Merck Sharp + Dohme Corp.

Pharmacopeia Drug Discovery, Inc.

Pharmacopeia Inc.

Johannes H Voight

Andrew William Stamford

Jared N Cumming

Tao Guo

Ying Huang

Corey Strickland

Ulrich Iserloh

Suresh D Babu

Yusheng Wu

Kurt William Saionz

William J Greenlee

Zhaoning Zhu

Brian Alexander McKittrick

Elizabeth M Smith

Guoqing Li

Robert D Mazzola, Jr

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

Dawit Tadesse

Gaifa Lai

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Samuel Chackalamannil

Yan Xia

Douglas Walsh Hobbs

Thuy X H Le

Thuy X E Le

Jeffrey H Lowrie

Xiaoiang Liu

Xiaoxiang Liu

Thuy Xe Le

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein  and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amide BACE-1 inhibitors having a benzamide substituent

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 or a pharmaceutically acceptable salt or solvate thereof, wherein Ris  R is &#x2014;C(O)&#x2014;N(R)(R) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amine BACE-1 inhibitors having a benzamide substituent

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Cranford, NJ, United States of America

Johannes H Voight