| abstract |
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 NR?5¿; or A and B are taken together to form -C C-; R?1, R4, and R5¿ are hydrogen, alkyl, alkenyl, alkynyl, (CH¿2?)n aryl, (CH2)n cycloalkyl, C1 C6 alkanoyl, or (CH2)n heteroaryl; R?2 and R3¿ are hydrogen, alkyl, alkenyl, alkynyl CN, NO¿2?, NR?4R5, (CH¿2)n cycloalkyl, (CH2)n aryl, or (CH2)n heteroaryl; R2 may further be halo; n is an integer of from 0 to 5; and R?4 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 C¿1-?C6 alkyl. |