3,5-substituted benzoylguanidines, process for their...

Details 3,5-substituted benzoylguanidines, process for their... 3,5-substituted benzoylguanidines, process for their...

C - Chemistry, Metallurgy

07

C

C07C 317/32 (2006.01) A61K 31/16 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07C 217/44 (2006.01) C07C 311/16 (2006.01) C07C 311/47 (2006.01) C07C 323/65 (2006.01) C07D 295/26 (2006.01)

Patent

CA 2089439

Benzoylguanidines of the formula I (see formula I) are described where R(1) is R(4)-SO m or R(5)R(6)N-SO2-, where R(4) and R(5) are alk(en)yl or -C n H2- 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)m C p F2p+11, -X-R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl-(methyl) or -C n H2n-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 (see formula II). 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).

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