481631-45-2Relevant academic research and scientific papers
PROCESSES AND COMPOUNDS FOR THE PREPARATION OF SUBSTITUTED NAPHTHYLINDOLE DERIVATIVES
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Page/Page column 18-19; 23-24, (2008/06/13)
The present invention provides processes for the preparation of substituted naphthyl indole derivatives of formula (I) that can be used as inhibitors of plasminogen activator inhibitor-1 (PAI-I) . In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxidation, a Fischer indole synthesis, a methyl ether cleavage, or coupling a substituted methyl tetrazole with a substituted naphthol.
Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
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, (2008/06/13)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are eachH, alkyl,, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 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.
