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公开(公告)号：US4404137A
公开(公告)日：1983-09-13
申请号：US193200
申请日：1980-10-02
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。
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12.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
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.
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公开(公告)号：US4431589A
公开(公告)日：1984-02-14
申请号：US327143
申请日：1981-12-03
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。
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公开(公告)号：US4977150A
公开(公告)日：1990-12-11
申请号：US390029
申请日：1989-08-04
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 ##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 wherein 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 cental nervous system activity.
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15.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
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.
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公开(公告)号：US4492699A
公开(公告)日：1985-01-08
申请号：US541605
申请日：1983-10-13
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.
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