| 摘要 |
Described herein are indole compounds with affinity for the 5-HT6 receptor, which have general formula (I) wherein, R<1> is selected from the group consisting of H and C1-4alkyl; R<2> is selected from the group consisting of H, C1-4alkyl and benzyl; ----- represents a single or double bond; R<3> is selected from the group consisting of COR<5> and SO2R<5>; R<4a> is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R<4b> is selected from the group consisting of H, hydroxy, halo, C3-7cycloalkyloxy, C1-4alkoxy, C1-4alkyl, benzyloxy, phenoxy, trifluoromethyl, trifluoromethoxy and vinyl; R<4c> is selected from the group consisting of H, OH, halo, C1-4alkyl and C1-4alkoxy; R<4d> is selected from the group consisting of H, OH, halo, C1-4alkyl 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 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. |
