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公开(公告)号:EP0520674B1
公开(公告)日:1995-08-16
申请号:EP92305535.4
申请日:1992-06-17
发明人: Stack, Gary Paul , Abou-Gharbia, Magid Abdel-Megid , Andree, Terrance Harold , Scherer, Noreen Theresa
IPC分类号: C07D319/20 , C07D407/12 , C07D493/04 , C07D405/12 , A61K31/335
CPC分类号: C07D405/12 , C07D319/20 , C07D407/12 , C07D493/04
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公开(公告)号:EP0520674A1
公开(公告)日:1992-12-30
申请号:EP92305535.4
申请日:1992-06-17
发明人: Stack, Gary Paul , Abou-Gharbia, Magid Abdel-Megid , Andree, Terrance Harold , Scherer, Noreen Theresa
IPC分类号: C07D319/20 , C07D407/12 , C07D493/04 , C07D405/12 , A61K31/335
CPC分类号: C07D405/12 , C07D319/20 , C07D407/12 , C07D493/04
摘要: The compounds:
wherein R¹ and R² are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido, or sulfonamido, or R¹ and R² together form methylenedioxy, ethylenedioxy, or propylenedioxy; R³ is hydrogen or alkyl; n is one of the integers 2, 3 or 4; R¹² is NR⁴R⁵ in which R⁴ and R⁵ are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, aroyl, alkylsulfonyl or arylsulfonyl, or R⁴ and R⁵ together form a 3-7 membered polymethylene ring; R¹⁰ is hydrogen or, when taken with R¹², R¹⁰ and R¹² complete the six membered ring-
in which X is O or NR⁸, in which R⁸ is hydrogen or alkyl; 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; R 3是氢或烷基; n是整数2,3或4之一; R 1是NR 4 R 5,其中R 4和R 5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R 4是氢, 和R 5一起形成3-7元多亚甲基环; R 1是氢或当R 1与R 2取代时,R 1和R 2都完成六元环 - CHEM,其中X是 O或NR 8,其中R 8是氢或烷基; 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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