申请人:American Home Products Corporation
公开号:US04748240A1
公开(公告)日:1988-05-31
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 3 to 5 carbon atoms; Y is alkylene of 1 to 3 carbon atoms or alkenylene of 2 to 3 carbon atoms; n is one of the integers 0 to 1; m 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; or a pharmaceutically acceptable salt thereof.
以下公式中的替代酰亚胺是抗精神病、抗焦虑剂,具有非常少的锥体外系副作用:##STR1## 其中X为--O--,--S--,--SO--,--SO.sub.2--,--CR.sub.3R.sub.4--,其中R.sub.3和R.sub.4独立地为氢、1到4个碳原子的烷基或与它们连接的碳原子形成3到5个碳原子的环烷基;Y为1到3个碳原子的烷基或2到3个碳原子的烯基烷基;n为0到1之间的整数;m为2、3、4或5之一的整数;R为苯基、卤代苯基、三氟甲基苯基、取代基含有1到3个碳原子的烷氧基苯基、2-嘧啶基、卤代2-嘧啶-2-基、2-吡嗪基、卤代2-吡嗪-2-基、2-吡啶基、氰基2-吡啶-2-基、卤代2-吡啶-2-基、喹啉基或卤代喹啉基;或其药学上可接受的盐。