申请人:Yoshitomi Pharmaceutical Industries, Ltd.
公开号:US03952006A1
公开(公告)日:1976-04-20
Thiophene derivatives of the formula: ##SPC1## Wherein R.sup.1 is H or CH.sub.3 ; R.sup.2 is CH.sub.3 or C.sub.2 H.sub.5, or R.sup.1 and R.sup.2 combinedly represent --(CH.sub.2).sub.4 --; each of R.sup.3 and R.sup.4 is H, alkyl of from 1 to 4 carbon atoms or cyclohexyl, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form 1-pyrrolidinyl, piperidino, 4-methyl-1-piperazinyl or morpholino; X is H, halogen or OCH.sub.3 ; A is -CH= or --C(CH.sub.3)=, and B is =N-- or =CH--; or A is --C(CH.sub.2 OH)= or --N=, and B is =N--, and pharmaceutically acceptable acid addition salts thereof possess excellent pharmacological properties such as sedative, anxiolytic and anticonvulsant effects and protective effects against hypoxia or anoxia.
分子式为:##SPC1##
其中R.sup.1为H或CH.sub.3;R.sup.2为CH.sub.3或C.sub.2H.sub.5,或R.sup.1和R.sup.2合并表示--(CH.sub.2).sub.4--;R.sup.3和R.sup.4中的每一个都是H、1到4个碳原子的烷基或环己基,或者R.sup.3和R.sup.4与相邻的氮原子一起形成1-吡咯啉基、哌啶基、4-甲基-1-哌嗪基或吗啡环;X为H、卤素或OCH.sub.3;A为-CH=或--C(CH.sub.3)=,B为=N--或=CH--;或者A为--C(CH.sub.2OH)=或--N=,B为=N--,以及其药学上可接受的酸盐具有出色的药理学特性,例如镇静、抗焦虑和抗癫痫作用以及对缺氧或无氧的保护作用。