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US 2008/0188543 A1Published application
Pharmaceutical compositions containing substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
AssigneeWyeth
InventorsArun A. THAKUR, Mannching Sherry Ku, Hsueh-Ling Wu
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Abstract
Pharmaceutical compositions containing compounds of formula I are provided: wherein the constituent variables are as defined herein. The compounds are inhibitors of plasminogen activator inhibitor-1 (PAI-1) and the compositions are useful for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, Alzheimer's disease and pulmonary fibrosis.
Claims46
A composition comprising a compound of formula (I), or a pharmaceutically acceptable salt, solvate or ester thereof:
- wherein:
- R1 is selected from C1-C8 alkyl, (—CH2)n—C3-C6 cycloalkyl, wherein n is an integer of from 0 to 3, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of the cycloalkyl, pyridinyl, phenyl and benzyl groups being optionally substituted by, from 1 to 3 groups independently selected from halogen, C1-C4 alkyl, C1-C3 perfluoroalkyl, —O—C1-C3 perfluoroalkyl, C1-C3 alkoxy, —OH, —NH2, and —NO2;
- R2 is selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, —CH2—C3-C6 cycloalkyl, or C1-C3 perfluoroalkyl, —CH2OH or CH2OAc;
- R3 is selected from H, halogen, C1-C6 alkyl, C1-C3 perfluoroalkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, —CH2—C3-C6 cycloalkyl, C3-C6 cycloalkenyl, —CH2—C3-C6 cycloalkenyl, —NH2, or —NO2;
- R4 is phenyl substituted by from 1 to 3 groups independently selected from halogen, C1-C4 alkyl, C1-C3 alkoxy, C1-C3 perfluoroalkyl, and —O—C1-C3 perfluoroalkyl;
- and
- from 1% to 25% w/w of one or more surfactants.
4 more elements
Dependencies are inferred from the claim text.