PIPERIDINYL-AND PIPERAZINYL-SULFONYLMETHYL HYDROXAMIC ACID AND THEIR USE AS PROTEASE INHIBITORS

PIPERIDINYL-AND PIPERAZINYL-SULFONYLMETHYL HYDROXAMIC ACID AND THEIR USE AS PROTEASE INHIBITORS

This invention is directed generally to proteinase (also known as "protease") inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as "matrix metalloprotease" or "MM...

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Hauptverfasser: MISCHKE, DEBORAH, A, MASSA, MARK, BEDELL, LOUIS, J, GRAPPERHAUS, MARGARET, BECKER, DANIEL, P, FRESKOS, JOHN, N, BOEHM, TERRI, L, BROWN, DAVID, L, FOBIAN, YVETTE, BARTA, THOMAS, E, HOCKERMAN, SUSAN, L, HEINTZ, ROBERT, M, CHEN, YIYUAN, GASIECKI, ALAN, F, MISCHKE, BRENT, V, KOLODZIEJ, STEPHEN, A, KHANNA, ISH, KUMAR, KASSAB, DARREN, J, MCDONALD, JOSEPH, CARROLL, JEFFERY, N
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:This invention is directed generally to proteinase (also known as "protease") inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as "matrix metalloprotease" or "MMP") activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.