Patents Represented by Attorney William H. Edgerton

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  • Substituted 2H-pyran-2,6(3H)-dione derivatives
    Patent number: 4160021
    Abstract: Substituted 2H-pyran-2,6(3H)-dione derivatives useful in the treatment of allergic conditions are prepared by reaction of 3,5-diacetyl-4,6-dihydroxy-2H-pyran-2-one with an appropriate aniline.
    Type: Grant
    Filed: March 10, 1978
    Date of Patent: July 3, 1979
    Assignee: SmithKline Corporation
    Inventor: Kenneth M. Snader
  • N-oxy and N-amino guanidines
    Patent number: 4160030
    Abstract: The compounds are N-oxy and N-amino guanidines which are histamine H.sub.2 -antagonists. A compound of this invention is N-hydroxy-N'-methyl-N"-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]guanidi ne.
    Type: Grant
    Filed: February 22, 1978
    Date of Patent: July 3, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen
  • 7-Acyl-3-(sulfonic acid and sulfamoyl substituted tetrazolyl thiomethyl) cephalosporins
    Patent number: 4159373
    Abstract: The compounds of this invention are cephalosporins having a 3- or 4-aminomethylphenylacetamido substituent at the 7-position and a sulfonic acid substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus. The compounds have antibacterial activity.
    Type: Grant
    Filed: April 4, 1978
    Date of Patent: June 26, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 4-Pyrimidones compositions, and methods of use
    Patent number: 4159329
    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-p yrimidone and 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-6-benzyloxy-4-pyrimidone .
    Type: Grant
    Filed: December 15, 1977
    Date of Patent: June 26, 1979
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • 7.beta.-Acyloxy-3-acetoxymethyl cephalosporins
    Patent number: 4158733
    Abstract: The compounds of this invention are cephalosporins having a 7.beta.-acyloxy group and 7.beta.-hydroxy intermediates for the preparation thereof. The compounds have antibacterial activity.
    Type: Grant
    Filed: December 1, 1976
    Date of Patent: June 19, 1979
    Assignee: SmithKline Corporation
    Inventor: John G. Gleason
  • Alkoxy pyridine compounds
    Patent number: 4156727
    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: January 13, 1978
    Date of Patent: May 29, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Alkoxy pyridine
    Patent number: 4154838
    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: January 13, 1978
    Date of Patent: May 15, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Substituted isocytosines having histamine H.sub.2 -antagonist activity
    Patent number: 4154834
    Abstract: The compounds are substituted isocytosines which are histamine H.sub.2 -antagonists. Two specific compounds of the present inventon 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-pyrimi done.
    Type: Grant
    Filed: December 16, 1977
    Date of Patent: May 15, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin
  • Pharmacologically active guanidine compounds in compositions and methods of use
    Patent number: 4154844
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: October 31, 1977
    Date of Patent: May 15, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Imidazo alkylamino pyrimidones
    Patent number: 4153793
    Abstract: Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
    Type: Grant
    Filed: March 17, 1977
    Date of Patent: May 8, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • 6-Hydroxy-5,6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles
    Patent number: 4153706
    Abstract: The compounds are 6-hydroxy-5,6-substituted-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles which have antiarthritic activity and are useful as intermediates for preparing 2,3-dihydroimidazo[2,1-b]thiazole antiarthritic compounds. A particular compound of this invention is 5,6-bis-(p-fluorophenyl)-6-hydroxy-2,3,5,6-tetrahydroimidazo[2,1-b]thiazol e.
    Type: Grant
    Filed: February 13, 1978
    Date of Patent: May 8, 1979
    Assignee: SmithKline Corporation
    Inventors: Paul E. Bender, David T. Hill
  • Ethylene derivatives
    Patent number: 4153704
    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: November 22, 1977
    Date of Patent: May 8, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin, Hunter D. Prain
  • 3-Acyl-5-alkyl-2H-pyran-2,4,6-(3H,5H)-triones and their 4-hydroxy tautomers
    Patent number: 4153720
    Abstract: 3-Acyl-5-alkyltetrahydro-2,4,6-pyrantriones are prepared by catalytic hydrogenation of their 3,5-diacyl congeners. They have been found to have anti-allergic activity useful for treating the symptoms of asthma.
    Type: Grant
    Filed: January 19, 1978
    Date of Patent: May 8, 1979
    Assignee: SmithKline Corporation
    Inventor: Theodore M. Resnick
  • Pharmacologically active compounds and compositions and methods of use
    Patent number: 4152453
    Abstract: The compounds are substituted S-(aminoalkyl)isothioureas which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are S-[6-(N'-methylthioureido)hexyl]isothiourea and S-[5-(N'-cyano-(N"-methylguanidino)pentyl]isothiourea.
    Type: Grant
    Filed: January 18, 1978
    Date of Patent: May 1, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Robert J. Ife
  • Imidazolyl thioureas, ureas and guanidines
    Patent number: 4152443
    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-imidazolyl)methylthio)ethyl]-N"-cyanoguanidine.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: May 1, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Synthesis of 6-(2-hydroxyphenyl)-3(2H)-pyridazinones from trihalocarbinols
    Patent number: 4152517
    Abstract: A new synthesis for the preparation of 6-(2-hydroxyphenyl)-3-pyridazinones whose key reaction is cyclizing a 1,1,1-trihalo-2-hydroxy-4-(2-hydroxyphenyl)-1-butanone with hydrazine. 6-(2-Hydroxyphenyl)-3-pyridazinones are important intermediates for preparing medicinally active compounds.
    Type: Grant
    Filed: October 19, 1977
    Date of Patent: May 1, 1979
    Assignee: SmithKline Corporation
    Inventors: Sidney H. Levinson, Wilford L. Mendelson
  • Pharmacologically active thiourea and urea compounds
    Patent number: 4151288
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: September 29, 1977
    Date of Patent: April 24, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Nitromethylene amidino derivatives containing imidazole groups
    Patent number: 4151289
    Abstract: The compunds 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-(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: September 8, 1977
    Date of Patent: April 24, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • 7-Acylamino-3-(1-car boxymethylthioethyltetrazolyl-5-thiomethyl)-3-cephem-4-carboxylic acids
    Patent number: 4147701
    Abstract: New semisynthetic cephalosporins characterized by having structures with a 1-carboxymethylthioethyltetrazolyl-5-thiomethyl group at position 3. Exemplary is the antibacterially effective 7-D-mandelamido-3-(1-carboxymethylthioethyltetrazolyl-5-thiomethyl)-3-ceph em-4-carboxylic acid disodium salt.
    Type: Grant
    Filed: November 2, 1977
    Date of Patent: April 3, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 4-Pyrimidone compounds
    Patent number: 4145546
    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-p yrimidone and 2-?2-(5-methyl-4-imidazolylmethylthio)ethylamino!-5-benzyloxy-4-pyrimidone .
    Type: Grant
    Filed: September 21, 1977
    Date of Patent: March 20, 1979
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, John C. Emmett, Charon R. Ganellin