申请人:Asahi Kasei Kogyo Kabushiki Kaisha
公开号:US05621142A1
公开(公告)日:1997-04-15
Disclosed are a novel optically active compound represented by formula (1), a racemic modification thereof, and a pharmaceutically acceptable acid addition salt of the optically active compound or racemic modification thereof: ##STR1## wherein R is a straight chain or branched C.sub.1 -C.sub.5 aliphatic group which is saturated or unsaturated, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are each independently selected from the group consisting of a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a nitro group, an amino group, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group; and mark * indicates an asymmetric carbon atom. The novel optically active aminoalkylcyclopropane derivative of the present invention, a racemic modification thereof, and a pharmaceutically acceptable acid addition salt of the optically active aminoalkylcyclopropane derivative or racemic modification thereof have remarkably high antagonistic activity with respect to NMDA receptor, as compared to known aminomethylcyclopropane derivatives and is useful as a preventive agent for cerebral infarction and a protective agent against ischemic diseases.
本发明公开了一种新的光学活性化合物,其表示为式(1),其外消旋异构体以及所述光学活性化合物或其外消旋异构体的药学可接受酸盐:
##STR1##
其中,R是一种直链或支链C.sub.1-C.sub.5脂肪族基,其饱和或不饱和,或者是一种苯基,其未被取代或被取代1至3个取代基,每个取代基都是从卤素原子,C.sub.1-C.sub.4烷基,硝基,氨基,羟基和C.sub.1-C.sub.4烷氧基中独立选择的;标记*表示一个不对称碳原子。本发明的新型光学活性氨基烷基环丙烷衍生物,其外消旋异构体以及所述光学活性氨基烷基环丙烷衍生物或其外消旋异构体的药学可接受酸盐在与已知的氨甲基环丙烷衍生物相比,具有显着的高拮抗NMDA受体的活性,并且可用作脑梗死的预防剂和缺血性疾病的保护剂。