Imperial Chemical Industries Limited

Ici Pharma

Colin J Strawson

Graham C Crawley

David C Aldridge

Frederick H Jung

Dominique Boucherot

Gareth Morse Davies

David Huw Davies

Jean J Lohmann

Jean C Arnould

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

Cephalosporin antibiotics having a 3-position substituent of the formula:

Intermediates for cephalosporin compounds

Cephalosporin compounds

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;

The invention concerns novel racemic and optically active mono- and di-hydroxy alkanoic acids bearing phenyl and/or alkyl substituents, processes for their preparation, and pharmaceutical compositions for therapeutic use in the treatment of duodenal or gastric ulcers. Representative compounds of the invention are 2-(5.beta.-n-butyl-4.beta.-hydroxy-2-oxo-tetrahydrofuran-3.beta.-yl)-2.alp ha.-methyl-acetic acid and 3.alpha.-methyl-5.beta.-(1.beta.-hydroxy-n-pentyl)-2-oxo-tetrahydrofuran-4 .beta.-ylcarboxylic acid.

Hydroxy acids

Pharmaceutical compositions containing 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives including canadensolide and 3-epi-dihydrocanadensolide. Novel 3,3a,6,6a-tetrahydrofuro[3,4-b]furan derivatives bearing a variety of substituents in the 3- and 6-positions selected from alkyl, phenyl, alkoxycarbonyl, methylene, benzylthiomethyl and optionally substituted phenylthiomethyl. The compositions and novel compounds show anti-ulcer activity and are useful in the treatment of gastric or duodenal ulcers.

Growing community of inventors

Congleton, United Kingdom

Colin J Strawson