Patents Represented by Attorney Joan S. Keps

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  • Pyrimidine compounds
    Patent number: 4539207
    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: June 4, 1980
    Date of Patent: September 3, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert J. Ife
  • 2-(3,5-Substituted-2-pyridylalkylamino)-5-oxopyridylmethyl-4-pyrimidones useful as histamine H.sub.1 -antagonists
    Patent number: 4537890
    Abstract: Pyridone derivatives useful as histamine H.sub.1 -antagonists are disclosed.
    Type: Grant
    Filed: November 23, 1983
    Date of Patent: August 27, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Pharmacologically active compounds
    Patent number: 4537779
    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: June 18, 1984
    Date of Patent: August 27, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • 2-(3,5-Substituted-2-pyridylalkylamino)-5-benzyl-4-pyrimidones
    Patent number: 4537891
    Abstract: 3,5-Disubstituted-2-pyridylalkylamino-5-optionally substituted benzyl-4-pyrimidones having histamine H.sub.1 -antagonist activity are disclosed.
    Type: Grant
    Filed: September 29, 1983
    Date of Patent: August 27, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • 2-Aminoalkyl-pyridine derivatives
    Patent number: 4535163
    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: February 2, 1984
    Date of Patent: August 13, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • 3,5-Substituted-2-pyridylalkylamino compounds having histamine H.sub.1 -antagonist activity
    Patent number: 4532252
    Abstract: 3,5-Substituted-2-pyridylalkylamino derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: December 9, 1983
    Date of Patent: July 30, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • 2-(2-Pyridylaminoalkylamino)-4-pyrimidones
    Patent number: 4532246
    Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: July 30, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Robert J. Ife
  • Process for preparing 6-(2-hydroxyphenyl)-3-pyridazinone
    Patent number: 4528371
    Abstract: A process for preparing 6-(2-hydroxyphenyl)-3-pyridazinone which comprises reacting 2-hydroxyacetophenone with glyoxylic acid under alkaline conditions, adjusting the pH of the reaction mixture to give a mixture within a pH range of about pH 4.0-9.5 and which contains a weak base, and subsequently reacting with hydrazine.6-(2-Hydroxyphenyl)-3-pyridazinone is a useful intermediate in the preparation of anti-hypertensive agents.
    Type: Grant
    Filed: June 14, 1983
    Date of Patent: July 9, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: William J. Coates, Brian H. Warrington
  • Synthesis of 2-pyridylalkylamines
    Patent number: 4526974
    Abstract: The invention provides a process for preparing 2-pyridylalkylamines by reacting an alkali metal derivative of a 2-methylpyridine with a haloalkylamine. The compounds are useful as intermediates in the preparation of compounds having histamine H.sub.1 - and H.sub.2 -antagonist activity.
    Type: Grant
    Filed: March 22, 1983
    Date of Patent: July 2, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Brian M. Adger, Antonietta R. Mastrocola
  • 2-Thiazolyl, isothiazolyl, oxazolyl and isoxazolyl alkylamino-3-nitro-heterocyclic compounds
    Patent number: 4525477
    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: April 25, 1983
    Date of Patent: June 25, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Process and nitroaminopyrimidone intermediates for histamine H.sub.2 -antagonists
    Patent number: 4523015
    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-benzodioxyolyl )methyl]-4-pyrimidone. Also claimed are 2-nitroaminopyrimidone intermediates for use in this process. One specific intermediate is 2-nitroamino-5-[5-(1,3-benzodioxyolyl)methyl]-4-pyrimidone.
    Type: Grant
    Filed: May 19, 1980
    Date of Patent: June 11, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Dioxocyclobutene compounds
    Patent number: 4521625
    Abstract: 1-(Hydroxypropylamino)-2-aminocyclobut-1-ene-3,4-dione compounds are disclosed as useful intermediates in the preparation of histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: June 4, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Rodney C. Young
  • Guanidinothiazolyl derivatives
    Patent number: 4521418
    Abstract: The compounds are guanidinothiazolyl derivatives which are histamine H.sub.2 -antagonists. A specific compound of the present invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-5-(6-methyl-3-pyridylm ethyl)-4-pyrimidone.
    Type: Grant
    Filed: February 12, 1980
    Date of Patent: June 4, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Graham J. Durant
  • Synthesis of 2-pyridylalkylamines substituted on the pyridyl ring by bromine
    Patent number: 4515952
    Abstract: The invention provides a process for preparing 2-pyridylalkylamines, substituted in one of the 3- or 5-positions by bromo and in the other by C.sub.1-4 alkyl, by reacting an appropriate C.sub.1-4 alkyl substituted 2-pyridylalkylamine with an electrophilic brominating agent. Said 2-pyridylalkylamines are useful as intermediates in the synthesis of compounds useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: March 22, 1983
    Date of Patent: May 7, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Brian M. Adger, David J. O'Rourke
  • N-Substituted pyrrolidineacetic acids and their esters
    Patent number: 4514414
    Abstract: N-Substituted pyrrolidineacetic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an esters of an N-unsubstituted pyrrolidineacetic acid followed by hydrolysis of the ester.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: April 30, 1985
    Assignee: Smithkline Beckman Corporation
    Inventors: William E. Bondinell, John J. Lafferty, Charles L. Zirkle
  • Pharmacologically active isoxazole and triazole compounds
    Patent number: 4499101
    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 4, 1983
    Date of Patent: February 12, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • Phenyl alkylaminopyrimidones
    Patent number: 4496567
    Abstract: The compounds are phenyl alkylaminopyrimidones which are histamine H.sub.2 -antagonists. A specific compound of the present invention is 2-[2-[3-(dimethylaminomethyl)benzylthio]ethylamino]-5-(6-methyl-3-pyridylm ethyl)-4-pyrimidone.
    Type: Grant
    Filed: November 6, 1979
    Date of Patent: January 29, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert J. Ife
  • Pharmaceutical compositions
    Patent number: 4490387
    Abstract: S-(Aminoalkyl)isothiourens which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.
    Type: Grant
    Filed: January 17, 1983
    Date of Patent: December 25, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Margaret R. Vickers
  • Histamine H.sub.1 -antagonists
    Patent number: 4486434
    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: December 4, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Nitro pyrrols and their pharmaceutical use
    Patent number: 4482563
    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: June 27, 1983
    Date of Patent: November 13, 1984
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young