Selective inhibition of aggrecanase in osteoarthritis treatment

Details Selective inhibition of aggrecanase in osteoarthritis treatment Selective inhibition of aggrecanase in osteoarthritis treatment

C - Chemistry, Metallurgy

07

D

C07D 211/96 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61P 19/00 (2006.01) A61P 25/00 (2006.01) C07D 241/04 (2006.01) C07D 241/08 (2006.01)

Patent

CA 2315481

This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50S of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metalloproteinases (ADAMs or reprolysins). This invention also relates to compounds, methods of treatment and composition of Formula I: (see formula I) or a therapeutically acceptable salt thereof, wherein X is carbon or nitrogen; R1 and R2 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1 and R2 is methyl; R3 and R4 are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3 and R4 may be taken together to form a carbonyl group; and R5 and R6 are independent substituents in the ortho, meta, or para positions and are independently selected from the group consisting of hydrogen, halogen, cyano, methyl, and ethyl; with the provisos: when X is carbon, then R7 and R8 are both hydrogen and at least one of R1, R2, R3, and R4 is hydroxy; when X is carbon and R5 is para-halo, then at least one of R6, R3, and R4 is not hydrogen; when X is nitrogen, then R8 is not present and R7 is hydrogen or a group of the formula: Image wherein, Y is -CH2-NH2 or -NH-CH3; and when X is nitrogen and R7 is H, then R3 and R4 are taken together to form a carbonyl group.

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