申请人:Kyorin Pharmaceutical Co., Ltd.
公开号:US07902367B2
公开(公告)日:2011-03-08
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds.
A cyclic amino benzoic acid derivative represented by the general formula (1)
[wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
本发明涉及循环氨基苯甲酸衍生物,其作为人类过氧化物酶体增殖物激活受体(PPAR)激动剂在治疗脂质代谢异常、糖尿病等方面具有有效性,特别是作为人类PPARα亚型的激动剂,以及其加成盐和含有这些化合物的制药组合物。其中循环氨基苯甲酸衍生物的一般式(1)表示为[其中环Ar表示可能具有取代基的芳基基团或类似物;Y表示C1-C4烷基,C2-C4烯基,C2-C4炔基或类似物;Z表示氧原子、硫原子或—(CH2)n—(n表示0、1或2);X表示氢原子、卤原子、可能被卤原子取代的低烷基基团或类似物;R表示氢原子或低烷基基团,而—COOR代替环W的连接位置的邻位或甲位]或其药学上可接受的盐。