Inventors:
Kevin Chapman - Scotch Plains NJ
William Hagmann - Westfield NJ
Philippe Durette - New Providence NJ
Craig Esser - Belford NJ
Ihor Kopka - Millburn NJ
Charles Caldwell - Scotch Plains NJ
Assignee:
Merck & Co., Inc. - Rahway NJ
International Classification:
A61K 3702
C07C25906
C07C23752
C07D27762
Abstract:
Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##.