Bayer Aktiengesellschaft

Bayer Intellectual Property Gmbh

Thomas Kramer

Walter Hubsch

Johannes-Peter Stasch

Stefan Wohlfeil

Martin Beuck

Rudolf H Hanko

Stanislav Kazda

Ulrich E Muller

Matthias Muller-Gliemann

Jurgen Dressel

Andreas Knorr

Peter Fey

Siegfried Zaiss

Ozkan Yalkinoglu

Hilmar Bischoff

Dirk Denzer

Claudia Hirth-Dietrich

Ulrich Niewohner

Ulrich Rosentreter

Siegfried Raddatz

Michael Matzke

Thomas Krahn

Nicole Diedrichs

Klaus Mohrs

Klaus Dembowsky

Andrea Vaupel

Kerstin Henninger

Mitsuyuki Shimada

Ulrich E M Uller

Matthias M uller-Gliemann

J Urgen Dressel

Hans-Peter Bellemann

Walter Husch

Stanisiav Kazda

Hans-Peter Belleman

The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R-Rare as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.

Substituted 2, 6-diamino-3, 5-dicyano-4-arylpyridines and their use as adenosine-receptor-selective ligands

Compounds of the formula (I) a process for preparing them, and their use as medicaments are described.

Substituted 2-thio-3, 5-dicyano-4-phenyl-6-aminopyridines and their use as adenosine receptor-selective ligands

Trisubstituted biphenyls are prepared by reacting corresponding pyridones with biphenylmethyl halogen compounds. The trisubstituted biphenyls can be employed as active compounds in medicaments.

Trisubstituted biphenyls

Heterotricyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted by benzyl halide radicals. The compounds can be employed as active compounds in medicaments.

Heterotricyclically substituted phenyl-cyclohexane-carboxylic acid

The invention relates to phenylacetic acid derivatives which are substituted by a five-membered nitrogen heterocycle bonded via an N atom. They are prepared by reaction of phenylacetic acid derivatives substituted with leaving groups with the appropriate nitrogen heterocycles and can be used as active substances in medicaments for the treatment of high blood pressure and atherosclerosis.

Heterocyclically substituted phenylacetic acid derivatives and their use

Substituted pyridines and 2-oxo-1,2-dihydropyridines are prepared by reaction of correspondingly substituted halogenobenzenes with tetrazolylboronic acids. The substituted pyridines and 2-oxo-1,2-dihydropyridines according to the invention can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.

Substituted pyridines and 2-oxo-1,2-dihydropyridines

Heterotricyclically substituted phenyl-cyclohexane-carboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted by benzyl halide radicals. The compounds can be employed as active compounds in medicaments.

Antihypertensive and antiatherosclerotic trisubstituted biphenyls of the formula ##STR1## in which R.sub.1 represents a carboxyl radical or represents a C.sub.1 -C.sub.8 -alkoxycarbonyl radical,

Novel substituted 2,4-imidazolidinediones are prepared either by reaction of .alpha.-aminocarboxylic acid derivatives with appropriately substituted biphenylmethyl halides and subsequent cyclization with isocyanates or by reaction of N-benzyl-substituted .alpha.-aminocarboxylic acid derivatives with tetrazolylphenylboronic acids or by reaction of sulphonyl-substituted benzyl halides with .alpha.-aminocarboxylic acid derivatives and subsequent cyclization with isocyanates. The compounds according to the invention can be employed as active compounds in medicaments, preferably for the treatment of arterial hypertension and arteriosclerosis.

Substituted 2,4-imidazolidinediones

Substituted imidazo[4,5-b]pyridines and benzimidazoles are prepared by reacting imidazo[4,5-b]pyridines or benzimidazoles with appropriately substituted benzyl halides. The substituted imidazo[4,5-b]pyridines or benzimidazoles can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.

Substituted imidazo[4,5-b]pyridines and benzimidazoles

The invention relates to phenylacetic acid derivatives of the formula ##STR1## which are substituted by a five-membered nitrogen heterocycle bonded via an N atom. They are prepared by reaction of phenylacetic acid derivatives substituted with leaving groups with the appropriate nitrogen heterocycles and can be used as active substances in medicaments for the treatment of high blood pressure and atherosclerosis.

Imidazolyl-substituted cyclohexane derivatives are prepared by reacting appropriate cyclohexane derivatives with substituted imidazoles and subsequent variation of the substituents. The imidazolyl-substituted cyclohexane derivatives can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.

Imidazolyl-substituted cyclohexane derivatives

Sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be prepared by reacting sulphonylbenzyl-substituted aldehydes with appropriate CH-acidic compounds and then dehydrating. The sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be used in medicaments, in particular for the treatment of high blood pressure and atherosclerosis.

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Wuppertal, Germany

Thomas Kramer