Merck Frosst Canada & Co.

Merck Frosst Canada, Inc.

Merck Sharp + Dohme Corp.

Actelion Pharmaceuticals Ltd

Merck Canada Inc.

Idorsia Pharmaceuticals Ltd

Patrick Lacombe

Daniel Dube

Michel Gallant

Laurence Dube

Yves Girard

Denis Deschenes

Dwight Macdonald

Renee Aspiotis

Dwight MacDonald

Marc Labelle

Rejean Ruel

Erich L Grimm

Tom Yao-Hsiang Wu

Daniel J McKay

Anthony Mastracchio

Zhaoyin Wang

Rejean Fortin

Daniel Guay

Joseph G Atkinson

Claude Dufresne

Patrick Roy

Claudio F Sturino

Christopher I Bayly

Carl Berthelette

Austin Chen

Sebastien Laliberte

Lianhai Li

Helene Juteau

Helene Perrier

Daniel McKay

D Bruce MacKay

Austin Chih-Yu Chen

Jeremy Peter Scott

Pierre-Andre Fournier

Louis-Charles Campeau

David A Powell

Nadine Bremeyer

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 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 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 encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases, Formula (I). The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula 1. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events. 

Nitric oxide releasing prodrugs of diaryl-2-(5H)-furanones as cyclooxygenase-2 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

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

Novel 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

Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment

The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a non-toxic therapeutically effective amount of compound of Formula II, and the like.

Biphenylene lactams as prostaglandin receptor ligands

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Montreal, Canada

Patrick Lacombe