Merck + Co., Inc.

Merial Limited

Evotec Oai

Michael H Fisher

Matthew J Wyvratt

Helmut H Mrozik

Ann E Weber

Mark T Goulet

Peter T Meinke

Hyun O Ok

Thomas L Shih

Lin Chu

William R Schoen

Wallace T Ashton

John C Chabala

Arthur A Patchett

Richard L Tolman

Emma R Parmee

Mitree M Ponpipom

Peter Lin

Elizabeth M Naylor

Tesfaye Biftu

Edward J Grabowski

Danqing D Feng

Richard J Bochis

Thomas R Beattie

Robert Joseph Devita

Bruce O Linn

Gui-Bai Liang

Narindar N Girotra

William V Ruyle

Jan Ten Broeke

Lars M Flataker

Thomas F Walsh

William H Parsons

Prasun K Chakravarty

Scott D Edmondson

Byron H Arison

Steven L Colletti

Malcolm Maccoss

Dooseop Kim

Jonathan R Young

XiaoXia Qian

Robert L Bugianesi

Jinyou Xu

Peter Kulsa

Sriram Tyagarajan

Ching C Wang

Burton G Christensen

Stephen Colin Price

Edward Andrew Boyd

Richard Berger

Dennis M Schmatz

Maria L Garcia

Gregory J Kaczorowski

Mu T Wu

Roy G Smith

Robert J Mathvink

Chan-Hwa Kuo

Bishan Zhou

Dale R Hoff

Aino Lusi

Tesfaye Bitfu

Dong Ok

Yi Tien Yang

Howard C H Kuo

George B Smith

Thomas M Jacks

Jeffrey M Fisher, Legal Representative

John Stibbard

Helmut Mrozik

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

Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s). 

Antiprotozoal imidazopyridine compounds

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

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ('DP-IV inhibitors') and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (&ldquo;DP-IV inhibitors&rdquo;) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

C1 to C4 side chain modified nodulisporic acid analogs

Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.

Aliphatic hydroxy substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents

Nonacyclic nodulisporic acid derivatives

Diaryl piperidyl pyrrole derivatives as antiprotozoal agents

Nodulisporic acid derivatives

There are disclosed compounds of formula (I)

Antagonists of gonadotropin releasing hormone

There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Oxadiazole benzenesulfonamides as selective .beta..sub.3 Agonist for the

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Ringoes, NJ, United States of America

Michael H Fisher