| abstract |
There are described ortho-substituted benzoylguanidines of the formula I <IMAGE> in which: R(1) is H, Hal, CN, NO2, (cyclo)alkyl, (O)(S)[NR(5)](CH2)b-(CF2)c-CF3, R(5) is H, (C1-C4)-alkyl, -CdH2dR(6), R(6) is cycloalkyl, (bi)phenyl(yl), naphthyl, or R(1) is -SR(10), -OR(10), -CR(10)R(11)R(12), R(10) is -CfH2f-(C3-C8)-cycloalkyl, -(C1-C9)-heteroaryl or phenyl, R(11) and R(12) are defined as R(10) or are hydrogen, (C1-C4)-alkyl, or R(1) is naphthyl, (bi)phenyl(yl), (C1-C9)-heteroaryl, or R(1) is -SR(13), -OR(13), -NHR(13), -NR(13)R(14), -CHR(13)R(15), -C[R(15)R(16)]OH, -C IDENTICAL CR(18), -C[R(19)]=CR(18), -[CR(20)R(21)]k-(CO)-[CR(22)R(23)R(24)]l, R(13) and R(14) are -(CH2)g-(CHOH)h-(CH2)l-(CHOH)j-R(17), R(17) is hydrogen, methyl, -(CH2)g-O-(CH2-CH2O)h-R(24), R(15) and R(16) are hydrogen, alkyl or, together with the carbon atom carrying them, cycloalkyl, R(18) is phenyl, heteroaryl, (cyclo)alkyl, R(19), R(20), R(21), R(22) and R(23) are hydrogen, methyl, R(24) is H, (cyclo)alkyl, -CmH2m-R(18), R(2) and R(3) are defined as R(1), R(4) is alkyl, Hal, CN, -(CH2)n-(CF2)o-CF3, and their pharmaceutically tolerable salts. Compounds I have no unwanted salidiuretic properties, but very good antiarrhythmic properties. They are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris, where they also preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischaemically induced damage. Because of their protective actions against pathological hypoxic and ischaemic situations, the compounds of the formula I according to the invention, as a result of inhibition of the cellular Na<+>/H<+> exchange mechanism, can be used as medicaments for the treatment of all acute or chronic damage caused by ischaemia or illnesses primarily or secondarily induced thereby. |