利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

11 条记录 (耗时 0.03 秒)

    Benzodiazepine compounds and their use as pharmaceuticals
    4.
    发明授权
    Benzodiazepine compounds and their use as pharmaceuticals 失效
    苯并二氮杂类化合物及其作为药物的用途

    公开(公告)号：US5051516A

    公开(公告)日：1991-09-24

    申请号：US562055

    申请日：1990-08-02

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/55 ,  A61P25/18 ,  A61P25/20 ,  C07D277/56 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D277/56

    摘要： Pharmaceutical thiazolo-[1,5]benzodiazepines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula formula ##STR2## where R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, benzyl or ZO--C.sub.2-6 alkyl where Z is hydrogen or an acyl group, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio; and in which ##STR3## represents a thiazole ring selected from ##STR4## and acid addition salts thereof. The compounds have central nervous system activity.

    Pyrazolo [3,4-b][1,5]benzodiazepine compounds
    5.
    发明授权
    Pyrazolo [3,4-b][1,5]benzodiazepine compounds 失效
    吡唑并[3,4-b] [1,5]苯并二氮杂化合物

    公开(公告)号：US4404137A

    公开(公告)日：1983-09-13

    申请号：US193200

    申请日：1980-10-02

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： A61K31/00 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D231/38 ,  C07D487/04 ,  A61K31/55

    CPC分类号： C07D231/38 ,  C07D487/04

    摘要： Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula --SO.sub.2 N(R.sup.8).sub.2, --SO.sub.2 R.sup.8 or --SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, benzyl, C.sub.1-6 alkanoyl, C.sub.1-4 carbalkoxy or benzoyl; and in which R.sup.7 is one of the values of R.sup.6 or halogen, nitro, cyano, amino or C.sub.1-4 acylamino. The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system. Intermediate compounds in which R.sup.5 is thiol, hydroxy, or amino are also described.

    摘要翻译： 化合物描述为式“IMAGE”或其酸加成盐; 其中R 1，R 2，R 3和R 4独立地表示氢，C 1-4烷基，C 2-4烯基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，卤素，C 1-4卤代烷基，C 1-4烷酰基，硝基 ，氨基，C2-4酰氨基，氰基，羟基，C1-4烷氧基，C1-4烷硫基，C1-4卤代烷氧基或式-SO2N（R8）2，-SO2R8或-SO3R8的基团，其中R8为C1-4 烷基，C 1-4卤代烷基或任选取代的苯基; 其中R 5是下式的基团，其中R 9是氢，C 1-4烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，C 1-4卤代烷基，C 2-4链烯基，C 1-4烷酰基 苄基，氰基或任选取代的苯基，其中R 10是氢，C 1-4烷基或任选取代的苯基，其中n是0或1; 其中R 6是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，C 1-4卤代烷基，苄基，C 1-6烷酰基，C 1-4烷氧基或苯甲酰基; 并且其中R 7是R 6或卤素，硝基，氰基，氨基或C 1-4酰氨基的值之一。 这些化合物作为药物是有活性的，特别是用于治疗中枢神经系统疾病。 还描述了其中R 5为硫醇，羟基或氨基的中间体化合物。

    4-Substituted-1-(3-[2-aminoanilino]-1-pyrazole-4-carbonyl)piperazine
    6.
    发明授权
    4-Substituted-1-(3-[2-aminoanilino]-1-pyrazole-4-carbonyl)piperazine 失效
    4-取代的1-（3- [2-氨基苯胺基] -1-吡唑-4-羰基）哌嗪

    公开(公告)号：US4486591A

    公开(公告)日：1984-12-04

    申请号：US426580

    申请日：1982-09-29

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： A61K31/00 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D231/38 ,  C07D487/04 ,  C07D403/06

    CPC分类号： C07D231/38 ,  C07D487/04

    摘要： Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula -SO.sub.2 N(R.sup.8).sub.2, -SO.sub.2 R.sup.8 or -SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, benzyl, C.sub.1-6 alkanoyl, C.sub.1-4 carbalkoxy or benzoyl; and in which R.sup.7 is one of the values of R.sup.6 or halogen, nitro, cyano, amino or C.sub.1-4 acylamino. The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system.

    Benzodiazepine compounds and their use as pharmaceuticals
    7.
    发明授权
    Benzodiazepine compounds and their use as pharmaceuticals 失效
    苯二氮卓类化合物及其作为药物的用途

    公开(公告)号：US4431589A

    公开(公告)日：1984-02-14

    申请号：US327143

    申请日：1981-12-03

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten ,  David J. Steggles

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten ,  David J. Steggles

    IPC分类号： C07D243/12 ,  A61K31/00 ,  A61K31/55 ,  A61K31/5517 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D243/28 ,  C07D249/04 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D249/04

    摘要： These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.5 H with a triazolobenzodiazepine intermediate appropriately substituted at the 10-position or by ring-closing the appropriate anilinotriazole.

    摘要翻译： 这些是式（I）化合物或其酸加成盐; 其中R 1，R 2，R 3和R 4独立地表示氢，C 1-4烷基，C 2-4烯基，卤素，C 1-4卤代烷基，硝基，C 1-4烷氧基，C 1-4卤代烷氧基，C 1-4烷硫基或苯基磺酰基。 其中R 5是下式的基团，其中R 7是氢或C 1-6烷基，R 8是氢或C 1-4烷基，n是0或1，条件是当R 7是氢时，n是0; 并且其中R6连接到三唑环的1,2或3位，并且是氢，C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，苄基或酰基。 这些化合物是药学活性的并且特别可用于治疗中枢神经系统疾病。 它们通过使式R5H的胺与在10位适当取代的三唑并苯并二氮杂中间体或通过闭环合适的苯胺三唑反应来制备。

    Substituted diazolo[b][1,5]benzodiazepines and their use as CNS agents
    8.
    发明授权
    Substituted diazolo[b][1,5]benzodiazepines and their use as CNS agents 失效
    取代的重氮[b] [1,5]苯并二氮杂类及其用作CNS剂

    公开(公告)号：US4542131A

    公开(公告)日：1985-09-17

    申请号：US638181

    申请日：1984-08-06

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten

    IPC分类号： A61K31/00 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D231/38 ,  C07D487/04 ,  A61K31/33

    CPC分类号： C07D231/38 ,  C07D487/04

    摘要： Compounds are described of the formula ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, halogen, C.sub.1-4 haloalkyl, C.sub.1-4 alkanoyl, nitro, amino, C.sub.2-4 acylamino, cyano, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 haloalkoxy or a group of the formula --SO.sub.2 N(R.sup.8).sub.2, --SO.sub.2 R.sup.8 or --SO.sub.3 R.sup.8 where R.sup.8 is C.sub.1-4 alkyl, C.sub.1-4 haloalkyl or optionally substituted phenyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.9 is hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkanoyl, benzyl, cyano or optionally substituted phenyl, where R.sup.10 is hydrogen, C.sub.1-4 alkyl or optionally substituted phenyl and where n is 0 or 1; in which R.sup.6 is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl. C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, benzyl, C.sub.1-6 alkanoyl, C.sub.1-4 carbalkoxy or benzoyl; and in which R.sup.7 is one of the values of R.sup.6 or halogen, nitro, cyano, amino or C.sub.1-4 acylamino.The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system.

    Triazolobenzodiazepine derivatives
    9.
    发明授权
    Triazolobenzodiazepine derivatives 失效
    三唑并苯并二氮杂衍生物

    公开(公告)号：US4492699A

    公开(公告)日：1985-01-08

    申请号：US541605

    申请日：1983-10-13

    申请人： Jiban K. Chakrabarti ,  Terrence M. Hotten ,  David J. Steggles

    发明人： Jiban K. Chakrabarti ,  Terrence M. Hotten ,  David J. Steggles

    IPC分类号： C07D243/12 ,  A61K31/00 ,  A61K31/55 ,  A61K31/5517 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  C07D243/28 ,  C07D249/04 ,  C07D487/04 ,  A61K31/495

    CPC分类号： C07D487/04 ,  C07D249/04

    摘要： These are described compounds of formula (I) ##STR1## or an acid addition salt thereof; in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, halogen, C.sub.1-4 haloalkyl, nitro, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio or phenylsulphonyl; in which R.sup.5 is a group of the formula ##STR2## where R.sup.7 is hydrogen or C.sub.1-6 alkyl, R.sup.8 is hydrogen or C.sub.1-4 alkyl and n is 0 or 1, provided that when R.sup.7 is hydrogen n is 0; and in which R.sup.6 is attached to the 1, 2 or 3 position of the triazole ring and is hydrogen, C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl C.sub.1-4 alkyl, phenyl, benzyl or acyl. These compounds are pharmaceutically active and are especially useful in the treatment of disorders of the central nervous system. They are prepared by reacting an amine of formula R.sup.5 H with a triazolobenzodiazepine intermediate appropriately substituted at the 10-position or by ring-closing the appropriate anilinotriazole.