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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：US4797488A
公开(公告)日：1989-01-10
申请号：US34820
申请日：1987-04-03
IPC分类号： C07D221/22 , A61K31/495 , A61K31/535 , A61P25/18 , C07C61/125 , C07D221/24 , C07D313/06 , C07D401/00 , C07D401/06 , C07D401/12 , C07D491/00 , C07D491/18 , C07D498/00 , C07D498/08 , C07D513/00 , C07D513/08 , C07D513/22 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
CPC分类号： C07C61/125 , C07D221/24 , C07D313/06 , C07D401/12
摘要： Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 -- where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of of 3 to 5 carbon atoms; 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, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R.sub.1 and R.sub.2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R.sub.1 and R.sub.2 complete a benzene ring, or a group of the formula: ##STR2## where Y is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --O-- or --S-- and the dotted line represents optional unsaturation; or a pharmaceutically acceptable salt thereof. In addition, the intermediate b3-dicarboxylic and the corresponding anhydrides - 2,3,3a,3b,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopenta[a]pentalene-1,3-dicarboxylic acid and octahydro-1,5-methano-6,8,9-metheneopentaleno[1,2-d]oxepin-2,4(1H,5H)-dione represent especially significant aspects of the invention.
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公开(公告)号：US5235055A
公开(公告)日：1993-08-10
申请号：US939198
申请日：1992-09-02
IPC分类号： A61K31/47 , A61P25/00 , A61P25/18 , A61P39/02 , C07D405/12 , C07D493/04
CPC分类号： C07D405/12 , C07D493/04
摘要： A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.
摘要翻译： 下式的化合物，其中R 1和R 2独立地是氢，烷基，烷氧基，芳烷氧基，烷酰氧基，羟基，卤素，氨基，单或二烷基氨基，烷酰胺基或亚磺酰氨基，或者R 1和R 2一起是亚甲二氧基， 亚乙二氧基或亚丙二氧基; R3是氢或烷基; n是整数2,3或4之一; 或其药学上可接受的盐是抗精神病药。
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公开(公告)号：US4797489A
公开(公告)日：1989-01-10
申请号：US127740
申请日：1987-12-02
IPC分类号： C07D295/088 , C07D295/14
CPC分类号： C07D295/088 , C07C2103/18
摘要： The compounds ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 9-fluorenyl or 1-fluorenyl;n is 0 or 1;m is 1, 2, 3, 4 or 5; andX is ##STR2## where R.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl, ##STR3## where R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or nitro;or pharmaceutically acceptable salts thereof are useful antidepressant and/or anxiolytic agents.
摘要翻译： 化合物＆lt; IMAGE＆gt;其中R 1是1-金刚烷基，3-甲基-1-金刚烷基，9-芴基或1-芴基; n为0或1; m为1,2,3,4或5; 并且X是其中R 2是苯基，苄基，吡啶基，嘧啶基，吡嗪基或取代的苯基或苄基，其中取代基是1至6个碳原子的烷基，具有1至6个碳原子的烷氧基，卤素，氰基，硝基或 三氟甲基，其中R 3为氢，1至6个碳原子的烷基，1至6个碳原子的烷氧基，卤素，氰基或硝基; 或其药学上可接受的盐是有用的抗抑郁剂和/或抗焦虑剂。
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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：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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7.发明授权3-Aminoalkyl derivatives of 5,5-disubstituted hydantoins with psychotropic activity 失效具有精神活性的5,5-二取代乙内酰脲的3-氨基烷基衍生物
公开(公告)号：US4675403A
公开(公告)日：1987-06-23
申请号：US787358
申请日：1985-10-16
IPC分类号： C07D233/74 , C07D235/02 , C07D401/06 , C07D403/12 , C07D403/14 , C07D401/14
CPC分类号： C07D235/02 , C07D233/74 , C07D401/06 , C07D403/12
摘要： There are disclosed compounds of the formula ##STR1## wherein Y represents ##STR2## R and R.sup.1 are each, independently, hydrogen, lower alkyl, phenyl or naphthyl, with that proviso that when R and R.sup.1 are both phenyl, R.sup.2 is other than phenyl;Z is ##STR3## R.sup.2 is 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyridinyl, halopyridin-2-yl, cyanopyridin-2-yl, phenyl or phenyl substituted with lower alkyl, halo or trifluoromethyl;R.sup.3 is phenyl or phenyl substituted with halo or trifluoromethyl;m is 2-7;n is 2-5; andand 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IMA的化合物，其中Y代表R，R 1各自独立地是氢，低级烷基，苯基或萘基，条件是当R 1和R 2均为苯基时，R 2不是苯基 ; Z是R 2是2-嘧啶基，卤代嘧啶-2-基，2-吡啶基，卤代吡啶-2-基，氰基吡啶-2-基，苯基或被低级烷基，卤素或三氟甲基取代的苯基; R3是苯基或被卤素或三氟甲基取代的苯基; m为2-7; n为2-5; 及其药学上可接受的盐及其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。
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公开(公告)号：US4957913A
公开(公告)日：1990-09-18
申请号：US440573
申请日：1989-11-22
IPC分类号： A61K31/495 , A61K31/505
CPC分类号： A61K31/505 , A61K31/495
摘要： Hypertension in the mammal is controlable by administration of a compound of the formula: ##STR1## wherein R is ##STR2## in which X is methylene, ethylene or ethylidene and Q is alkylene, alkylidene, or Q is a ##STR3## in which the dotted line represents optional unsaturation; n is one of the integers 2,3 or 4;Ar is phenyl or phenyl substituted with halo. trifluoromethyl or alkoxy, or Ar is 2-pyrimidinyl or halopyrimidin-2-yl, 2-pyrazinyl or halo-pyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl or halopyridin-2-yl;or a pharmaceutically acceptable salt thereof.
摘要翻译： 哺乳动物的高血压可以通过给予下式化合物来控制：其中R是其中X是亚甲基，亚乙基或亚乙基且Q是亚烷基，亚烷基或Q是一个“IMAGE”，其中 虚线表示可选的不饱和度; n是整数2,3或4之一; Ar是苯基或被卤素取代的苯基。 三氟甲基或烷氧基，或Ar为2-嘧啶基或卤代嘧啶-2-基，2-吡嗪基或卤代吡嗪-2-基，2-吡啶基，氰基吡啶-2-基或卤代吡啶-2-基; 或其药学上可接受的盐。
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公开(公告)号：US5126367A
公开(公告)日：1992-06-30
申请号：US719881
申请日：1991-06-21
IPC分类号： C07D319/20
CPC分类号： C07D319/20
摘要： A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; R.sup.1 is hydrogen, alkyl, alkoxy, alkanoyloxy, hydroxy, halo, nitro, amino, alkylamino, dialkylamino and alkanoylamino; X is O, S or CH.sub.2 ; n is an integer 2, 3 or 4; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, phenyl or benzyl; R.sup.4 is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.5 is H or CH.sub.3 ; Z is H.sub.2 or O; Y is OCO, NHCO, NHCONH, CONH, and in addition, when R.sup.4 is II, Y may be NHSO.sub.2 CH.sub.2 ; or a pharmaceutically acceptable salt thereof are useful as antipsychotic/anxiolytic agents.
摘要翻译： 下式的化合物：其中虚线表示任选的不饱和度; R 1是氢，烷基，烷氧基，烷酰氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基和烷酰基氨基; X是O，S或CH 2; n是整数2,3或4; R2是氢或低级烷基; R3是氢，低级烷基，苯基或苄基; R4是其中m是整数0,1或2之一的结构
之一; R5是H或CH3; Z是H 2或O; Y是OCO，NHCO，NHCONH，CONH，另外当R4是II时，Y可以是NHSO2CH2; 或其药学上可接受的盐可用作抗精神病药/抗焦虑剂。 -
公开(公告)号：US5126366A
公开(公告)日：1992-06-30
申请号：US719887
申请日：1991-06-21
IPC分类号： C07D319/20
CPC分类号： C07D319/20
摘要： The compounds: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido, or sulfonamido, or R.sup.1 and R.sup.2 together form methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, aroyl, alkylsulfonyl or arylsulfonyl, or R.sup.4 and R.sup.5 together form a 3-7 membered polymethylene ring; or a pharmaceutically acceptable salt thereof, are antipsychotic, antidepressant and anxiolytic agents useful in the treatment of multi-CNS disease states.
摘要翻译： 化合物：其中R 1和R 2独立地为氢，烷基，烷氧基，芳烷氧基，烷酰氧基，羟基，卤素，氨基，单或二烷基氨基，烷酰氨基或亚磺酰氨基，或者R 1和R 2一起形成亚甲二氧基，亚乙二氧基， 或亚丙二氧基; R3是氢或烷基; n是整数2,3或4之一; R4和R5独立地是氢，烷基，环烷基，烷酰基，芳酰基，烷基磺酰基或芳基磺酰基，或R4和R5一起形成3-7元多亚甲基环; 或其药学上可接受的盐是可用于治疗多CNS疾病状态的抗精神病药，抗抑郁药和抗焦虑剂。
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