| abstract |
Selective MMP-13 inhibitors are fused pyrimidinones of the formula n n n or a pharmaceutically acceptable salt thereof, wherein: n W, together with the carbon atoms to which it is attached, form a 5-membered ring diradical n n n X is O, S, SO, SO 2 , NR 5 , or CH 2 ; n n n B is O or NR 5 ; or n A and B are taken together to form —C≡C—; n R 1 , R 4 , and R 5 are hydrogen, alkyl, alkenyl, alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, C 1 -C 6 alkanoyl, or (CH 2 ) n heteroaryl; n R 2 and R 3 are hydrogen, alkyl, alkenyl, alkynyl CN, NO 2 , NR 4 R 5 , (CH 2 ) n cycloalkyl, (CH 2 ) n aryl, or (CH 2 ) n heteroaryl; n R 2 may further be halo; n n is an integer of from 0 to 5; and n R 4 and R 5 when taken together with a nitrogen to which they are both attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing O, S, or N, and substituted or unsubstituted; n with the proviso that R 1 and R 3 are not both selected from hydrogen and C 1 -C 6 alkyl. |