| 摘要 |
This invention provides methods of inhibiting plasminogen activator inhibitory (PAI-1) in a mammal, utilizing compounds of the formula: (I) wherein: A is C or N; B is 0, S, N, or CH=CH; E is (II), (III), or -X-D; D is (IV), (V), or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH>2<, or -CH-S-2-benzothiazole; Y is H, alkyl, or halo; Z is 0, S, or N; R is H, nitro, alkyl, alkoxy, halo, or CF>3<; R?1> is alkyl, aryl, aralkyl, halo, Het-alkyl, or optionally substituted aryl; Het is (VI) or (VII); G is 0, S, or N; R<2> is H, halo, alkyl, or -OR<5>; R<3> and R<4> are H, halo, alkyl, aryl, nitro, amino, alkylsulfoamide, arylsulfoamide, cycloalkyl, heterocycle, or optionally substituted aryl; R<5> is H, alkyl, -CH(R<7>)R<8>, -C(CH2)nCO2R<9>, -C(CH3)2CO2R<9>, CH(R<7>)(CH2)nCO2R<9>, or -CH(R<7>)C6H4CO2R<9>; R<6> is alkylene; R<7> is H, alkyl, aryl, aralkyl, cycloalkyl, phthalic acid, or Q-alkyl; Q is (VIII), (IX), (X), (XI); R<8> is -CO2R<11>, -CONHR<11>, tetrazole, or -PO3R<11>; R<9> is H, alkyl, aryl, or aralkyl; W is 0, N, or S; R<11> is H, alkyl, aryl, or aralkyl; n = 1-6; or a pharmaceutically acceptable salt or ester form thereof.
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