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