Compounds having the following formula:
are useful in treating disease conditions mediated by matrix metalloproteinases and TACE, such as tumor growth, osteoarthritis, rheumatoid arthritis and degenerative cartilage loss.
Compounds are provided having the following formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined in the specification, which have matrix metalloproteinase inhibiting activity.
A ruthenium‐catalyzed highly selective difluoromethylation of 8‐aminoquinoline amides at the C5 position has been developed. It tolerates a broad range of functional groups, providing the corresponding difluoromethylated products in moderate to good yields. Preliminary experimental results indicate that the tricoordinate ruthenium intermediate is the key factor in achieving the C5‐position selectivity.