Bayer Aktiengesellschaft

Saltigo Gmbh

Karsten Von Dem Bruch

J&ouml;rg Baumgarten

Horst-Peter Antonicek

Arnd Voerste

Hans-Georg Lerchen

Jean-Marie-Viktor De Vry

Andreas Stolle

Michael Sperzel

Rudy Schreiber

Udo Stropp

Ervin Horv&aacute;th

Thomas M&uuml;ller

Gerhard M&uuml;ller

Stephen Lensky

Uwe Petersen

Franz-Josef Mais

Robert Horst Bloodworth

Klaus Dieter Bremm

Jorg Baumgarten

G&uuml;nter Rauchschwalbe

Bernd Griehsel

Walter Weichel

Andreas Sattler

Michael Sander

Norbert Piel

Andreas Scherwitzki

J&ouml;rg Buamgarten

Wolfgang Stirner

Frank Laschinski

Michael Konrad

The present invention relates to a method for preparing 2-alkoxy-4-amino-5-methylpyridines of the formula (I) and/or 2-alkoxy-4-alkylamino-5-methylpyridines of the formula (II) from the corresponding 2-haloaminopyridines and the appropriate alcohols in the presence of base, and to the compounds resulting therefrom.

Process for preparing 2-alkoxy-4-amino-5-methyl-pyridines and/or 2-alkoxy-4-alkylamino-5-methyl-pyridines

The present invention relates to a process for preparing 2-haloacrylic esters from 2-hydroxymethyl- or 2-halomethyl- or 2-chlorosulfinyloxymethyl-2-halomalonic diesters. The invention further provides novel 2-halomethyl-2-halomalonic diesters or 2-chlorosulfinyloxymethyl-2-halomalonic diesters which can be used for preparation of the 2-haloacrylic esters.

Method for producing 2-halogen-acrylic acid esters

The present invention relates to novel substituted &agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.

Substituted &agr;, &bgr;-anellated butyrolactones

The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.

20(S) camptothecin glycoconjugates

The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the 20-hydroxyl group of a camptothecin derivative. The invention furthermore relates to processes for preparing the compounds according to the invention and to their use as medicaments, in particular in connection with cancer.

Glycoconjugates from modified camptothecin derivatives (20-O-linkage)

The present invention relates to novel substituted (&agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.

Method for the production of 2,6-dichloro-5-fluoro-nicotinic acid and coarse and particularly pure 2,6-dichloro-5-fluoro-nicotinic acid

The present invention relates to novel substituted &bgr;,&ggr;-fused lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.

Substituted &bgr;,&ggr;-anellated lactones

The present invention relates to novel substituted bicyclic lactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, cranial cerebral trauma, states of pain or CNS-mediated spasms.

Substituted bicyclic lactones

The invention relates to cytostatics which, by modification with sugar, are tumor-specific. Suitable spacers ensure serum stability and at the same time an intracellular action.

Sugar-modified cytostatics

Glycoconjugates of modified camptothecin derivatives (A-or B-ring

A method for preparing 2,4-Dichloro-3,5-dimethylfluorobenzene, wherein the 2,4-Dichloro-3,5-dimethylfluorobenzene can be prepared in highisomeric selectivities when 3,5-dimethylfluorobenzene is chlorinated in the presence of Friedel-Crafts catalysts and a sulfur-containing co-catalyst. The invention is also directed to an intermediary for preparing a pharmaceutically-active compound including 4-dichloro-3,5-dimethyl fluorobenzene.

Process for the preparation of 2,4-dichloro-3,5-dimethyl-fluorobenzene

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Leverkusen, Germany

Karsten Von Dem Bruch