The Procter Gamble Company

Steven Karl Laughlin

Biswanath De

Michael G Natchus

Michael Philip Clark

Jane Far-Jine Djung

Joshua Spector Tullis

Neil Gregory Almstead

Stanislaw Pikul

Adam Golebiowski

Todd Andrew Brugel

Mark Sabat

Norman Eugene Ohler

Paul Mitchell Hershberger

The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2&#x3b1;]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2&#x3b1;]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.

Bicyclic pyrazolone cytokine inhibitors

Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I):where R, R, R, n, A, E, X, G, G', M and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Heterocyclic side chain containing, n-substituted metalloprotease inhibitors

Isoxazolone compounds having the generic structure:are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.

Isoxazolone compounds useful in treating diseases associated with unwanted cytokine activity

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Taylor Mill, KY, United States of America

Steven Karl Laughlin