| 摘要 |
Pyranopyridine 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, CH3, OCH3, sulphamoyl or methanesulphonyl); or R1+R2 = 2-10C alkylene (with one CH2 group optionally replaced by O, CO, S, SO, SO2 or NR10); R10 = H or 1-3C alkyl; R3 = R12-CaH2aÄNR13)Üm-; R12 = H, 3-8C cycloalkyl, CF3, C2H5 or C3H7; a = 0-10; m = 0 or 1; R13 = H or 1-6C alkyl; or R12+R13 = 4-8C alkylene (with one CH2 group optionally replaced by O, S, SO, SO2, CO or NR10); R4 = R14-CrH2r-; r = 0-20; R14 = H, 3-8C cycloalkyl, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, CF3, C2H5, C3H7, pyridyl, thienyl, imidazolyl or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl, methanesulphonyl or methanesulphonylamino); one CH2 group in CrH2r may be replaced by O, CH=CH, CC, CO, COO, OCO, CO-R11, S, SO, SO2 or NR11; or R3+R4 = 3-8C alkylene (with one CH2 group optionally replaced by O, S, SO, SO2, CO or NR11); R11 = H or -(CaH2a)-R10 (with one CH2 group optionally replaced by O, CH=CH, CC, CO, COO, OCO, S, SO, SO2, NR10 or CONR10); R5+R6 = -CR15=CR16-CR17=N-, -CR15=CR16-N=CR17-, -CR15=N-CR17=N-, -CR15=N-N=CR17-, -N=CR16-CR17=N- or -S-CR15=CR16; R15, R16, R17 = H, F, Cl, Br, I, 1-4C alkyl, 3-8C cycloalkyl, CN, CF3, C2H5, C3H7, NO2, CONR19R21, COOR21, R22-CsH2s-Z or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl); R21 = H, methyl, ethyl, phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl) or CuH2uNR19R20 ; R19, R20 = H or 1-3C alkyl; u = 2 or 3; R22 = H, 3-8C cycloalkyl, COOR21, CONR19R21, thienyl, imidazolyl, pyridyl, quinolyl, isoquinolyl, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, CF3, C2H5, C3H7 or phenyl (optionally substituted by 1 or 2 F, Cl, Br, I, CF3, CH3, OCH3, sulphamoyl or methanesulphonyl); s = 0-6; Z = S, SO, SO2, CO, S-NR11, SO-NR11, SO2-NR11, SO2-O, O, NR11 or CO-NR11; R7 = H, OH, 1-4C alkoxy, 1-4C acyloxy, Cl, Br, F or 1-4C alkyl; and R8 = H or 1-6C alkyl. |
