Beecham Group Plc

Steven Coulton

Norman H Rogers

John P Clayton

Roger J Ponsford

Robert Southgate

David F Corbett

Nigel J Broom

Gerald Brooks

Pamela Brown

Compounds of the general formula (II): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof, in which

Penem compounds

The present invention provides a process for inversion of the absolute stereochemistry at the .alpha.-carbon atom of a C-6 substituent of a bicyclic carbapenem antibiotic via a phosphorus - azodicarboxylate mediated reaction. Novel azides, amines and formates are described as useful intermediates and as antibacterial agents.

.beta.-Lactam antibiotics their preparation and their use

The present invention provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in-vivo hydrolyzable ester thereof wherein R.sup.1 is a hydrogen atom, an .alpha.-sulphonato-oxyethyl group, an .alpha.-sulphonato-oxypropyl group or is a group CR.sup.3 R.sup.4 R.sup.5 wherein R.sup.3 is a hydrogen atom or a hydroxy group; R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl group; and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl group, a benzyl group, a phenyl group or is joined to R.sup.4 to form together with the carbon atom to which they are joined a carbocyclic ring of 5 to 7 carbon atoms; R.sup.2 is a pyrimidinyl group substituted by one two or three groups selected from nitro, halo, amino or substituted amino, and in addition may be optionally substituted by one or two C.sub.1-6 alkyl groups as the degree of substitution permits; and x is zero or one. These compounds are antibacterial agents. Their preparation and use are described.

.beta.-Lactam antibiotics, their preparation and use

A ketone of formula (II): ##STR1## wherein Y represents ##STR2## and R represents a C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, aryl, aralkyl or cycloalkylalkyl group, optionally substituted with halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, carboxy or C.sub.1-6 alkoxy carbonyl, or represents a 5 or 6 membered heterocyclic group containing a nitrogen, oxygen or sulphur atom, has antibacterial and antimycloplasmal activity and is of value in the treatment of bacterial and mycoplasma-induced human and veterinary diseases.

Antibacterial compounds, processes for their preparation and

A thiol acid and esters thereof of formula (II): ##STR1## wherein R is hydrogen, a salt forming ion or a pharmaceutically acceptable ester-forming radical, have antibacterial and antimycoplasmal activity and are therefore useful in the treatment of human and veterinary bacterial and mycoplasmal infections.

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Cranleigh, United Kingdom

Steven Coulton