Patent ID: 6600072
Filing Date: 2003-07-29
Classification: A61P,C07C

Abstract:
A substituted 1-naphthoylguanidine of the formula Iin which:R2, R3, R4, R5, R6, R7 and R8 independently of one another are H, F, Cl, Br, I, CN, NO2, CF3, C2F5 or XaYbZ, but at least one of the substituents R2, R3, R4, R5, R6, R7 and R8 is not equal to hydrogen; X is O, S, NR(10), CR(11)R(12), C&boxH;O, C(&boxH;O)NR(10), C(&boxH;O)O, SO, SO2, SO2NR(10), OC&boxH;O, NR(10) C&boxH;O or NR(10)SO2, where the linkage with the naphthalene ring in each case takes place via the left atom; R(10), R(11) and R(12) independently of one another are H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; a is 1; Y is alkylene having 1, 2, 3, 4, 5, 6, 7 or 8 CH2 groups, where one of these CH2 groups can be replaced by O, S, NR(13) or o-, p- or m-phenylene; R(13) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5 or 6 carbon atoms; b is zero or 1; Z is alkyl having 1, 2, 3, 4, 5, 6 or 7 carbon atoms, cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms, C(&boxH;O)R(15), SO2R(15), NR(16)R(17) or phenyl, which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, CF3, methyl, methoxy and NR(21)R(22); R(21) and R(22) independently of one another are H, alkyl having 1, 2, 3 or 4 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; R(1 5) is N&boxH;C(NH2)2, NR(18)R(19), N(CH2)cNR(18)R(19) or OR(20); c is 2 or 3; R(18) and R(19) independently of one another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; or R(18) and R(19) together are 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, Nâ€”CH3, N-benzyl or N-(p-chlorophenyl); R(20) is H, alkyl having 1, 2, 3, 4, 5 or 6 carbon atoms, perfluoroalkyl having 1, 2, 3 or 4 carbon atoms or cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; R(16) and R(17) independently of one another are H, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or perfluoroalkyl having 1, 2, 3 or 4 carbon atoms; or R(16) and R(17) together are 4 or 5 methylene groups, of which one CH2 group can be replaced by oxygen, S, NH, Nâ€”CH3, N-benzyl or N-(p-chlorophenyl); or Z is an N-containing heterocycle having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, where the N-containing heterocycle is linked via N or C and is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, CF3, methyl, methoxy and NR(21)R(22); but where, in the case where R(4) is an alkoxy radical, at least one of the substituents R(2), R(3), R(5), R(6), R(7) and R(8) is not equal to hydrogen; or its pharmaceutically tolerable salts.