Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gmbh

Merck Patent Gesellschaft

Merck Patent Gesellschaft MIT Beschr&auml;nkter Haftung

Manfred Baumgarth

Rolf Gericke

Norbert Beier

Klaus-Otto Minck

Jacques De Peyer

Hans-Eckart Radunz

Dieter Dorsch

Hans-Peter Buchstaller

Rolf Bergmann

Dieter Orth

Reinhard Lissner

Inge Lues

Jurgen Harting

Hanns Wurziger

Hans-Joachim Enenkel

Josef Kramer

Jurgen Maisenbacher

Filippus J Zeelen

Michael Wolf

Frank Zenke

Pierre Schelling

Christian Sirrenberg

Ingeborg Lues

Christiane Amendt

Maria Christadler

Matthias Wiesner

Hans-Jochen Schliep

Dirk Finsinger

Klaus Otto Minck

Matthias Grell

David Bruge

Gunther Hausler

Willy Kinzy

Hans Schaefer

Gerd-Albrecht Luckenbach

Bernhard Ladstetter

Hans Radunz

Hans Markus Bender

Achim Zesch

De Peyer

Hans-Micahel Eggenweiler

Pyrimidine derivatives of the formula (I) and physiologically acceptable salts thereof, in which R, R, R, R, W, X, Y and Z are as defined in claimexhibit phosphodiesterase V inhibition and can be employed for the treatment of diseases of the cardiovascular system and for the treatment and/or therapy of potency disorders 

Pyrimidine derivatives

The present invention relates to an NHE-1 selective Na&plus;/H&plus; antiporter inhibitor N-(4,5-bismethanesulfonyl-2-methylbenzoyl)guanidine, hydrochloride, to its hydrochloride hydrate, and to a process for the preparation.

Method of producing n-(4,5-bis-methanesulfonyl-2-methyl-benzoyl)-guanidine, the hydrochloride thereof

Chroman derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 have the meanings defined herein, and their salts have an effect on the cardiovascular system.

Chroman derivatives

Heterocyclyl-condensed benzoylguanidines, their production and use as

Heterocyclyloxybenzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and Het have the given meanings, and also the pharmaceutically acceptable salts thereof, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Heterocyclyloxybenzoylguanidines

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

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

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

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

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Darmstadt, Germany

Manfred Baumgarth