Beecham Group Plc

Peter Hubert Bentley

John P Clayton

Peter H Milner

Kenneth D Hardy

Gerald Brooks

A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxy phenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;

Penicillin derivatives

A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is phenyl, 4-hydroxyphenyl, or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;

Cephalosporin derivatives, and compositions containing them

A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## wherein R is phenyl 4-hydroxy phenyl, or a 5- 6- membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;

Penicillin derivatives and compositions containing them

A penicillin of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R is C.sub.1-6 alkyl; an optionally substituted 5-membered heterocyclic ring containing one or two heteroatoms selected from oxygen, sulphur and nitrogen; phenyl; mono-substituted phenyl where the substituent is halogen, hydroxy, C.sub.1-6 alkoxy, nitro, amino, C.sub.1-6 alkyl, or C.sub.1-6 haloalkyl, C.sub.1-6 alkylcarbonyloxy, or C.sub.1-6 alkyl sulphonylamino; or di-substituted phenyl where the substituents are selected from hydroxy, halogen, methoxy, acetoxy and amino; and X represents a group of formula: ##STR2## wherein R.sup.1 represents C.sub.1 to C.sub.6 alkyl, or C.sub.1 to C.sub.6 alkoxy. Their preparation and use is described.

The use of an iodolactone as an esterifying derivative in the preparation of lactonyl esters of cephalosporins substantially reduces double bond migration during the esterification reaction.

Process for preparing 7-aminocephalosporanic acid derivatives

Phthalidyl and substituted phthalidyl esters of certain cephalosporins are absorbed by the oral route into the serum, where they are hydrolyzed to the parent antibacterially active cephalosporin.

Phthalidyl ester of 3-carbomoyloxy cephalosporin derivatives

Phthalidyl esters of 7-[(.alpha. amino, 2 substituted

A class of 6-methoxy-.alpha.-carboxy penicillins have antibacterial activity against a wide range of Gram-negative organisms.

Penicillins

Intermediates useful in the preparation of compounds having a penam or cephem ring structure, particularly penicillins and cephalosporins, and their preparation.

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Rudgwick, United Kingdom

Peter Hubert Bentley