Bayer Aktiengesellschaft

Wilfried Schrock

Hans-Bodo Konig

Karl G Metzger

Karl-Georg Metzger

Hans Disselnkotter

Michael Preiss

Karl Georg Metzer

Hans-Joachim Zeiler

Michael Walkowiak

Rainer Endermann

Dieter Habich

Ekkehard Niemers

Klaus Grohe

Uwe Petersen

Thomas Schenke

Rolf Angerbauer

Andreas Krebs

Gunter Schmidt

Klaus-Dieter Bremm

Ingo Haller

Wolfgang Hartwig

Thomas Philipps

Paul Naab

Michael Boberg

Gunther Kinast

The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives.

Quinolonecarboxylic acids

A heteroanellated phenylglycine-.beta.-lactam antibiotic of the formula ##STR1## in which R.sup.1 - stands for a radical of the formula ##STR2##

Carbacephem antibiotics

Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,

Cephalosporins

A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.

.beta.-Lactam antibiotics

Anti-bacterially active penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,

Penicillin 1,1-dioxides

New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,

Penicillin 1,1-dioxides, compositions thereof and methods of use

6-[.alpha.-(Imidazolidin-2-on-1-ylcarbonylamino)-substutited acetamido]penicillanic acids, and the correspondingly 7-substituted ceph-3-em-4-carboxylic acids, characterized by the presence of a methyleneamino or substituted methyleneamino group on the 3-nitrogen atom of the imidazolidine ring are antibacterial agents. The compounds, of which 6-[.alpha.-(3-benzaliminoimidazolidin-2-on-1-ylcarbonylamino)cyclohe xa-1,4-dien-1-ylacetamido]penicillanic acid and 7-[.alpha.-(3-furylideneaminoimidazolidin-2-on-1-ylcarbonylamino)phenylace tamido]-3-(3-methylthiadiazol-5-ylthiomethyl)ceph-3-em-4-carboxylic acid are typical examples, are prepared through acylation of an 6-[.alpha.-(amino)substituted acetamido]penicillanic acid or the corresponding 7-[.alpha.-(amino)substituted acetamido]ceph-3-em-4-carboxylic acid with a reactive nucleofugic derivative of a 3-methyleneaminoimidazolidin-2-on-1-carboxylic acid.

.beta.Lactam antibiotics and process for their use

Cephalosporins of the formula ##STR1## their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, wherein

Oxo-imidazolidine substituted cephalosporins and antibacterial

Sulfonylimidazolidone substituted cephalosporins, antibacterial

Cephalosporins and their production

.beta.-Lactams of the formula ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein A is hydrogen or alkyl of 1 to 4 carbon atoms;

Penicillins and cephalosporins and their production

Oxoimidazolidinylthiocarbonyl derivatives of ceph-3-em-4-carboxylic acids

6-[.alpha.-(Imidazolidin-2-on-1-carbonylamido)acetamido]-penicillanic acids substituted in the 3-position of the imidazolidinone ring with phenyl or a substituted phenyl group and on the .alpha.-carbon atom of the acetamido bridge with a phenyl, thienyl, cyclohexenyl or cyclohexadienyl group, and their salts, are antibacterial agents. The compounds, of which .alpha.-(3-phenylimidazolidin-2-on-1-ylcarbonylamino)benzylpenicillin is a representative example, are prepared by acylation of the corresponding 6-(.alpha.-aminoacetamido)penicillanic acid or a derivative thereof.

Penicillins and processes for their preparation and use

6-(.alpha.-3-Acyl-ureidoacetamido)-penicillanic acids and pharmaceutically acceptable non-toxic salts thereof in which the hydrogen atom of the nitrogen atom present in the 3-position is substituted, are effective against Gram-positive and Gram-negative infections, particularly Klebsiella aerobacter infections.

Growing community of inventors

Wuppertal-Elberfeld, Germany

Wilfried Schrock