Urea-substituted benzoylguanidines, process for their preparatio

Details Urea-substituted benzoylguanidines, process for their preparatio Urea-substituted benzoylguanidines, process for their preparatio

1994-08-11

1996-09-24

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...

514255, 5142375, 514330, 514423, 514586, 544160, 544168, 544169, 544390, 546226, 548538, 564 27, 564 51, A61K 3116, A61K 31535, A61K 3140, A61K 31445

Patent

active

055591531

ABSTRACT:
Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing them
There are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,
the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).
On account of their pharmacological properties, the compounds are outstandingly suitable for use as anti-arrhythmic pharmaceuticals having a cardioprotective component for the prophylaxis and treatment of infarction as well as for the treatment of angina pectoris, the compounds also inhibiting or strongly reducing, in a preventive manner, the pathophysiological processes in association with the occurrence of ischemically induced damage, in particular in association with the elicitation of ischemically induced cardiac arrhythmias.
They are obtained by reacting a compound of the formula II. ##STR2## in which L is a leaving group which can readily be substituted nucleophilically, with guanidine.

REFERENCES:
patent: 3780027 (1973-12-01), Cragoe, Jr. et al.
patent: 4024183 (1977-05-01), Swallow
patent: 5091394 (1992-02-01), Englert et al.
patent: 5292755 (1994-03-01), Englert et al.

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