Amidino substituted tetrahydrobenzo thiophene or furan derivatives and their use as urokinase inhibitors
    2.
    发明授权
    Amidino substituted tetrahydrobenzo thiophene or furan derivatives and their use as urokinase inhibitors 失效
    脒基取代的四氢苯并噻吩或呋喃衍生物及其用作尿激酶抑制剂

    公开(公告)号:US06274619B1

    公开(公告)日:2001-08-14

    申请号:US09584136

    申请日:2000-05-31

    Abstract: A compound of the formula: in which R1 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 arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is 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.

    Abstract translation: 下式化合物: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,被保护的羧基 ,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,受保护羧基(低级)烷酰基,芳酰基,低级烷酰基或任选取代 芳基氨基甲酰基(低级)烷基,R2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,R3是氢或脒基保护基,A是低级亚烷基或羰基,X是Y 低级亚烷基,-S-或-SO 2 - ,Z是-S-或-O-,并且行:是 单键或双键,或其药学上可接受的盐,其可用作药物。

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