Pharmacia Corporation

Jeffrey N Carroll

Gary A DeCrescenzo

John Nicholas Freskos

Daniel Paul Becker

Deborah A Mischke

Joseph J McDonald

Yvette M Fobian

Thomas E Barta

Clara I Villamil

Joseph Gerace Rico

Susan Landis Hockerman

Terri L Boehm

Louis J Bedell

Steve A Kolodziej

John Jeffrey Talley

Daniel P Getman

Michael B Tollefson

Lijuan Jane Wang

Monica B Norton

William F Vernier

Darren J Kassab

Susan C Howard

Nathan W Stehle

Madeleine H Li

This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as 'matrix metalloprotease' or 'MMP') activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Aromatic sulfone hydroxamic acids and their use as protease inhibitors

A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,

Aromatic sulfone hydroxamic acid metalloprotease inhibitor

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Columbia, IL, United States of America

Jeffrey N Carroll