申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US05096902A1
公开(公告)日:1992-03-17
The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group; R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group; R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group; R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group; R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group; R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group; m is 0 or 1; and n is 1 or 2, with the proviso that R.sup.2 means hydrogen when m is 0. The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer's disease or disturbances of the cognitive function.
该发明涉及一种新的含氮和硫杂环化合物,其化学式为(I),以及其酸盐、含有它们的药物组合物和制备它们的方法。在化学式(I)中,Ar代表可选择地单取代或多取代的芳基或杂芳基;R1表示羰基或(C2-6烯基)羰基基团;R2代表氢、C1-6烷基、苯基或苯基(C1-4烷基)基团;R3表示氢或(C1-6烷氧基)羰基基团;R4和R5独立地代表氢或C1-6烷基基团;R6 ogen、C1-6烷基基团或卤苯基团;m为0或1;n为1或2,但R2在m为0时表示氢。化合物(I)表现出显著的脑部抗缺氧作用,因此可以用于治疗由缺氧性脑损伤引起的疾病,如老年性痴呆、阿尔茨海默病或认知功能障碍。