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    • 9. 发明申请
    • NOVEL BENZOTHIOPHENE DERIVATIVES, THEIR PREPARATION AND USE AS UROKINASE INHIBITORS
    • 新型苯并噻吩衍生物,其制备和用作尿激酶抑制剂
    • WO1998011089A1
    • 1998-03-19
    • PCT/JP1997003215
    • 1997-09-12
    • FUJISAWA PHARMACEUTICAL CO., LTD.TANAKA, AkitoMIZUNO, HiroakiSAKURAI, Minoru
    • FUJISAWA PHARMACEUTICAL CO., LTD.
    • C07D333/60
    • C07D513/04C07D307/85C07D333/70C07D333/80Y02P20/55
    • A compound of formula (I) in which R is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbymoyl(lower)alkyl; R is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl; R is hydrogen or amidino-protective group; A is lower alkylene or carbonyl; X is (1), (2) or (3); Y is lower alkylene, -S- or -SO2-; Z is -S- or -O-; and the line: ----- is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.
    • 式(I)化合物,其中R 1为氢,任选取代的低级烷基氨基甲酰基(低级)亚烷基,低级亚烷基,低级烷基,任选取代的芳(低级)烷基,环(低级)烷基(低级)烷基,保护基 羧基(低级)烷基,羧基(低级)烷基,羟基(低级)烷基,任选取代的低级烷基氨基甲酰基(低级)烷基,低级烷硫基(低级)烷基,羧基(低级)烷酰基,被保护的羧基(低级)烷酰基,芳酰基, 烷酰基或任选取代的芳基羰基(低级)烷基; R 2是氢,羧基,保护的羧基,甲酰基或N-(低级)烷基-N-(低级)烷氧基氨基甲酰基; R 3是氢或脒基保护基; A是低级亚烷基或羰基; X为(1),(2)或(3); Y是低级亚烷基,-S-或-SO 2 - ; Z是-S-或-O-; 并且线: ----- 是单键或双键,或其药学上可接受的盐,其可用作药物。