Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Wayne J Thompson

David A Claremon

Peter M Munson

Nigel J Liverton

John A McCauley

Christopher F Claiborne

Ian M Bell

John W Butcher

Brian T Phillips

William H Parsons

Frank Kayser

Kathleen M Rupprecht

Jianming Bao

Andrew Kotliar

Richard W Ransom

Michael F Sugrue

Pierre J Mallorga

Robert K Baker

Joel R Huff

Charles J McIntyre

Anthony M Smith

Brian E Libby

Kevin T Nguyen

Willie Whitter

Joseph P Vacca

Janusz Jozef Kulagowski

Byron H Arison

John S Wai

Peter D Williams

Steven D Young

Mark E Layton

Shankar Venkatraman

Philip E Sanderson

Dai-Shi Su

Terry A Lyle

Mark W Embrey

Peter Emmanuel Maligres

Zhiguo Jake Song

Shouwu Miao

Russell B Lingham

Joseph J Romano

Maria L Garcia

Thorsten E Fisher

Gregory J Kaczorowski

James P Guare

Laszlo R Treiber

Susan F Britcher

Tao Pei

Suresh K Balani

Sandor L Varga

Ian Thomas Huscroft

Jingjun Yin

David C Dubost

Georgette Dezeny

Lawrence F Colwell, Jr

Daria Jean Hazuda

Neil A Strotman

Jeffrey Melamed

Michael Shevlin

Jennie B Nerenberg

Richard C A Isaacs

Richard G Ball

Matthew L Maddess

Dietrich P Steinhuebel

Christine Dieckhaus

Gabriel F Eilon

Eric J Choi

Jennifer Chee

Sarah L Trice

Hee Y Lee

Neil Campbell

Arun K Ghosh

Hee-Yoon Lee

William A Schmalhofer

Chou Juitsai Liu

Matthew Maddess

John A Mccauley

Brian Phillips

Jeffrey Y Melamed

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which prokineticin receptors are involved.

Morpholine carboxamide prokineticin receptor antagonists

Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke, and other conditions. 

4-cycloakylaminopyrazolo pyrimidine NMDA/NR2B antagonists

Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists

Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain 

N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists

The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Carbocyclic potassium channel inhibitors

4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C -C alkyl, C -C alkenyl, C -C alkynyl, C -C alkoxy, amino, aminoC -C alkyl, hydroxyC -C alkyl, carbonyl, cycloC -C alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.

2-cyclohexyl imidazopyridine NMDA/NR2B antagonists

Novel 2-aza-bicyclo&lsqb;2.2.2&rsqb;octanes substituted in the 2-position are effective as NMDA NR2B antagonists useful for relieving pain.

2-aza-bicyclo&lsqb;2.2.2&rsqb;octane NMDA/NR2B antigonists

Novel piperidinyl compounds substituted in the 1- and 4-positions are effective as NMDA NR2B antagonists useful for relieving pain.

1,4 substituted piperidinyl NMDA/NR2B antagonists

Novel 3-substituted 8-aza-bicyclo&lsqb;3.2.1&rsqb;octanes (commonly known as &ldquo;tropanes&rdquo;) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.

8-aza-bicyclo&lsqb;3.2.1&rsqb;octane NMDA/NR2B antagonists

4-substituted cyclohexanes substituted in the 1-position with quinazoline either directly or through a C -C alkyl, C -C alkenyl, C -C alkynyl, C -C alkoxy, amino, aminoC -C alkyl, hydroxyC -C alkyl, carbonyl, cycloC -C alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.

2-cyclohexyl quinazoline NMDA/NR2B antagonists

Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.

5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists

The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Heterocyclic potassium channel inhibitors

Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C,-C,alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.

2-cyclohexyl benzimidazole NMDA/NR2B antagonists

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Lansdale, PA, United States of America

Wayne J Thompson