Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with an imidazolo, oxazolo or thiazolopyridinium-methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino]-3-iodomethyl-3-cephem-4-carboxyl ic acid with an imidazolopyridine, and oxazolopyridine or a thiazolopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.
Abstract: Crystalline (7R)-7-amino-3-(1'-pyridiniummethyl)-3-cephem-4-carboxylate monohydrate compound is an intermediate in the synthesis of the cephalosporin antibiotic ceftazidime.
Abstract: The instant invention is a pharmaceutical composition suitable for storage in plastic containers which comprises a pharmaceutical compound in powder form coated with a surfactant. A second aspect of the invention is a method for making the composition. This method encompasses applying a solution of a surfactant to the surface of a pharmaceutical compound in powder form and then drying the composition.
Abstract: Antibiotic A47934 is produced by submerged, aerobic fermentation of new Streptomyces toyocaensis NRRL 15009. The antibiotic is active against gram-positive bacteria in vitro and in vivo. It promotes growth in poultry and swine and serves to enhance feed efficiency in ruminant animals having a developed rumen.
Abstract: There is described a process for preparing a sulphoxide of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4, taken individually, are alkyl, alkoxy or aryl groups, X is an alkylene group, R.sup.5 is a carboxylic acid protecting group and Y is a linking group through one or two carbon atoms forming a penam or cephem nucleus, which comprises reacting a compound of formula ##STR2## with an oxidizing agent. .alpha.-Sulphoxide compounds of formula (I) are also provided as novel intermediates.
Abstract: 7.beta.-[2'-triazepinone-2'-(oximine ether) acetamido] cephalosporin antibiotics are claimed. Also claimed are the 2'-triazepinone-2'-(oxime ether) acetic acid intermediates and the esters, salts and halides thereof.
Abstract: 3-(alkynylalkyloxy)cephalosporin antibiotics and the intermediates therefor are disclosed. Pharmaceutical compositions for the antibiotics are also disclosed.
Abstract: Antibiotic A-51568 is produced by submerged, aerobic fermentation of new Nocardia orientalis NRRL 15232. The antibiotic is effective against gram-positive organisms.
Type:
Grant
Filed:
December 27, 1983
Date of Patent:
December 10, 1985
Assignee:
Eli Lilly and Company
Inventors:
LaVerne D. Boeck, Marvin M. Hoehn, Gary G. Marconi
Abstract: There is described a process for preparing a sulphoxide of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4, taken individually, are alkyl, alkoxy or aryl groups, X is an alkylene group, R.sup.5 is a carboxylic acid protecting group and Y is a linking group through one or two carbon atoms forming a penam or cephem nucleus, which comprises reacting a compound of formula ##STR2## with an oxidizing agent. .alpha.-Sulphoxide compounds of formula (I) are also provided as novel intermediates.
Abstract: The novel glycopeptide antibiotic A-51568B is produced by submerged, aerobic fermentation of Nocardia orientalis NRRL 15232. A-51568B demonstrates antibiotic activity against gram-positive bacteria.
Type:
Grant
Filed:
December 13, 1983
Date of Patent:
December 10, 1985
Assignee:
Eli Lilly and Company
Inventors:
LaVerne D. Boeck, Gary G. Marconi, Marvin M. Hoehn
Abstract: Crystalline 7-(R)-amino-3-(1'-pyridiniummethyl)-ceph-3-em-4-carboxylate monohydrochloride monohydrate compound is an intermediate in the synthesis of the cephalosporin antibiotic ceftazidime.
Abstract: N-substituted-2-(R)-(sulfinic acid)-3-(S)-(acylamino)-4-oxo-azetidines, which are useful as intermediates in 1-oxa .beta.-lactam antibiotics, are synthesized by electrolytic reduction of 7-(S)-acylamino-3-hydroxymethyl-3-cephem-4-carboxylic acid compounds.
Abstract: Antibiotic A47934 is produced by submerged, aerobic fermentation of new Streptomyces toyocaensis NRRL 15009. The antibiotic is active against gram-positive bacteria in vitro and in vivo. It promotes growth in poultry and swine and serves to enhance feed efficiency in ruminant animals having a developed rumen.
Abstract: The instant invention is a pharmaceutical composition suitable for storage in plastic containers which comprises a pharmaceutical compound in powder form coated with a surfactant. A second aspect of the invention is a method for making the composition. This method encompasses applying a solution of a surfactant to the surface of a pharmaceutical compound in powder form and then drying the composition.
Abstract: N-ethylidene azetidinones are new antibiotic compounds. They are produced from the reaction of a Grignard reagent with a cephalosporin substituted at the 3 position with a chloro, oxy, amino or sulfide moieties.
Abstract: 7.beta.-[2'-Triazepinone-2'-(oxime ether) acetamido] cephalosporin antibiotics are claimed. Also claimed are the 2'-triazepinone-2'-(oxime ether) acetic acid intermediates and the esters, salts and halides thereof.
Abstract: This invention encompasses 7-(S)-acylamino-3-acetoxymethyl-3-cephem-4-carboxylic acid sulfones and the epimerization process for making them. The epimerization process employs an organic nitrogen base reagent having a pKa between about 9.0 to about 11.5. The compounds of this invention are intermediates in the synthesis of 1-oxa-.beta.-lactam antibiotics.
Abstract: This invention relates to a process for preparing 7-(S)-acylamino-3-hydroxymethyl-3-cephem-4-carboxylic acid sulfones and the salts and esters thereof. The instant process involves contacting a 7-(S)-acylamino-3-acetoxymethyl cephalosporin sulfone in an aqueous solution buffered from about pH 6 to about pH 8 with citrus acetylesterase, which is immobilized on silica gel. The 3-hydroxymethyl cephalosporin sulfones produced by the process of this invention are intermediates in the synthesis of 1-oxa .beta.-lactam antibiotics.