Merck Sharp + Dohme Corp.

Pharmacopeia Inc.

Schering Corporation

Ligand Pharmaceuticals, Inc.

Pharmacopeia Drug Discovery, Inc.

Jingqi Duo

Suresh D Babu

Kurt William Saionz

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

Robert D Mazzola, Jr

Yusheng Wu

Lingyan Wang

Zhong-Yue Sun

John P Caldwell

Jianping Pan

Yuanzan C Ye

Rachael Catherine Hunter

Yuefei Shao

Michelle Lee Morris

Gang Qian

Huizhong Gu

Gaifa Lai

Dawit Tadesse

Jeffrey A Misiaszek

Chuanxing Qu

Johannes H Voight

Thuy X E Le

Xiaoxiang Liu

Xiaoiang Liu

Koc-Kan Ho

Brian F McGuinness

Johannes H Voigt

Thuy X H Le

Guizhen Dong

Thuy Xe Le

Rachael C Hunter

Michelle L Morris

Jr Robert D Mazzola

Brian Mckittrick

Thuy X Le

Robert D Mazzola

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

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 

Biaryl oxyacetic acid compounds

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

Jingqi Duo