C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 417/14 (2006.01) A61K 31/445 (2006.01) A61K 31/4523 (2006.01) A61K 31/4535 (2006.01) A61K 31/4545 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/497 (2006.01) A61K 31/501 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61P 35/00 (2006.01) C07D 211/66 (2006.01) C07D 211/96 (2006.01) C07D 213/74 (2006.01) C07D 309/08 (2006.01) C07D 335/02 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/04 (2006.01) C07D 405/06 (2006.01) C07
Patent
CA 2483314
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 formula (I), (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.
L'invention concerne des inhibiteurs de protéase, et plus particulièrement des acides pipéridinylsulfonylméthylhydroxamiques et pipérazinylsulfonylméthylhydroxamiques qui, entre autres, inhibent l'activité de métalloprotéases matricielles (MMP) et/ou l'activité d'aggrécanase. Lesdits acides hydroxamiques sont généralement représentés par la formule développée (I), (dans laquelle A?1¿, A?2¿, Y, E?1¿, E?2¿, E?3¿, et R?x¿ ont la signification indiquée dans la description), et comprennent, entre autres, des sels desdits composés. L'invention concerne également des compositions desdits acides hydroxamiques, des intermédiaires pour la synthèse de ces derniers, des procédés pour produire lesdits acides hydroxamiques, ainsi que des méthodes pour traiter des états (notamment des états pathologiques) associés à l'activité des MMP et/ou de l'aggrécanase.
Barta Thomas E.
Becker Daniel P.
Bedell Louis J.
Boehm Terri L.
Brown David L.
Osler Hoskin & Harcourt Llp
Pharmacia Corporation
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