Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing them

US5559153A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Jan-Robert Schwark · Frankfurt am Main, DE
• Hans-Jochen Lang · Hofheim, DE
• Heinz-Werner Kleemann · Bischofsheim, DE
• Andreas Weichert · Egelsbach, DE
• Wolfgang Scholz · Beverly, US
• Udo Albus · Florstadt, DE

Key dates

• Filing date: Aug 11, 1994
• Grant date: Sep 24, 1996
• Expiry date: Aug 11, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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, wi…