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    • 9. 发明申请
    • PHOSPHONIC DIESTER DERIVATIVE
    • WO1994018212A1
    • 1994-08-18
    • PCT/JP1994000209
    • 1994-02-10
    • OTSUKA PHARMACEUTICAL FACTORY, INC.SHOJI, YasuoTSUDA, YoshihikoTSUTSUMI, KazuhikoINOUE, Yasuhide
    • OTSUKA PHARMACEUTICAL FACTORY, INC.
    • C07F09/650
    • C07F9/6561C07F9/6541
    • A phosphonic diester derivative represented by general formula (I), which is excellent is hypolipidemic and hypoglycemic effects, reduced in the side effects, and hence useful for treating and preventing hyperlipidemia, treating cataract, and treating and preventing diabetes, wherein R , R , R and R represent each independently hydrogen, lower alkyl, lower alkoxy, halogenated lower alkyl, nitro, halogen, cyano, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylated lower alkoxy, phenylated lower alkylthio or benzoyloxy substituted by di(lower alkoxy)phosphorylated lower alkyl, provided R and R may be combined together to form -CH = CH-CH = CH-; R represents hydrogen, lower alkyl or phenyl; R and R represent each independently lower alkoxy, phenyl or phenylated lower alkoxy; A represents optionally phenylated lower alkylene; B represents a benzene or thiophene ring; D represents -CO-, -CS- or -SO2-; E represents (a), (b) or (c) wherein R represents lower alkyl; Z represents a single bond or -O-; Y represents optionally phenylated lower alkylene or vinylene; and n represents 0 or 1.
    • 由通式(I)表示的膦酸二酯衍生物是优异的降血脂和降血糖作用,副作用降低,因此可用于治疗和预防高脂血症,治疗白内障和治疗和预防糖尿病,其中R 1, R 2,R 3和R 4各自独立地表示氢,低级烷基,低级烷氧基,卤代低级烷基,硝基,卤素,氰基,苯硫基,苯基亚磺酰基,苯基磺酰基,苯基低级烷氧基,苯基低级烷硫基或 由二(低级烷氧基)磷酸化低级烷基取代的苯甲酰氧基,只要R 3和R 4可以组合在一起形成-CH = CH-CH = CH-; R 5表示氢,低级烷基或苯基; R 6和R 7各自独立地表示低级烷氧基,苯基或苯基低级烷氧基; A代表任选地是苯基的低级亚烷基; B代表苯或噻吩环; D表示-CO - , - CS-或-SO 2 - ; E表示(a),(b)或(c)其中R 8表示低级烷基; Z表示单键或-O-; Y代表任选地是苯基的低级亚烷基或亚乙烯基; n表示0或1。