发明名称 HEXAHYDRO-PYRIDO[4,3-B]INDOLE DERIVATIVES AND THEIR USE AS ANTIPSYCHOTIC DRUGS
摘要 Hexahydro-pyrido(4,3-b)indole derivatives of formula (I), their N-oxides, salts and stereoisomers are new. Alk = 1-6C alkanediyl; R1 = H, 1-6C alkyl, aryl or aryl(1-6C alkyl); R2-R4 = H, halo, OH, NO2, CN, CF3, 1-6C alkyl, 1-6C alkyloxy, 1-6C alkylthio, mercapto, amino, mono- or di(1-6C alkyl)amino, carboxyl, 1-6C alkyloxycarbonyl or 1-6C alkylcarbonyl; R5 = H, 1-6C alkyl, phenyl or phenyl(1-6C alkyl); R6 = H, 1-6C alkyl, 1-6C alkyloxy, 1-6C alkylthio or NR8R9; R8, R9 = H, 1-6C alkyl, phenyl or phenyl(1-6C alkyl); R7 = H or 1-6C alkyl; or R6+R7 = a bivalent radical -R6-R7- which may be CH2CH2CH2 (a1), CH2CH2CH2CH2 (a2), CH=CHCH2 (a3), CH2CH=CH (a4), CH=CHCH=CH (a5); SCH2CH2 (a6), SCH2CH2CH2 (a7), SCH=CH (a8), NHCH2CH2 (a9), NHCH2CH2CH2 (a10), NHCH=CH (a11), NHCH=N (a12), SCH=N (a13) or CH=CH-O (a14); (a1)-(a5) are all optionally mono- or disubstituted by halo, 1-6C alkyl, aryl(1-6C alkyl), CF3, amino, OH, 1-6C alkyloxy or 1-10C alkylcarbonyloxy, or where possible two geminal H atoms are replaced by 1-6C alkylidene or aryl(1-6C alkylidene); and (a6)-(a14) are all optionally mono-, di- or trisubstituted by 1-6C alkyl or aryl; aryl = phenyl optionally substituted by up to three of halo, OH, NO2, CN, CF3, 1-6C alkyl, 1-6C alkyloxy, 1-6C alkylthio, mercapto, amino, mono- or di(1-6C alkyl)amino, carboxyl, 1-6C alkyloxycarbonyl and 1-6C alkylcarbonyl.
申请公布号 HU9903110(A2) 申请公布日期 2000.01.28
申请号 HU19990003110 申请日期 1997.05.15
申请人 Janssen Pharmaceutica N.V. 发明人 KENNIS, LUDO EDMOND JOSEPHINE;MERTENS, JOSEPHUS CAROLUS
分类号 A61K31/505;C07D471/04 主分类号 A61K31/505
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