Merck + Co., Inc.

Peter M Munson

Wayne J Thompson

David A Claremon

John A McCauley

Nigel J Liverton

John W Butcher

Brian T Phillips

Christopher F Claiborne

Ian M Bell

Charles J McIntyre

Brian E Libby

Kevin T Nguyen

Willie Whitter

Joseph P Vacca

Janusz Jozef Kulagowski

Steven D Young

Mark E Layton

Philip E Sanderson

Joseph J Romano

James P Guare

Richard W Ransom

Ian Thomas Huscroft

Michael F Sugrue

Pierre J Mallorga

Daria Jean Hazuda

Christine Dieckhaus

Wayne J Thomspon

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

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

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

Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Benzodiazepine hydrazide derivatives as inhibitors of HIV integrase

This invention is concerned with novel 1-�cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.

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Harleysville, PA, United States of America

Peter M Munson