Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)

   
   

This invention provides PAI-1 inhibiting compounds of Formula I: ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R.sub.8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R.sub.5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R.sub.8, alkanoyl, aroyl optionally substituted with R.sub.8 ; R.sub.6 is H, alkyl, alkylaryl, benzyl optionally substituted with R.sub.8, alkanoyl, aroyl optionally substituted with R.sub.8 ; R.sub.7 is H, alkyl, alkylaryl, aryl optionally substituted with R.sub.8 ; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO.sub.3 H, PO.sub.3 H.sub.2, tetronic acid, etc.; R.sub.8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.

Deze uitvinding verstrekt het1 verbieden samenstellingen van Formule I: ## STR1 ## waarin: R.sub.1, R.sub.2, R.sub.3, En R.sub.4 zijn eachH, alkyl., alkanoyl, halo, OH, aryl die naar keuze met R.sub.8, perfluoroalkyl wordt gesubstitueerd, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R.sub.5 is H, alkyl, perfluoroalkyl, aryl die naar keuze met R.sub.8, alkanoyl, aroyl wordt gesubstitueerd die naar keuze met R.sub.8 wordt gesubstitueerd; R.sub.6 is H, alkyl, alkylaryl, benzyl naar keuze gesubstitueerd met R.sub.8, alkanoyl, aroyl die naar keuze met R.sub.8 wordt gesubstitueerd; R.sub.7 is H, alkyl, alkylaryl, aryl die naar keuze met R.sub.8 wordt gesubstitueerd; n is 0-6; A is COOH, of een zure nabootser zoals tetraazole, SO.sub.3 H, PO.sub.3 H.sub.2, tetronic zuur, enz. R.sub.8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; of een farmaceutisch aanvaardbaar zout daarvan; evenals farmaceutische samenstellingen en methodes van behandeling die deze samenstellingen gebruikt.

 
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