PYRROLIDINE-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 C1-4alkyl; R2 is selected from the group consisting of H, C1-4alkyl and benzyl; R3 is selected from the group consisting of COR5, SO2R5, CONHC1-4alkyl and C(S)SR6; R4a is selected from the group consisting of H, OH, halo, C14alkyl 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; R5 is selected from the group consisting of phenyl, pyridyl, thienyl, quinolinyl and naphthyl which are optionally substituted with 1-4 substituents selected from C14alkoxy, C1-4alkyl, halo, nitro, trifluoromethyl, trifluoromethoxy, 1,2methylenedioxy, C1-4alkylcarbonyl, C1-4alkoxycarbonyl and C1-4alkylS-; and R6 is selected from C1-4alkyl, 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 5HT6 receptor is implicated, such as schizophrenia.