| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a new compound which has a strong matrix metalloproteinase-13 (collagenase-3)-inhibiting activity and a strong aggrecanase- inhibiting activity. SOLUTION: A compound of formula I [R1 is OH or hydroxyamino; R2 is H, a 3 to 7C cycloalkyl or the like; R3 is H, a (substituted) lower alkyl or the like; R4 is a (substituted)arylene, a (substituted) heteroarylene; R5 is a (substituted) lower alkyl, a (substituted) aryl or the like; but when R2 is H, a (substituted) lower alkyl or the like; R3 is a (substituted)alkynyl], for example, (±)-N-hydroxyl-Nα-(4-methoxybenzene sulfonyl)-2-[2-(quinazoline-2,4-dion-3-yl) ethyl]glycinamide. The compound of formula I is produced, for example, by reacting a compound of formula II (G1 is a COOHprotecting group) with a sulfonyl halide compound of the formula: R5-O-R4-SO4-Q (Q is a halogen) and the removing the G1 group of the obtained compound of formula III to obtain the compound of formula IV.</p> |
