Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Eberhard Ehlers

Walter Durckheimer

Elmar Schrinner

Rene Heymes

Dieter Bormann

Werner Aretz

Heinrich Decker

Laszlo Vertesy

Michael Kurz

Jurgen Blumbach

Karl Seeger

Sebastian Rissom

Burkhard Mencke

Hubert Georg Seliger

Laszl&oacute; V&eacute;rtesy

Frank Rainer Schmidt

Udo Hedtmann

Reiner Olliger

Andreas Stark

Guido Seidel

The invention relates to a method for the enzymatic elimination of the N-acyl side chain from lipopeptides to form the corresponding nucleus, wherein the lipopeptide is prepared by fermentation, the lipopeptide being bound to the cells of the biomass, and the biomass is removed with the adhering lipopeptide, the biomass with the adhering lipopeptide is resuspended in an aqueous system, a suitable deacylase is added in dissolved or solid form to the suspension of the biomass, and the corresponding nucleus is formed, and the nucleus is optionally isolated and purified, wherein the lipopeptide obtained by fermentation is reacted after the end of the fermentation as cell-bound biomass without further purification directly with a deacylase, whereby the N-acyl chain linked via an amide linkage is eliminated.

Method for the deacylation of lipopeptides

Calcium salts of lipopeptide antibiotics, method for producing same and their use

Moenomycin A can be prepared by fermentation of a moenomycin-producing microorganism and subsequent separation of moenomycin A from the other components of the culture filtrate by chromatography, using an anion exchanger as chromatography material.

Process for the preparation of moenomycin A

Cephem derivatives of the general formula ##STR1## in which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.

Cephem derivatives and processes for their manufacture

The invention relates to a process for the preparation of MA, which ensures MA production by enzymatic catalysis in glycine/NaOH buffer, and by the use of a phosphate-containing culture medium for Bacillus sp. DSM 4675 and by extraction of the biomass with acetone.

Process for the preparation of MA

Cephem derivatives

What are disclosed are cephem compounds of the formula ##STR1## useful for combating bacterial infections, and methods of making and using the same.

What are disclosed are cephem compounds of the formula ##STR1## in which R.sub.1 denotes hydrogen, an optionally substituted alkyl, acyl, arylsulfonyl or alkylsulfonyl group or an amino-protective group which is known from peptide chemistry, R.sub.2 denotes hydrogen or an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, acyl, aryl, arylsulfonyl, alkylsulfonyl or heterocyclic group, R.sub.3 denotes hydrogen, an ester group or a cation, R.sub.4 denotes hydrogen, a lower alkoxy group or a group which can be converted to this, X denotes a SO group in the R or S configuration or a SO.sub.2 group and A denotes hydrogen, an optionally substituted alkoxy or alkenyloxy group, halogen or a group --CH.sub.2 Y, in which Y represents hydrogen, halogen or the radical of a nucleophilic compound, and in which the R.sub.2 O group is in the syn-position, which compounds are valuable chemotherapeutic agents having a very powerful antimicrobial action against Gram-positive and Gram-negative bacteria and an unexpectedly good action against penicillinase-forming Staphilococci.

Cephem derivative

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Hofheim, Germany

Eberhard Ehlers