Bayer Aktiengesellschaft

Bayer Animal Health Gmbh

Bernard Schmidt

Rudolf Schohe-Loop

Bodo Junge

Zhan Gao

Heinrich Meier

Wolfgang Hartwig

Teunis Schuurman

Maarten De Jonge

Franz-Josef Van Der Staay

Joachim Schuhmacher

Achim Feurer

Peter-Rudolf Seidel

Georg Terstappen

William Bullock

Jane C Chisholm

Richard J Fanelli

Richard T McCarthy

Hans-Georg Lerchen

Karl-Heinz Schlemmer

Kozo Shiokawa

Walter Hubsch

Bernd Riedl

Ulrich Niewohner

Christoph Methfessel

Toshiya Moriwaki

Nagahiro Yoshida

Klaus Tietjen

Bernd-Wieland Kr Uger

Chantal F&uuml;rstner

Gabriele Handke

Wolfgang Roben

Werner Schr&ouml;der

Dirk Mertin

Frank B&ouml;ss

Alfred Maelicke

Fritz Maurer

Jens-Kerim Erg&uuml;den

Ute Spiecker-Hauser

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

The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R , R are the same or different and independently&equals;H, halogen, C C alkyl C C alkoxy, C C perfluoroalkyl, or a group NR R ; R , R are the same or different and independently&equals;C C alkyl, whose carbon chain is optionally interrupted by an O, S or NR and is optionally singly or severally substituted by C C cycloalkyl, C C alkoxy, OH, halogen or NR R ; C C cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR and is optionally singly or severally substituted by C C alkoxy, OH, halogen or NR R , or R and R together with a nitrogen atom form a saturated or partially unsaturated - to -membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C C alkyl, C C alkoxy, OH, halogen, COOR or NR R and X&equals;O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other forms of dementia, cerebral infarct, skull and brain trauma and pain.

3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases

The present invention relates to bis-(quinolyl)-diamines of the general formula (I):

Bis-(quinolyl)-diamines

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 2,2'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides processes for the preparation of the compounds of the formula (I), their use for the preparation of drugs, and drugs containing said compounds.

2,2'-bridged bis-2,4-diaminoquinazolines

The present invention relates to ring-bridged bis-quinolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides a process for the preparation of compounds of the formula (I), their use for the preparation of drugs, and drugs containing said compounds.

Ring-bridged bis-quinolines

4,4'-Bridged bis-2,4-diaminoquinazolines of the general formula (I) ##STR1## processes for their preparation and use as agents acting on the potassium channels of the brain.

4, 4'-bridged bis-2, 4-diaminoquinazolines

The present invention relates to the use of bisquinolines of the general formula ##STR1## in which the substituents mentioned have the meanings given in the description. The invention furthermore relates to new bisquinolines of the general formula (I), to a process for the preparation of the known and the new bisquinolines, to the use of the new bisquinolines as medicaments, to their use for the preparation of medicaments, and to medicaments comprising them.

Use of bisquinoline compounds in the treatment of cerebral disorders

The present invention provides 2,4'-bridged bis-2,4-diaminoquinazolines of the general formula (I): ##STR1## in which the indicated substituents are as defined in the description. The invention also provides a process for the preparation of the compounds of the formula (I), drugs containing said compounds and processes for the preparation of drugs containing said compounds.

2,4'-bridged bis-2,4-diaminoquinazolines

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

The invention relates to the use of substituted amines for the treatment and prevention of brain function disorders. The substituted amines are suitable on the basis of their properties as agonistic or antagonistic ligands for nicotinergic receptors, in particular for the treatment and prevention of senile and presenile dementia and dementia of the Alzheimer type, and of depressions.

Use of substituted amines for the treatment of brain function disorders

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Lindlar, Germany

Bernard Schmidt