Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1993-02-10
1994-12-13
O'Sullivan, Peter
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514522, 514603, 514634, 514821, 558413, 564 86, 564162, 564237, C07C27922, A61K 3118, A61K 31155
Patent
active
053730240
ABSTRACT:
Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --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 C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --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 ##STR2## 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.sup.+ /H.sup.+ exchanger).
REFERENCES:
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Duff et al., "Amiloride", Circulation, vol. 79, No. 6, Jun. 1989 pp. 1257-1263.
Eur. Heart of J.9 (suppl. 1):25 and 167 (1988) book of abstracts.
A. Schmid et al., "Na.sup.+ /H.sup.+ Exchange in Porcine Cerebral Capillary Endothelial Cells is Inhibited by a Benzoylguanidine Derivative," Biochemical and Biophysical Research Communications, Apr. 15, 1992, pp. 112-117.
Albus Udo
Englert Heinrich
Lang Florian
Lang Hans-Jochen
Mania Dieter
Hoechst Aktiengesellschaft
O'Sullivan Peter
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