Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula Ior 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.
Pharmacopeia Inc. Merck Sharp & Dohme Corp.
C A A C A A C A A A A A C C C C A A C C A C C A
C07D A61K A61K C07D A61P A61P C07D A61P A61P A61P A61P A61P C07D C07D C07D C07D A61P A61P C07D C07D A61P C07D C07D A61P
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Brian Zhaoning Gaifa Xiaoiang Dawit Jeffrey A. Guoqing Johannes H. Jianping Corey O. Thuy X.E. Yuanzan C. William J. Jared N. Jingqi Elizabeth M. Andrew W. Rachael C. Zhong-Yue John P. Gang Chuanxing Yusheng Ulrich Tao Robert D. Kurt W. Yuefei Michelle L. Ying Lingyan Suresh D. Huizhong
McKittrick Zhu Lai Liu Tadesse Misiaszek Li Voight Pan Strickland Le Ye Greenlee Cumming Duo Smith Stamford Hunter Sun Caldwell Qian Qu Wu Iserloh Guo Mazzola, Jr. Saionz Shao Morris Huang Wang Babu Gu