Selective inhibition of aggrecanase in osteoarthritis treatment

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

2006-04-18

2006-04-18

McKenzie, Thomas C. (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C514S255010

Reexamination Certificate

active

07030242

ABSTRACT:
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:or a therapeutically acceptable salt thereof, whereinX is carbon or nitrogen;R1and R2are independently selected from the group consisting of hydrogen, hydroxy, and methyl, wherein at least one of R1and R2is methyl;R3and R4are independently selected from the group consisting of hydrogen, hydroxy, and methyl, or R3and R4may be taken together to form a carbonyl group; andR5and R6are 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 R7and R8are both hydrogen and at least one of R1, R2, R3, and R4is hydroxy;when X is carbon and R5is para-halo, then at least one of R6, R3, and R4is not hydrogen;when X is nitrogen, then R8is not present and R7is hydrogen or a group of the formula:wherein, Y is —CH2—NH2or —NH—CH3; andwhen X is nitrogen and R7is H, then R3and R4are taken together to form a carbonyl group.

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