- 专利标题: Heterocyclic aspartyl protease inhibitors
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申请号: US11710582申请日: 2007-02-23
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公开(公告)号: US20080200445A1公开(公告)日: 2008-08-21
- 发明人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
- 申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
- 专利权人: Schering Corporation & Pharmacopeia Drug Discovery, Inc.
- 当前专利权人: Schering Corporation & Pharmacopeia Drug Discovery, Inc.
- 主分类号: A61K31/506
- IPC分类号: A61K31/506 ; A61K31/4178 ; A61K31/4245 ; A61K31/4439 ; A61K31/454 ; A61K31/541 ; A61P31/00 ; C07D233/02 ; C07D271/00 ; C07D413/14 ; C07D409/14 ; C07D409/04 ; C07D403/06 ; C07D401/14 ; C07D401/12 ; C07D401/10 ; C07D401/06 ; C07D239/04 ; A61P9/00 ; A61P25/00 ; A61K31/5377 ; A61K31/4545 ; A61K31/4709 ; A61K31/498
摘要:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula 1. 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 m1 agonist or m2 antagonist.
公开/授权文献
- US07763609B2 Heterocyclic aspartyl protease inhibitors 公开/授权日:2010-07-27