Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: ##STR00001## wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.