Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Merck Patent Gmbh

Klaus-Otto Minck

Norbert Beier

Dieter Dorsch

Christoph Seyfried

Ingeborg Lues

Werner Mederski

Rolf Gericke

Manfred Baumgarth

Pierre Schelling

Henning Bottcher

Hans-Heinrich Hausberg

Rudolf Gottschlich

Rochus Jonas

Mathias Osswald

Peter Raddatz

Claus J Schmitges

Johannes Sombroek

Hanns Wurziger

Hans-Jochen Schliep

Hans J Enenkel

Michael Kloft

Helmut Prucher

Michael Klockow

Jurgen Uhl

Inge Lues

Juergen Harting

Hans-Peter Wolf

Anton Haase

Alfred Jonczyk

Joachim Gante

Andreas Bathe

Hans-Eckart Radunz

Gunter Holzemann

Klaus Irmscher

Jurgen Harting

Helmut Muller-Calgan

Wighard Strehlow

Thorsten Hartig

Dieter Marx

Otto Saiko

Matthias Osswald

Manfred Haumgarth

Henning Bottch

Imidazopyridine derivatives ad pharmacologically acceptable salts having antagonistic properties towards angiotensin II can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.

Imidazopyridines

Heterocyclyl-condensed benzoylguanidines, their production and use as

Ortho-substituted benzoic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and Q is guanidyl, and also their physiologically harmless salts, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter. In addition, the compounds of the formula I, in which R.sup.1 to R.sup.3 and also Q have the given meanings, are suitable for use as valuable intermediates for the preparation of medicaments, in particular of inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Ortho-substituted benzoil acid derivatives

Alkylbenzoylguanidines of the formula I ##STR1## in which A, R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and their physiologically harmless salts exhibit antiarrhythmic properties and act as inhibitor of the cellular Na.sup.+ /H.sup.+ antiporter.

Alkylbenzoylguanidine derivatives

Arylbenzoylguanidines of the formula I ##STR1## in which R.sup.1 R.sup.2, R.sup.3 and Ph have the given meanings herein, and also the physiologically harmless salts thereof, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Arylbenzoylguanidines

Imidazopyridine derivatives and pharmacologically acceptable salts having antagonistic properties towards angiotensin II can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.

Heterocyclyl-benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Het have the meanings given herein, and physiologically unobjectionable salts thereof, display antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Heterocyclyl-benzoylguanidines

Fluorine-containing benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated, and their physiologically acceptable salts, have antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter, for example.

Fluorine-containing benzoylguanidines

4-Sulfonyl- or 4-sulfinylbenzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.6 and n have the meanings indicated, and their physiologically acceptable salts exhibit antiarrhythmic properties and, act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Sulfonyl- or sulfinylbenzoylguanidine derivatives

4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

4-aminobenzoylguanidine derivatives

Alkyl-benzoylguanidines of the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given, and physiologically acceptable salts thereof show antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Alkenyl-benzoylguanidine derivatives

3-Alkoxycarbonyl thiadiazinones of the formula I ##STR1## and physiologically unobjectionable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Q and n have the meanings described herein, exhibit a positively inotropic action and can be employed for the therapy of cardiac insufficiency.

3-alkoxycarbonyl-thiadiazinones

Benzoylguanidines of the formula I ##STR1## wherein R.sup.1 and R.sup.2 have the meanings indicated herein, and their physiologically acceptable salts, show anti-arrhythmic properties and act as inhibitors of the cellular NA.sup.+ /H.sup.+ antiporter.

Alkyl-5-methylsulfonylbenzoylguanidine derivatives

4-Mercaptobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

4-mercaptobenzoylguanidine derivatives

Described herein are novel imidazopyridine derivatives of the formula I ##STR1## wherein R is ##STR2## and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in Patent Claim 1, and their salts, which exhibit antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and increased intraocular pressure, and of disorders of the central nervous system.

Imidazopyridines as pharmaceutical agents

Growing community of inventors

Ober-Ramstadt, Germany

Klaus-Otto Minck