申请人:Japan Tobacco Inc.
公开号:EP1553091A1
公开(公告)日:2005-07-13
A 5-membered heteroaromatic ring compound represented by the formula [I]
wherein V is CH or N; W is S or O; R1 and R2 are each H etc.; X is -N(R4)-, -O-, -S-, -SO2-N(R5)-, -CO-N(R7)- etc.; L is
wherein R20, R21, R22 and R25 are each H etc.; E is aryl or heteroaromatic ring group; R is -COOH etc.; B is aryl etc.; R3 is H etc.; Y is -C(R13)(R14)-N(R12)-, -C(R13)(R14)-O-, -N(R11)-, -O- etc.; A is alkylene; and Z is aryl etc., a prodrug thereof and a pharmaceutically acceptable salt thereof.
The compound [I] has a superior protein tyrosine phosphatase 1B inhibitory activity and is useful as a therapeutic agent for diabetes, diabetic complications, hyperlipidemia, obesity and the like.
由式[I]代表的 5 元杂芳环化合物
其中 V 是 CH 或 N;W 是 S 或 O;R1 和 R2 各自是 H 等;X 是 -N(R4)-、-O-、-S-、-SO2-N(R5)-、-CO-N(R7)- 等;L 是
其中 R20、R21、R22 和 R25 各为 H 等;E 为芳基或杂芳环基团;R 为-COOH 等;B 为芳基等;R3 为 H 等;Y 为-C(R13)(R14)-N(R12)-、-C(R13)(R14)-O-、-N(R11)-、-O- 等;A 为亚烷基;Z 为芳基等、其原药及其药学上可接受的盐。
化合物[I]具有优异的蛋白酪氨酸磷酸酶 1B 抑制活性,可作为糖尿病、糖尿病并发症、高脂血症、肥胖症等的治疗剂。