4-arylquinazolines and use thereof as nhe-3 inhibitors

Details 4-arylquinazolines and use thereof as nhe-3 inhibitors 4-arylquinazolines and use thereof as nhe-3 inhibitors

C - Chemistry, Metallurgy

07

D

C07D 239/84 (2006.01) A61K 31/517 (2006.01)

Patent

CA 2471524

The invention relates to compounds of formula (I), where Ar = phenyl or naphthyl substituted by X and additionally substituted by R3 and R4, Y = (A), (B) or (C), X = H, NR6R7 or a saturated 5-7 membered ring with two N atoms, R1, R2, R3, R4 independently = H, A, OA, Hal, CF3, OH, NO2, NH2, NHA, NA2, NH- CO-A, NH-CO-Ph, SA, SO-A, SO2-A, SO2-Ph, CN, OCF3, CO-A, CO2H, CO2A, CO-NH2, CO-NHA, CO-NA2, SO2NH2, SO2NHA, SO2NA2 or unsubstituted or mono- or poly- substituted phenyl with A, OA, Hal or CF3, the salts, solvates and use thereof as NHE-3 inhibitors.

L'invention concerne des composés de formule (I), dans laquelle Ar est phényl ou naphtyl substitué par X, également substitué par R<sp>3 </sp> et R<sp>4</sp> ; Y est (A), (B) ou (C)? ¿; X est H, NR<sp>6</sp>R<sp>7</sp> ou un cycle saturé à 5-7 éléments comportant deux atomes de N ; et, R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, R<sp>4</sp> sont indépendamment l'un de l'autre H, A, OA, Hal, CF<sb>3</sb>, OH, NO<sb>2</sb>, NH<sb>2</sb>, NHA, NA<sb>2</sb>, NH-CO-A, NH-CO-Ph, SA, SO-A, SO<sb>2</sb>-A, SO<sb>2</sb>-Ph, CN, OCF<sb>3</sb>, CO-A, CO<sb>2</sb>H, CO<sb>2</sb>A, CO-NH<sb>2</sb>, CO-NHA, CO-NA<sb>2</sb>, SO<sb>2</sb>NH<sb>2</sb>, SO<sb>2</sb>NHA, SO<sb>2</sb>NA<sb>2</sb> ou phényl non susbstitué ou substitué une ou plusieurs fois par A, OA, Hal ou CF<sb>3</sb>. L'invention concerne également les sels et solvates desdits composés ainsi que leur utilisation en tant qu'inhibiteurs de NHE-3.

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