Bayer Aktiengesellschaft

Maarten De Jonge

Rudolf Schohe-Loop

Bodo Junge

Zhan Gao

Heinrich Meier

Wolfgang Hartwig

Teunis Schuurman

Bernard Schmidt

Hartmund Wollweber

Ulrich Niewohner

Siegfried Zaiss

Hans-Georg Dellweg

Bruno Rosen

Novel phenyl-substituted 1,4-dihydropyridines, prepared by reacting halogenophenyl-aldehydes with &bgr;-ketoesters, if appropriate with isolation of the ylidene compounds and enamines. The substances can be employed as active compounds in medicaments, in particular in cerebrally active compositions.

Phenyl-substituted 1,4-dihydropyridines

4-Phenyl-3-substituted 1,4-dihydropyridine esters are prepared by reaction of benzaldehydes with ketoesters and enamines, if appropriate with isolation of the ylidene intermediate products, or by esterification of corresponding dihydropyridinecarboxylic acids with alcohols. The new 4-phenyl-3-substituted 1,4-dihydropyridine esters can be employed as active compounds in medicaments for the treatment of the central nervous system, in particular as cerebral therapeutics.

4-phenyl-3-substituted 1,4-dihydropyridine esters

4-Heterocyclyl-substituted dihydropyridines are prepared by reacting appropriate aldehydes with .beta.-keto esters and aminocrotonic acid esters, or by esterifying 4-heterocyclyl-substituted dihydropyridinecarboxylic acids. The 4-heterocyclyl-substituted dihydropyridines can be employed in medicaments, in particular for the treatment of disorders of the central nervous system.

Heterocyclyl substituted dihydropyridines

The present invention relates to the new compound rac-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)1,4 -dihydro-2,6-dimethylpyridine-3,5-dicarboxylate and its pure enantiomers, processes for their preparation and their use as medicaments, in particular for the treatment of cerebral and neuronal disorders, and a new intermediate for their preparation.

Isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,

The invention relates to new aryl-substituted alkoxycarbonyl-1,4-dihydropyridine-5-carboxylic acid esters, processes for their preparation and their use in medicaments, in particular as agents having a cerebral action.

Aryl-substituted alkoxycarbonyl-1,4-dihydropyridine-5-carboxylic acid

4-Heterocyclyl-substituted dihydropyridines are prepared by reacting appropriate aldehydes with .beta.-keto esters and aminocrotonic acid esters, or by esterifying 4-hetero-cyclyl-substituted dihydropyridinecarboxylic acids. The 4-heterocyclyl-substituted dihydropyridines can be employed in medicaments, in particular for the treatment of disorders of the central nervous system.

4-heterocyclyl-substituted dihydropyridines

4-Heterocyclophenyl-substituted dihydropyridines ##STR1## are prepared either by reacting suitable aldehydes with amino esters and .beta.-keto esters, or preparing the heterocyclic substituents of the 4-phenyl by cyclization of corresponding amidines or hydrazides, or esterifying dihydropyridinecarboxylic acids, which are already substituted by heterocyclic radicals, with corresponding alcohols. The 4-heterocyclophenyl-substituted dihydropyridines can be employed in medicaments, in particular for treatment of diseases of the central nervous system.

4-heterocyclophenyl-substituted dihydropyridines

N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be prepared either by reaction of aldehydes with acetoacetic esters and amines, optionally with isolation of the corresponding ylidene compounds, or by reaction of aminocrotonic acid esters with ylidene compounds and subsequent alkylation of the NH function. The N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be employed as active compounds in medicaments, in particular as cerebral therapeutics.

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Overath, Germany

Maarten De Jonge