Substituted naphthyl indole derivatives as inhibitors of...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/12 (2006.01) A61K 31/40 (2006.01) A61P 7/02 (2006.01) C07D 209/12 (2006.01)

Patent

CA 2448798

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.

L'invention concerne des composés d'inhibition PAI-1 représentés par la formule (I). Dans cette formule, R¿1?, R¿2?, R¿3? et R¿4? représentent chacun H, alkyle alcanoyle, halo, OH, aryle éventuellement substitué par R¿8?, perfluoroalkyle, alcoxy, amino, alkylamino, dialkylamino, perfluoroalcoxy; R¿5? représente H, alkyle perfluoroalkyle, aryle éventuellement substitué par R¿8?, alcanoyle, aroyle éventuellement substitué par R¿8?; R¿6? représente H, alkyle, alkylaryle, benzyle éventuellement substitué par R¿8?, alcanoyle, aroyle éventuellement substitué par R¿8?; R¿7? représente H, alkyle, alkylaryle, aryle éventuellement substitué par R¿8?; n est un nombre compris entre 0 et 6; A représente COOH ou un analogue d'acide tel que tétraazole, SO¿3?H, PO¿3?H¿2?, acide tétronique, etc.; R¿8? représente H, alkyle, cycloalkyle, alcanoyle, halo, OH, perfluoroalkyle, alcoxy, amino, alkylamino, dialkylamino, perfluoroalcoxy. L'invention concerne également un sel pharmaceutiquement acceptable de ces composés ainsi que des compositions pharmaceutiques et des méthodes de traitement utilisant lesdits composés.

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