Hoechst Aktiengesellschaft

Aventis Pharma Deutschland, Gmbh

Hoeschst Aktiengesellschaft

Meck Patent Gmbh

Merck Patent Gmbh

Sanofi-A Ventis Deutschland Gmbh

Wolfgang Scholz

Udo Albus

Andreas Gerhard Weichert

Heinz-Werner Kleemann

Jan-Robert Schwark

Hans-Jochen Lang

Joachim Brendel

Hans Jochen Lang

Heinrich Christian Englert

Wolfgang Linz

Bernward Scholkens

Peter Crause

Bansi Lal

Dieter Mania

Florian Lang

Norbert Beier

Hansjorg Urbach

Rainer Henning

Volker Teetz

Hans-Willi Jansen

Ulrich Betz

Gabriele Wiemer

Ravindra Dattatraya Gupte

Heinz-Werner Kleeman

Anil Vasantrao Ghate

Anagha Suhas Kulkarni

Ramanujam Rajagopalan

Rao Venkata Vadlamudi

Marian Braendle

Tulsidas Sitaram More

Nigrogi Venkata Ramakrishna

Ramesh Gidwani

Radha Panicker

Chinnakulandai Sankar

The invention relates to a pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the prophylaxis and therapy of Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy. Another object of the invention concerns the use of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the enhancement of insulin sensitivity and the preservation or increase of &#xdf;-cell compensation.

Pharmaceutical composition comprising rimeporide for treating diseases associated with insulin resistance and &#x3b2;-cell dysfunction

Monoacyl-substituted guanidines, a process for their preparation, their use as a medicament or diagnostic aid, and pharmaceutical compositions containing them

Fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them

Diacyl-substituted guanidines, a process for their preparation, their use as medicine or diagnostic aid, and medicine containing them

Pharmaceutical combination preparation of an inhibitor of the sodium/hydrogen exchanger and a medicament for the treatment of cardiovascular diseases

Ortho-substituted benzoylguanidines of the formula I

Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them

There are described benzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m, R(5)R(6)N--SO.sub.2 --; O.sub.p --(CH.sub.2).sub.q --(CF.sub.2).sub.r --CF.sub.3 ; --SR(10), --OR(10) or --CR(10)R(11)R(12); R(2) is --(CH.sub.2).sub.u --(CF.sub.2).sub.t --CF.sub.3 ; R(3) is hydrogen or independently defined as R(1); and their pharmaceutically tolerable salts. They are obtained by reaction of a compound of the formula II ##STR2## with guanidine. They are compounds of outstanding activity on the cardiovascular system.

4-fluoroalkyl-substituted benzoylguanidines, process for their

Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.

Ortho-substituted benzoylguanidines, process for their preparation,

Substituted bicyclic heteroaroylguanidines, a process for their preparation, their use as a medicament or a diagnostic agent, and a medicament containing them are described, as are the pharmaceutically tolerated salts thereof. A process for their preparation, and their use as medicines and diagnostic aids in cardiovascular diseases, is also described.

Substituted bicyclic heteroaroylguanidines, a process for their

Benzoylguanidines of formula I ##STR1## with R(1) to R(4) as defined in the specification, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment of angina pectoris. They inhibit, in a preventive manner, the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias.

Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.

Basically-substituted benzoylguanidines, a process for preparing them,

Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them. Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## in which the substituents have the meanings stated in the description, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine, in which R(1) to R(5) and R(A), R(B), R(C) and R(D) have the stated meaning, and L is a leaving group which easily undergoes nucleophilic substitution. Compounds I are excellent cardiovascular therapeutic agents.

Phenyl.-substituted alkenylcarboguanidides carrying perfluoroalkyl

There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.

Substituted benzyloxy-carbonylguanidines, a process for their

Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.

Compounds of the formula ##STR1## where T is ##STR2## and R(A), R(B), R(C), R(D), R(E), R(F), x and y have the meanings indicated in the claims, and their pharmaceutically acceptable salts are effective inhibitors of the cellular sodium-proton antiporter (Na.sup.+ /H.sup.+ exchanger). These compounds are therefore outstandingly suitable for treatment of all illnesses which are to be attributed to increased Na.sup.+ /H.sup.+ exchange.

Phenyl-substituted alkenylcarboxylic acid guanidides, process for their

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Wolfgang Scholz