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111 条记录 (耗时 0.087 秒)

    Muscarinic antagonists
    67.
    发明授权
    Muscarinic antagonists 失效
    毒蕈碱拮抗剂

    公开(公告)号：US06458812B1

    公开(公告)日：2002-10-01

    申请号：US10023277

    申请日：2001-12-17

    申请人： Brian A. McKittrick ,  Guihua Guo ,  Zhaoning Zhu ,  Yuanzan Ye

    发明人： Brian A. McKittrick ,  Guihua Guo ,  Zhaoning Zhu ,  Yuanzan Ye

    IPC分类号： A61K31445

    CPC分类号： C07D451/04 ,  C07D211/34 ,  C07D405/04

    摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula: or a pharmaceutically acceptable salt, ester or solvate thereof, wherein R1 is optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R2 is H, alkyl, or optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl, or bridged heterocycloalkyl; R3 is alkyl or —CH2OH; and R4 is H or alkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

    摘要翻译： 其中R1是任选取代的环烷基，环烷基烷基，芳基，芳基烷基或杂芳基; R2是H，烷基或任意取代的环烷基 环烷基烷基，杂环烷基，桥连环烷基或桥连杂环烷基; R3是烷基或-CH2OH; 和R 4是H或烷基;是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。

    Aspartyl protease inhibitors
    69.
    发明授权
    Aspartyl protease inhibitors 失效
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：US07560451B2

    公开(公告)日：2009-07-14

    申请号：US11589387

    申请日：2006-10-30

    申请人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    发明人： Zhaoning Zhu ,  Andrew W. Stamford ,  Brian McKittrick

    IPC分类号： C07D411/04 ,  A61K31/553

    CPC分类号： C07D413/04 ,  C07F9/65848

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中W，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D 和原生动物酶。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合来治疗认知或神经变性疾病的方法。