Patents Represented by Attorney William H. Edgerton

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  • 1-(2-Sulfamidoethyl)-1,4-dihydro-5H-tetrazole-5-thione
    Patent number: 4174323
    Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a sulfamidoethyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: November 13, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Thiourea compounds, compositions and methods and use
    Patent number: 4173644
    Abstract: The compounds are dithiocarbamates and isothioureas which are histamine H.sub.2 -antagonists. Two compounds of the invention are 2-(5-methyl-4-imidazolylmethylthio)ethyl N-methyldithiocarbamate and S-[2-(5-methyl-4-imidazolyl-methylthio)ethyl]-N-cyano-N'-methylisothiourea .
    Type: Grant
    Filed: July 28, 1978
    Date of Patent: November 6, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin, Robert J. Ife
  • 2,3,4,5-Tetrahydro-1H-3-benzazepine-7,8-diones
    Patent number: 4172890
    Abstract: Novel benzazepine derivatives having central and peripheral dopaminergic activity useful in treating Parkinson's and cardiovascular diseases. The compounds have additional use as intermediates for the synthesis of other benzazepines with similar useful properties. The 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-dione derivatives are particularly useful.
    Type: Grant
    Filed: May 11, 1978
    Date of Patent: October 30, 1979
    Assignee: SmithKline Corporation
    Inventor: Kenneth G. Holden
  • Benz-tetrasubstituted 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4171359
    Abstract: A group of 6,9-disubstituted-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepi nes have dopaminergic activity. Examples of leading species of the invention are 6,9-dichloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and 6,9-dichloro-7,8-dihydroxy-1-(p-hydroxy-phenyl)-2,3,4,5-tetrahydro-1H- 3-benzazepine in the form of an acid addition salt.
    Type: Grant
    Filed: April 12, 1978
    Date of Patent: October 16, 1979
    Assignee: SmithKline Corporation
    Inventor: Joseph Weinstock
  • 7-Acylamino-3-(sulfaminoalkyl substituted tetrazolylthiomethyl)cephalosporins, antibacterial compositions containing them and methods of treating bacterial infections with them
    Patent number: 4171368
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
    Type: Grant
    Filed: July 14, 1978
    Date of Patent: October 16, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Phosphinegold (I) salts having antiarthritic activity
    Patent number: 4171360
    Abstract: The compounds are (pyridine) (trisubstituted phosphine) gold(I) salts which have antiarthritic activity.
    Type: Grant
    Filed: February 21, 1978
    Date of Patent: October 16, 1979
    Assignee: SmithKline Corporation
    Inventor: David T. Hill
  • 7-Acylamino-3-(sulfaminoalkyl substituted tetrazolylthiomethyl)cephalosporins antibacterial compositions containing them and methods of treating bacterial infections with them
    Patent number: 4171362
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
    Type: Grant
    Filed: July 14, 1978
    Date of Patent: October 16, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 7-Amino-3-(sulfaminoalkyl substituted tetrazolylthiomethyl)cephalosporin intermediates for preparing 7-acylamino cephalosporins
    Patent number: 4171433
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
    Type: Grant
    Filed: July 14, 1978
    Date of Patent: October 16, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Chemical process
    Patent number: 4171325
    Abstract: Process for preparing heterocyclicalkylthioalkyl-N-cyanoguanidines and thioureas by treating a heterocyclicalkyl derivative with a mercaptoalkyl-N-cyanoguanidine or thiourea. Two specific products are N-cyano-N'-methyl-N"-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]guanidine and N-methyl-N'-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]thiourea, both useful as histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: February 16, 1978
    Date of Patent: October 16, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Heterocyclic-methylthioalkyl-guanidines
    Patent number: 4170652
    Abstract: The compounds are N-(heterocyclomethylthioalkyl)derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkylisothioureas. The compounds may also have N'-lower alkyl or N'-(heterocyclomethylthioalkyl)substituents. Three compounds of the invention are S-methyl-N-[2-(5-methyl-4-imidazolylmethylthio)ethyl]isothiourea, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: April 17, 1978
    Date of Patent: October 9, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Thiazole and isothiazole derivative as blockers of histamine H.sub.2 -receptors
    Patent number: 4166856
    Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: March 31, 1978
    Date of Patent: September 4, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • N-Hetero substituted cyclobutenones
    Patent number: 4166857
    Abstract: The compounds are 1-amino-2-heterocyclic-alkylamino-cyclobut-1-ene-3,4-diones which are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: July 27, 1978
    Date of Patent: September 4, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Charon R. Ganellin, Rodney C. Young
  • Methods and intermediates for preparing cis-4-oxoazetidine intermediates
    Patent number: 4166816
    Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
    Type: Grant
    Filed: August 3, 1977
    Date of Patent: September 4, 1979
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • 2H-imidazole-2-thione derivatives
    Patent number: 4166184
    Abstract: Imidazole derivatives which are useful intermediates for the production of compounds having pharmacological activity at histamine H.sub.2 receptors. A specific compound of the present invention is 4-(4-aminobutyl)-1,3-dihydro-5-methyl-2H-imidazole-2-thione, hereinafter referred to as 4-(4-Aminobutyl)-5-methylimidazole-2-thione.
    Type: Grant
    Filed: December 8, 1977
    Date of Patent: August 28, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Ronald J. King, George R. White
  • Use of cyclic esters to prepare 2,3-dichloro-4-(2-thenoyl)phenoxyacetic acid
    Patent number: 4166061
    Abstract: A new process and intermediates for preparing 2,3-dichloro-4-(2-thenoyl)phenoxyacetic acid (ticrynafen, a diuretic agent) using as a key reaction a Friedel-Crafts acylation of an esterified 3-(2,3-dichlorophenoxy)-1,2-propanediol using a thenoyl halide.
    Type: Grant
    Filed: November 2, 1977
    Date of Patent: August 28, 1979
    Assignee: SmithKline Corporation
    Inventors: Antonietta R. Mastrocola, Robert L. Webb
  • 6-Carboxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds and use as dopaminergic agents
    Patent number: 4165372
    Abstract: A group of 1-phenyl-3-benzazepines with structures characterized by having a carboxy derived substituent at position 6 which are dopaminergic agents or are intermediates for preparing other dopaminergic agents. Particular illustrative species include 6-carbomethoxy-7,8-dihydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-ben zazepine, 6-carboxy-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and 6-carbomethoxy-7,8-dihydroxy-1-(4'-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3- benzazepine.
    Type: Grant
    Filed: November 17, 1977
    Date of Patent: August 21, 1979
    Assignee: SmithKline Corporation
    Inventors: Charles K. Brush, Joseph Weinstock
  • Bis(sulfide)gold(1+) salts
    Patent number: 4165380
    Abstract: The compounds are bis(sulfide)gold(1+) salts which have antiarthritic activity.
    Type: Grant
    Filed: June 2, 1978
    Date of Patent: August 21, 1979
    Assignee: SmithKline Corporation
    Inventor: David T. Hill
  • Process for preparing new imidazolemethylphosphonium salts
    Patent number: 4163858
    Abstract: New imidazolemethylphosphonium salts having a degradable group at the 2-position which are useful intermediates for preparing histamine H.sub.2 antagonists. This invention concerns the preparation of imidazolemethylphosphonium salts having no substituent at the 2-position by heating the compounds referred to above.
    Type: Grant
    Filed: March 8, 1978
    Date of Patent: August 7, 1979
    Assignee: SK&F Lab Co.
    Inventors: Clifford S. Labaw, Robert L. Webb, George R. Wellman
  • 3-Aminoazetidinone derivatives
    Patent number: 4162250
    Abstract: New lactam intermediates and methods for preparing a new series of 7-acylamino-8-oxo-3-oxa-1-azabicyclo[4.2.0]-octane-2-carboxylic acid derivatives are described. The end product compounds have antibacterial activity especially against certain Gram negative organisms.An example of the compounds of this invention are cis-3-blocked amino-4-ketoazetidinyl-2-acetaldehydes and their acetal derivatives.
    Type: Grant
    Filed: June 6, 1978
    Date of Patent: July 24, 1979
    Assignee: SmithKline Corporation
    Inventors: Thomas F. Buckley, John G. Gleason
  • Method for 6-bromination of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds
    Patent number: 4160765
    Abstract: The preparation of 6-bromo-7,8-dimethoxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines is described by direct bromination of the nucleus.
    Type: Grant
    Filed: November 17, 1976
    Date of Patent: July 10, 1979
    Assignee: SmithKline Corporation
    Inventor: Joseph Weinstock