Merck Sharp + Dohme Corp.

Pharmacopeia Inc.

Schering Corporation

Pharmacopeia Drug Discovery, Inc.

Thuy X E Le

William J Greenlee

Andrew William Stamford

Jared N Cumming

Zhaoning Zhu

Brian Alexander McKittrick

Tao Guo

Elizabeth M Smith

Ying Huang

Corey Strickland

Ulrich Iserloh

Guoqing Li

Suresh D Babu

Yusheng Wu

Robert D Mazzola, Jr

Lingyan Wang

Zhong-Yue Sun

Kurt William Saionz

John P Caldwell

Jianping Pan

Yuanzan C Ye

Yuefei Shao

Rachael Catherine Hunter

Michelle Lee Morris

Gang Qian

Huizhong Gu

Dawit Tadesse

Gaifa Lai

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Xiaoxiang Liu

Johannes H Voight

Johannes H Voigt

Xiaoiang Liu

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 magonist or mantagonist.

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 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 magonist or mantagonist.

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Also disclosed is the method 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 magonist or mantagonist.

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Monmouth Junction, NJ, United States of America

Thuy X E Le