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    • 2. 发明公开
    • 간 섬유화 억제작용을 나타내는 벤조[3,4-d]1,3-디옥솔란 유도체
    • 含有BENZO(3,4-D)1,3-DIOXOLAN衍生物的IVER纤维蛋白酶抑制组合物
    • KR1020010039263A
    • 2001-05-15
    • KR1019990047570
    • 1999-10-29
    • 제이더블유중외제약 주식회사
    • 문성환황태섭이수진정재욱이희윤김병규하종렬김대훈
    • C07D317/02
    • PURPOSE: A liver fibrosis inhibiting composition containing benzo(3,4-d) 1,3-dioxolan derivatives is provided for the inhibition and treatment of liver fibrosis in damaged liver. CONSTITUTION: The liver fibrosis inhibiting composition contains benzo(3,4-d) 1,3-dioxolan derivatives represented by formula (1), in which D is ethylthio, acethylthio, hydroxyethylthio, or any one compound selected from the compound of the formula (a-1) to (a-8), wherein R1, R1', R3 and R3' are independently hydrogen, hydroxy, lower alkyl, lower alkoxy, or carboxy, or R1 and R1' or R3 and R3' are individually oxo, lower alkyliden, lower alkoxyimino or hydroxyimino; R2 is hydrogen, lower alkyl substituted or unsubstituted with halogen, aryl, ar- lower alkyl, 5 to 6 ring heteroaryl containing hetero selected from nitrogen, oxygen and sulfur; R4, R6, R7 and R8 are individually hydrogen, lower alkoxy, hydroxycarbonyl, lower alkoxycarbonyl, lower ethylcarbamoyl, lower alkenylcarbamoyl, lower alkylidencarbamoyl or tri(lower alkyl)sillyl, or lower alkyl or aryl substituted or unsubstituted with halogen, hydroxy or lower alkoxy, 5 to 6 ring heteroaryl substituted or unsubstituted with hydroxy and carboxy and having at least one nitrogen; and R5 is hydrogen, halogen, nitro, cyano, hydroxy, lower alkoxy, amino, lower alkanoylamino, carboxy or lower alkoxycarbonyl.
    • 目的:提供含有苯并(3,4-d)1,3-二氧戊环衍生物的肝纤维化抑制组合物,用于抑制和治疗受损肝脏的肝纤维化。 构成:肝纤维化抑制组合物含有式(1)所示的苯并(3,4-d)1,3-二氧戊环衍生物,其中D为乙硫基,乙硫基,羟乙硫基,或选自式 (a-1)至(a-8),其中R1,R1',R3和R3'独立地是氢,羟基,低级烷基,低级烷氧基或羧基,或R1和R1'或R3和R3' ,低级亚烷基,低级烷氧基亚氨基或羟基亚氨基; R 2是氢,被卤素,芳基,芳基 - 低级烷基取代或未取代的低级烷基,含有选自氮,氧和硫的杂原子的5至6个环杂芳基; R4,R6,R7和R8分别是氢,低级烷氧基,羟基羰基,低级烷氧基羰基,低级乙基氨基甲酰基,低级链烯基氨基甲酰基,低级亚烷基氨基甲酰基或三(低级烷基)甲硅烷基,或被卤素,羟基或低级烷氧基取代或未取代的低级烷基或芳基 5至6个被羟基和羧基取代或未取代的且具有至少一个氮的环杂芳基; R 5为氢,卤素,硝基,氰基,羟基,低级烷氧基,氨基,低级烷酰氨基,羧基或低级烷氧基羰基。