THIENO 2,3-D PYRIMIDINDIONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS.

摘要

Selective MMP-13 inhibitors are fused pyrimidinones of the formula or a pharmaceutically acceptable salt thereof, wherein: W, together with the carbon atoms to which it is attached, form a 5-membered ring diradical Y is O, S, SO, SO2, NR5, or CH ??2, ?A is-C-or S-; B is O or NR5; or A and B are taken together to form -Cequiv;C-; R1, R4, and R5 are hydrogen, alkyl, alkenyl, alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, C1 C6 alkanoyl, or (CH2)n heteroaryl; R2 and R3 are hydrogen, alkyl, alkenyl, alkynyl CN, NO2, NR4R5, (CH2)n cycloalkyl, (CH2)n aryl, or (CH2)n heteroaryl; R2 may further be halo; n is an integer of from 0 to 5; and R4 and R5 when taken together with the nitrogen to which they are attached complete a 3-to 8-membered ring containing carbon atoms and optionally containing O, S, or N, and substituted or unsubstituted; with the proviso that R?1 ??and R3 are not both selected from hydrogen and C1-C6 alkyl.