3,5-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them.

摘要

There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na<+>/H<+> exchanger).