Abstract: A special crystalline form of the L-lysine salt of the antibiotic cefuroxime is described. The salt has improved properties that permit it to be used in areas where cefuroxime itself and known derivatives of cefuroxime cannot be used.
Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group is syn 2-aryl-2-(etherified imino) acetamido and in which the 3-position substituent is an alkyl-, alkenyl-etc. substituted carbamoyloxymethyl group exhibit high antibacterial activity against a broad range of gram positive and gram negative organisms, particularly high stability to .beta.-lactamases produced by various organisms, and stability in vivo. The compounds are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer.
Abstract: 1-Aminoethyl, 1-aminopropyl and 1-aminobutyl derivatives of 7,7-dimethylnorbornane are described. The amino groups are optionally substituted, for example by alkyl groups, or may be saturated heterocyclic amino groups. The alkylene group at the 1-position can also be substituted, and the 2-position can be substituted by chlorine. The compounds have CNS activity.
Abstract: The invention relates to a novel method for the preparation of a 7.beta.-acylamido-3-bromomethylceph-3-em-4-carboxylic acid-1-oxide compound by brominating a 7.beta.-acylamido-3-methylceph-3-em-4-carboxylic acid-1-oxide compound.
Type:
Grant
Filed:
December 10, 1976
Date of Patent:
September 12, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Brian Laundon, Brian Richard Cowley, David Cedric Humber
Abstract: The invention is concerned with the preparation of .DELTA..sup.3 -4-carboxy cephalosporin antibiotics possessing a 3-vinyl group or substituted 3-vinyl group by means of phosphorous intermediates.
Type:
Grant
Filed:
April 21, 1976
Date of Patent:
August 29, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
John C. Clark, James Kennedy, Alan G. Long, Niall G. Weir
Abstract: The invention is concerned with .DELTA..sup.3 -4-carboxy cephalosporin antibiotics possessing a 3-vinyl or substituted 3-vinyl groups as well as with phosphorous intermediates useful in the preparation thereof.
Type:
Grant
Filed:
July 8, 1974
Date of Patent:
August 15, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
John Colin Clark, James Kennedy, Alan Gibson Long, Niall Galbraith Weir
Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## (where R is thienyl or furyl; R.sup.a and R.sup.b are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; and m and n are each 0 or 1 such that the sum of m and n is 0 or 1) exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; compounds wherein at least one of R.sup.a and R.sup.
Type:
Grant
Filed:
March 19, 1976
Date of Patent:
July 25, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Janice Bradshaw, Martin Christopher Cook, Gordon Ian Gregory
Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## (where R is thienyl or furyl; R.sup.a and R.sup.b are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; and m and n are each 0 or 1 such that the sum of m and n is 0 or 1) exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; compounds wherein at least one of R.sup.a and R.sup.
Type:
Grant
Filed:
March 18, 1976
Date of Patent:
June 13, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Janice Bradshaw, Martin Christopher Cook, Gordon Ian Gregory
Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
Type:
Grant
Filed:
January 26, 1977
Date of Patent:
June 6, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Martin Christopher Cook, Gordon Ian Gregory, Janice Bradshaw
Abstract: The specification describes anti-inflammatory steroids having the following formula ##STR1## wherein X represents a hydrogen or fluorine atom, R' represents a methyl, ethyl, n-propyl or iso-propyl group, R" represents a methyl, chloromethyl, fluoromethyl, bromomethyl or 2-fluoroethyl group and represents a single or double bond. The specification describes processes for preparing such compounds as well as pharmaceutical compositions containing the compounds.
Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
Type:
Grant
Filed:
January 26, 1977
Date of Patent:
May 30, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Martin Christopher Cook, Gordon Ian Gregory, Janice Bradshaw
Abstract: A process for the preparation of diazo compounds, particularly diazo alkanes, is described in which a hydrazone is oxidized to a corresponding diazo compound in a two phase reaction medium in the presence of a phase transfer catalyst, and an oxidation catalyst which is iodine, and iodide or an iodonium salt, preferably in the presence of a base.
Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
Type:
Grant
Filed:
January 26, 1977
Date of Patent:
May 23, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Martin Christopher Cook, Gordan Ian Gregory, Janice Bradshaw
Abstract: Pharmaceutical compositions are described in which the active ingredient is a 7,7-dimethyl-[2,2,1]-bicycloheptane having at the 1-position a substituted or unsubstituted amino or aminomethyl group. The active ingredients have been found to possess antiviral and central nervous system activity.
Abstract: A process for the preparation of diazo compounds, particularly diazoalkanes, is described in which a hydrazone is oxidized with an oxidizing agent, said oxidizing agent comprising an organic peracid, chloramine-T or N-chlorosuccinimide to a corresponding diazo compound, preferably in the presence of a base. The reaction may be catalyzed by an oxidation catalyst such as iodine.
Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## WHERE R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range or gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.
Type:
Grant
Filed:
December 19, 1975
Date of Patent:
March 14, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Martin Christopher Cook, Gordon Ian Gregory, Janice Bradshaw
Abstract: Novel syn-7.beta.-(2-aryl-2-hydroxyiminoacetamido)ceph-3-em-4-carboxylic acids carrying a 7.alpha.-lower alkoxy substituent, particularly a 7.alpha.-methoxy group, which are broad spectrum antibiotics exhibiting low serum binding are described.
Abstract: Novel polymers are provided which carry diazomethylene or hydrazonomethylene groups. Such polymers are of special use in immobilizing carboxylic acids, such as amino acids, with a view to subsequent chemical transformation of such acids, e.g. peptide synthesis. Alcohols and thiols may also be immobilized using the new polymers. Methods for the preparation of the polymers are provided, starting from a variety of polymer types.
Abstract: A novel O-transcarbamoylase enzyme and its use in preparing a variety of 3-carbamoyloxymethyl cephalosporins from 3-hydroxymethyl cephalosporins and carbamoyl compounds are described.
Type:
Grant
Filed:
February 15, 1977
Date of Patent:
February 21, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Ian D. Fleming, Michael K. Turner, Stephen J. Brewer
Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## (WHERE R is phenyl, thienyl or furyl; R.sup.a and R.sup.b are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl, aminocarbonyl, N-substituted aminocarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c is hydrogen or C.sub.1-4 alkyl; and m and n are each 0 or 1 such that the sum of m and n is 0 or 1) exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases.
Type:
Grant
Filed:
June 9, 1976
Date of Patent:
February 14, 1978
Assignee:
Glaxo Laboratories Limited
Inventors:
Michael W. Foxton, Gordon I. Gregory, David M. Rogers