申请人:OTSUKA PHARMACEUTICAL FACTORY, INC.
公开号:EP0749974A1
公开(公告)日:1996-12-27
The invention provides a phosphonic diester derivative of the formula:
wherein R1, R2, R3 and R6 are the same or different and each represents a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, a lower alkoxy group, a cyano group, a phenylsulfonylamino group, a benzoylamino group, an amino group or a halogen-substituted lower alkyl group, R4 represents a phenyl group, a lower alkyl group, a phenyl(lower)alkyl group optionally substituted by halogen on the phenyl ring, a lower alkenyl group, a carboxy(lower)alkyl group, a (lower)alkoxy-carbonyl(lower)alkyl group, a (lower)alkoxy(lower)alkyl group, a lower alkynyl group, a benzoyl(lower)alkyl group, an amino group, a di(lower)alkanoylamino group, a benzylideneamino group optionally having lower alkoxy on the phenyl ring or a pyridylmethylideneamino group, R5 represents a lower alkyl group, R7 represents a lower alkoxy group, a hydroxyl group, a phenyl group, a phenyl(lower)alkoxy group optionally having halogen on the phenyl ring or a phenyl(lower)alkylamino group, X1 and X2 independently represent an oxygen atom or a sulfur atom, A represents an oxygen atom or a single bond, and Z represents a lower alkylene group.
The derivatives according to the invention are useful as therapeutic or preventive compositions for hyperlipidemia, hypertension, and diabetes.
本发明提供了一种式如下的膦酸二酯衍生物:
其中 R1、R2、R3 和 R6 相同或不同,各自代表氢原子、低级烷基、卤素原子、硝基、低级烷氧基、氰基、苯磺酰氨基、苯甲酰氨基、氨基或卤素取代的低级烷基、R4 代表苯基、低级烷基、苯基环上任选被卤素取代的苯基(低级)烷基、低级烯基、羧基(低级)烷基、(低级)烷氧基-羰基(低级)烷基、(低级)烷氧基(低级)烷基、低级炔基、苯甲酰基(低级)烷基、氨基、二(低级)烷酰氨基、苯基环上可选带有低级烷氧基的亚苄基氨基或吡啶亚甲基氨基,R5 代表低级烷基,R7 代表低级烷氧基、羟基、X1和X2分别代表氧原子或硫原子,A代表氧原子或单键,Z代表低级亚烷基。
根据本发明的衍生物可用作高脂血症、高血压和糖尿病的治疗或预防组合物。