申请人:Kyoto Pharmaceutical Industries, Ltd.
公开号:EP1403253A1
公开(公告)日:2004-03-31
The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I)
R15―C(R14)=N-O―
wherein R1 is H or C1-6 alkyl, R2 is H, -CO-C(R4)=C(R4)-R5 wherein R4 is H or C1-4 alkyl, and R5 is C4-8 alkyl, C2-8 alkenyl and the like, and the like, Y is the following group wherein X is O or S, R7 is the same as R4, R8 is R10-C(R9)=C(R9)- wherein R9 is the same as R4, R10 is C3-6 alkyl and the like, and the like, R14 is the same as R4, and R15 is aryl and the like, Y-(CH2)n-O- is bonded to the 6- or 7-position of the tetrahydroisoquinoline skeleton, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases or an agent for the prophylaxis or treatment of syndrome X.
本发明的新型杂环化合物是一种具有式 (I) 的新型杂环化合物
r15-c(r14)=n-o-
其中 R1 是 H 或 C1-6 烷基,R2 是 H、-CO-C(R4)=C(R4)-R5 其中 R4 是 H 或 C1-4 烷基,R5 是 C4-8 烷基、C2-8 烯基及类似物及类似物,Y 是以下基团 其中 X 是 O 或 S,R7 与 R4 相同,R8 是 R10-C(R9)=C(R9)- 其中 R9 与 R4 相同、R10为C3-6烷基等,R14与R4相同,R15为芳基等,Y-(CH2)n-O-键合在四氢异喹啉骨架的6位或7位,n为1~4的整数,或其药学上可接受的盐。本发明的化合物(I)可用作降血糖剂、降血脂剂、胰岛素抵抗改善剂、糖尿病治疗剂、糖尿病并发症治疗剂、葡萄糖耐量改善剂、抗动脉硬化剂、抗肥胖剂、抗炎剂、预防或治疗 PPAR 介导的疾病的药物或预防或治疗 X 综合征的药物。