发明公开
- 专利标题: THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
- 专利标题(中): 生产和化合物的蛋白酶抑制剂的用途
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申请号: EP06772948.3申请日: 2006-06-12
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公开(公告)号: EP1896406A2公开(公告)日: 2008-03-12
- 发明人: MCKITTRICK, Brian , ZHU, Zhaoning , STAMFORD, Andrew
- 申请人: Schering Corporation
- 申请人地址: 2000 Galloping Hill Road Kenilworth, NJ 07033-0530 US
- 专利权人: Schering Corporation
- 当前专利权人: Schering Corporation
- 当前专利权人地址: 2000 Galloping Hill Road Kenilworth, NJ 07033-0530 US
- 代理机构: Adams, Harvey Vaughan John
- 优先权: US690543P 20050614
- 国际公布: WO2006138230 20061228
- 主分类号: C07D205/06
- IPC分类号: C07D205/06
摘要:
Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is -C(R3 R4)-; Y is -N(R5)-; Z is -C(=N-R5’)-; and R1, R2, R3, and R4 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.
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