Patents Assigned to Smith Kline & French Laboratories Limited
  • Sulphoxides
    Patent number: 4255425
    Abstract: The compounds are sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines which are useful to produce inhibition of histamine H-2 receptors.
    Type: Grant
    Filed: November 13, 1978
    Date of Patent: March 10, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George R. White
  • 5-(Hydroxypyridylalkyl)-4-pyrimidones
    Patent number: 4255428
    Abstract: The compounds are substituted 2-amino-4-pyrimidones with a 5-(hydroxypyridylalkyl) substituent which are histamine H.sub.2 -antagonists. Two specific compounds are 2-[2-(3-bromo-2-pyridylmethylthio)ethylamino]-5-(2-hydroxy-4-pyridylmethyl )-4-pyrimidone and 2-[4-(3-methoxy-2-pyridyl)butylamino]-5-(2-hydroxy-4-pyridylmethyl)-4-pyri midone.
    Type: Grant
    Filed: April 24, 1979
    Date of Patent: March 10, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant, Charon R. Ganellin
  • Pyridyl alkylguanidines
    Patent number: 4247558
    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: May 2, 1979
    Date of Patent: January 27, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • 2-Heterocyclic alkylamino-3-nitropyrroles
    Patent number: 4238494
    Abstract: 3-Nitro-2-substituted aminopyrroles are histamine H.sub.2 -receptor antagonists. The 2-position substituent is a fully-unsaturated heterocyclyl alkyl group preferably with with alkyl group interrupted by sulfur or oxygen. The 4- and 5-positions of the pyrrole ring can also be substituted.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: December 9, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • 2-(Substituted amino)-3-nitro-2,3-unsaturated nitrogen heterocycles
    Patent number: 4238493
    Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: May 30, 1979
    Date of Patent: December 9, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Pyrimidine compounds
    Patent number: 4234588
    Abstract: The compounds are substituted pyrimidine compounds which are histamine H.sub.2 -antagonists. A specific compound of the present invention is 2-[2-(5-dimethylaminomethyl)-2-furylmethylthio)ethylamino]-5-(3-pyridylmet hyl)-4-pyrimidone.
    Type: Grant
    Filed: February 7, 1979
    Date of Patent: November 18, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert J. Ife
  • Pharmacologically active triazole and thiadiazole thiourea and urea compounds
    Patent number: 4230865
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: September 8, 1978
    Date of Patent: October 28, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pharmacologically active thiadiazole guanidine compounds
    Patent number: 4228291
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: October 4, 1978
    Date of Patent: October 14, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Genellin
  • Intermediates in the process for making histamine antagonists
    Patent number: 4227000
    Abstract: A process for making substituted 2-aminopyrimidones which are histamine H.sub.2 - antagonists which comprises reacting a 2-nitroaminopyrimidone with a heteroarylalkylamine, heteroarylalkylthioalkylamine, or heteroarylalkoxyalkylamine. One particular compound which can be made by this process is 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-[5-(1,3-benzodioxolyl) methyl]-4-pyrimidone. Also claimed are 2-nitroaminopyrimidone intermediates for use in this process. One specific intermediate is 2-nitroamino-5-[5-(1,3-benzodioxolyl)methyl]-4-pyrimidone.
    Type: Grant
    Filed: April 6, 1979
    Date of Patent: October 7, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Pharmacologically active thiourea and urea compositions and methods of use
    Patent number: 4226874
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: January 15, 1979
    Date of Patent: October 7, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charo R. Ganellin
  • 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
  • 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
  • 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
  • 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
  • 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
  • Pharmacologically active compounds
    Patent number: RE30457
    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: August 10, 1978
    Date of Patent: December 23, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Robert J. Ife