Merck Frosst Canada, Inc.

Bristol-myers Squibb Compnay

Universitéde Montreal

Merck Canada Inc.

Laurence Dube

Daniel Dube

Michel Gallant

Patrick Lacombe

Dwight Macdonald

R Michael Lawrence

Edward H Ruediger

Yves Girard

Shoshana L Posy

Daniel H Deon

Jacques Banville

Eldon Scott Priestley

Michael Matthew Miller

Marc Gagnon

Roger Remillard

Denis Deschenes

Pancras C Wong

Brad D Maxwell

Julia Guy

Renee Aspiotis

Dwight MacDonald

Erich L Grimm

Christopher I Bayly

Austin Chen

Daniel J McKay

David A Powell

The present invention provides thiazole compounds of Formula I wherein W, Y, R, R, R, R, R, R, X, X, Xand Xare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor4 (PAR4) inhibitors for treating platelet aggregation

The present invention provides thiazole compounds of Formula I wherein W, Y, R, R, R, R, R, R, X, X, Xand Xare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders. 

Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation

The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency. 

Renin inhibitors

Novel substituted 8-phenylquinolines represented by Formula (I), wherein the phenyl group at the 8-position contains an aryl or heteroaryl substituent in the meta position, are PDE4 inhibitors.

8-(3-Biaryl)phenylquinoline phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition 

4-Oxo-1-3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition.

4-oxo-1-(3-substituted phenyl-1,4-dihydro-1,8-naphthyridine-3-carboxamide phosphodiesterase-4 inhibitors

8-(biaryl) quinolines wherein the bi-aryl group at the 8-position is in a meta relationship to the quinoline group, are PDE4 inhibitors useful in the treatment of asthma, chronic bronchitis, chronic obstructive pulmonary disease, eosinophilic granuloma, psoriasis and other benign or malignant proliferative skin diseases, endotoxic shock, laminitis in horses, colic in horses, septic shock, ulcerative colitis, Crohn's disease, reperfusion injury of the myocardium and brain, inflammatory arthritis, chronic glomerulonephritis, atopic dermatitis, urticaria, adult respiratory distress syndrome, chronic obstructive pulmonary disease in animals, diabetes insipidus, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, arterial restenosis, ortherosclerosis, atherosclerosis, neurogenic inflammation, pain, cough, rheumatoid arthritis, ankylosing spondylitis, transplant rejection, graft versus host disease, hypersecretion of gastric acid, bacterial, fungal induced sepsis, viral induced sepsis, fungal induced septic shock, viral induced septic shock, inflammation-mediated chronic tissue degeneration, cytokine-mediated chronic tissue degeneration, osteoarthritis, cancer, cachexia, muscle wasting, depression, memory impairment, tumour growth, or cancerous invasion of normal tissues. In another aspect, the present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and cognition enhancing amount of a phosphodiesterase-4 inhibitor.

8-(biaryl)quinoline PDE4 inhibitors

8-arylquinolines wherein the aryl group at the 8-position contains a meta one or two atom bridge to a phenyl, 5 or 6 member heteroaryl or fused bicyclic heteroaryl group, and wherein at least one of the bridge atoms is not carbon, are PDE4 inhibitors.

Hetero-bridge substituted 8-arylquinoline pde4 inhibitors

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Laval, Canada

Laurence Dube