| 摘要 |
4-Sulphonamido-chroman derivatives of formula (I) and their salts are new: R1, R2 = H, CF3, C2F5, C3F7, 1-6C alkyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, Me, OMe, SONH2 and/or SO2Me); or CR1R2 = 2-10C alkylene; Ra = OH, 1-6C alkanoyloxy or 1-6C alkylsulphonyloxy; Rb = H; or Ra+Rb = bond; R3 = R9-CnH2n(NR11)m- (one CH2 group of CnH2n is optionally replaced by O, S, SO, SO2 or NR10); R9 = H or 3-8C cycloalkyl; n = 0-10; m = 0 or 1; R11 = H or 1-6C alkyl; or R9+R11 = 1-8C alkylene; R10 = H, Me or Et; R4 = R12-CrH2r- (one CH2 of CrH2r is optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, S, SO, SO2 or NR10); R12 = H, 3-8C cycloalkyl, piperidinyl, pyrrolidino, N-morpholino, N-methyl-piperazino, CF3, C2F5 or C3F7, pyridyl, thienyl, imidazolyl or phenyl (the latter 4 all optionally substituted by 1 or 2 of F, Cl, Br, I, CF3, Me, OMe, SO2NH2, S2Me and NHSO2Me); r = 0-20; R5-R8 = H, F, Cl, Br, I, 1-6C alkyl, 3-8C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, CONR13R14, CO2R15, CsH2s-Y- or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, Me, OMe, SO2NH2 and SO2Me); R13, R14 = H or 1-3C alkyl; R15 = H, Me, Et, Ph or -CuH2u-NR13R14; u = 2 or 3; R16 = H, 3-8C cycloalkyl, CO2R15, thienyl, imidazolyl, pyridyl, quinolyl, isoquinolyl, piperidyl, pyrrolidino, morpholino, N-methyl-piperazino, CF3, C2F5, C3F7 or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, Me, OMe, SO2NH2 and SO2Me); s = 0-6; Y = S, SO, SO2, CO, SO2NR10, O, NR10 or CONR10; provided that two of R5-R8 are not H.
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