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公开(公告)号：US5036070A
公开(公告)日：1991-07-30
申请号：US537551
申请日：1990-06-13
IPC分类号： C07D239/42 , C07D241/20 , C07D295/092 , C07D319/20
CPC分类号： C07D239/42 , C07D241/20 , C07D295/088 , C07D319/20
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, or phenyl, or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 -- or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, alkyl, alkoxy, or halo;Z is oxygen, or --N(R.sup.6), where R.sup.6 is hydrogen or alkyl;m is 1-4;n is 0-2; ##STR3## wherein R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl, 3-pyridazinyl, or diphenylmethyl, where the substituents are selected from the group of alkyl, alkoxy, halo, cyano, nitro and trifluoromethyl;R.sup.8 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, or NHR.sup.9 where R.sup.9 is hydrogen, alkyl, phenyl, tolyl, xylyl, mesityl, methoxyphenyl, or halophenyl with the proviso when Z is oxygen, R.sup.7 is other than phenyl or pyridyl;or a pharmaceutically acceptable salt thereof, which by virtue of high affinity for the dopamine D-2 receptor and the serotonin 5-HT-.sub.1A receptor, are useful as antipsychotic and anxiolytic agents for the treatment of a variety of central nervous system disorders such as paranoia, schizophrenia, anxiety, sleep disorders, and related problems.
摘要翻译： 公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，烷基或苯基，或者R 1和R 2一起表示 - （CH 2）4 - 或
，其中虚线表示任选的 双键; R3是氢，烷基，烷氧基或卤素; Z是氧或-N（R6），其中R6是氢或烷基; m为1-4; n为0-2; 其中R 7为未取代或取代的苯基，2-吡啶基，2-嘧啶基，2-吡嗪基，3-哒嗪基或二苯基甲基，其中取代基选自烷基，烷氧基，卤素，氰基， 硝基和三氟甲基; R8是氢，羟基，氰基，烷基，烷氧基，卤素或NHR9，其中R9是氢，烷基，苯基，甲苯基，二甲苯基，三甲苯基，甲氧基苯基或卤代苯基，条件是Z是氧时，R7不是苯基或吡啶基 ; 或其药学上可接受的盐，其由于对多巴胺D-2受体和5-羟色胺5-HT-1A受体的高亲和力可用作抗精神病药和抗焦虑剂，用于治疗各种中枢神经系统疾病，例如 偏执狂，精神分裂症，焦虑症，睡眠障碍和相关问题。 -
公开(公告)号：US4968792A
公开(公告)日：1990-11-06
申请号：US412256
申请日：1989-09-25
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.
摘要翻译： 本文公开了具有药理活性的新的苯并异噻唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种中枢神经系统疾病中的用途。
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公开(公告)号：US4957909A
公开(公告)日：1990-09-18
申请号：US459874
申请日：1990-01-02
IPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
CPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
摘要： The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.
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公开(公告)号：US4942234A
公开(公告)日：1990-07-17
申请号：US316888
申请日：1989-02-28
IPC分类号： C07D417/06 , C07D513/18
CPC分类号： C07D417/06
摘要： There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
摘要翻译： 公开了式（IMAGE）的化合物，其中R 1和R 2各自独立地为氢，低级烷基，芳基或卤素，或者R 1和R 2一起表示
+ TR 其中 虚线表示可选的双键; R 3，R 4和R 5各自独立地为氢，低级烷基，芳基或卤素; R6是2-吡啶基，2-吡嗪基，2-喹啉基，2-喹喔啉基或由低级烷基，低级烷氧基，三氟甲基，氰基，硝基或卤素取代的任何前述R 6部分; 或其中R 7为苯基，2-吡啶基，2-嘧啶基，3-哒嗪基或2-吡嗪基或由低级烷基，低级烷氧基，卤素，氰基，三氟甲基或硝基取代的前述R7部分中的任一个。 Z是低级亚烷基，亚乙烯基，O或NH; m为1-5; n为0-4; p为1-4; q是1-2; 及其药学上可接受的盐，以及它们作为锥体束外副作用负担低的抗精神病药/抗焦虑剂的用途。 -
45.发明授权
公开(公告)号：US4924008A
公开(公告)日：1990-05-08
申请号：US347538
申请日：1989-05-04
IPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
CPC分类号： A61K31/135 , A61K31/34 , C07D307/52 , C07D333/20
摘要： The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.
摘要翻译： 化合物的用途：其中R是氢，烷基，烷氧基，羟基，烷酰氧基，苯基烷氧基，卤素或三氟甲基; R1是烷基，烯基或苯基烷基; R2是氢，烷基，苯基烷基，烯基，炔基，噻吩烷基或呋喃基烷基; n是整数2,3,4,5或6之一; 或其药学上可接受的盐作为治疗惊厥和神经变性疾病状态的NMDA拮抗剂。 其中R2是杂环烷基胺的化合物是新的和有用的NMDA拮抗剂。
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公开(公告)号：US4910302A
公开(公告)日：1990-03-20
申请号：US286576
申请日：1988-12-19
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.
摘要翻译： 下式的化合物：其中Z是
+ TR ，其中X是亚烷基，亚乙炔基或亚烷基; Q是与其连接的碳原子一起形成苯环或取代的苯环的亚烷基，亚烷基，或亚甲基，其中所述取代基是-OH，-OCH 3，烷基，卤素，-CF 3 ，-NH 2，单烷基氨基，二烷基氨基或烷酰基氨基; R1是氢或烷基; R2和R3独立地是氢或烷基或与它们所连接的碳原子一起形成环烷烃或环烯烃环; m是整数2-5之一; R4是氢，羟基，氰基，烷基，烷氧基，卤素，氨基，烷基氨基，苯基氨基，甲苯基氨基，二甲苯基氨基，均三甲氨基，甲氧基苯基氨基或卤代苯基氨基; 虚线表示可选的不饱和键; 或其药学上可接受的盐。 -
公开(公告)号：US4837325A
公开(公告)日：1989-06-06
申请号：US179105
申请日：1988-04-08
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The compounds ##STR1## in which R is halo or trifluoromethyl;n is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof are useful as histamine H.sub.1 -receptor antagonists.
摘要翻译： 其中R为卤素或三氟甲基的化合物
+ TR n是整数2,3或4之一; 或其药学上可接受的盐可用作组胺H1-受体拮抗剂。 -
公开(公告)号：US4766124A
公开(公告)日：1988-08-23
申请号：US19089
申请日：1987-02-26
IPC分类号： C07D471/04 , A61K31/495 , C07D403/14
CPC分类号： C07D471/04
摘要： The method of using compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or 4-halophenyl; R.sup.2 is 4-halophenyl when R.sup.1 is 4-halophenyl and 3-trifluoromethylphenyl and R.sup.1 is hydrogen; and n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof as histamine H.sub.1 -receptor antagonists and the novel compound 2,3,4,9-tetrahydro-2-[3-[4-[3-(trifluoromethyl)benzyl]-1-piperazinyl]propyl]-1H-pyridol[3,4-b]indole represent the inventive aspects of this disclosure.
摘要翻译： 使用下式的化合物的方法：其中R 1是氢或4-卤代苯基; 当R1是4-卤代苯基和3-三氟甲基苯基且R 1是氢时，R 2是4-卤代苯基; n是整数2,3或4之一; 或其药学上可接受的盐作为组胺H1受体拮抗剂和新化合物2,3,4,9-四氢-2- [3- [4- [3-（三氟甲基）苄基] -1-哌嗪基]哌嗪基] -1H-吡唑并[3,4-b]吲哚代表本公开的发明方面。
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公开(公告)号：US4732983A
公开(公告)日：1988-03-22
申请号：US34522
申请日：1987-04-03
IPC分类号： C07D209/70 , C07D221/22 , C07D401/12 , C07D403/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14
CPC分类号： C07D221/22 , C07D209/70 , C07D401/12 , C07D403/12
摘要： Substituted imides of the following formulae are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which n is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, halopyridin-2-yl, cyanopyridin-2-yl, quinolyl, or haloquinolyl; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.
摘要翻译： 下列化学式的取代酰亚胺是抗精神病药，抗焦虑剂，具有很少的锥体束外副作用：其中n是整数2,3,4或5之一; R是苯基，卤代苯基，三氟甲基苯基，烷氧基取代基含有1至3个碳原子的烷氧基苯基，2-嘧啶基卤代嘧啶-2-基，2-吡嗪基，卤代吡嗪-2-基，2-吡啶基，卤代吡啶-2-基， 氰基吡啶-2-基，喹啉基或卤代喹啉基; 虚线表示可选的不饱和键; 或其药学上可接受的盐。
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50.发明授权2,3,4,9-tetrahydro-2-heteroarylalkyl-1H-pyrido(3,4-B)indoles having antihypertensive properties 失效具有抗高血压性质的2,3,4,9-四氢-2-杂芳基烷基-1H-吡啶并（3,4-B）吲哚
公开(公告)号：US4719211A
公开(公告)日：1988-01-12
申请号：US837612
申请日：1986-03-07
IPC分类号： C07D471/04 , A61K31/495 , C07D471/06
CPC分类号： C07D471/04
摘要： This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties.Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen. The compounds of Formula XX exhibit antipsychotic properties.
摘要翻译： 本发明涉及下式的四氢吡啶并吲哚：其中Q代表其中R3是氢，C1-4烷基，C1-4烷氧基或-COO（C1-2）烷基，其中n是 1至7; R 1是氢，卤素，羟基或C 1-3烷基; 其中A为-N（CH 3）2，-N（C 2 H 5）2，其中Ar为2-嘧啶基，2-吡嗪基，苯基或 被甲基，乙基，甲氧基，乙氧基或三氟甲基取代的苯基; 并且m是1-4的整数或其生理上可接受的盐，但是当n为1时，Q可能不是喹啉基。 这些化合物显示抗高血压性质。 所公开的化合物中的四种也显示出抗精神病性质。 还公开了式XX的化合物，其中式I的Q被Q1代替，其中Q1是2-或3-吡啶基，式I的R2限于氢。 式XX的化合物显示出抗精神病性质。
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