Hoechst Aktiengesellschaft

Rudolf Lattrell

Gerd Fischer

Theodor Wollmann

Walter Durckheimer

Elisabeth Defossa

Uwe Gerlach

Norbert Krass

Ulrich Stache

Dieter Isert

Reiner Kirrstetter

Rolf Horlein

Wilfried Schwab

Hermann J Gerhards

Wilhelm Bartmann

Gerhard Seibert

Joachim-Heiner Jendralla

Heinrich Kief

Hermann Bahr

Rolf H Orlein

Rainer Henning

Joachim Kaiser

Adolf Heinz Linkies

Jurgen Blumbach

Karl Seeger

Astrid Markus

Peter Hammann

Michael Limbert

Karl-Heinz Budt

Holger Wallmeier

Fritz Bauer

Wolfgang Martin

Peter Klatt

Manfred Wieduwilt

Peter Schmid

Walter Durokheimer

Rolf Hoerlein

Theo Wollmann

Elisabeth Defobetaa

Novel crystalline cephem acid addition salts and processes for their preparation

Crystalline cepham acid addition salts and processes for their

The invention relates to a process which comprises a compound of the formula II ##STR1##

Process for the preparation of cephem prodrug esters

Lipopeptide derivatives of the formula I ##STR1## with R.sup.1 equal to OH or NH.sub.2 and R.sup.2 a C.sub.8 -C.sub.22 -acyl radical, pharmaceutical products which are effective for bacterial infections and contain such lipopeptide derivatives, process for preparing the lipopeptide derivatives and the pharmaceutical products, and the use of the lipopeptide derivatives for controlling bacterial infections are described.

Lipopeptide derivatives, a process for their preparation and their use

Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R, 7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxyme thyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive steps.

Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate

Crystalline acid addition salts of diastereomerically pure 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate The invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group =N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.

Crystalline acid addition salts of diastereomerically pure

The invention relates to a process for the preparation of cephem prodrug esters of the formula: ##STR1## in which R.sup.1 is C.sub.1 -C.sub.5 -alkanoyloxy-C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.5 -alkoxycarbonyloxy-C.sub.1 -C.sub.3 -alkyl and X is an inorganic or organic anion, and in which the hydroxyimino group is present in the syn-form.

The invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group .dbd.N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.

Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(metho xymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive partial steps and any desired sequence of addition of different acid components HY being possible, and optionally further purifying the obtained salts by crystallization, are described.

Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate

The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage. The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.

Process for the cleavage of cephalosporin prodrug esters to

Tetracyclic antibiotics and processes for their preparation .beta.-Lactam antibiotics of the formula I, and their pharmaceutically tolerable salts ##STR1## where X is (CH.sub.2).sub.0-2, CR(a)R(b), O, SO.sub.0-2 or NR(c),

Tetracyclic antibiotics and processes for their preparation

Compound I ##STR1## is obtained by reaction of compound II with compound III

Process for the preparation of penem compounds

What are disclosed are anti-bacterially active cephalosporin compounds of the formula ##STR1## pharmaceutical preparations containing such compounds, methods of making the compounds, methods for combatting bacterial infections therewith, and intermediates for such compounds.

Cephalosporin derivatives

Penem derivatives of the formula ##STR1## having R.sup.1 equal to 3-oxocyclobutyl and R.sup.2 equal to H or an ester-forming group, pharmaceutical preparations active against bacterial infections and which contain penem derivatives of this type, processes for the preparation of the penem derivatives and the pharmaceutical preparations, and use of the penem derivatives for the control of bacterial infections are described.

Penem derivatives

Crystallized cephem-acid addition salts of the general formula ##STR1## pharmaceutical preparations which contain such cephem derivatives and are active against bacterial infections, a process for the preparation of the cephem derivatives and the pharmaceutical preparations, and the use of the cephem derivatives for combating bacterial infections.

Growing community of inventors

Konigstein/Taunus, Germany

Rudolf Lattrell