)日：1993-04-13

    申请号：US708260

    申请日：1991-05-28

    申请人： Jacob Berger ,  Robin D. Clark ,  Richard M. Eglen ,  William L. Smith ,  Klaus K. Weinhardt

    发明人： Jacob Berger ,  Robin D. Clark ,  Richard M. Eglen ,  William L. Smith ,  Klaus K. Weinhardt

    IPC分类号： C07D401/04 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08

    CPC分类号： C07D401/04 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08 ,  Y10S514/872

    摘要： Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.3 is independently selected from hydrogen, hydroxy, alkyl and alkoxy;each R.sup.4 is independently hydrogen or alkyl; andR.sup.5 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, alkenyl, alkynyl or a group R.sup.7 -C.sub.1-3 alkyl in which R.sup.7 is phenyl or phenoxy optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

    摘要翻译： 式I化合物：其中Z为CH 2或C = O; X和Y独立地选自氢，卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二（低级烷基）氨基和（低级烷酰基）氨基; （a），（b），（c）（d）和（e）所示的基团：（a） （e）其中p为0或1; n为1,2或3; R 2是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 12烷基或其中R 6是噻吩基的R6-C 1-2烷基，任选地被一个或两个选自下列的取代基取代的吡咯基或呋喃基：低级烷基， 低级烷氧基，三氟甲基或卤素，或者是被一个或两个选自C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基取代的C 1-4烷基取代的苯基 ，羧基，酯化羧基或体内可水解酰氧基; 每个R 3独立地选自氢，羟基，烷基和烷氧基; 每个R 4独立地是氢或烷基; R 5是氢，低级烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基，链烯基，炔基或其中R 7是任选被一个或两个取代基所取代的苯基或苯氧基的基团 由C 1-4烷氧基，三氟甲基，卤素，硝基，羧基，酯化羧基和任选进一步被羟基，C 1-4烷氧基，羧基，酯化羧基或体内可水解酰氧基进一步取代的C 1-4烷基; 和其药学上可接受的盐，各异构体，异构体的混合物，制备方法，组合物及其使用方法。

    1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines
    4.
    发明授权
    1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines 失效
    1,9-链烷基-2,3,4,5-四氢-1H-3-苯并氮杂

    公开(公告)号：US4957914A

    公开(公告)日：1990-09-18

    申请号：US231818

    申请日：1988-08-12

    申请人： Robin D. Clark ,  Jacob Berger ,  Klaus K. Weinhardt

    发明人： Robin D. Clark ,  Jacob Berger ,  Klaus K. Weinhardt

    IPC分类号： C07D223/14 ,  C07D223/32

    CPC分类号： C07D223/32 ,  C07D223/14

    摘要： 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.

    摘要翻译： 1,9-烷基桥-2,3,4,5-四氢-1H-3-苯并吖庚因及其衍生物，即式I化合物：其中：R选自 由氢，氰基，低级烷基，低级烯基和芳烷基组成的基团; R 1，R 2和R 3各自独立地选自：氢，羟基，卤素，三氟甲基，硝基，酰氨基，低级烷氧基，低级烷基和低级烷硫基; Y是具有2至4个碳原子的低级亚烷基; 和其药学上可接受的盐可用作CNS剂，例如作为抗抑郁药，抗焦虑药和抗高血压药，和/或作为其前体。

    Isoquinolinone and dihydroisoquinolinone 5-HT.sub.3 receptor antagonists
    6.
    发明授权
    Isoquinolinone and dihydroisoquinolinone 5-HT.sub.3 receptor antagonists 失效
    异喹啉酮和二氢异喹啉酮5-HT 3受体拮抗剂

    公开(公告)号：US5491148A

    公开(公告)日：1996-02-13

    申请号：US692407

    申请日：1991-04-26

    申请人： Jacob Berger ,  Robin D. Clark

    发明人： Jacob Berger ,  Robin D. Clark

    IPC分类号： C07D451/04 ,  C07D453/02 ,  C07D471/08 ,  A61K31/44

    CPC分类号： C07D451/04 ,  C07D453/02 ,  C07D471/08

    摘要： 5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;R.sup.2 is a group selected from Formulae (a), (b), (c) and (d): ##STR2##

    摘要翻译： 式I的5-HT 3受体拮抗剂化合物：其中X和Y独立地选自氢，卤素，羟基，低级烷氧基，低级烷基，硝基，氨基，氨基羰基，（低级烷基）氨基，二 （低级烷基）氨基和（低级烷酰基）氨基; R1是氢，低级烷基，苯基或卤素; （a），（b），（c）和（d）中选择的基团：（a）

    Arylsulfonyl derivatives with 5-HT6 receptor affinity
    10.
    发明授权
    Arylsulfonyl derivatives with 5-HT6 receptor affinity 失效
    具有5-HT 6受体亲和力的芳基磺酰基衍生物

    公开(公告)号：US06825202B2

    公开(公告)日：2004-11-30

    申请号：US10215769

    申请日：2002-08-09

    申请人： Jacob Berger ,  Robin Douglas Clark ,  Shu-Hai Zhao

    发明人： Jacob Berger ,  Robin Douglas Clark ,  Shu-Hai Zhao

    IPC分类号： A61K31495

    CPC分类号： C07D295/096

    摘要： This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

    摘要翻译： 本发明涉及通常具有5-HT 6受体亲和力并由式（I）表示的化合物：其中Ar，R 1，R 2，R 3或R 4如 说明书或其药学上可接受的盐或溶剂化物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。