申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:EP0394440A1
公开(公告)日:1990-10-31
Phenylcarboxylic acid derivatives represented by formula (I), and their salts, wherein R1 and R2 each represents H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, -0-D-R5 (wherein D represents alkylene, and R5 represents H, amino, morpholino, carboxyl, phthalimido, phenyl or epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl or, when taken together, represent alkylenedioxy: R3 represents H, -E-R6 (wherein E represents alkylene, and R6 represents H carboxyl, cyano, OH, phenylalkoxy or halogen-substituted phenyl or phenylcarbamoyl) -CO-G-R7 (wherein G represents alkylene, and R7represents H or substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl or halophenyl: R4 represents H, alkyl: A represents alkylene, cycloalkyl ring-fuzed alkylene or alkenylene; B represents alkylene or alkenylene; and ℓ represents 0 or 1. These compounds have an activity of inhibiting synthesis of fatty acids and cholesterol, and are useful for treating hyperlipemia, arteriosclerosis, obesity and diabetes.
由式(I)代表的苯基羧酸衍生物及其盐,其中 R1 和 R2 各自代表 H、卤素、烷基、卤代烷基、烷酰基、环烷基、硝基、氨基、-0-D-R5(其中 D 代表亚烷基,R5 代表 H、氨基、吗啉基、羧基、邻苯二甲酰亚胺基、苯基或环氧基)、取代或未取代的苯氧基、取代或未取代的苯烷基氨基、羧基烯基,或者合在一起代表亚烷基二氧基:R3代表H、-E-R6(其中E代表亚烷基,R6代表H羧基、氰基、OH、苯基烷氧基或卤素取代的苯基或苯基氨基甲酰基)、取代或未取代的苯甲酰基、烯基、氨基甲酰基、苯基或卤代苯基:R4 代表 H、烷基:A 代表亚烷基、环烷基环化亚烷基或烯基;B 代表亚烷基或烯基;ℓ 代表 0 或 1。这些化合物具有抑制脂肪酸和胆固醇合成的活性,可用于治疗高脂血症、动脉硬化、肥胖症和糖尿病。