| abstract |
Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: 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 these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia. |