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Glaxo Laboratories Limited Patents
Assignee:
Glaxo Laboratories Limited
Address:
London, GB2
No. of patents:
92
Patents:


1 2










Patent Number Title Of Patent Date Issued
4529734 2-formyloxymethyl-clavam July 16, 1985
2-Formyloxymethyl-clavam is described and its use as an antifungal compound against a range of fungi for both medical and horticultural and agricultural use is disclosed. Processes for isolating the compound from fermentations of strains of Streptomyces clavuligerus are described.
4367175 Pure potassium salt of clavulanic acid January 4, 1983
The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]-heptane -2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueou
4351842 N-Cyclopropylisoindolines September 28, 1982
Compounds of the general formula: ##STR1## in which A is a benzene ring or a carbocyclic aromatic group consisting of two or three fused benzene rings, the group A being linked to the nitrogen containing ring at two adjacent carbon atoms and the benzene ring or each benzene ring
4230622 Halogen derivatives of clavulaic acid October 28, 1980
Novel halogen derivatives of clavulanic acid are described which are of value in the preparation of a range of clavulins which either inhibit .beta.-lactamases or show activity against strains of both gram-positive and gram-negative bacteria. Processes for preparing the halogen deriv
4228074 Azetidinone derivatives October 14, 1980
.beta.-Lactam compounds of the formula (I) ##STR1## (wherein R represents an esterified carboxyl group, --NR.sup.1 R.sup.2 R.sup.3 represents the residue of a nitrogen base, and R.sup.4 represents a hydrogen atom, a hydroxyl group or acylated or etherified hydroxyl group or the r
4209616 Syn isomers of cephalosporins having .alpha.-hydroximino- or .alpha.-acyloxyiminoacylamido group June 24, 1980
The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure
4193917 Chemical compounds March 18, 1980
Novel semisynthetic .beta.-lactam intermediates of use in the production of cephalosporins, penicillins and related .beta.-lactam antibiotic compounds are provided. The novel compounds are prepared from .beta.-lactams obtained by cleavage of the 1,2-sulphur-carbon bond of a penicillin
4192871 Chemical compounds March 11, 1980
Pregnanes and androstanes are described which essentially possess a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4.5- or 5,6-double bond, a 17.alpha.-hydrogen atom and an 11.beta.-aminoester group. Other optional substituents or double bonds may be present. The compounds have
4169547 Ointment container with finger actuated piston October 2, 1979
A container has a body with a nozzle at one end. A plunger can be pushed through the body by the insertion of a finger of the user through the opening in the body so as to force the contents of the container out through the nozzle.
4168309 Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group September 18, 1979
Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl
4165430 Cephalosporins having a 7-carboxy substituted .alpha.-etherified oximinoarylacetamido) group August 21, 1979
Cephalosporin antibiotics having the formula: ##STR1## (where R is thienyl, furyl or phenyl; R.sup.a is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, carboxy
4164447 O-Transcarbamoylase August 14, 1979
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.
4162360 3-Carbamoyloxymethyl-7-substituted oximino acetamido cephalosporanic acid derivatives July 24, 1979
3-Carbamoyloxymethyl and 3-N-methylcarbamoyloxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen,
4157278 Immunostimulatory agents June 5, 1979
This invention relates to a process for the production of water-soluble fractions from Streptomyces griseus mycelium and containing peptidoglycan material having immunostimulatory properties and to formulations containing such fractions. Several examples of the process are given.
4144393 3-Acetoxymethyl cephalosporins having at position-7 a carboxy substituted .alpha.-etherified hyd March 13, 1979
3-Acetoxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, carboxy, C.sub.2 -C.sub.5 carbalk
4144392 Cephalosporins having at position-7 a carboxy substituted .alpha.-etherified hydroxyimino-arylac March 13, 1979
Cephalosporin antibiotics having the formula: ##STR1## (where R is thienyl, furyl or phenyl; R.sup.a is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, carboxy
4144242 Process for the purification of clavulanic acid March 13, 1979
The invention provides the compound (2R,5R,Z)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0]-heptane -2-carboxylic acid and its salts in purified form and pharmaceutical compositions containing them and a process for the purification of such compounds by conversion in aqueou
4138555 (6R,7R)-7-[2-aryl-2-(etherified oximino)acetamido]-3-carbamoyloxymethylceph-3-em-4-carboxylic ac February 6, 1979
Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R.sup.1 is a furyl, thienyl or phenyl group and R.sup.2 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl group and in which the 3-position substituent is a carbamoylo
4132849 Process for the preparation of 3-hydroxymethyl cephalosporins January 2, 1979
A process for the preparation of a 3-hydroxymethyl cephalosporin compound which comprises selectively hydrolyzing a 3-formyloxymethyl cephalosporin compound under acidic conditions in the presence of a protic solvent whereby a 3-hydroxymethyl cephalosporin is produced.
4128715 Cephalosporin antibiotics December 5, 1978
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.
4122259 7.beta.-[2-Aryl-2-(etherified oximino)acetamido]-3-N-substituted carbamoyloxymethylceph-3-em-4-c October 24, 1978
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 positi
4118499 Anti-anxiety and anti-parkinsonian 1-aminoalkyl-2-endo-chloro-7,7-dimethylnorbornanes October 3, 1978
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
4113591 Preparation of cephalosporin compounds September 12, 1978
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.
4110534 Process for the preparation of 3-vinyl and substituted vinyl cephalosporins August 29, 1978
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.
4107431 .DELTA..sup.3 -3-Vinyl or substituted vinyl-4-carboxy cephalosporins August 15, 1978
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.
4103084 7-(Carboxy substituted .alpha.-etherified oximino arylacetamido) cephalosporins having a 3-vinyl July 25, 1978
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.
4095021 3-Carbamoyloxymethyl or N-methyl-carbamoyloxymethyl-7-[2-carboxymethoxyimino-2-(fur-2-yl or June 13, 1978
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.
4093803 7.beta.-[2-Etherified oximino-2-(thienyl-, furyl- or pyridylacetamido)] cephalosporins June 6, 1978
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 ether
4093721 Pharmaceutical compositions of 6.alpha.,9.alpha.-difluoro-androst-4-ene-17.beta.-carboxylates an June 6, 1978
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-fluoroe
4092477 7.beta.-[2-Etherified oximino-2-(phenyl- or naphthylacetamido)] cephalosporins May 30, 1978
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 ether
4092306 Oxidation of hydrazones to the corresponding diazo compounds in the presence of a phase transfer May 30, 1978
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
4091209 7.beta.-[2-Etherified oximino-2-(phenyl or naphthylacetamido)]cephalosporins having a 2-halo May 23, 1978
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 ether
4087551 Amino-bicycloheptanes May 2, 1978
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
4083837 Oxidation of hydrazones to the corresponding diazo compound April 11, 1978
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
4079178 Cephalosporins having (.alpha.-etherified oximino) acylamido groups at the 7-position March 14, 1978
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 ether
4076936 7.beta.-(2-Aryl-2-hydroxyiminoacetamido)ceph-3-em-4-carboxylic acids carrying a 7.alpha.-lower a February 28, 1978
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.
4075061 Method for producing cephalosporins February 21, 1978
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.
4074047 7[2-(Aminocarbonylalkoxyimino)acetamido] derivatives of cephalosporin February 14, 1978
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
4067858 Acid derivative immobilized cephalosporin carboxylic carrying polymer January 10, 1978
There are provided cephalosporin and penicillin carboxylic acid derivatives which comprise polymers carrying a plurality of molecules of said acid, the carboxyl groups of which are blocked by attachment to the polymer, principally by forming ester linkages to aliphatic carbon atoms in th
4064346 3-Acetoxym ethyl-7.beta.-(2-carboxy-methoxyimino-2-arylacetamido)ceph-3-em-4-carboxy lic acids December 20, 1977
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 ether
4062955 Analgesic basic naphthalene derivatives December 13, 1977
Compounds of the general formula: ##STR1## wherein the groups CHR.sup.1 NR.sup.2 R.sup.3 and CHR.sup.4 NR.sup.5 R.sup.6 may be the same or different and where the group CHR.sup.4 NR.sup.5 R.sup.6 is in either the 1 or the 3 position and R.sup.1 and R.sup.4 independently represent
4059573 Extraction of N-blocked amino acids from aqueous media November 22, 1977
N-blocked amino acids, particularly derived from natural sources such as fermentation liquors, are extractively esterified from aqueous media by treatment of the aqueous solution with a diazoalkane, e.g. diphenyldiazomethane, in the presence of a water-immiscible organic solvent. Use
4038469 Aqueous insoluble polymers containing a plurality of diazomethylene groups July 26, 1977
Novel polymers are provided which carry diazomethylene or hydrazonomethylene groups. Such polymers are of especial 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 m
4033950 3-Hydroxymethyl-7.beta.-(2-alkoxy-or benzyloxyimino-2-arylacetamido)ceph-3-em-4-carboxylic acids July 5, 1977
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 ether
4024137 7.beta.-[2-Etherified oximino-2-(phenyl- or naphthylacetamido)] cephalosporins May 17, 1977
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 ether
4024134 Syn isomers of cephalosporins having .alpha.-hydroximino- or .alpha.-acyloxyiminoacylamido group May 17, 1977
The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure
4024133 7.beta.-[2-Etherified oximino-2-(thienyl-,furyl- or pyridylacetamido)]cephalosporins May 17, 1977
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 ether
4020077 Antibiotics April 26, 1977
Novel 6.beta.-isocyano penicillin and 7.beta.-isocyano cephalosporin esters of value as intermediates in the synthesis of penicillin and cephalosporin antibiotics are provided. The novel compounds may be prepared by reaction of the corresponding 6.beta.-formamido penicillin ester or
4020058 Improvements in or relating to cephalosporin antibiotics April 26, 1977
Cephalosporin antibiotics of formula ##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
4017515 .alpha.-(Etherified oximino) carboxylic acids and acid chlorides April 12, 1977
.alpha.-(Etherified oximino)carboxylic acids, represented by the formula:- ##STR1## where R is hydrogen or an organic group having 1-20 carbon atoms and R.sup.a is an etherifying monovalent organic group having 1-16 carbon atoms linked to the oxygen atom through a carbon atom, and th
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