Substituted indole oxo-acetyl amino acetic acid derivatives...

Details Substituted indole oxo-acetyl amino acetic acid derivatives... Substituted indole oxo-acetyl amino acetic acid derivatives...

2006-06-06

2006-06-06

Saeed, Kamal A. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S492000, C548S490000

Reexamination Certificate

active

07056943

ABSTRACT:
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: R1is alkyl or optionally substituted cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl; R8is hydrogen, alkyl, cycloalkyl, —CH2-cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; R9is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylymethylene, 4-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(═O)CH2—, H2NC(═O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(═NH)NHCH2CH2CH2—, or taken together with R8as —CH2CH2CH2—; or a pharmaceutically acceptable salt or ester form thereof.

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