Substituted benzoylguanidines, process and their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing them

US5665739A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Hans-Jochen Lang · Hofheim, DE
• Heinz-Werner Kleeman · Bischofsheim, DE
• Wolfgang Scholz · Beverly, US
• Udo Albus · Florstadt, DE

Key dates

• Filing date: May 15, 1995
• Grant date: Sep 9, 1997
• Expiry date: May 15, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D215/20
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Benzoylguanidines of the formula I are described ##STR1## in which R(1)=hydrogen, Hal, --NO.sub.2, --C.tbd.N, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, R(4) and R(5) are alk(en)yl or CF.sub.3, R(5) also having the meaning of H, PA1 R(2)=is heteroaryl or --SR(10), --OR(10), --NR(10)R(11), --CR(10)R(11)R(12); where R(10) is --C.sub.a H.sub.2a -heteroaryl, and R(11) and R(12) are as defined for R(10) and also hydrogen or alkyl, PA1 R(3) is as defined for R(1) or is alkyl, --X--R(13) where X is oxygen, S, NR(14), where R(13) is H or (cyclo)alkyl. They are obtained from a compound of the formula II ##STR2## by reacting it with guanidine. The compounds are outstandingly suitable as antiarrhythmic pharmaceuticals with a cardioprotective component for the prophylaxis and treatment of infarctions and for the treatment of angine pectoris, and they also preventively inhibit, or greatly reduce, the pathophysiological processes in the formation of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias.