abstract |
Selective MMP-13 inhibitors are benzothiadiazines of the formula: (see 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) mbiphenyl or (CH2) substituted biphenyl; X is O or NH, n is O, 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 selected diseases of osteoarthritis, rheumatoid arthritis, cancer, inflammation and heart failure. |