| 摘要 |
The invention concerns compounds of formula (I) in which R1 and R2 represent hydrogen, halogen, -NH2, -OH, -NO2, -CN, (C1-C6)alkyl, (C1-C6)alkoxy, -CF3, -OCF3, -COOH, -COOR4; -CONH2, -CONHR4, -CONR4R5, -SR4, -SO2R4, -NHCOR4, -NHSO2R4, -N(R4)2, (R4 and R5 represent (C1-C4)alkyl); R3 represents hydrogen, (C1-C6)alkyl, -(CH2)pOH, -(CH2)nCH(OH) (CH2)nOH, -(CH2)pNH2, -(CH2)pNHR7; (R7 = -C (=NH)-NH2), -(CH2)pNH2, -(CH2)nCOOH, -(CH2)nCOOR4, -(CH2)nCN, -(CH2)n-tetrazol-5-yl, (a) (G = -CH2-, -CH(OH)- or -NH-), -(CH2)nCONHR8 (R8 = -OH, (C1-C4) alkoxy or 1-methylpiperidin-4-yl), -(CH2)nCONH(CH2)nR9 (R9 = hydroxy or -NR4R5), (CH2)nCONAA (AA = amino acid), -(CH2)nCONH2, -(CH2)pSH, -(CH2)nSO3H, -(CH2)nSO2NH2, -(CH2)nSO2NHR4, -(CH2)nSO2NR4R5, -(CH2)nCONHR4, -(CH2)nCONR4R5, -(CH2)pNHSO2R4, -(CH2)pNHCOR4, -(CH2)pOCOR4 (n = 1 to 4 and p = 2 to 4), Q represents two hydrogen atoms or an oxygen atom, Z is -N- or -CH-, A is (1) or (2) (b) B being nitrogen, oxygen, sulphur, -NH or -NR4 and R6 identical to R1 and R2 but independent. The compounds have serotonin antagonist properties.
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