申请人:Fisons Corporation
公开号:US05073560A1
公开(公告)日:1991-12-17
Compounds of general formula I, ##STR1## wherein: A represents (CH.sub.2).sub.m optionally substituted by R.sub.3, B represents (CH.sub.2).sub.n optionally substituted by R.sub.4, R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1-6 alkenyl or C.sub.1-6 alkynyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl or COOR.sub.5, in which R.sub.5 represents C.sub.1 -C.sub.6 alkyl, R.sub.3 and R.sub.4 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl, in addition, any two of R.sub.2, R.sub.3 and R.sub.4 may together form a C.sub.1-3 alkylene chain, n and m independently represent an integer from 1-3 inclusive, Y represents O or S, and pharmaceutically acceptable acid addition salts thereof are useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptor agonists. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome.
通式I的化合物,##STR1## 其中:A代表(CH.sub.2).sub.m,可选择地被R.sub.3取代,B代表(CH.sub.2).sub.n,可选择地被R.sub.4取代,R.sub.1代表氢,C.sub.1-C.sub.6烷基,C.sub.1-6烯基或C.sub.1-6炔基,R.sub.2代表氢,C.sub.1-C.sub.6烷基或COOR.sub.5,其中R.sub.5代表C.sub.1-C.sub.6烷基,R.sub.3和R.sub.4独立地代表氢或C.sub.1-C.sub.6烷基,此外,R.sub.2,R.sub.3和R.sub.4中的任意两个可以一起形成C.sub.1-3烷基链,n和m独立地表示从1-3的整数,Y代表O或S,并且其药学上可接受的酸盐是作为药物有用的,特别是作为中枢肌肉型乙酰胆碱受体激动剂。因此,这些化合物在治疗老年性痴呆症、亨廷顿舞蹈症、迟发性运动障碍、多动症、躁狂症和托瑞特综合症等疾病中有用。