Sulfonamidsubstituerte kondenserte 7-ringforbindelser, deres anvendelse som medikament samt farmasöytiske preparater inneholdende forbindelsene

摘要

Benzoxepine and benzocycloheptane derivatives of formula (I), their stereoisomers and salts are new. X1 = O, S, SO, SO2, CR1R2, NR6, CO or CR1R7; R1, R2 = H, CF3, C2F5, C3F7, 1-6C alkyl or phenyl (optionally substituted by 1 or 2 of halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me; or R1+R2 = 2-10C alkylene; R6 = H or CnH2nR8 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR9 or CONR9; R9 = H or 1-4C alkyl; n = 0-8; R8 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NMe2, NEt2, piperidino, pyrrolidino, morpholino, 4-methyl-1-piperazinyl or pyridyl, thienyl, imidazolyl or phenyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); X2 = CR1R2 or CR2R10; or X2 = O, S, SO, SO2 or NR6 if X3 and X1 are CR1R2; R10+R7 = bond; X3 = CR1R2; or X3 = O, S, SO, SO2 or NR6 if X2 and X4 are CR1R2; X4 = CR1R2, NR6, NR11, CH(OR30) or CR2R11; R30 = H, 1-3C alkyl or 1-4C acyl; R11+R5 = bond; Y1-Y4 = CR12 or N with no more than two being N; R12 = H, halo, 1-5C alkyl, 3-8C cycloalkyl, CN, CF3, C2F5, C3F7, N3, NO2, ZCmH2mR13 or phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); Z = O, CO, COO, OCO, S, SO, SO2, SO2NR14, NR14 or CONR14; R14 = H or 1-3C alkyl; m = 0-6; R13 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR15R16, CONR15R16, OR30a or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R15, R16 = H or 1-3C alkyl; or R15+R16 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); R30a = H, 1-3C alkyl or 1-4C acyl; or Y1+Y2 = S and Y3, Y4 = CR12; R3 = NR18CxH2xR17 or CxH2xR17 (with one CH2 group optionally replaced by O, CO, S, SO, SO2 or NR19); R19 = H, Me or Et; R17 = H, Me, 3-8C cycloalkyl, CF3, C2F5 or C3F7; x = 0-10; R18 = H or 1-8C alkyl; or R18+R17 = bond if x = 3-10; or R3 = phenyl (optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); or R3+R4 = 3-8C alkylene (with one CH2 optionally replaced by O, CO, S, SO or SO2); R4 = CrH2rR20 (with one CH2 group optionally replaced by O, CH=CH, C IDENTICAL C, CO, COO, OCO, S, SO, SO2, NR21 or CONR21); R21 = H or 1-3C alkyl; r = 0-20; R20 = H, CF3, C2F5, C3F7, 3-8C cycloalkyl, NR22R23 or phenyl, thienyl or 1-9C N-containing heterocyclyl (all optionally substituted by 1 or 2 halo, CF3, NO2, CN, NH2, OH, Me, Et, OMe, NMe2, SO2NH2, SO2Me and NHSO2Me); R22, R23 = H or 1-3C alkyl; or R22+R23 = 4-5C methylene (with one carbon optionally replaced by O, S, NH, NMe or N(benzyl)); and R5 = H; or R5+R11 = bond.