Reverse hydroxamic acid derivatives

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 317/40 (2006.01) A61K 31/165 (2006.01) A61K 31/357 (2006.01) A61K 31/435 (2006.01) A61K 31/47 (2006.01) A61K 31/4709 (2006.01) A61K 31/496 (2006.01) A61K 31/55 (2006.01) A61P 1/14 (2006.01) A61P 1/16 (2006.01) A61P 3/10 (2006.01) A61P 7/06 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) A61P 11/02 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 17/00 (2006.01) A61P 19/02 (2006.01) A61P 19/08 (2006.01) A61P 21/00 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01) A61P 37

Patent

CA 2459380

Reverse hydroxamic acid derivatives having specific structure represented by a general formula (Ia): (see formula Ia) (wherein A is a hydrogen atom or the like; Ar1 is an arylene or the like; Ar2 is an optionally substituted aryl, a heteroaryl or the like; R1 is a hydrogen atom, an alkyl or the like; R2a is a substituted cycloaryl, a heterocycloaryl or the like) and a general formula (I): (see formula I) (wherein A, Ar1, Ar2, and R1 are the same as defined above and R2 is an hydrogen atom, R2a or the like) and salts thereof, which have TNF-.alpha. converting enzyme (TACE) inhibitory activity.

L'invention concerne des dérivés d'acide hydroxamique inverse présentant des structures spécifiques représentées par la formule générale (Ia) : (Ia) (dans laquelle A représente l'hydrogène etc., Ar?1¿ représente l'arylène etc., Ar?2¿ représente l'aryle, l'hétéroaryle éventuellement substitués etc., et R?2a¿ représente le cycloalkyle, l'hétérocycloalkyle substitués etc.) et la formule générale (I) : (I) (dans laquelle A, Ar?1¿, Ar?2¿ et R?1¿ sont tels que défini ci-dessus, et R?2 ¿représente l'hydrogène, R?2a¿ etc.) ainsi que les sels de ces dérivés. Ces dérivés exercent une activité inhibitrice sur l'enzyme de conversion du TNF-.alpha. (TACE).

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