Patents Represented by Attorney William H. Edgerton

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  • Pharmacologically active guanidine compounds for inhibiting H-2 histamine receptors
    Patent number: 4221802
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: February 7, 1979
    Date of Patent: September 9, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Isothiazolyl alkylaminoethylene compounds
    Patent number: 4220652
    Abstract: The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]e thylene.
    Type: Grant
    Filed: August 1, 1978
    Date of Patent: September 2, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin, Hunter D. Prain
  • Triazinones
    Patent number: 4220767
    Abstract: The compounds are substituted 1,2,4-triazin-5-ones which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are 3-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-6-(3-methoxybenzyl)-1,2, 4-triazin-5-one and 3-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-6-(3-pyridylmethyl)-1,2, 4-triazin-5-one.
    Type: Grant
    Filed: June 20, 1979
    Date of Patent: September 2, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert J. Ife
  • Alkoxy pyridyl substituted alkanes
    Patent number: 4219553
    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 thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(3-methoxy-2-pyridylmethylthio)ethyl)guanidino]propane and 1-[N-(2-(3-methoxy-pyridylmethylthio)ethyl)guanidino]-3-[N'-2-(5-methyl-4- imidazolylmethylthio)ethyl)guanidino]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: October 4, 1978
    Date of Patent: August 26, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Substituted 4-pyrimidone compounds, compositions and methods of use
    Patent number: 4218452
    Abstract: The compounds are substituted isocytosines which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-(3-methoxybenzyl)-4-py rimidone and 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-benzyloxy-4-pyrimidone .
    Type: Grant
    Filed: December 15, 1977
    Date of Patent: August 19, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • 4- and 5-Substituted 2,3-dihydro-1H-isoindoles, pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
    Patent number: 4218464
    Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using novel 2,3-dihydro-1H-isoindole compounds having 4- and 5-substituents.
    Type: Grant
    Filed: March 2, 1979
    Date of Patent: August 19, 1980
    Assignee: SmithKline Corporation
    Inventors: William E. Bondinell, Robert G. Pendleton
  • Heterocyclic alkyl 4-pyrimidones
    Patent number: 4216318
    Abstract: The compounds are substituted isocytosines which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-(3-pyridylmethyl)-4-py rimidone and 2-[2-(3-bromo-2-pyridylmethylthio)-ethylamino]-5-(4-pyridylmethyl)-4-pyrim idone.
    Type: Grant
    Filed: February 16, 1979
    Date of Patent: August 5, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin
  • Process for preparing 4-substituted imidazole compounds
    Patent number: 4215217
    Abstract: A process for preparing 4-(oxy, thio or amino)methylimidazole compounds via displacement of the trisubstituted phosphonium group from 4-(trisubstituted phosphonium)-methylimidazole compounds is disclosed.
    Type: Grant
    Filed: June 14, 1978
    Date of Patent: July 29, 1980
    Assignee: SK&F Lab Co.
    Inventors: Joseph J. Lewis, Robert L. Webb
  • Pyridyl ureas, thioureas and guanidines
    Patent number: 4215125
    Abstract: The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. A compound of this invention is N,N'-bis-[2-(2-pyridylmethylthioethyl]-N"-cyanoguanidine.
    Type: Grant
    Filed: January 22, 1979
    Date of Patent: July 29, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Alkoxy pyridine compounds
    Patent number: 4215126
    Abstract: The compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N"-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitroeth ylene.
    Type: Grant
    Filed: February 21, 1979
    Date of Patent: July 29, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Imidazolyl alkyl bisamidines
    Patent number: 4212875
    Abstract: Bisamidines carrying one unsaturated nitrogen heterocycle-containing substituent, representative of which is 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methyl-g uanidino]octane, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: May 2, 1978
    Date of Patent: July 15, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Peter D. Miles
  • 7-Acylamino-3-[1-[2-(carboxymethylamino)ethyl]tetrazol-5-ylthio methyl]-3-cephem-4-carboxylic acids
    Patent number: 4210587
    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: July 3, 1978
    Date of Patent: July 1, 1980
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Amidinosulphonic acid derivatives
    Patent number: 4210658
    Abstract: Amidinosulphonic acid derivatives carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'[2-(5-methyl-4-imidazolylmethylthio)-ethyl]amidinosulphonic acid and N-methyl-N'[2-(3-chloropyrid-2-ylmethylthio) ethyl]amidinosulphonic acid, are histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: September 6, 1978
    Date of Patent: July 1, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Rodney C. Young, Zev Tashma
  • Pharmacologically active 1,3-bis[1-(2-heteroalkylthio)ethylamino)-2-nitrovinyl-1-amino]propane derivatives
    Patent number: 4210652
    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 thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido)groups. Two compounds of the invention are 1,3-bis-[N'-(2-(3-methoxy-2-pyridylmethylthio)ethyl)guanidino]propane and 1-[N-(2-(3-methoxy-pyridylmethylthio)ethyl)guanidino]-3-[N'-2-(5-methyl-4- imidazolylmethylthio)ethyl)guanidino]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: October 4, 1978
    Date of Patent: July 1, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
    Patent number: 4208430
    Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using substituted carbamimidothioic acid phenylalkyl esters.
    Type: Grant
    Filed: March 15, 1979
    Date of Patent: June 17, 1980
    Assignee: SmithKline Corporation
    Inventors: William E. Bondinell, Robert G. Pendleton
  • Alkylthio-7,8-dihdroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having dopaminergic activity
    Patent number: 4206210
    Abstract: A new series of lower alkylthio-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having potent central dopaminergic activity of utility in treating Parkinson's disease. The 6-and 9-methylthio compounds are particularly of use.
    Type: Grant
    Filed: June 2, 1978
    Date of Patent: June 3, 1980
    Assignee: SmithKline Corporation
    Inventor: Kenneth G. Holden
  • Pharmaceutical compositions having immunosuppressant activity and methods therefor
    Patent number: 4205071
    Abstract: S-(Aminoalkyl)isothioureas which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.
    Type: Grant
    Filed: November 21, 1977
    Date of Patent: May 27, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Margaret R. Vickers
  • Bis[triethylphosphine)aurio]sulfonium sugars
    Patent number: 4201775
    Abstract: A new series of gold containing sugars having anti-arthritic activity are characterized by the presence of a bis[(triethylphosphine)aurio]sulfonium salt moiety at the 1-position of the glucopyranoside. The compounds are prepared by reacting a 1-S-triethylphosphinegold-1-thio-glucopyranoside with a triethylphosphinegold halide.
    Type: Grant
    Filed: March 23, 1979
    Date of Patent: May 6, 1980
    Assignee: SmithKline Corporation
    Inventors: John J. Filan, Walter W. Holl, George R. Wellman
  • Method for preparing auranofin
    Patent number: 4200738
    Abstract: A new synthesis of auranofin comprising reacting 2,3,4,6-tetra-O-acetyl-.alpha.-D-glucopyranosyl bromide with a S-(triethylphosphineaurous)thiouronium salt.
    Type: Grant
    Filed: April 21, 1977
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: David T. Hill, Blaine M. Sutton, Ivan Lantos
  • Method for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
    Patent number: 4200754
    Abstract: A novel process for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline by cyclizing N-acetyl-2,3-dichlorobenzylaminoacetaldehyde dimethyl acetal with a Lewis acid, reducing, and hydrolyzing the resulting acylated isoquinoline is disclosed.
    Type: Grant
    Filed: February 2, 1979
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl D. Perchonock