Merck Frosst Canada, Inc.

Other

Merck + Co., Inc.

Actelion Pharmaceuticals Ltd

Merck Frosst Canada & Co.

Idorsia Pharmaceuticals Ltd

Dwight Macdonald

Daniel Dube

Patrick Lacombe

Yves Girard

Michel Gallant

Laurence Dube

Denis Deschenes

Renee Aspiotis

John Howard Hutchinson

Mark T Goulet

Feroze Ujjainwalla

Michel Therien

Richard Frenette

Erich L Grimm

Marc Labelle

Tom Yao-Hsiang Wu

Lin Chu

Claudio F Sturino

Linda L Chang

Guo-Jie Ho

Sebastien Laliberte

Nicolas Lachance

Daniel J McKay

Sophie-Dorothee Clas

David Alan Conlon

D Bruce MacKay

Austin Chih-Yu Chen

Anant Vailaya

Nadine Bremeyer

Elizabeth Kwong

Helene Perrier

Roch Thibert

Pierre-Andre Fournier

Louis-Charles Campeau

Jeremy Peter Scott

Daniel James Mckay

D Bruce Mackay

The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency. 

3,4-substituted piperidine derivatives as renin inhibitors

The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents. 

Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use

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

Novel sulfuric acid, methanesulfonic acid, p-toluenesulfonic acid, 2-naphthalenesulfonic acid, hydrochloride acid, or benzenesulfonic acid salts of substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

Substituted 8-arylquinoline phosphodiesterase-4 inhibitors

PDE IV inhibiting amides, compositions and methods of treatment

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L'lle Bizard, Canada

Dwight Macdonald