申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0471298A1
公开(公告)日:1992-02-19
This invention relates to compounds of the formula
where
R₁is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl or loweralkynyl;
R₂is hydrogen, loweralkyl, loweralkenyl, formyl or cyano;
R₃is hydrogen or loweralkyl;
R₄is loweralkyl, arylloweralkyl, cycloalkyl, aryl, heteroaryl, heteroarylloweralkyl,
or NR₃R₄ taken together constitute
R₅is hydrogen, loweralkyl or aryl;
R₆is hydrogen, loweralkyl, aryl, arylloweralkyl, formyl, loweralkanoyl or arylloweralkanoyl,
X and Yare independently hydrogen, nitro, amino, halogen, loweralkyl, loweralkoxy or hydroxy; or the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof.
The compounds of this invention are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.
本发明涉及式如下的化合物
式中
R₁是氢、低级烷基、芳基低级烷基、低级烯基或低级炔基;
R₂ 是氢、低级烷基、低级烯基、甲酰基或氰基;
R₃ 是氢或低级烷基;
R₄是低级烷基、芳基低级烷基、环烷基、芳基、杂芳基、杂芳基低级烷基、
或 NR₃R₄ 共同构成
R₅ 是氢、低级烷基或芳基;
R₆ 是氢、低级烷基、芳基、芳低级烷基、甲酰基、低级烷酰基或芳低级烷酰基、
X和Y独立地为氢、硝基、氨基、卤素、低级烷基、低级烷氧基或羟基;或其药学上可接受的酸加成盐,以及(如适用)其几何异构体、光学异构体和外消旋混合物。
本发明的化合物可用于治疗以胆碱能功能下降为特征的各种记忆功能障碍,如阿尔茨海默病。