Aromatic sulfone hydroxamic acid metalloprotease inhibitor

Details Aromatic sulfone hydroxamic acid metalloprotease inhibitor Aromatic sulfone hydroxamic acid metalloprotease inhibitor

C - Chemistry, Metallurgy

07

D

C07D 211/66 (2006.01) A61K 31/351 (2006.01) A61K 31/4406 (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 2306460

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. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with atoms to which they are bonded form a 5- to 8-membered ring containing one, two or three heteroatoms in the ring that are oxygen, sulfur or nitrogen. R3 in formula (I) is an optionaly substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

L'invention concerne un procédé de traitement qui consiste à administrer une quantité efficace d'acide hydroxamique aromatique sulfoné exerçant un excellent effet inhibiteur sur une ou plusieurs enzymes métalloprotéase en matrice (MMP), par exemple MMP-2, MMP-9 et MMP-13, tout en ayant un effet sensiblement moins inhibiteur au moins sur le type MMP-1, chez un sujet souffrant d'un état lié à une activité MMP pathologique. L'inhibiteur enzymatique administré a une structure représentée par la formule (I), ou un sel pharmaceutique acceptable. Dans ladite formule, R?1¿ et R?2¿ sont tous deux hybrido ou forment tous deux avec les atomes auxquels ils sont liés une chaîne comprenant entre 5 et 8 éléments, dans laquelle un, deux ou trois hétéroatomes sont oxygène, soufre ou azote. R?3¿ est un radicale aryle ou hétéroaryle éventuellement substitué. L'invention concerne des composés inhibiteurs présentant cette activité inhibitrice sélective, des procédés relatifs à la fabrication desdits composés, ainsi que des compositions pharmaceutiques faisant appel à un inhibiteur.

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