This invention provides compounds which act as inhibitors of plasminogen
activator inhibitor-1 (PAI-1) of the formula:
##STR1##
wherein: R, R.sub.1, R.sub.2, and R.sub.3 are H, alkyl, cycloalkyl,
--CH.sub.2 -(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl,
heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino,
--NH(alkyl), --N(alkyl).sub.2, or perfluoroalkoxy; R.sub.4 is H, alkyl,
perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted
heteroaryl, alkenyl, alkenyl-aryl, aryl, --CH.sub.2 R.sub.5,
--CH(OH)R.sub.5, --C(O)R.sub.5, --CH(SH)R.sub.5, or --C(S)R.sub.5 ;
R.sub.5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl,
substituted heteroaryl, alkenyl, alkenyl-aryl; R.sub.6 is H, alkyl,
cycloalkyl, --CH.sub.2 -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 or prevent conditions resulting from fibrinolytic
disorders such as deep vein thrombosis and coronary heart disease, and
pulmonary fibrosis.
Esta invención proporciona los compuestos que actúan como inhibidores del activador plasminógeno inhibitor-1 (PAI-1) del fórmula: ## del ## STR1 en donde: R, R.sub.1, R.sub.2, y R.sub.3 son H, alkyl, cycloalkyl, -- CH.sub.2 el -(cycloalkyl), alkanoyl, halo, aryl hydroxy, aryl, substituido, heteroaryl, substituyó el heteroaryl, perfluoroalkyl, alkoxy, amino, -- NH(alkyl), -- N(alkyl).sub.2, o perfluoroalkoxy; R.sub.4 es H, alkyl, perflouroalkyl, aryl, aryl substituido, heteroaryl, heteroaryl substituido, alkenyl, alkenyl-alkenyl-aryl, aryl, -- CH.sub.2 R.sub.5, -- CH(OH)R.sub.5, -- C(O)R.sub.5, -- CH(SH)R.sub.5, o -- C(S)R.sub.5; R.sub.5 es H, alkyl, perflouroalkyl, aryl, aryl substituido, heteroaryl, heteroaryl substituido, alkenyl, alkenyl-alkenyl-aryl; R.sub.6 es H, alkyl, cycloalkyl, -- CH.sub.2 - cycloalkyl, alkylaryl, aryl, aryl substituido, heteroaryl, o heteroaryl substituido; n es un número entero de 0-6; A es COOH, o un imitador del ácido; o una forma farmacéutico aceptable de la sal o del éster de eso, tan bien como las composiciones y métodos farmacéuticos usando estos compuestos para tratar o para prevenir condiciones resultando de desórdenes fibrinolóticos tales como trombosis profunda de la vena y enfermedad cardíaca coronaria, y fibrosis pulmonar.
