| abstract |
SOLUTION: Expression The present invention is an indoleoxo-acetylaminoacetic acid derivative that is useful as an inhibitor of plasminogen activator inhibitor-1 (PAI-1), which is useful in the treatment of fibrinolytic diseases. Wherein R 1 is alkyl or optionally substituted cycloalkyl, —CH 2 -cycloalkyl, pyridinyl, —CH 2 -pyridinyl, phenyl or benzyl; 2 is hydrogen, alkyl, cycloalkyl, —CH 2 -cycloalkyl, or perfluoroalkyl; R 3 is hydrogen, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH 2 -cycloalkyl, —NH 2 or be -NO 2,; R 4 is phenyl which is optionally substituted, benzyl, Benjiruo Shi, pyridinyl, or -CH 2, - pyridinyl; R 8 is hydrogen, alkyl, cycloalkyl, -CH 2 - cycloalkyl, perfluoroalkyl, aryl, substituted aryl, alkyl - aryl, or substituted alkyl - aryl R 9 is hydrogen, alkyl, hydroxyalkyl, 4-hydroxybenzyl, 3-indolylmethylene, 4-imidazolylmethylene, HSCH 2 —, CH 3 SCH 2 CH 2 —, H 2 NC (═O) CH 2 —. , H 2 NC (═O) CH 2 CH 2 —, HO 2 CCH 2 —, HO 2 CCH 2 CH 2 —, H 2 NCH 2 CH 2 CH 2 CH 2 —, H 2 NC (═NH) NHCH 2 CH 2 CH 2 —, or said compound being —CH 2 CH 2 CH 2 — together with R 8 ; Provided is a salt form or an ester form that is pharmaceutically acceptable. |