Merck Frosst Canada & Co.

Merck Frosst Canada, Inc.

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Merck Forsst Canada & Co.

Merck Canada Inc.

Richard W Friesen

Daniel Dube

Rejean Fortin

Yves Ducharme

Richard Frenette

Yves Girard

Zhaoyin Wang

Jacques Yves Gauthier

Pierre A Hamel

Erich L Grimm

Sebastien Laliberte

Daniel Guay

Marc Gagnon

Marc Blouin

Mario Girard

Daniel Delorme

Yves Gareau

Bernard Cote

Helene Juteau

Chun Li

Sylvie Desmarais

Carole Lepine

Robert J Zamboni

Denis Deschenes

Andre Giroux

Evelyn Martins

Sylvie Prescott

Bruce MacKay

Cedrickx Godbout

Anh Chau

Hongping Yu

Tom Wu

Robert N Young

Yves Leblanc

Patrick Roy

Claude Dufresne

Brian P Kennedy

Laird A Trimble

Anthony Ford-Hutchinson

Helene Perrier

Nathalie Chauret

D Bruce MacKay

Michael Gresser

Yvbes Ducharme

Daaniel Guay

Don Nicholson

Chidambaran Ramachandran

Kathryn Skorey

Daniel Dube'

Daniel Dub E

Annette Robichoud

Bruce Mackay

The instant invention provides compounds of Formula I which are leukotriene biosynthesis inhibitors. Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

Pharmaceutical phenylquinoline and chromen-2-one triazole compounds

The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.

2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors

The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors. Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.

Pharmaceutical compounds

The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents. 

7-(1,3-thiazol-2-YL)thio-coumarin derivatives and their use as leukotriene biosynthesis inhibitors

The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.  The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.

Substituted pyridines as selective cyclooxygenase-2 inhibitors

Alkyne-aryl phosphodiesterase-4 inhibitors

1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors

A PDE4 inhibiting compound is represented by

Fluoroalkoxy-substituted benzamide dichloropyridinyl N-oxide PDE4 inhibitor

Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, &mdash;SH (or &mdash;S ), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including caspases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compounds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.

Ligands for phosphatase binding assay

The invention encompasses compounds of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3&prime;,5&prime;-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV).

PDE IV inhibiting compounds, compositions and methods of treatment

The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3&prime;,5&prime;-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4).

Heterosubstituted pyridine derivatives as PDE4 inhibitors

Heterosubstituted pyridine derivatives as PDE 4 inhibitors

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Richard W Friesen