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US 5,849,775 AGranted
Substituted benzoylguanidines process for their preparation, their use as a medicament or diagnostic, and pharmaceutical containing them
AssigneeHoechst Aktiengesellschaft
InventorsJan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
Life of this patent
Estimating the term…
Abstract
Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
Claims22
A benzoylguanidine of the formula I ##STR6## in which:
- R(1) is R(6)--CO;
- R(6) being (C.sub.1 -C.sub.8)-alkyl, (C.sub.1 -C.sub.8)-perfluoroalkyl, (C.sub.3 -C.sub.8)-alkenyl or --C.sub.n H.sub.2n --R(9),
- n being zero, 1, 2, 3 or 4,
- R(9) being (C.sub.3 -C.sub.8)-cycloalkyl, phenyl, biphenylyl or naphthyl, where the aromatic radicals are unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, CF.sub.3, methyl, methoxy and NR(10)R(11);
- R(10) and R(11) being H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-perfluoroalkyl;
- R(2) is (C.sub.1 -C.sub.9)-heteroaryl, which is linked via C or N and which is unsubstituted or 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;
- or
- R(2) is SR(18), --OR(18), --NR(18)R(19) or --CR(18)R(19)R(20);
- R(18) is --C.sub.a H.sub.2a --(C.sub.1 -C.sub.9)-heteroaryl, which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, CF.sub.3, CH.sub.3, methoxy, hydroxyl, amino, methylamino or dimethylamino;
- a is zero, 1 or 2;
- R(19) and R(20) independently of each other, are defined as R(18) or are hydrogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-perfluoroalkyl;
- or
- R(2) is R(22)R(23)N--SO.sub.2 --;
- wherein R(22) and R(23) together are 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;
- or
- R(2) is --C.tbd.CR(45), or --CR(46)=CR(45)
- wherein R(45) is (C.sub.1 -C.sub.9)-heteroaryl, which is unsubstituted or substituted by phenyl;
- and R(46) is hydrogen or methyl;
- R(3) is defined as R(1) or R(2);
- R(4) and R(5) are, independently of each other, defined as R(2);
- and pharmaceutically tolerated salts thereof.
18 more elements
Dependencies are inferred from the claim text.