Merck + Co., Inc.

Other

Janssen Pharmaceutica Nv

Evotec Oai

William H Parsons

Kathleen M Rupprecht

Robert K Baker

Jianming Bao

Frank Kayser

Arthur A Patchett

Peter J Sinclair

Matthew J Wyvratt

Prasun K Chakravarty

Frederick Wong

Mark T Goulet

William R Schoen

Shouwu Miao

William J Greenlee

David A Claremon

Nigel J Liverton

Christopher F Claiborne

Wayne J Thompson

Hyun O Ok

Min K Park

Robert M Burk

Sander G Mills

Tesfaye Biftu

Michael H Fisher

Mark R Player

John J Acton, Iii

Eugene D Thorsett

Carl R Illig

Lihu Yang

Mitree M Ponpipom

Peter T Meinke

Robert L Bugianesi

Maria L Garcia

Alexander Pasternak

Stephen Colin Price

Scott L Dax

Ann E Weber

Mark Andrew Youngman

Sanath K Meegalla

Jian Liu

Jinsheng Chen

Edward Andrew Boyd

Gabor Butora

Richard J Bochis

Shelley K Ballentine

Andrew Kotliar

Joung L Goulet

Bishan Zhou

Brenda L Palucki

Masao Taniguchi

Helen M Organ

Gregory J Kaczorowski

Dennis M Zaller

Sriram Tyagarajan

Narindar N Girotra

Gregory D Berger

James D Bergstrom

Wing S Cheung

Sharmila Patel

Mark A Holmes

Louis L Zuegner, Iii, Legal Representative

Jennifer Chee

Lori L Whiting

Alan D Adams

Daniel J Parks

David Taub

Kenneth M Wells

Daljit S Dhanoa

Michele C Jetter

Yuan-Ching P Chiang

Raymond S Chang

Conrad Santini

A Brian Jones

Shawn T Branum

Julianne A Hunt

Raul R Calvo

Gerard R Kieczykowski

Claude Dufresne

Lloyd W Hillman

Chan-Hwa Kuo

Wenxi Pan

Jeffrey Donald Hermes

Rosemary Sisco

Scott Ballentine

Helen M Armstrong

Yu-Kai Lee

Richard Beresis

Christopher B Forbes

Xingfang Hong

Michael Richard Brandt

Robert W Marquis, Jr

Derek A Beauchamp

Howard C H Kuo

William A Schmalhofer

Chou Juitsai Liu

Mark G Steiner

Jill N Johanson

Thomas A Halgren

Jeffrey M Fisher, Legal Representative

The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.

Benzimidazole modulators of VR1

Benzimidazole TRPV1 inhibitors

Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.

Biaryl substituted pyrazoles as sodium channel blockers

Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Biaryl substituted triazoles as sodium channel blockers

Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

Substituted triazoles as sodium channel blockers

This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

Ophthalmic compositions for treating ocular hypertension

Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds and a pharmaceutically acceptable carrier, and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as initable bowel syndrome, Cnohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar depression, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are described.

Aryl-link-aryl substituted thiazolidine-dione and oxazolidine-dione as sodium channel blockers

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

Cyclopentyl modulators of chemokine receptor activity

Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.

Src kinase inhibitor compounds

3-alkyl substituted pyrrolidine modulators of chemokine receptor activity

4-alkyl piperidinyl pyrrolidine modulators of chemokine receptor activity

Pyrrolidine modulators of chemokine receptor activity

3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity

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Belle Mead, NJ, United States of America

William H Parsons