Glaxo Laboratories Limited

Glaxo Operations UK Limited

Michael Gregson

Gordon Ian Gregory

Martin Christopher Cook

Richard B Sykes

Godfrey Basil Webb

The invention provides novel antibiotic cefuroxime esters of the formula ##STR1## (wherein R is a primary or secondary alkyl group containing 1 to 4 carbon atoms). These compounds are useful as orally administrable broad spectrum antibiotics.

Cephalosporin antibiotics

The invention provides novel antibiotic cefuroxime esters of the formula ##STR1## (wherein R.sup.1 is a primary or secondary alkyl group containing 1 to 4 carbon atoms and R.sup.2 is a primary or secondary alkyl group containing 1 to 6 carbon atoms provided that at least one of the groups R.sup.1 and R.sup.2 is methyl). These compounds are useful as orally administrable broad spectrum antibiotics.

The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Syn isomers of cephalosporins having .alpha.-hydroximino- or

Novel antibiotic compounds which are 7.beta.-acrylamidoceph-3-em-4-carboxylic acids, and 6.beta.-acrylamidopenam-3-carboxylic acids and non-toxic derivatives thereof wherein the acrylamido group has the structure ##STR1## wherein A is aryl group and B is a substituted or unsubstituted lower alkyl, lower alkenyl or lower alkynyl group; or an aryl, cycloalkyl or cycloalkenyl group. These compounds possess antibacterial activity against gram-positive and gram-negative organisms coupled with stability to .beta.-lactamases. The invention further relates to the administration of the compounds.

Cephalosporin derivatives

The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## WHERE R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

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London, United Kingdom

Michael Gregson