发明申请
- 专利标题: HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
- 专利标题(中): 异源ASPARTYL蛋白酶抑制剂
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申请号: US13420007申请日: 2012-03-14
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公开(公告)号: US20120276118A1公开(公告)日: 2012-11-01
- 发明人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mazzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
- 申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mazzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
- 申请人地址: US CA La Jolla US NJ Rahway
- 专利权人: Pharmacopeia Inc.,Schering Corporation
- 当前专利权人: Pharmacopeia Inc.,Schering Corporation
- 当前专利权人地址: US CA La Jolla US NJ Rahway
- 主分类号: A61K39/395
- IPC分类号: A61K39/395
摘要:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods 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 m1 agonist or m2 antagonist.
公开/授权文献
- US08829036B2 Heterocyclic aspartyl protease inhibitors 公开/授权日:2014-09-09