Compounds having a matrix metaloproteinase-13 inhibitory activity and an aggrecanase inhibitory activity. They are compounds represented by general formula (I) or pharmacologically acceptable salts, esters, or other derivatives thereof wherein R1 is H or NHOH; R2 is H, optionally substituted alkyl, cycloalkyl, or -AR6 (wherein A is O, -S(O)¿m?-, or alkylene optionally interrupted by -N(R?9¿)-; and R6 is a group represented by formula (II), (III), or (IV) [wherein X is O, S, -N(R10)-, or -C(R11)(R12)-; Y is O, CO, -S(O)¿n?-, -N(R?10¿)-, or -C(R?11)(R12)-; R7 and R8¿ each is H, alkyl, COOH, optionally substituted alkyl, etc.; R?9, R10, R11, and R12¿ each is H, alkyl, etc.; and m and n each is 0 to 2]); R3 is H, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, or optionally substituted alkynyl; R4 is optionally substituted (hetero)arylene; and R5 is optionally substituted alkyl or optionally substituted (hetero)aryl.