Schering Corporation

Pharmacopeia Inc.

Merck Sharp + Dohme Corp.

Pharmacopeia Drug Discovery, Inc.

Gaifa Lai

John J Baldwin

William J Greenlee

Andrew William Stamford

Jared N Cumming

Arthur G Taveras

Zhaoning Zhu

Brian Alexander McKittrick

Tao Guo

Elizabeth M Smith

Ying Huang

Younong Yu

Corey Strickland

Ulrich Iserloh

Guoqing Li

Yusheng Wu

Robert D Mazzola, Jr

Suresh D Babu

Purakkattle J Biju

Lingyan Wang

Jianhua Chao

Kurt William Saionz

John P Caldwell

Zhong-Yue Sun

Yuanzan C Ye

Jianping Pan

Rachael Catherine Hunter

Yuefei Shao

Michelle Lee Morris

Gang Qian

Huizhong Gu

J Robert Merritt

Dawit Tadesse

Jeffrey A Misiaszek

Jingqi Duo

Chuanxing Qu

Ge Li

Cynthia J Aki

Johannes H Voight

Minglang Wu

Thuy X E Le

Michael P Dwyer

Jianping Chao

Xiaoxiang Liu

Johan A Ferreira

Bernd Kaiser

Richard W Bond

Kingsley H Nelson, Jr

Laura L Rokosz

Xiaoiang Liu

Evan A Hecker

Johannes H Voigt

Junying Zheng

Tony Priestley

Thuy X H Le

Daniel Lundell

Jay S Fine

James P Jakway

Thuy Xe Le

Brian Mckittrick

Robert D Mazzola

Thuy X Le

Rachael C Hunter

Michelle L Morris

Jr Robert D Mazzola

Angelo Reggiani

James Jakway

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.

There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

3,4-DI-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

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.

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.

Thiadiazoledioxides and thiadiazoleoxides as CXC- and CC-chemokine receptor ligands

Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.

Isothiazole dioxides as CXC- and CC-chemokine receptor ligands

3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands

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Monmouth Junction, NJ, United States of America

Gaifa Lai