[EN] PIPERIDINE-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY<br/>[FR] COMPOSES PIPERIDINE-INDOL AYANT UNE AFFINITE AVEC 5-HT6
申请人:ALLELIX BIOPHARMA
公开号:WO2000063203A1
公开(公告)日:2000-10-26
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 C¿1-4?alkyl; R?2¿ is selected from the group consisting of H, C¿1-4?alkyl and benzyl; ----- represents a single or double bond; R?3¿ is selected from the group consisting of COR5 and SO¿2?R?5; R4a¿ is selected from the group consisting of H, OH, halo, C¿1-4?alkyl and C1-4alkoxy; R?4b¿ is selected from the group consisting of H, hydroxy, halo, C¿3-7?cycloalkyloxy, C1-4alkoxy, C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R?4c¿ is selected from the group consisting of H, OH, halo, C¿1-4?alkyl and C1-4alkoxy; R?4d¿ is selected from the group consisting of H, OH, halo, C¿1-4?alkyl and C1-4alkoxy; and R?5¿ is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C¿1-4?alkoxy, 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.