3,5-substituted aminobenzoylguanidines, their use as a medicament or diagnostic and medicament containing them

US5516805A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Hans-Jochen Lang · Hofheim, DE
• Heinrich Englert · Hofheim, DE
• Andreas Weichert · Egelsbach, DE
• Heinz-Werner Kleemann · Bischofsheim, DE
• Wolfgang Scholz · Beverly, US
• Udo Albus · Florstadt, DE

Key dates

• Filing date: May 25, 1995
• Grant date: May 14, 1996
• Expiry date: May 25, 2015

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing them There are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen. The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties. They additionally exhibit protective properties against is chemically induced damage in vivo and in vitro in different organs and gastroprotective properties as a result of inhibition of gastric acid secretion. Moreover, they are distinguished by inhibitory action on the proliferation of cells.