发明名称 HETEROCYCLIC ASPARTYL PROTEASE INHIBITOR
摘要 <P>PROBLEM TO BE SOLVED: To provide heterocyclic aspartyl protease inhibitors, pharmaceutical compositions comprising the compounds, their use in the treatment of cardiovascular diseases, cognitive and neurodegenerative diseases, and their use as inhibitors of the Human Immunodeficiency Virus, plasmepsins, cathepsin D and protozoal enzymes. <P>SOLUTION: Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof; 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. <P>COPYRIGHT: (C)2013,JPO&INPIT
申请公布号 JP2013014628(A) 申请公布日期 2013.01.24
申请号 JP20120232894 申请日期 2012.10.22
申请人 MERCK SHARP & DOHME CORP;PHARMACOPEIA LLC 发明人 ZHU ZHAONING;MCKITTRICK BRIAN;SUN ZHONG-YUE;YE YUANZAN C;VOIGT JOHANNES H;STRICKLAND COREY;SMITH ELIZABETH M;STAMFORD ANDREW;GREENLEE WILLIAM J;MAZZOLA JR ROBERT D;CALDWELL JOHN;CUMMING JARED N;WANG LINGYAN;WU YUSHENG;ISERLOH ULRICH;LIU XIAOXIANG;HUANG YING;LI GUOQING;PAN JIANPING;MISIASZEK JEFFREY A;GUO TAO;LE THUY X H;SAIONZ KURT W;BABU SURESH D;HUNTER RACHAEL C;MORRIS MICHELLE L;GU HUIZHONG;QIAN GANG;TADESSE DAWIT;LAI GAIFA;DUO JINGQI;QU CHUANXING;SHAO YUEFEI
分类号 C07D233/88;A61K31/121;A61K31/13;A61K31/192;A61K31/22;A61K31/366;A61K31/40;A61K31/404;A61K31/4168;A61K31/4178;A61K31/421;A61K31/422;A61K31/427;A61K31/4439;A61K31/454;A61K31/496;A61K31/498;A61K31/505;A61K31/513;A61K31/527;A61K31/5377;A61K31/5395;A61K31/541;A61K31/551;A61K31/695;A61K45/00;A61P9/00;A61P25/28;A61P29/00;A61P31/18;A61P33/02;A61P43/00;C07D239/22;C07D239/26;C07D239/70;C07D243/04;C07D263/28;C07D273/04;C07D401/04;C07D401/06;C07D401/10;C07D401/12;C07D401/14;C07D403/04;C07D403/06;C07D403/08;C07D403/10;C07D403/12;C07D403/14;C07D405/04;C07D405/06;C07D405/10;C07D405/12;C07D405/14;C07D409/04;C07D409/06;C07D409/14;C07D413/04;C07D413/14;C07D417/04;C07D417/10;C07D417/12;C07D417/14;C07D471/04;C07D491/107;C07D495/04;C07D495/10;C07F7/10 主分类号 C07D233/88
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