| 摘要 |
PROBLEM TO BE SOLVED: To provide an agent for the selective inhibition of aggrecanase for the treatment of osteoarthrosis. SOLUTION: The objective inhibitor is a compound of formula I [X is C or N; R1 and R2 are each H, hydroxy or methyl and at least one of R1 and R2 is methyl; R3 and R4 are each H, hydroxy or methyl or R3 and R4 together form a carbonyl group; R5 and R6 are each an independent substituent selected from H, halogens, cyano, methyl and ethyl and substituted at ortho, meta or para-position; when X is C, both R7 and R8 are H and at least one of R1 to R4 is hydroxy; when X is N, R8 is absent and R7 is a group of formula II (Y is CH2-CH2 or NH-CH3); when X is N and R7 is H, R3 and R4 together form a carbonyl group] or its therapeutically permissible salt.
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