申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:EP0393607A2
公开(公告)日:1990-10-24
Phenylcarboxylic acid derivatives having a hetero ring in the substituent of the formula:
wherein R¹ is halogen, alkyl, cycloalkyl, hydroxy, alkoxy, phenoxy which has a substituent selected from halogen and alkyl, carboxyl, alkylsulfonyloxy, phenylsulfonyloxy optionally substituted by halogen, alkylsulfonyloxyalkoxy, amino, alkanoylamino, benzoylamino, alkenyloxy, phenylalkoxyalkoxy, hydroxyalkoxy, phenylalkoxy having optionally 1 to 3 substituents selected from halogen, alkyl and alkoxy, halogenoalkyl, cycloalkyloxy optionally substituted by hydroxy, alkoxy substituted by cycloalkyl having optionally hydroxy substituent, imidazolylalkyl, or imidazolylalkoxy; k is 0 or 1 to 3; or (R¹)k is alkylenedioxy; A is alkylene or alkylenoxy; ℓ is 0 or 1; B is methylene or carbonyl; m is 0 or 1; D is alkylene; E is alkylene or alkenylene; n is 0 or 1; and R² is hydrogen or alkyl, or a salt thereof, which have fatty acid synthesis-inhibitory activity, cholesterol synthesis-inhibitory activity and are useful as antilipidemic agent, prophylactic and treating agent of artherosclerosis, prophylactic and treating agent of obesity, antidiabetics.
苯基羧酸衍生物,其取代基中含有一个杂环:
其中 R¹ 是卤素、烷基、环烷基、羟基、烷氧基、具有选自卤素和烷基的取代基的苯氧基、羧基、烷基磺酰氧基、任选被卤素取代的苯基磺酰氧基、烷基磺酰氧基烷氧基、氨基、烷酰氨基、苯甲酰氨基、烯氧基、苯基烷氧基烷氧基、羟基烷氧基、具有 1 至 3 个任选自卤素、烷基和烷氧基的取代基的苯基烷氧基、卤代烷基、任选 被羟基取代的环烷氧基、被具有任选羟基取代基的环烷基取代的烷氧基、咪唑烷基或咪唑烷氧基;A 是亚烷基或亚烷氧基;ℓ 是 0 或 1;B 是亚甲基或羰基;m 是 0 或 1;D 是亚烷基;E 是亚烷基或烯基;n 是 0 或 1;和 R² 是氢或烷基,或其盐,它们具有脂肪酸合成抑制活性和胆固醇合成抑制活性,可用作降血脂剂、动脉硬化的预防和治疗剂、肥胖的预防和治疗剂、抗糖尿病剂。