Patents Represented by Attorney William H. Edgerton

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  • Heterocyclic-methylthioalkyl-amidines
    Patent number: 4118496
    Abstract: The compounds are N-(heterocyclomethylthioalkyl)derivatives of alkylguanidines, C-alkyl and C-aryl amidines and S-alkyl-isothioureas. 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-imidazolyl-methylthio)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: May 5, 1977
    Date of Patent: October 3, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin, Rodney Christopher Young
  • 3-Morpholino-2-heterocyclic-thiopropanamides
    Patent number: 4118567
    Abstract: The compounds are 3-morpholino-2-heterocyclicthiopropanamides which are inhibitors of gastric acid secretion.
    Type: Grant
    Filed: June 23, 1972
    Date of Patent: October 3, 1978
    Assignee: SmithKline Corporation
    Inventors: L. Martin Brenner, Bernard Loev
  • 7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl)cephalosporins and pharmaceutical compositions containing them
    Patent number: 4118490
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfonic acid or sulfamoyl substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds having antibacterial activity.
    Type: Grant
    Filed: May 11, 1977
    Date of Patent: October 3, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 7-Acylamino-3-[[3-(carboxymethyl)thio-1H-1,2,4-triazol-5-yl]thiom ethyl]-3-cephem-4-carboxylic acids
    Patent number: 4117124
    Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylthio substituted triazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.
    Type: Grant
    Filed: June 30, 1977
    Date of Patent: September 26, 1978
    Assignee: SmithKline Corporation
    Inventor: David Alan Berges
  • 7-Acylamino-3-[1-[2-(carboxymethylamino]ethyl) tetrazol-5-ylthiomethyl]-3-cephem-4-carboxylic acids
    Patent number: 4117125
    Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylaminoethyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.
    Type: Grant
    Filed: June 24, 1977
    Date of Patent: September 26, 1978
    Assignee: SmithKline Corporation
    Inventor: David Alan Berges
  • Sulfonyl benzofurans and benzothiophenes having coronary vasodilator activity
    Patent number: 4117128
    Abstract: The compounds are sulfonyl benzofurans and benzothiophenes having pharmacological activity, in particular, coronary vasodilator activity useful for the treatment of angina pectoris.
    Type: Grant
    Filed: August 3, 1976
    Date of Patent: September 26, 1978
    Assignee: SmithKline Corporation
    Inventor: L. Martin Brenner
  • 7-Acylamino-3-[1-(2-sulfamidoethyl)tetrazol-5-ylthiomethyl]-3- cephem-4-carboxylic acids
    Patent number: 4117123
    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: June 9, 1977
    Date of Patent: September 26, 1978
    Assignee: SmithKline Corporation
    Inventor: David Alan Berges
  • Method for preparing auranofin
    Patent number: 4115642
    Abstract: Auranofin and its congeners are prepared by reacting a bis(polyacetylsaccharide)disulfide with a tertiary phosphinegold mercaptide in a suitable organic solvent.
    Type: Grant
    Filed: June 30, 1977
    Date of Patent: September 19, 1978
    Assignee: SmithKline Corporation
    Inventors: David T. Hill, Ivan Lantos, Blaine M. Sutton
  • Pharmacologically active compounds
    Patent number: 4112104
    Abstract: The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. Two compounds of this invention are N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]thiourea and N,N'-bis]2-((4-methyl-5-imidazoly)methylthio)ethyl]-N"-cyanoguanidine.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: September 5, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin
  • 3-Chloro-6-phenylpyridazine compounds
    Patent number: 4111935
    Abstract: Substituted derivatives of 3-chloro-6-phenylpyridazine which are useful intermediates in the preparation of substituted phenylhydrazinopyridazines which have .beta.-adrenergic blocking and vasodilator activity.
    Type: Grant
    Filed: July 19, 1977
    Date of Patent: September 5, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: William John Coates, Anthony Maitland Roe, Robert Antony Slater, Edwin Michael Taylor
  • Intermediates for preparing substituted phenylglycylcephalosporins
    Patent number: 4111981
    Abstract: Cephalosporin compounds having a substituted phenylglycyl substituent at the 7-position and any of a variety of groups at the 3-position are prepared by acylation of a 7-aminocephalosporanic acid. The compounds have antibacterial activity.
    Type: Grant
    Filed: April 28, 1977
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventor: John Gerald Gleason
  • Pyridazinethiones
    Patent number: 4111936
    Abstract: Substituted phenyl pyridazinethiones which are useful intermediates in the preparation of substituted phenylhydrazinopyridazines which have .beta.-adrenergic blocking and vasodilator activity.
    Type: Grant
    Filed: July 19, 1977
    Date of Patent: September 5, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: William John Coates, Anthony Maitland Roe, Robert Antony Slater, Edwin Michael Taylor
  • 7-Acyl-3-(sulfoalkyl substituted oxadiazolylthiomethyl) cephalosporins
    Patent number: 4112088
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfoalkyl substituted oxadiazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
    Type: Grant
    Filed: April 25, 1977
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 7.beta.-Acylamino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins
    Patent number: 4112086
    Abstract: The compounds of this invention are cephalosporins having various acylamino substituents at the 7-position and a phosphonoalkyl or esterified phosphonoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
    Type: Grant
    Filed: November 2, 1976
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Bis(sulfide)gold(1+) salts
    Patent number: 4112113
    Abstract: The compounds are bis(sulfide)gold(1+) salts which have antiarthritic activity.
    Type: Grant
    Filed: February 25, 1977
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventor: David T. Hill
  • Substituted 1-thienyl and furyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds
    Patent number: 4111957
    Abstract: A group of 7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepines with structures containing a thienyl or furyl ring at position 1 which have dopaminergic activity. Particular species of this group include 7,8-dihydroxy-1-(5'-methyl-2'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether derivative, 7,8-dihydroxy-1-(2'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether as well as 7,8-dihydroxy-1-(3'-thienyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: September 5, 1978
    Assignee: SmithKline Corporation
    Inventors: Kenneth George Holden, Nelson Chi-Fai Yim
  • Pharmacologically active compounds
    Patent number: 4109003
    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: May 5, 1977
    Date of Patent: August 22, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin, Rodney Christopher Young
  • Process for preparing substituted glycines
    Patent number: 4108854
    Abstract: A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
    Type: Grant
    Filed: August 16, 1976
    Date of Patent: August 22, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, Nelson C. F. Yim
  • 2,3,4,5-Tetrahydro-1H-3-benzazepine-7,8-diones
    Patent number: 4108989
    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: April 1, 1977
    Date of Patent: August 22, 1978
    Assignee: SmithKline Corporation
    Inventor: Kenneth George Holden
  • Guanidino, thioureido and isothioureido derivatives containing imidazole groups
    Patent number: RE29761
    Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N', N"-disubstituted guanidino), N-(N'-substituted thiouredo), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: October 19, 1977
    Date of Patent: September 12, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin