Patent ID: 6093729
Filing Date: 2000-07-25
Classification: A61P,C07D

Abstract:
A bicyclic heteroaroylguanidine of the formula I ##STR18## in which: T, U, V, W, X, Y and Zare, independently of each other, nitrogen or carbon, with, however, the restriction that only one of the positions T, U, V, W, X, Y or Z is nitrogen, and that T, U, V, W, X, Y and Z do not carry any substituent when they are nitrogen,that T, U, V, W, X, Y and Z are not carbon at the same time; andthat R(3), R(4), R(5), R(6) and R(7) are not all hydrogen at the same time whena) T, U, V, W, X and Z are carbon and Y is nitrogen,orb) T, U, V, W, Y and Z are carbon and X is nitrogen;R(1) and R(2)are, independently of each other, hydrogen, F, Cl, Br, I, (C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.3)-perfluoroalkyl, OR(8) or NR(8)R(9);R(8) and R(9)are, independently of each other, hydrogen or (C.sub.1 -C.sub.3)-alkyl, orR(8) and R(9)are together 4 or 5 methylene groups of which one CH.sub.2 group can be replaced by oxygen, S, NH, N--CH.sub.3 or N-benzyl,R(3), R(4), R(5), R(6) and R(7)are, independently of each other, hydrogen, F, Cl, Br, I, --C.tbd.N, CF.sub.3, CH.sub.3 SO.sub.2 or CH.sub.3 CO;orR(3), R(4), R(5), R(6) and R(7)are, independently of each other, (C.sub.1 -C.sub.4)-alkyl or --C.sub.al H.sub.2al R(18);al is zero or 1;R(18) is phenyl, which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(19a)R(19b);R(19a) and R(19b)are hydrogen, CH.sub.3 or CF.sub.3 ;orR(3), R(4), R(5), R(6) and R(7)are independently of each other, (C.sub.1 -C.sub.9)-heteroaryl which is linked via C or N and which is unsubstituted or substituted by 1-3 substituents from the group consisting of F, Cl, CF.sub.3, CH.sub.3, methoxy, hydroxyl, amino, methylamino and dimethylamino;orR(3), R(4), R(5), R(6) and R(7)are, independently of each other, SR(29), --OR(30), --NR(31)R(32) or --R(33)R(34)R(35);R(29), R(30), R(31) and R(33) are, independently of each other, --C.sub.a H.sub.2a --(C.sub.1 -C.sub.9)-heteroaryl which is unsubstituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF.sub.3, CH.sub.3, methoxy, hydroxyl, amino, methylamino and dimethylamino;a is zero, 1 or 2;R(32), R(34) and R(35)are, independently of each other, defined as R(29) or hydrogen, CH.sub.3 or CF.sub.3 ;orR(3), R(4), R(5), R(6) and R(7)are, independently of each other, NR(84a)R(85), OR(84 b) or --C.sub.n H.sub.2n --R(84d);n is zero or 1;R(84d) is phenyl which is not substituted or is substituted by 1-3 substituents from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(16)R(17);R(16) and R(17)are hydrogen or CH.sub.3 ;R(84a), R(84b) and R(85)are, independently of each other, hydrogen, (C.sub.1 -C.sub.4)-alkyl,CF.sub.3 or (CH.sub.2)ax-R(84g);ax is zero or 1;84 g is phenyl which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(84u) and R(84v) are hydrogen or CH.sub.3 ;orR(84a) and R(85)are together 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,or a pharmaceutically tolerated salt thereof.