448965-31-9Relevant articles and documents
Combination of an allosteric carboxylic inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
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, (2008/06/13)
This invention provides a combination, comprising an allosteric carboxylic inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof. This invention also provides a method of treating a disease that is responsive to inhibition of MMP-13 and cyclooxygenase-2, comprising administering to a patient suffering from such a disease the invention combination comprising an allosteric carboxylic inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof. This invention also provides a pharmaceutical composition, comprising the invention combination comprising an allosteric carboxylic inhibitor of MMP-13, or a pharmaceutically acceptable salt thereof, with celecoxib, or a pharmaceutically acceptable salt thereof, or valdecoxib, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. The invention combination may also be further combined with other pharmaceutical agents depending on the disease being treated.
FUSED PYRIMIDINONE MATRIX METALLOPROTEINASE INHIBITORS
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, (2008/06/13)
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 X is O, S, SO, SO2, NR5, or CH 2; B is O or NR5; or A and B are taken together to form--C≡C--; R1, R4, and R 5 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, NR 4R5, (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 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; with the proviso that R1 and R3 are not both selected from hydrogen and C1-C6 alkyl.