ISOPHTHALIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS

摘要

Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula (I) wherein: R?1, R2, and R3¿ independently are hydrogen, halo, hydroxy, C¿1?-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR?4R5¿, CN, or CF¿3?; E is independently O or S; A and B independently are OR?4 or NR4R5¿; each R?4 and R5¿ independently are H, C¿1?-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R?4 and R5¿ when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.