Warner-lambert Company

Bristol-myers Squibb Compnay

Amy Mae Bunker

Jeremy John Edmunds

Joseph Thomas Repine

Annette Marian Doherty

Chitase Lee

Xue-min Cheng

Richard William Skeean

Gerald David Kanter

Joseph Armand Picard

Annette M Doherty

Patrick Michael O'Brien

Kent A Berryman

Drago R Sliskovic

Makonen Belema

Alain Martel

Van N Nguyen

William Howard Roark

Michael William Wilson

Anne Marinier

Yuping Qiu

Francis Beaulieu

Yunhui Zhang

Carl Ouellet

Stephan Roy

Xuejie Yang

William Glen Harter

James Lester Hicks

Mark Anthony Morris

Christopher Zusi

Ly Pham

Patrick Michael O'brien

This invention provides compounds defined by Formula I and pharmaceutically acceptable salts thereof,and pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of treating osteo- and rheumatoid arthritis.

Hetero biaryl 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

This invention provides compounds defined by Formula I:or a pharmaceutically acceptable salt thereof,wherein R, Q, 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.

3-isoquinolinone derivatives as matrix metalloproteinase inhibitors

Compounds having the formula (I),and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, are useful as anti-inflammatory agents, in which R, R, and Rare hydrogen, halogen, alkyl, or perfluoroalkyl; Ris an optionally substituted alkyl or cycloalkyl group; X is a linker; A is an aryl, heteroaryl, heterocycle, cycloalkyl, or is absent; and Ris a substituent on A as defined in the specification.

Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same

Phenylene alkyne matrix metalloproteinase inhibitors

Certain benzothiazine dioxide endothelin antagonists and processes for their preparation

The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1

Novel benzothiazine dioxides which are antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation, and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.

Benzothiazine dioxides as endothelin antagonists

Novel indole and indoline nonpeptide antagonists of endothelin I are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure and subarachnoid hemorrhage.

Nonpeptide endothelin antagonists

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Ann Arbor, MI, United States of America

Amy Mae Bunker