3-(Optionally substituted-but-1-en-3-ynyl) cephalosporins
US4666899A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 9, 1985 |
| Grant date | May 19, 1987 |
| Priority date | — |
| Expiry date | May 9, 2005 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F7/1804
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of general formula I ##STR1## (wherein R represents NH.sub.2 -- or an acylated or silylated amino group; PA1 R.sup.2 represents a hydrogen, halogen, alkyl, aryl, carboxyl or lower alkoxycarbonyl group; PA1 R.sup.3 is hydrogen or a carboxyl blocking group; PA1 B is >Sor>S.fwdarw.O (.alpha.- or .beta.-); and the dotted line represents .DELTA..sup.2 or .DELTA..sup.3 unsaturation) and salts, solvates and esters thereof are described. Compounds where R.sup.3 is hydrogen, the dotted line represents .DELTA..sup.3 unsaturation and R is a group of formula ##STR2## (where R.sup.a is an optionally substituted heterocyclic aryl group having one or more hetero atoms selected from S, N and O in the ring, R.sup.b is an optionally substituted aryl group, R.sup.c is hydrogen, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.d is as defined for R.sup.a or is an optionally substituted group and X is amino, hydroxyl, acylated hydroxyl, carboxyl or esterified carboxyl) and especially the compounds in which B is >S, have valuable antibiotic activities. Compounds in which the --CH.dbd.CH--C.tbd.C--R.sup.2 group is in the trans configuration have been found to h…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.