Patent ID: 6703411
Filing Date: 2004-03-09
Classification: A61P,C07D

Abstract:
A benzoylguanidine of the formula (I) in which:R1 is hydrogen, F, Cl, Br, I, NO2, CN, â€”Xoâ€”(CH2)pâ€”(CF2)qâ€”CF3, R5â€”SOmâ€”, R6â€”COâ€”, R6R7Nâ€”COâ€”, or R6R7Nâ€”SO2â€”; X is oxygen, â€”Sâ€”, or NR14; m is zero, 1, or 2; o is zero or 1; p is zero, 1, or 2; q is zero, 1, 2, 3, 4, 5, or 6; R5 and R6 each independently of one another are selected from (C1-C8)-alkyl, (C3-C6)-alkenyl, â€”CnH2nâ€”R8, and CF3; n is zero, 1, 2, 3, or 4; R8 is (C3-C7)-cycloalkyl, or phenyl which is unsubstituted, or is substituted by 1 to 3 substituents each independently selected from F, Cl, CF3, methyl, methoxy and NR9R10; R9 and R10 are each independently selected from H and (C1-C4)-alkyl; or R6 is hydrogen; R7 is hydrogen or (C1-C4)-alkyl; or R6 and R7 together can be 4 or 5 methylene groups, of which one methylene group is optionally replaced by oxygen, S, NH, Nâ€”CH3, or N-benzyl; R2 is â€”Y-p-(C6H4)â€”R11, â€”Y-m-(C6H4)â€”R11, or â€”Y-o-(C6H4)â€”R11; R11 is (C1-C9)-heteroaryl, which is linked via C or N and which is unsubstituted or substituted by 1 to 3 substituents each independently selected from F, Cl, CF3, CH3, methoxy, hydroxyl, amino, methylamino, dimethylamino, and benzyl; Y is oxygen, â€”Sâ€”, or NR12; R12 is H or (C1-C4)-alkyl; R3 is defined as R1; or R3 is (C1-C6)-alkyl or â€”Xâ€”R13; X is oxygen, â€”Sâ€” or NR14; R14 is H or (C1-C3)-alkyl; R13 is H, (C1-C6)-alkyl, (C3-C8)-cycloalkyl, or â€”CbH2bâ€”R15; b is zero, 1, 2, 3 or 4; R15 is phenyl which is unsubstituted or substituted by 1 to 3 substituents each independently selected from F, Cl, CF3, methyl, methoxy, and NR9R10; R9 and R10 are each independently selected from H and (C1-C4)-alkyl; or R13 and R14 together are 4 or 5 methylene groups, of which one methylene group is optionally replaced by oxygen, S, NH, Nâ€”CH3, or N-benzyl; R4 is F, Cl, Br, I, or C1-C4-alkyl; or a pharmaceutically tolerated salt thereof.