Heterocyclic aspartyl protease inhibitors

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 i...

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Hauptverfasser: GU HUIZHONG, LIU XIAOIANG, TADESSE DAWIT, VOIGHT JOHANNES H, GUO TAO, WU YUSHENG, DUO JINGQI, SUN ZHONG-YUE, ZHU ZHAONING, SAIONZ KURT W, SHAO YUEFEI, LE THUY X.E, STAMFORD ANDREW W, HUNTER RACHAEL C, MISIASZEK JEFFREY A, LAI GAIFA, CUMMING JARED N, HUANG YING, MAZZOLA, JR. ROBERT D, PAN JIANPING, CALDWELL JOHN P, ISERLOH ULRICH, BABU SURESH D, GREENLEE WILLIAM J, SMITH ELIZABETH M, MORRIS MICHELLE L, MCKITTRICK BRIAN, QIAN GANG, LI GUOQING, QU CHUANXING, STRICKLAND COREY O, YE YUANZAN C, WANG LINGYAN
Format: Patent
Sprache:eng
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Zusammenfassung: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.