3-(2-PYRROLIDINYLMETHYL)-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY

摘要

Described herein are 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; R?3¿ is selected from the group consisting of COR5, SO2R5, CONHC¿1-4?alkyl and C(S)SR?6; 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; 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-; and R?6¿ is selected from C¿1-4?alkyl, allyl, propargyl and optionally substituted benzyl wherein the benzyl group is optionally substituted with 1-4 substituents selected from cyano, C1-4alkyl and halo. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.