Patents Assigned to Glaxo Laboratories Limited
  • Patent number: 4128715
    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.
    Type: Grant
    Filed: April 27, 1977
    Date of Patent: December 5, 1978
    Assignee: Glaxo Laboratories Limited
    Inventor: Christopher J. Sharp
  • Patent number: 4122259
    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.
    Type: Grant
    Filed: December 10, 1976
    Date of Patent: October 24, 1978
    Assignee: Glaxo Laboratories Limited
    Inventor: David C. Humber
  • Patent number: 4118499
    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.
    Type: Grant
    Filed: October 8, 1976
    Date of Patent: October 3, 1978
    Assignee: Glaxo Laboratories Limited
    Inventors: Leslie Stephenson, Colin Smith
  • Patent number: 4113591
    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
  • Patent number: 4110534
    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
  • Patent number: 4107431
    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
  • Patent number: 4103084
    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
  • Patent number: 4095021
    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
  • Patent number: 4093803
    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
  • Patent number: 4093721
    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.
    Type: Grant
    Filed: January 6, 1977
    Date of Patent: June 6, 1978
    Assignee: Glaxo Laboratories Limited
    Inventors: Gordon H. Phillipps, Brian M. Bain
  • Patent number: 4092477
    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
  • Patent number: 4092306
    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.
    Type: Grant
    Filed: September 21, 1976
    Date of Patent: May 30, 1978
    Assignee: Glaxo Laboratories Limited
    Inventor: David Thomas Eastlick
  • Patent number: 4091209
    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
  • Patent number: 4087551
    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.
    Type: Grant
    Filed: March 4, 1975
    Date of Patent: May 2, 1978
    Assignee: Glaxo Laboratories Limited
    Inventor: Peter John May
  • Patent number: 4083837
    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.
    Type: Grant
    Filed: September 7, 1976
    Date of Patent: April 11, 1978
    Assignee: Glaxo Laboratories Limited
    Inventors: Gerard Gallagher, Derek Walker
  • Patent number: 4079178
    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
  • Patent number: 4076936
    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.
    Type: Grant
    Filed: December 1, 1976
    Date of Patent: February 28, 1978
    Assignee: Glaxo Laboratories Limited
    Inventor: Brian Laundon
  • Patent number: 4076913
    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.
    Type: Grant
    Filed: September 27, 1976
    Date of Patent: February 28, 1978
    Assignee: Glaxo Laboratories Limited
    Inventors: Derek Walker, Philip Howard Chapman
  • Patent number: 4075061
    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
  • Patent number: 4074047
    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