Patents Represented by Attorney Joan S. Keps

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  • 1-Benzyl-5-nitro-4-(pyridyl or imidazolyl) alkylamino-1,2,3,6-tetrahydropyrimidines and blocking of histamine H.sub.2
    Patent number: 4324789
    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: June 16, 1980
    Date of Patent: April 13, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Triazole-substituted ethylene derivatives
    Patent number: 4317829
    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: February 4, 1980
    Date of Patent: March 2, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin, Hunter D. Prain
  • Thiazole and isothiazole compounds, pharmaceutical compositions and their method of use
    Patent number: 4308275
    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]amidinosulphinic acid.
    Type: Grant
    Filed: August 10, 1979
    Date of Patent: December 29, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Inhibitors of H-2 histamine receptors
    Patent number: 4307101
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: March 17, 1980
    Date of Patent: December 22, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Guanidine compounds
    Patent number: 4307104
    Abstract: The compounds of this invention are 2,3-unsaturated nitrogen containing heterocyclic compounds with a 3-nitro group and a 2-(2-guanidino-4-thiazolyl alkylamino) group. These compounds have histamine H.sub.2 -antagonist activity. A particular compound of this invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-3-nitro-1,4,-5,6-tetra hydropyridine.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: December 22, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Isoureas and isothioureas
    Patent number: 4305945
    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-pyridylmethyl)-4-pyrimidone.
    Type: Grant
    Filed: July 10, 1979
    Date of Patent: December 15, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Charon R. Ganellin, Robert J. Ife, David A. A. Owen
  • Pharmacologically active compounds
    Patent number: 4301165
    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: August 30, 1979
    Date of Patent: November 17, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Pharmaceutical compositions
    Patent number: 4294854
    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: October 9, 1979
    Date of Patent: October 13, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Margaret R. Vickers
  • Pharmacologically active guanidine compounds
    Patent number: 4293699
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: March 21, 1980
    Date of Patent: October 6, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pharmacologically active thiourea and urea compounds
    Patent number: 4293697
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: April 9, 1980
    Date of Patent: October 6, 1981
    Assignee: Smith, Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pharmacologically active guanidine compounds
    Patent number: 4287198
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histarine activity.
    Type: Grant
    Filed: March 3, 1980
    Date of Patent: September 1, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Pyridyl, thiazolyl and isothiazolyl alkyl bisamidines
    Patent number: 4285952
    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'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: November 13, 1979
    Date of Patent: August 25, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Peter D. Miles
  • Ethylene derivatives
    Patent number: 4284640
    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: February 4, 1980
    Date of Patent: August 18, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin, Hunter D. Prain
  • Amidino and guanidino phosphonates
    Patent number: 4282213
    Abstract: Amidine phosphonates carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'-[2-(2-thiazolylmethylthio)ethyl]amidinophosphonic acid monoethyl ester and N'-methyl-N"-[2-((5-methyl-4-imidazolyl)-methylthio)ethyl]guanidinophospho nic acid monobenzyl ester, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: August 27, 1979
    Date of Patent: August 4, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Rodney C. Young, Zev Tashma
  • Pharmacologically active compounds to inhibit H-2 histamine receptors
    Patent number: 4282221
    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: July 25, 1979
    Date of Patent: August 4, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Certain heterocyclic-methylthioalkyl guanidine derivatives
    Patent number: 4282234
    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-imidazolymethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolymethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: August 4, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Alkoxy-pyridyl substituted alkanes
    Patent number: 4282224
    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: January 16, 1980
    Date of Patent: August 4, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Oxazole or isoxazole alkylamino ethylene compounds as inhibitors of H-2 histamine receptors
    Patent number: 4277485
    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] ethylene.
    Type: Grant
    Filed: February 4, 1980
    Date of Patent: July 7, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon F. Ganellin, Hunter D. Prain
  • Imidazole alkylthiourea compounds
    Patent number: 4276301
    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: August 27, 1979
    Date of Patent: June 30, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • N-Heterocyclic alkyl-N'-pyridyl alkylthioureas, ureas and guanidines
    Patent number: 4271169
    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-[2-(2-pyridylmethylthio)ethyl]-N'-[2-(4-methyl-5-imidazolylmethylthio)et hyl]thiourea is N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]thiourea and N,N'-bis[2-((methyl-5-imidazolyl)methylthio)ethyl]-N"-cyanoguanidine.
    Type: Grant
    Filed: December 20, 1979
    Date of Patent: June 2, 1981
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin