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摘要

Compounds of the formula in whic: R(1) and R(2) independently of one another are hydrogen, CF3, C2F5, C3F7, alkyl having 1 to 6 carbon atoms, or phenyl, which is substituted or unsubstituted by 1 or 2 substituents, selected from the group consisting of F, Cl, Br, I, CF3, NO2, CN, NH2, OH, methyl, ethyl, methoxy, 2138 ה' בחשון התשס" ד - October 31, 2003 dimethylamino, sulfamoyl, methylsulfonyl and methylsulfonylamino; or R(1) and R(2) together are an alkylene chain having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms; R(3) is R(10)-CnH2n-NR(11)- or R(10)-CnH2n-, where one CH2 group in the groups CnH2n can be replaced by -O-, -CO-, -S-, -SO-, -SO2- or -NR(12a)-; R(12a) is hydrogen, methyl or ethyl; R(10) is hydrogen, methyl, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, CF3, C2F5 or C3F7; n is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; R(11) is hydrogen or alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms; or R(10) and R(11) together are a bond, provided n is not smaller than 3; or R(3) together with R(4) is an alkylene chain having 3, 4, 5, 6, 7 or 8 carbon atoms, where one CH2 group of the alkylene chain can be replaced by -O-, -CO-, -S-, -SO-, -SO2- or -NR(12a)-; R(12a) is hydrogen, methyl or ethyl; R(4) is R(13)-CrH2r, R(13) is H, CF3, C2F5, C3F7, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, -NR(15)R(16), -OR(17), -COOR(17), phenyl or an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, where phenyl and the N-containing heterocycle are unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of F, Cl, Br, I, CF3, NO2, CN, NH2, OH, methyl, ethyl, methoxy, dimethylamino, sulfamoyl, methylsufonyl and methylsulfonylamino; R(15) and R(16) independently of one another are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; or R(15) and R(16) together are a chain of 4 or 5 methylene groups, of which one CH2 group can be replaced by -O-, -S-, -NH-, N(CH3)- or -N(benzyl)-; R(17) is hydrogen, alkyl having 1, 2 or 3 carbon atoms, 2139 ה' בחשון התשס" ד - October 31, 2003 r is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20; at least one of the subsitutents R(5), R(6), R(7) and R(8) is -Y-CsH2s-R(18), thienyl, furyl or an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, where thienyl, furyl and the N-containing heterocycle are unsubstituted or substituted by 1 or 2 subsituents selected from the group consisting of F, Cl, Br, I, CF3, NO2, CN, NH2, OH, methyl, ethyl, methoxy, methylamino, dimethylamino, ethylamino, diethylamino, sulfamoyl, methylsulfonyl and methylsulfonylamino; Y is -O-, -CO-, -O-CO-, -S-, -SO-, -SO2-, -SO2-O-, -SO2NR(12d)-, NR(12d)- or -CONR(12d)-, where the linkage to the benzene nucleus in each case takes place via the left atom; R(12d) is hydrogen, methyl or ethyl; s is 1, 2, 3, 4, 5 or 6; R(18) is substituted phenyl which carries one or two substituents selected from the group consisting of NO2, CN, NH2, N(methyl)2, OH, ethyl, -COOH, -COO methyl, -COOethyl, -CONH2, -CON(methyl)2; or R(18) is a substituted N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, which carries one or 2 substituents selected from the group consisting of F, Cl, Br, I, CF3, NO2, CN, NH2, OH, methyl, ethyl, methoxy, dimethyl- amino, sulfamoyl, methylsulfonyl and methylsulfonylamino; or R(18) is -OR(19), -SO2R(19), -NR(19)R(20), -CONR(19)R(20); R(19) and R(20) independently of one another are CtH2t-R(21); t is zero, 1, 2, 3, 4, 5 or 6; R(21) is hydrogen, CF3, C2F5, C3F7, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, NR(22)R(23), -OR(24), phenyl, thienyl or an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, where phenyl, thienyl and the N-containing heterocycle are unsubstituted or substituted by 1 or 2 substituents selected from the group consisting of F, Cl, Br, I, CF3, NO2, CN, NH2, OH, methyl, ethyl, methoxy, dimethylamino, sulfamoyl, methylsufonyl and methylsulfonylamino; R(22) and R(23) independently of one another are hydrogen, alkyl having 1, 2 or 3 carbon atoms; or R(22) and R(23) together are a chain of 4 or 5 methylene groups, of which one CH2 group can be replaced by -O-, -S-, -NH-, -N(CH3)- or -N(benzyl)-; R(24) is hydrogen, alkyl having 1, 2 or 3 carbon atoms; and the other substituents R(5), R(6), R(7) and R(8) in each case, which are still not assigned by the definition given above, independently of one another are hydrogen, F, Cl, Br, I, alkyl having 1, 2, 3, 4, or 5 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7 or 8 carbon atoms, CN, CF3, NO2, OR(12e) or NR(12e) R (12f); R(12e) and R(12f) independently of one another are hydrogen or alkyl having 1, 2, 3 or 4 carbon atoms; R(9) is hydrogen, OR(12g) or OCOR(12g); R(12g) is hydrogen or alkyl having 1, 2 or 3 carbon atoms; B is hydrogen; or R(9) and B together are a bond; or their physiologically tolerable salts.