Aromatic sulfone hydroxamic acid metalloprotease inhibitor

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 211/66 (2006.01) A61K 31/351 (2006.01) A61K 31/445 (2006.01) A61K 31/4545 (2006.01) C07D 213/56 (2006.01) C07D 309/08 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2371876

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.

Cette invention a trait à une méthode de traitement consistant à administrer une quantité efficace d'acide hydroxamique aromatique sulfoné, lequel acide fait montre d'une remarquable activité inhibitrice à l'encontre d'une ou de plusieurs enzymes métalloprotéases matricielles (MMP), telles que MMP-2, MMP-9 et MMP-13, tout en exerçant un activité inhibitrice sensiblement moindre, au moins à l'encontre du type MMP-1, chez un sujet atteint d'un état pathologique lié à une activité MMP pathogène. Cette invention concerne également des composés inhibiteurs de la métalloprotéase, dotés de ces activités sélectives, des procédés de production de ces composés et des compositions à usage pharmaceutique utilisant un agent inhibiteur.

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