SUBSTITUTED INDOLE OXO-ACETYL AMINO ACETIC ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1).

摘要

This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure of Formula (I) : wherein: R1 is alkyl or optionally substituted cycloalkyl, -CH2-cycloalkyl, pyridinyl, -CH2-pyridinyl, phenyl or benzyl; R2 is hydrogen, alkyl, cycloalkyl, -CH2-cycloalkyl, or perfluoroalkyl; R3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2-cycloalkyl, -NH2, or -N02; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or -CH2-pyridinyl; R8 is hydrogen, alkyl, cycloalkyl, -CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolyl-methylene, HSCH2-, CH3SCH2CH2-, H2NC(=O)CH2-, H2NC(=O)CH2CH2-, H02CCH2-, H02CCH2CH2-, H2NCH2CH2CH2CH2-, H2NC(=NH)NHCH2CH2CH2-, or taken together with R8 as -CH2CH2CH2-; or a pharmaceutically acceptable salt or ester form thereof.