申请人:ONO PHARMACEUTICAL CO., LTD.
公开号:EP1671962A1
公开(公告)日:2006-06-21
The compound represented by the general formula (I):
wherein, a fused ring AB represents a 5- to 10-membered fused heterocyclic ring; R1 represents (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) an oxo group, (5) an optionally protected hydroxyl group, (6) an optionally protected carboxyl group, (7) an optionally protected amino group, (8) a cyclic group which may have a substituent (s), (9) an aliphatic hydrocarbon group which may have a substituent (s), or (10) an optionally protected thiol group; n represents 0 or an integer of 1 to 8; provided that n represents an integer of not less than 2, plural R1 are the same or different; a salt thereof, a solvate thereof or a prodrug thereof has a kinase(especially c-Jun N-terminalkinase) inhibitory activity and an inhibitory activity of a function of AP-1 as a transcription factor, it is useful as a preventive and/or therapeutic agent for a for example, a diabetes of metabolic disease, etc., a rheumatoid arthritis of inflammatory, etc.
化合物的一般式(I):其中,融合环AB代表一个5-至10-成员的融合杂环;R1代表(1)氢原子,(2)卤素原子,(3)氰基,(4)氧基,(5)可选保护的羟基,(6)可选保护的羧基,(7)可选保护的氨基,(8)可能具有取代基的环状基团,(9)可能具有取代基的脂肪烃基团或(10)可选保护的硫醇基团; n代表0或1至8的整数; 假设n代表不小于2的整数,则复数R1相同或不同;其盐,溶剂化物或前药具有激酶(尤其是c-Jun N末端激酶)抑制活性和AP-1作为转录因子的功能抑制活性,因此可用作预防和/或治疗代谢疾病(例如糖尿病等)和炎症性风湿性关节炎等的药物。