Arzneimittelwerk Dresden Gmbh

Arzneimettelwerk Dresden Gmbh

Gottfried Faust

Andreas Rolfs

Hans-Joachim Jansch

Alexander Knoll

Peter Scharfenberg

Dieter Lohman

Eveline Morgenstern

Aleksej Uschmajew

Sabine Heer

Klaus Unverferth

Reni Bartsch

Angelika Rostock

Dieter Lohmann

Wolfgang Sauer

Volker Hagen

Christine Siegemund

Erhard Klauschenz

Angela Hagen

Ju/ Rgen Liebscher

Peter Muschick

Jurgen Liebscher

Brigitte Schlegel

Jurger Liebscher

The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles. Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents. The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations. Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

3-aminopyrroles, methods for their synthesis and for their

A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without producing harmful byproducts.

Method for producing 1-unsubstituted 3-aminopyrroles

The substituted 5-(phenoxyalkanoylamino)-uracil compounds have the following formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen; a branched or linear alkyl group having 1 to 6 carbon atoms; a branched or straight chain alkenyl or alkynyl group having 1 to 6 carbons atoms; a cycloalkyl group having from 3 to 7 carbon atoms or a cycloalkylmethyl group having a cycloalkyl residue of 3 to 7 carbon atoms; or a phenylalkyl group having an alkyl residue having from 1 to 3 carbon atoms and a phenyl residue, the phenyl residue being unsubstituted or having a halogen, methoxy, methyl or trifluoromethyl substituent; R.sub.3 is a hydrogen, methyl or amino groups; R.sub.4 is halogen, methoxy or methyl groups, and n is 1 or 2. Pharmaceutical compositions for treating cerebrovascular, neuronal-degenerative and senility-induced disorders associated with learning, memory and cognitive dysfunctions are described which contain a therapeutically effective amount of the substituted 5-(phenoxyalkanoylamino)-uracil in a pharmaceutically acceptable carrier.

Substituted 5-(phenoxyalkanoylamino)-uracil compounds, methods for

A 3-cyano-5,4'-bipyridine-1'-oxide of the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R is an amino, alkoxy, oxyalkoxy or chloro residue, have heart stimulating cardiotonic and vasodiolatory properties. They can be preparaed by (a) converting an R-substituted-3-cyano-bipyridine to its corresponding N-oxide, or (b) by substituting an R-residue or an R-unsubstituted precursor of the conpound of fomula (i), and if required, converting the product into its pharmaceutically acceptable acid addition salt.

3-cyano-5,4'-bipyridine-1'-oxide compounds and pharmaceutical

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Radebeul, Germany

Gottfried Faust