Beecham Group Plc

Pfizer Corporation

Clive L Branch

Michael J Pearson

Angela W Guest

Stephen C Finch

Arun C Kaura

Richard G Adams

7.beta.- 2-(aminothiazolyl and thiadiazolyl)-2-oxyiminoacetamido!cephalosporin derivatives having a 3- N-(optionally substituted) aminopyridiniumthiomethyl! substituent have antibacterial activity and are of use in antibacterial therapy. Processes for the preparation of such cephalosporins plus intermediates for use in the preparation thereof, including N-(optionally substituted)amino-thiopyridones, are also described.

Cephalosporin compounds

7 .alpha.-formamido cephalosporin derivatives having a 3[N-(optionally substituted)aminothiopyridinium thiomethyl] substituent have anti-bacterial activity and are of use in anti-bacterial therapy. Processes for the preparation thereof and intermediates for use in these processes are also disclosed.

Cephalosporin derivatives

.beta.-Lactam antibiotics are disclosed which have the formula (IA) or pharmaceutically acceptable salts or pharmaceutically acceptable in vivo hydrolyzable esters thereof: ##STR1## wherein R.sub.1 is phenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-aminophenyl, 4-aminophenyl, or 3,4-dihydroxyphenyl, the hydroxy and amino groups being optionally protected, and R is C.sub.1-8 alkyl; and also the use thereof. Processes for the preparation of the compounds are disclosed together with intermediates for use therein.

Cephem compounds

A compound of formula (I) or a salt thereof: ##STR1## wherein R.sup.1 is an amino group, an azido group, or an acylamino group as found in antibacterially active penicillins or cephalosporins;

Azeto triazolo pyrazine .beta.-lactam antibacterial agents

The present invention provides the compounds of the formula (II): ##STR1## and pharmaceutically acceptable salts and cleavable esters thereof wherein RCONH is an organic acylamino group and E is a carboxy group or pharmaceutically acceptable salt or ester thereof or is a cyano group. Their preparation is described as is their use in compositions containing them. Compounds wherein RCONH is replaced by an azido group are described as useful intermediates.

.beta.-Lactam antibacterial compounds, their preparation and

Novel cephalosporin analogues, salts and esters thereof, their preparation, intermediates and antibacterial compositions containing them. The compositions are formulated for human use into unit dosage form containing 100-4,000 mg of antibacterial compound. The cephem analogues are characterized by having a ring O-heteroatom instead of a ring N-heteroatom and are designated as oxacephems.

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Betchworth, United Kingdom

Clive L Branch