C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 285/24 (2006.01) A61P 35/00 (2006.01) C07D 285/22 (2006.01) C07D 417/12 (2006.01)
Patent
CA 2433075
Selective MMP-13 inhibitors are benzo thiadiazines of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen or alkyl; R1 and R3 include hydrogen, alkyl, and aryl, with the proviso that R3 is not (CH2)m biphenyl or (CH2)m substituted biphenyl; X is O or NH, n is 0, 1, or 2. The compounds of Formula (I), or a pharmaceutically acceptable salt thereof, are useful for treating diseases mediated by an MMP-13 enzyme, including diseases selected from osteoarthritis, rheumatoid arthritis, cancer, inflammation, and heart failure.
La présente invention concerne des inhibiteurs sélectifs de la MMP-13 qui sont des benzo-thiadiazines de la formule (1), ou un sel pharmaceutiquement acceptable de ces dernières, dans laquelle R?2¿ est hydrogène ou alkyle; R?1¿ et R?3¿ comprennent hydrogène, alkyle et aryle, à condition que R?3¿ ne soit pas (CH¿2?)¿m? biphényle ou (CH¿2?)¿m? biphényle substitué; X est O ou NH, n est 0, 1, ou 2. Les composés de la formule (1), ou un sel pharmaceutiquement acceptable de ces derniers, sont utilisés pour traiter les maladies dans lesquelles les enzymes MMP-13 jouent un rôle de médiateur, y compris des maladies choisies parmi l'ostéoarthrite, l'arthrite rhumatoïde, le cancer, l'inflammation et l'insuffisance cardiaque.
Picard Joseph Armand
Wilson Michael William
Sim & Mcburney
Warner-Lambert Company
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