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    • 7. 发明授权
    • Aspartyl protease inhibitors
    • 天冬氨酰蛋白酶抑制剂
    • US07560451B2
    • 2009-07-14
    • US11589387
    • 2006-10-30
    • Zhaoning ZhuAndrew W. StamfordBrian McKittrick
    • Zhaoning ZhuAndrew W. StamfordBrian McKittrick
    • C07D411/04A61K31/553
    • C07D413/04C07F9/65848
    • 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.
    • 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。