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

US7629377B2 · kind B2 · utility

Assignee

• Wyeth, LLC · US

Inventors

• David LeRoy Crandall · Doylestown, US
• Scott Mayer · Lawrence, US
• Eric Gould Gundersen · Royersford, US
• Hassan Mahmoud Elokdah · North Wales, US

Key dates

• Filing date: Feb 5, 2008
• Grant date: Dec 8, 2009
• Expiry date: Feb 5, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention provides PAI-1 inhibiting compounds of Formula I:wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, 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.