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