SUBSTITUTED DIHYDROPYRANO INDOLE-3,4-DIONE DERIVATIVES AND 3-OXOACETIC ACID SUBSTITUTED 2-HYDROXYMETHYLINDOLE DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1(PAI-1)

摘要

Compounds of formula (I) and (II) are provided wherein: X is an alkali metal or a basic amine moiety; R 1 is alkyl, cycloalkyl, -CH2-cycloalkyl, pyridinyl, -CH 2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2-cycloalkyl, -NH2, or -NO 2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or -CH 2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.