3,5-SUBSTITUTED BENZOYLGUANIDINES, PROCESS FOR THEIR PREPARATION, THEIR USE AS A MEDICAMENT OR DIAGNOSTIC AND MEDICAMENT CONTAINING THEM

摘要

HOE 92/F 034 3,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them Benzoylguanidines of the formula I ( I ) are described where R(1) is R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are alk(en)yl or -CnH2n-R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, O-(CH2)mCpF2p+1, -X-R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl- (methyl) or -CnH2n-R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts. The compounds I are obtained by reaction of compounds of the formula II ( I I ) with guanidine, in which L is a leaving group which can be easily nucleophilically substituted. Compounds I are outstandingly suitable as antiarrythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris, where they also preventively inhibit or greatly reduce the pathophysiological processes during the formation of ischemically induced damage. They are moreover distinguished by strong inhibitory action on the proliferation of cells. They can therefore be used as antiatherosclerotics, agents against late-onset diabetic complications, cancers, and fibrotic diseases such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/proton antiporter (Na+/H+ exchanger).