Hoechst Aktiengesellschaft

Elmar Schrinner

Walter Durckheimer

Dieter Bormann

Eberhard Ehlers

Rene Heymes

Michael Limbert

Manfred Schorr

Wilfried Schmitt

Bernd Knabe

Manfred Worm

Gerhard Seibert

Jurgen Blumbach

Hermann J Gerhards

Irvin Winkler

Helmut Diery

Heinz Hanel

Matthias Helsberg

Christoph Meichsner

Gerhart Schneider

Wolfgang Martin

Herbert Hartung

Hubert Georg Seliger

Norbert Klesel

Kurd Gunther

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

Pharmaceutical combination preparations containing cefotaxime and at least one xanthine derivative are suitable for the treatment of bacterial infectious diseases and for the treatment of septic shock.

Pharmaceutical combination preparations containing cephalosporin and

Pharmaceuticals which contain a substance releasing tumor necrosis factor (TNF) are better tolerated and can be given in higher doses when they contain a TNF inhibitor, especially a xanthine derivative.

Pharmaceutical containing TNF inhibitor

Cephem derivatives

A pharmaceutical combination product containing or composed of

Pharmaceutical combinations product and the preparation and use thereof

A pharmaceutical formulation having a synergistic anti-bacterial activity and comprising

Pharmaceutical formulation for the treatment of bacterial infections

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.

Cephalosporin derivatives of the formula ##STR1## processes for their manufacture and their use for combating bacterial infections.

Cephalosporin derivatives

What is disclosed are cephalosporin compounds of the formula ##STR1## pharmaceutical preparations having an action against bacterial infections and containing such cephem compounds, a process for the manufacture of the cephem compounds and of pharmaceutical preparations containing the same, and the use of the cephem compounds to combat bacterial infections.

Cephem derivative

Cephem derivatives of the formula ##STR1## in which R.sup.1 denotes hydrogen or low-molecular alkoxy, R.sup.2 denotes hydrogen, optionally substituted alkyl, phthalide or a cation, X denotes sulfur, oxygen or CH.sub.2 and A denotes hydrogen, alkoxy, halogen or a group --CH.sub.2 Y, in which Y represents hydrogen, acyloxy, alkoxy, optionally substituted carbamoyloxy or a group --SR.sup.3, in which R.sup.3 can represent acyl, alkyl or an optionally substituted 5-membered or 6-membered heterocyclic structure are disclosed as valuable antibiotics which are well suited for combating Gram-positive and in particular Gram-negative infections and also have an unexpectedly good action against penicillinase-forming staphylococci.

7[(2-Amino-thiazol-4-yl)glyoxylamido]-cephem derivatives and processes

Acylaminopenicillanic acids of the general formula ##STR1## in which A represents phenyl which may be substituted, an aromatic monocyclic heterocycle which may be substituted or dihydrophenyl, and X represents one of the groups --SO.sub.2 --, --CO--, --P(R)-- or --P(O)(R)-- in which R represents low molecular weight alkyl, alkenyl, alkoxy, aralkyl, aralkoxy, aryl or aryloxy which may be substituted, non-toxic salts of these compounds and pharmaceutical compositions containing these compounds.

Acylaminopenicillanic acids and process for preparing them

Acylaminopenicillanic acids of the general formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 represent hydrogen or lower alkyl which may be substituted, and in which the radicals R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 may form together an alkylene radical which may be substituted, R.sup.4 and R.sup.5 represent hydrogen or lower alkyl, R.sup.6 represents phenyl which may be substituted, a monocyclic aromatic heterocycle which may be substituted, or dihydrophenyl, A represents a benzene or thiophene ring which may be substituted, and X represents oxygen or a single bond, a process for preparing them and pharmaceutical compositions active against bacterial infections containing these compounds.

Acylamino-cephem-carboxylic acids of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 represent hydrogen or alkyl, R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together may form an alkylene radical which may be substituted, X represents a single bond or NH, A represents a phenylene or thienylene radical which may be substituted, Y represents a single bond or oxygen and Z represents a 5- or 6-membered ring which may be substituted and which may be bound to an anellated ring system, and their physiologically tolerated salts and esters, a process for preparing these compounds and preparations containing them.

Growing community of inventors

Wiesbaden, Germany

Elmar Schrinner