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    • 86. 发明公开
    • 무스카린 길항제
    • 心理拮抗剂
    • KR1020000022380A
    • 2000-04-25
    • KR1019980710811
    • 1997-06-26
    • 머크 샤프 앤드 돔 코포레이션
    • 코즐로우스키조셉에이로우데렉비창웨이케이듀거선디프
    • C07D295/096
    • C07D317/62C07B2200/07C07C2601/14C07C2602/08C07C2602/10C07C2602/12C07D211/58C07D239/34C07D295/088C07D295/096C07D311/68C07D317/58
    • PURPOSE: The Invention is the use of a compound of formula I, including stereoisomers, pharmaceutically acceptable salts, esters, and solvates thereof, for the preparation of a pharmaceutical composition useful in the treatment of cognitive disorders and neuro degenerative diseases such as Alzheimer's disease. CONSTITUTION: Di-N-substituted piperazine or 1,4-I-substituted piperidine compounds in accordance with formula (I) (incluIng all isomers, salts, esters, and solvates), wherein Q, n, R, R¬1, R¬2, R¬3, R¬4, R¬21, R¬27, R¬28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetylcholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.
    • 目的:本发明是使用式I化合物,包括立体异构体,其药学上可接受的盐,酯和溶剂化物,用于制备用于治疗认知障碍和神经变性疾病如阿尔茨海默氏病的药物组合物。 构成:根据式(I)的二-N-取代的哌嗪或1,4-I取代的哌啶化合物(包括所有异构体,盐,酯和溶剂合物),其中Q,n,R,R 1,R R 2,R 3,R 4,R 21,R 27,R 28,X和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱性拮抗剂。 还公开了药物组合物和制备方法。 还公开了与能够增强乙酰胆碱释放并具有上式的化合物的乙酰胆碱酯酶抑制剂的协同组合。