Patent ID: 6025349
Filing Date: 2000-02-15
Classification: A61P,C07C,Y10S

Abstract:
A phenyl-substituted alkenylcarboguanidide carrying perfluoroalkyl groups, of the formula I ##STR7## in which R(A) is hydrogen, F, Cl, Br, I, CN, OH, OR(6), (C.sub.1 -C.sub.8)-alkyl, O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+ 1, (C.sub.3 -C.sub.8)-cyclo-alkyl or NR(7)R(8);r is zero or 1;a is zero, 1, 2, 3 or 4;b is 1, 2, 3, 4, 5, 6, 7 or 8;R(6) is (C.sub.1 -C.sub.8)-alkyl, (C.sub.1 -C.sub.4)-perfluoroalkyl, (C.sub.3 -C.sub.8)-alkenyl, (C.sub.3 -C.sub.8)-cycloalkyl, phenyl or benzyl,where the aromatic radicals phenyl or benzyl are unsubstituted or substituted by 1-3 substituents from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(9)R(10);R(9) and R(10) are, independently of one another, H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-perfluoroalkyl;R(7) and R(8) are defined independently of one another as R(6); orR(7) and R(8) together are 4 or 5 methylene groups, of which one CH.sub.2 group can be replaced by oxygen, sulfur, NH, N--CH.sub.3 or N-benzyl;R(B) is independently defined as R(A);X is zero, 1 or 2;Y is zero, 1 or 2;R(C) is hydrogen, F, Cl, Br, I, CN, OR(12), (C.sub.1 -C.sub.8)-alkyl, O.sub.p (CH.sub.2).sub.f C.sub.g F.sub.2g+1 or (C.sub.3 -C.sub.8)-cycloalkyl;p is zero or 1;f is zero, 1, 2, 3 or 4;g is 1, 2, 3, 4, 5, 6, 7 or 8;R(12) is (C.sub.1 -C8)-alkyl, (C.sub.1 -C.sub.4)-perfluoroalkyl, (C.sub.3 -C8)-alkenyl, (C.sub.3 -C.sub.8) -cycloalkyl, phenyl or benzyl,where the aromatic radicals phenyl or benzyl are unsubstituted or substituted by 1-3 substituents from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(13)R(14);R(13) and R(14) are independently of one another H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-perfluoroalkyl;R(D) is defined independently as R(C);R(1) is hydrogen, (C.sub.1 -C.sub.8)-alkyl, -O.sub.t (CH.sub.2).sub.d C.sub.e F.sub.2e+1, (C.sub.3 -C.sub.8)-cycloalkyl, F, Cl, Br, I or CN;t is zero or 1;d is zero, 1, 2, 3 or 4;e is 1, 2, 3, 4, 5, 6, 7 or 8;R(2), R(3), R(4) and R(5) are defined independently of one another as R(1);but with the condition that at least one of the substituents R(A), R(B), R(C), R(D), R(1), R(2), R(4) or R(5) is a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1, O.sub.p (CH.sub.2).sub.f C.sub.g F.sub.2g+1 or O.sub.t (CH.sub.2).sub.d C.sub.e F.sub.2e+1 group and R (3) is not a O.sub.t (CH.sub.2).sub.d C.sub.e F.sub.2e+1 group;as well as the pharmaceutically suitable salts thereof.