摘要 |
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 C1-4alkyl; R2 is selected from the group consisting of H , C1-4alkyl and benzyl; ----- represents a single or double bond; R3 is select ed 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 th e 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 the compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
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申请人 |
ALLELIX BIOPHARMACEUTICALS INC. |
发明人 |
SLASSI, ABDELMALIK;O'BRIEN, ANNE;EDWARDS, LOUISE;XIN, TAO;TEHIM, ASHOK |