DERIVATIVES OF INDOL-OXO-ACETILAMINOACETIC ACID REPLACED AS INHIBITORS OF THE PLASMINOGEN-1 ACTIVATOR INHIBITOR (PAI-1).

摘要

Compound of formula I: ** see formula ** in which: R 1 is C 1 -C 8 alkyl, C 3 -C 6 cycloalkyl, -CH 2 -C 3 -C 6 cycloalkyl, pyridinyl, -CH 2 -pyridinyl, phenyl or benzyl, the rings of the cycloalkyl, pyridinyl, phenyl and benzyl groups may be optionally substituted with 1 to 3 groups independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, C 1-C 6 -o-perfluoroalkyl, C 1 alkoxy -C 6, -OH, -NH 2, and -NO 2; R 2 is hydrogen, C 1 -C 6 alkyl, C 3-C 6 cycloalkyl, -CH 2-C 3-C 6 cycloalkyl, or C 1-C 3 perfluoroalkyl; R 3 is hydrogen, halogen, C 1 -C 6 alkyl, C 1-C 3 perfluoroalkyl, C 1-C 6 alkoxy, C 3-C 6 cycloalkyl, -CH 2-C 3-C 6 cycloalkyl, -NH 2, or -NO 2; R 4 is phenyl, benzyl, benzyloxy, pyridinyl, or -CH 2-pyridinyl, in which the rings of these groups may be optionally substituted with 1 to 3 groups independently selected from the group consisting of halogen, C1-C3 alkyl, perfluoroalkyl C1-C3, -O-perfluoroalkyl C1-C3, C1-C3 alkoxy, -OH, -NH2, and -NO2; R8 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, or C1-C3 perfluoroalkyl, aryl, substituted aryl, alkyl-aryl, or substituted alkyl-aryl; and R9 is hydrogen, C1-C6 alkyl, branched C3-C6 alkyl, C1-C6 hydroxyalkyl, 4-hydroxybenzyl, 3-indolylmethylene, 4-imidazolylmethylene, HSCH 2-, CH 3SCH 2CH 2-, H 2NC (= O) CH 2-, H 2NC (= O) CH 2CH 2-, HO 2CCH 2-, HO 2CCH 2 CH 2-, H 2NCH 2CH 2CH 2CH 2-, H 2NC (= NH) NHCH 2CH 2CH 2-, or, taken together with R 8, -CH 2CH 2CH 2-; or a pharmaceutically acceptable salt or ester form thereof.