Pyrrolo(1,2-b)cinnolines, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0308912A2
公开(公告)日:1989-03-29
There are described pyrrolo[1,2-b]cinnolines having the formula
where R₁ when present is hydrogen, loweralkyl, arylloweralkyl or -CH₂CO₂C₂H₅; R₂ is hydrogen, loweralkyl, arylloweralkyl, chlorine, bromine, iodine, formyl, nitro, -CH=CR₃R₄ or -CH₂CHR₃R₄, R₃ and R₄ being independently hydrogen, loweralkyl, aryl or arylloweralkyl; X is oxygen, amino, loweralkylamino, arylloweralkylamino or methoxy; and Y is hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl or nitro, and pharmaceutically acceptable acid addition salts thereof which are useful as analgesic agents and as enhancers of cholinergic function and hence for the treatment of memory dysfunctions and senile dementia's such as Alzheimer's disease characterized by diminished cholinergic function.
所描述的
吡咯并[1,2-b]噌啉具有以下式子
其中 R₁为氢、低级烷基、芳低级烷基或-CH₂CO₂C₂H₅;R₂ 是氢、低级烷基、芳低级烷基、
氯、
溴、
碘、甲酰基、硝基、-CH=CR₃R₄ 或 -CH₂CHR₃R₄,R₃ 和 R₄ 独立地是氢、低级烷基、芳基或芳低级烷基;X 是氧、
氨基、低级烷基
氨基、芳基低级烷基
氨基或甲氧基;和 Y 是氢、
氟、
氯、
溴、
碘、三
氟甲基或硝基,及其药学上可接受的酸加成盐,可用作镇痛剂和
胆碱能功能增强剂,因此可用于治疗以
胆碱能功能减退为特征的记忆功能障碍和老年痴呆症,如阿尔茨海默氏症。