C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 317/32 (2006.01) A61K 31/155 (2006.01) A61K 31/18 (2006.01) A61K 31/33 (2006.01) C07C 311/47 (2006.01) C07C 317/44 (2006.01) C07C 323/15 (2006.01) C07D 207/337 (2006.01) C07D 209/18 (2006.01) C07D 213/56 (2006.01) C07D 213/58 (2006.01) C07D 215/14 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01)
Patent
CA 2099445
Abstract 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them Benzoylguanidines of the formula I Image (I) where R(1) is R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are alk(en)yl, -CnH2n-R(7), and where R(7) is cyclo- alkyl or phenyl, where R(5) is also H, R(6) is H or C1-C4- alkyl, R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl, R(3) is defined as R(2) and their pharmaceutically tolerable salts are described. The compounds I are obtained by reaction of compounds of the formula II (II) Image with guanidine, in which L is a leaving group which can be easily nucleophilically substituted. Compounds I are outstandingly suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct - 2 - 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 ischemically induced damage. Compounds I are moreover distinguished by strong inhibitory action on the proliferation of cells. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, and fibrotic diseases such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are active inhibitors of the cellular sodium- proton antiporter (Na+/H+ exchanger).
Albus Udo
Lang Florian
Lang Hans-Jochen
Scholz Wolfgang
Weichert Andreas
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Aktiengesellschaft
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