申请人:A. H. Robins Company, Incorporated
公开号:US05066654A1
公开(公告)日:1991-11-19
There are disclosed compounds of the formula ##STR1## wherein Ar is ##STR2## Het is ##STR3## R.sup.1, R.sup.2, and R.sup.3 are each, independently, hydrogen, alkyl, aralkyl, alkoxy, carbalkoxy, trifluoromethyl, halo, cyano, or nitro; R.sup.4 is hydrogen, alkyl, aralkyl, alkoxy, carbalkoxy, halo, or trifluoromethyl; Y is NH, O, or S; X is CH, or N; or a pharmaceutically acceptable salt thereof, which, by virtue of their ability to bind to the benzodiazepine receptor, and prevent electrically or chemically induced seizures are useful as anxiolytic and anticonvulsant agents.
公开了具有以下结构的化合物 ##STR1## 其中 Ar 是 ##STR2## Het 是 ##STR3## R.sup.1、R.sup.2 和 R.sup.3 分别独立地是氢、烷基、芳基烷基、烷氧基、羰基烷氧基、三
氟甲基、卤素、
氰基或硝基;R.sup.4 是氢、烷基、芳基烷基、烷氧基、羰基烷氧基、卤素或三
氟甲基;Y 是 NH、O 或 S;X 是 CH 或 N;或其药用可接受盐,由于它们具有结合到苯二氮卓受体并防止电或
化学诱导的癫痫发作的能力,因此可用作抗焦虑和抗抽搐剂。