发明名称 PIPERIDINE-INDOLE COMPOUNDS HAVING 5-HT6 AFFINITY
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.
申请公布号 CA2370147(A1) 申请公布日期 2000.10.26
申请号 CA19992370147 申请日期 1999.04.21
申请人 ALLELIX BIOPHARMACEUTICALS INC. 发明人 SLASSI, ABDELMALIK;O'BRIEN, ANNE;EDWARDS, LOUISE;XIN, TAO;TEHIM, ASHOK
分类号 A61K31/454;A61P21/00;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P43/00;C07D401/04;C07D409/14;(IPC1-7):C07D401/04 主分类号 A61K31/454
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