Merck Frosst Canada, Inc.

Merck Frosst Canada & Co.

Actelion Pharmaceuticals Ltd

Merck Canada Inc.

Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Idorsia Pharmaceuticals Ltd

Daniel Dube

Rejean Fortin

Yves Girard

Richard W Friesen

Michel Gallant

Patrick Lacombe

Denis Deschenes

Laurence Dube

Zhaoyin Wang

Jacques Yves Gauthier

Dwight Macdonald

Dwight MacDonald

Tom Yao-Hsiang Wu

Renee Aspiotis

Daniel Delorme

Yves Ducharme

Pierre A Hamel

Erich L Grimm

Sebastien Laliberte

Helene Juteau

Thomas Weller

Michel Therien

John W Gillard

Daniel Bur

Sylvia Richard-Bildstein

Richard Frenette

Patrick Roy

Olivier Corminboeuf

Corinna Grisostomi

Lubos Remen

Marc Blouin

Austin Chen

Olivier Bezencon

Daniel J McKay

Austin Chih-Yu Chen

Anthony Mastracchio

Robert N Young

Christoph Boss

Thierry Sifferlen

Daniel Guay

Walter Fischli

Christopher I Bayly

John Scheigetz

Dan McKay

Laird A Trimble

Chun Li

Helene Perrier

Sylvie Prescott

Nathalie Chauret

Rick Friesen

Daniel McKay

D Bruce MacKay

Carol Lepine

Nadine Bremeyer

Jeremy Peter Scott

David A Powell

David Powell

Yvbes Ducharme

Louis-Charles Campeau

Erich I Grimm

Pierre-Andre Fournier

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 present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.

Case of renin inhibitors

The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.

Renin inhibitors

The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency. 

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. 

The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.

Secondary amines as renin inhibitors

The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.

Piperidine carboxylic acid amide derivatives

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

This invention encompasses a method for treating a prostaglandin E mediated disease or condition comprising administering to a mammalian patient in need of such treatment a compound of Formula (A) in an amount that is effective to treat the prostaglandin E mediated disease or condition 

Quinolinones as prostaglandin receptor ligands

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

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

8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R-Rand Ar are as in claim

Substituted 8-arylquinolune PDE4 inhibitors

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Daniel Dube