Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicaments or diagnostic agents, and medicaments containing them

US5547953A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

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

Key dates

• Filing date: Dec 22, 1994
• Grant date: Aug 20, 1996
• Expiry date: Dec 22, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D279/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and also a medicament containing them. Acylguanidines I ##STR1## with X equal to carbonyl or sulfonyl; R(1) equal to H, (cyclo)alkyl, phenyl; R(2) equal to H, alkyl, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine. The compounds have no unwanted salidiuretic but very good antiarrhythmic properties. They are able, as a consequence of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, to be used for the treatment of all acute or chronic ischemia-induced damage.