Ici Pharma

Imperial Chemical Industries Limited

Frederick H Jung

Colin J Strawson

Dominique Boucherot

David Huw Davies

Jean C Arnould

Thomas G Bird

Patrice J Siret

William Bell

Cephalosporins derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom

Bicyclo-heterocyclic intermediates for cephalosporin compounds

Cephalosporin derivatives having a 3-position substituent of formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any two adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;

Cephalosporin derivatives

A compound of the formula (II): ##STR1## and pharmaceutically acceptable salts an in vivo hydrolysable esters are described as is their preparation and use as antibacterial agents.

3-tetrazolylthiomethyl cephalosporin antibiotics

Cephalosporin derivatives having a 3-position substituent of the formula I are described: ##STR1## wherein R.sup.1 is hydrogen, alkenyl or optionally substituted alkyl, Het us a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the amide linkage, wherein Het is selected from a group of the formulae II-III: ##STR2## wherein A is CH or a nitrogen atom; B is oxygen, sulphur or a group NR.sup.4 ; one or two of D, E, F and G are nitrogen atoms and the remainder are CH groups: or Het is a pyrazinone, pyridinone, pyridazinone or pyrimidinone ring, or is a thione equivalent of such a ring, said rings having a substituent R.sup.4 on one nitrogen atom, or is pyranone, or pyranthione; the ring Het being fused by any adjacent carbon atoms to the benzene ring; and Het being attached to the --CH.sub.2 NR.sup.1 CO-- group via a carbon atom;

Cephalosporin compounds

Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein R.sup.1 is hydrogen or certain optionally substituted alkyl groups; X is a benzene ring or certain 5 or 6-membered heterocyclic ring and is fused to ring Y which is a nitrogen containing heteroaryl group; R.sup.2 and R.sup.3 are independently hydroxy or an in vivo hydrolysable ester thereof, and ring system X-Y is optionally substituted. Processes for their preparation and use are described.

Cephalosporin compounds having as a 3-substituent the group: ##STR1## wherein Y represents a bond, optionally substituted alkylene or --CH.sub.2 CH.sub.2 NHCO--, P is a benzene ring substituted by groups W and Z ortho with respect to one another wherein W is hydroxy or an in vivo hydrolyzable ester thereof, Z is hydroxy, an in vivo hydrolyzable ester thereof, carboxy, sulpho, hydroxymethyl, --NHSO.sub.2 CH.sub.3 or NHCONH.sub.2, Q is a mono- or bicyclic ring system substituted by R.sup.7 wherein R.sup.7 is hydrogen or a range of groups and ring Q is optionally further substituted; are described as antibacterial agents. Processes for their preparation and their methods of use are described.

Growing community of inventors

Rilly La Montagne, France

Frederick H Jung