Patents Represented by Attorney Joan S. Keps

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  • Pharmacologically active compounds
    Patent number: 4470985
    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: April 15, 1983
    Date of Patent: September 11, 1984
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Dioxocyclobutene compounds
    Patent number: 4466970
    Abstract: 1-(4-Dialkylaminomethylpyrid-2-yloxypropylamino)-2-aminocyclobut-1-ene-3,4- dione compounds having histamine H.sub.2 -antagonist activity are disclosed.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: August 21, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Rodney C. Young
  • 1,2,4-Triazines
    Patent number: 4467087
    Abstract: Heterocyclic alkyl(or methylthioalkyl)amino-1,2,4-triazine compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: September 24, 1982
    Date of Patent: August 21, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pyrimidone salt and its preparation
    Patent number: 4450161
    Abstract: The invention provides 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-[5-(1,3-benzodioxolyl) methyl]-4-pyrimidone di(methanesulphonate) which is useful as a histamine H.sub.2 -antagonist. The compound can be prepared by reacting 2-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-5-[5-(1,3-benzodioxolyl) methyl]-4-pyrimidone with methanesulphonic acid.
    Type: Grant
    Filed: May 26, 1982
    Date of Patent: May 22, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George R. White
  • Use of N-cyano-N'-methyl-N"-[2-(5-methyl-4-imidazolylmethyldithio)ethyl]guanidi ne in the preparation of cimetidine
    Patent number: 4447621
    Abstract: A process for preparing cimetidine by sulfur extrusion from N-cyano-N'-methyl-N"-[2-(5-methyl-4-imidazolylmethyldithio)ethyl]guanidine .
    Type: Grant
    Filed: October 21, 1982
    Date of Patent: May 8, 1984
    Assignee: SK&F Lab Co.
    Inventors: Clifford S. Labaw, George R. Wellman
  • Histamine H.sub.1 -antagonists
    Patent number: 4444772
    Abstract: The invention provides 2-(3,5-disubstituted pyridylalkyl amino)-5-pyridylmethyl-4-pyrimidone derivatives which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: June 22, 1982
    Date of Patent: April 24, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Tetrahydroimidazo(3,4-c)-1,3-diazocine intermediates for production of guanidines
    Patent number: 4443375
    Abstract: This invention relates to a process for preparing imidazolylalkylguanidines, in particular N-[3-(4-imidazolyl)propyl]-N'-[2-(5-methyl-4-imidazolylmethylthio)ethyl]gu anidine (impromidine) which has histamine H.sub.2 -agonist activity, to intermediates for use in this process and to processes for preparing these intermediates.
    Type: Grant
    Filed: October 26, 1982
    Date of Patent: April 17, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Derek W. Hills, George R. White
  • Azolyl alkylthioureas and guanidines alkylaminonitroethylene compounds
    Patent number: 4440775
    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: June 18, 1982
    Date of Patent: April 3, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • Pyridines
    Patent number: 4439609
    Abstract: This invention relates to 4-substituted aminomethyl pyridines with a butanamine, oxypropioamine or thiomethylamine substituent at the 2 position. The compounds are reacted with pyridones to form compounds which have histamine H.sub.2 -antagonist activity.
    Type: Grant
    Filed: February 16, 1983
    Date of Patent: March 27, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • Isoureas and isothioureas
    Patent number: 4439435
    Abstract: The compounds are isoureas and isothioureas which have an O- or S- alkylpyrimidone substituent and which are histamine H.sub.2 -antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-methyl-3-pyridyl-methyl)-4-pyrimidone.
    Type: Grant
    Filed: August 6, 1981
    Date of Patent: March 27, 1984
    Assignee: Smith Kline & French Laboratories Ltd.
    Inventors: Charon R. Ganellin, Robert J. Ife, David A. A. Owen
  • 2-[2-Thiazolyl or 2-guanidino-4-thiazolyl methylthioethyl(or butyl)amino]-3-(hydroxy or carboxy)pyridines, compositions containing same and method of use
    Patent number: 4439437
    Abstract: This invention relates to 2-amino-3-hydroxy, and 3-carboxy pyridine derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal heterocyclic group. The compounds have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethyl]amino pyridine 3-carboxylic acid.
    Type: Grant
    Filed: April 5, 1982
    Date of Patent: March 27, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Martin Jones, Rodney C. Young
  • Pharmacologically active compounds
    Patent number: 4438127
    Abstract: Amidinoformic acids and amidinosulphinic acids which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-[2-(5-methyl-4-imidazolylmethylthio)-ethyl]amidinoformic acid and N-methyl-N'-[2-(5-methyl-4-imidazolylmethylthio)ethyl]amidiniosulphinic acid.
    Type: Grant
    Filed: March 7, 1983
    Date of Patent: March 20, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Alkoxypyridyl alkylamines
    Patent number: 4426526
    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: November 19, 1980
    Date of Patent: January 17, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Sulphoxides
    Patent number: 4413130
    Abstract: The compounds are sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines which are useful to produce inhibition of histamine H-2 receptors.
    Type: Grant
    Filed: March 26, 1982
    Date of Patent: November 1, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George R. White
  • 2-Heterocyclic alkylamino-3-nitropyrroles
    Patent number: 4407808
    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 alkyl group interrupted by sulfur or oxygen. The 4- and 5- positions of the pyrrole ring can also be substituted.
    Type: Grant
    Filed: January 28, 1982
    Date of Patent: October 4, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Nitro-substituted dihydropyrroles and tetrahydropyridines, compositions, compounds, and medicinal use
    Patent number: 4405624
    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 tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: December 2, 1981
    Date of Patent: September 20, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Heterocyclic thioureas, isothioureas, guanidines and nitromethylene-amidines
    Patent number: 4405621
    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-(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: June 11, 1981
    Date of Patent: September 20, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Pharmacologically active compounds
    Patent number: 4399142
    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-imidazolymethylthio)ethylamino]-4-pyrimidone.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: August 16, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pharmacologically active compounds
    Patent number: 4395419
    Abstract: Amidinoformic acids and amidinosulphinic acids which are histamine H.sub.2 -antagonists. A specific compound of this invention is N-[2-(3-(1,2,5)-thiadiazolylmethylthio)ethyl]amidinoformic acid.
    Type: Grant
    Filed: August 10, 1981
    Date of Patent: July 26, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • N-Heterocyclic alkyl-N'-thiadiazolyl, thiazolyl and isothiazolyl alkylthioureas, ureas and guanidines
    Patent number: 4388319
    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-cyano-N'-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]-N"-[2-(2-thiazolyl methylthio)ethyl]guanidine.
    Type: Grant
    Filed: December 11, 1980
    Date of Patent: June 14, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin