Bayer Aktiengesellschaft

Jurgen Dressel

Stefan Wohlfeil

Ulrich E Muller

Martin Beuck

Rudolf H Hanko

Matthias Muller-Gliemann

Thomas Kramer

Stanislav Kazda

Walter Hubsch

Johannes-Peter Stasch

Andreas Knorr

Peter Fey

Siegfried Zaiss

Ozkan Yalkinoglu

Hilmar Bischoff

Dirk Denzer

Claudia Hirth-Dietrich

Ulrich Niewohner

Siegfried Raddatz

Michael Matzke

Klaus Mohrs

Walter Husch

Stanisiav Kazda

Hans-Peter Belleman

Hans-Peter Bellemann

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.

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.

Sulphonylbenzyl-substituted imidazolypropenoic acid derivatives

Imidazolyl-substituted phenylacetic acid prolinamides are prepared by reacting corresponding imidazolyl-substituted phenylacetic acids with prolines. The imidazolyl-substituted phenylacetic acid prolinamides can be used as active compounds in medicaments, preferably for the treatment of hypertension and atherosclerosis.

Imidazolyl-substituted phenylacetic acid prolinamides

Imidazolyl-substituted phenylacetic acid derivatives are prepared by first reacting suitably substituted phenylacetic acid with imidazoles and subsequently converting the product into an amide. The compounds can be employed as active compounds in medicaments, in particular for treating hypertension and atherosclerosis.

Imidazolyl-substituted phenylacetamides

Imidazolyl-substituted phenylpropionic and cinnamic acid derivatives are prepared by reacting appropriate benzyl compounds with imidazoles and optionally varying the substituents. The imidazolyl-substituted phenylpropionic and cinnamic acid derivatives can be used as active compounds in medicaments, in particular in the treatment of arterial hypertension and atherosclerosis.

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Wuppertal, Germany

Jurgen Dressel