Warner-Lambert Company

Joseph Armand Picard

Drago R Sliskovic

Patrick Michael O'Brien

Bruce D Roth

Helen Tsenwhei Lee

Andrew David White

William Howard Roark

Claude Forsey Purchase, Jr

Michael William Wilson

William Chester Patt

Amy Mae Bunker

Linda Lea Johnson

Donald John Hupe

Qi-Zhuang Ye

Wendell Wierenga

Daniel Fred Ortwine

Bernard Gaudilliere

Randy Ranjee Ramharack

Nicole Chantel Barvian

Henri Jacobelli

Kevon Ray Shuler

William Glen Harter

James Lester Hicks

Ly Pham

Christopher Alan Conrad

This invention provides compounds defined by Formula IR-Q-D-(V)&#x2014;RI

Monocyclic derivatives as matrix metalloproteinase inhibitors

This invention provides compounds defined by Formula Ior a pharmaceutically acceptable salt thereof,wherein R, Q, Y, R, R, R, R, and n are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.

Azaisoquinoline derivatives as matrix metalloproteinase inhibitors

A compound selected from those of formula (I):

Alkynylated quinazoline compounds

The present invention provides compounds of Formula (I) wherein Q, Q, Q, Q, Y, Y, and Z are as defined in the description, and pharmaceutically acceptable salts thereof, and C-Calkyl esters thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of Formula (I) and their pharmaceuticalyl acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

6,5-Fused bicyclic heterocycles

The present invention provides compounds of formula (I) wherein R, Z, Y, W, R, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

1,2,4-tribsubstituted benzenes as inhibitors of 15-lipoxygenase

The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.

Method of inhibiting matrix metalloproteinases

Phenylene alkyne matrix metalloproteinase inhibitors

Pyrimidinone fused bicyclic metalloproteinase inhibitors

Hydroxamic acid compounds useful as matrix metalloproteinase inhibitors

Benzo thiadiazine matrix metalloproteinase inhibitors

Matrix metalloproteinase inhibitors and their therapeutic uses

Sulfonamide matrix metalloproteinase inhibitors

Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Tricyclic sulfonamides and their derivatives as inhibitors of matrix metalloproteinases

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Canton, MI, United States of America

Joseph Armand Picard