Patent number: 7160918
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: 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 —NO2; 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-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(?O)CH2—, H2NC(?O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(?NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptab
Type:
Grant
Filed:
January 19, 2006
Date of Patent:
January 9, 2007
Inventors:
Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li
Patent number: 7056943
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: 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 —NO2; 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-imidazolylmethylene, HSCH2—, CH3SCH2CH2—, H2NC(?O)CH2—, H2NC(?O)CH2CH2—, HO2CCH2—, HO2CCH2CH2—, H2NCH2CH2CH2CH2—, H2NC(?NH)NHCH2CH2CH2—, or taken together with R8 as —CH2CH2CH2—; or a pharmaceutically acceptab
Type:
Grant
Filed:
December 9, 2003
Date of Patent:
June 6, 2006
Assignee:
Wyeth
Inventors:
Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li
Patent number: 6599925
Abstract: This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula:
wherein: R, R1, R2, and R3 are H, alkyl, cycloalkyl, —CH2-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, —NH(alkyl), —N(alkyl)2, or perfluoroalkoxy; R4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, —CH2R5, —CH(OH)R5, —C(O)R5, —CH(SH)R5, or —C(S)R5; R5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R6 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treat
Type:
Grant
Filed:
June 18, 2002
Date of Patent:
July 29, 2003
Assignee:
Wyeth
Inventors:
Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, Scott Christian Mayer, David LeRoy Crandall