Piperidine-indole compounds having 5-ht6 affinity

Details Piperidine-indole compounds having 5-ht6 affinity Piperidine-indole compounds having 5-ht6 affinity

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/4439 (2006.01) A61K 31/454 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2370147

Described herein are indole compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein, R1 is selected from the group consisting of H and C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; represents a single or double bond; R3 is selected from the group consisting of COR5 and SO2R5; R4a is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4b is selected from the group consisting of H, hydroxy, halo, C3-7cycloalkyloxy, C1-4alkoxy, C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R4c is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R4d is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; and R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C1-4alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2-methylenedioxy, C1-4alkylcarbonyl, C1-4alkoxycarbonyl and C1-4alkylS-. Also described is the use of the compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

La présente invention concerne des composés indols ayant une affinité avec le récepteur 5-HT6, représentés par la formule générale (I). Dans cette formule R<1> est H ou C1-4 alkyle; R<2> est H, C1-4 alkyle ou benzyle; ----- représente une simple ou une double liaison; R<3> est COR<5> ou SO2R<5>; R<4a> est H, OH, halo, C1-4 alkyle ou C1-4 alcoxy; R<4b> est H, hydroxy, halo, C3-7 cycloalkyloxy, C1-4 alcoxy, C1-4 alkyle, benzyloxy, phénoxy, trifluorométhyle, trifluorométhoxy ou vinyle; R<4c> est H, OH, halo, C1-4 alkyle ou C1-4 alcoxy; R<4d> est H, OH, halo, C1-4 alkyle ou C1-4 alcoxy; et R<5> est phényle, pyridyle, thiényle, quinolinyle ou naphthyle, groupes éventuellement 1-4 substitués par C1-4 alcoxy, C1-4 alkyle, halo, nitro, trifluorométhyle, trifluorométhoxy, 1,2-methylènedioxy, C1-4 alkylecarbonyle, C1-4 alcoxycarbonyle ou C1-4 alkyleS-. Cette invention concerne aussi l'utilisation de ces composés comme produits pharmaceutiques destinés à traiter des cas dans lesquels l'inhibition du récepteur 5-HT6 est concernée, par exemple dans la schizophrénie.

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