申请人:TAIHO PHARMACEUTICAL COMPANY, LIMITED
公开号:EP0429685A1
公开(公告)日:1991-06-05
Oxoindole derivatives of general formula (1), remarkably useful for treating senile dementia, i.e., improving brain functions and activating and protecting brain metabolism. In the formula, R1 represents hydrogen, halogen, lower alkyl, or lower alkoxy; R2 represents hydrogen or lower alkyl; R3 represents -CH2-R5, wherein R5 represents alkyl which may be cyclic, benzodioxanyl, or phenyl which may be substituted with a plurality of halogen, lower alkyl, lower alkoxy, hydroxy, diethylamino, trifluoromethyl, nitrile, nitro or benzyloxy; alternatively R2 and R3 may be combined together to from = CH-RS, wherein R5 is as defined above; and R4 represents 1 -propylbutyl, pyridyl, or phenyl which may be substituted with lower alkoxy, halogen, diethylamino, benzyloxy, trifluoromethyl, nitrile, nitro, or lower alkyl.
通式(1)的
氧化
吲哚衍
生物,对治疗老年痴呆症,即改善大脑功能、激活和保护大脑新陈代谢有显著作用。式中,R1 代表
氢、卤素、低级烷基或低级烷
氧基;R2 代表
氢或低级烷基;R3 代表 -
CH2-R5,其中 R5 代表烷基,可以是环状烷基、
苯并
二恶烷基或
苯基,可以被多个卤素、低级烷基、低级烷
氧基、羟基、
二乙胺基、三
氟甲基、腈基、硝基或苄
氧基取代;另一种情况是 R2 和 R3 结合为 CH-RS,其中 R5 如上定义;R4 代表可被低级烷
氧基、卤素、
二乙胺基、苄
氧基、三
氟甲基、腈基、硝基或低级烷基取代的 1-丙基丁基、
吡啶基或
苯基。