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: wherein: R.sub.1 is alkyl or optionally substituted
cycloalkyl, --CH.sub.2-cycloalkyl, pyridinyl, CH.sub.2-pyridinyl, phenyl
or benzyl; R.sub.2 is hydrogen, alkyl, cycloalkyl, --CH.sub.2-cycloalkyl,
or perfluoroalkyl; R.sub.3 is hydrogen, halo, alkyl, perfluoroalkyl,
alkoxy, cycloalkyl, --CH.sub.2-cycloalkyl, --NH.sub.2, or --NO.sub.2;
R.sub.4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl,
or --CH.sub.2-pyridinyl; R.sub.8 is hydrogen, alkyl, cycloalkyl,
--CH.sub.2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl,
alkyl-aryl, or substituted alkyl-aryl; R.sub.9 is hydrogen, alkyl,
hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene,
4-imidazolylmethylene, HSCH.sub.2--, CH.sub.3SCH.sub.2CH.sub.2--,
H.sub.2NC(.dbd.O)CH.sub.2--, H.sub.2NC(.dbd.O)CH.sub.2CH.sub.2--,
HO.sub.2CCH.sub.2--, HO.sub.2CCH.sub.2CH.sub.2--,
H.sub.2NCH.sub.2CH.sub.2CH.sub.2CH.sub.2--,
H.sub.2NC(.dbd.NH)NHCH.sub.2CH.sub.2CH.sub.2--, or taken together with
R.sub.8 as --CH.sub.2CH.sub.2CH.sub.2--; or a pharmaceutically acceptable
salt or ester form thereof.
