Patents Represented by Attorney Joan S. Keps

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  • Pyrimidones having histamine H.sub.2 -antagonist activity
    Patent number: 4388317
    Abstract: The compounds of this invention are 5-[dialkylaminoalkylfuranyl (or thienyl, phenyl or pyridyl)]-4-pyrimidones having histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(5-dimethylaminomethyl-2-furanylmethylthio)ethylamino]-5-(5-dimethyla minomethyl-2-furanylmethyl)-4-pyrimidone.
    Type: Grant
    Filed: March 27, 1981
    Date of Patent: June 14, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Thomas H. Brown
  • Pyrimidone derivatives
    Patent number: 4385058
    Abstract: This invention relates to 2-amino-4-pyrimidone derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal 4-dialkylaminomethyl-2-pyridyl group. The compounds have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(4-dimethylaminomethyl-2-pyridylmethylthio)ethylamino]-5-(6-methyl-3- pyridylmethyl)-4-pyrimidone.
    Type: Grant
    Filed: September 16, 1981
    Date of Patent: May 24, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, George S. Sach
  • Process for preparing an imidazole derivative
    Patent number: 4381395
    Abstract: This invention relates to new processes for preparing an imidazole derivative, i.e. cimetidine, by (1) reacting an imidazolylmethylthioethylamine with an amidine or (2) reacting a N-cyano-N'-imidazolylmethylthioethyl formamidine with methylamine or (3) reacting a N-methyl-N'-imidazolylmethylthioethyl formamidine with cyanamide.
    Type: Grant
    Filed: April 3, 1981
    Date of Patent: April 26, 1983
    Assignee: SK & F Lab Co.
    Inventors: Tsutomu Teraji, Yoshiharu Nakai, Graham J. Durant
  • Pharmaceutical compositions
    Patent number: 4378365
    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: June 1, 1981
    Date of Patent: March 29, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Margaret R. Vickers
  • 3-,4-Dihydroimidazo (3,4-c)-1,3-pyrimidines and 4,5-dihydroimidazo (3,4-c)-1,3-diazepines
    Patent number: 4375435
    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: June 3, 1981
    Date of Patent: March 1, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Derek W. Hills, George R. White
  • Amidinosulphonic acid derivatives
    Patent number: 4375472
    Abstract: Amidinosulphonic acid derivatives carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'[2-(5-methyl-4-imidazolylmethylthio)- ethyl] amidinosulphonic acid and N-methyl-N'-[2-(3-chloropyrid-2-ylmethylthio) ethyl] amidinosulphonic acid, are histamine H.sub.2 -receptor antagonists.
    Type: Grant
    Filed: November 24, 1980
    Date of Patent: March 1, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Rodney C. Young, Zev Tashma
  • Pharmacologically active 1,3-bis[(2-heterocyclyl-methyl-thio)ethyl)ethyl)guanidino]alkane derivatives
    Patent number: 4374839
    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: November 24, 1980
    Date of Patent: February 22, 1983
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, George S. Sach
  • Disulfide intermediate for cimetidine
    Patent number: 4374996
    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: June 3, 1981
    Date of Patent: February 22, 1983
    Assignee: SK & F Lab Co.
    Inventors: Clifford S. Labaw, George R. Wellman
  • Benzyl 5-methyl-4-imidazolecarboxylate
    Patent number: 4374252
    Abstract: A process for the preparation of 5-methyl-4-imidazolecarboxylic acid esters from acetoacetic acid esters. The products of this process are useful as intermediates for preparing cimetidine.
    Type: Grant
    Filed: December 10, 1981
    Date of Patent: February 15, 1983
    Assignee: SK&F Lab Co.
    Inventors: Harold Graboyes, Thomas J. Kasper, Praful D. Vaidya
  • Imidazoline containing imidazoles
    Patent number: 4374251
    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)ethylamio]-4-pyrimidone.
    Type: Grant
    Filed: November 14, 1980
    Date of Patent: February 15, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Oxazolyl, isoxazolyl, triazolyl and thiadiazolyl alkyl bisamidines
    Patent number: 4372963
    Abstract: Bisamidines carrying one unsaturated nitrogen heterocyclo-containing substituent, representative of which i; 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: March 27, 1981
    Date of Patent: February 8, 1983
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Peter D. Miles
  • Guanidine compounds
    Patent number: 4359466
    Abstract: The compounds of this invention are 2-(2-guanidino-4-thiazolyl alkylamino)-3-nitropyrroles which have histamine H.sub.2 -antagonist activity.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: November 16, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Process for the preparation of 5-dimethylaminomethyl-2-furanmethanol
    Patent number: 4347191
    Abstract: A process for preparing 5-dimethylaminomethyl-2-furanmethanol by reacting 2-furanmethanol with bis(dimethylamino)methane. The product is useful as a chemical intermediate, in particular to prepare H.sub.2 -histamine antagonists.
    Type: Grant
    Filed: March 5, 1981
    Date of Patent: August 31, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: John Cooper, Dennis V. Lee
  • Pyridyl alkylthiourea and alkylamino-nitroethylene
    Patent number: 4347250
    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: September 2, 1980
    Date of Patent: August 31, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • Pharmacologically active compounds
    Patent number: 4341787
    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 3, 1981
    Date of Patent: July 27, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Process for preparing 3-chloro-6-(2-hydroxyphenyl)-pyridazines
    Patent number: 4340733
    Abstract: A process for preparing 3-chloro-6-(2-hydroxyphenyl)pyridazines by the reaction of 6-(2-hydroxyphenyl)-3(2H)-pyridazinones with phosphorus oxychloride and a disubstituted formamide. The chloropyridazine compounds are useful intermediates for preparing compounds which have .beta.-adrenergic blocking and vasodilator activity and are useful as antihypertensive agents.
    Type: Grant
    Filed: September 2, 1980
    Date of Patent: July 20, 1982
    Assignee: SmithKline Corporation
    Inventor: Bing L. Lam
  • Sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines
    Patent number: 4338328
    Abstract: The compounds are sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines which are useful to produce inhibition of histamine H-2 receptors.
    Type: Grant
    Filed: October 16, 1980
    Date of Patent: July 6, 1982
    Assignee: SmithKline & French Laboratories Limited
    Inventor: George R. White
  • Blocking histamine H.sub.2 -receptors with imidazolylalkyl guanidine derivatives
    Patent number: 4333946
    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: January 29, 1981
    Date of Patent: June 8, 1982
    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: 4331668
    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 16, 1980
    Date of Patent: May 25, 1982
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Michael L. Roantree, Rodney C. Young
  • Process for preparing 5-methyl-4-imidazolecarboxylic acid esters
    Patent number: 4328349
    Abstract: A process for the preparation of 5-methyl-4-imidazolecarboxylic acid esters from acetoacetic acid esters. The products of this process are useful as intermediates for preparing cimetidine.
    Type: Grant
    Filed: October 8, 1980
    Date of Patent: May 4, 1982
    Assignee: SK&F Lab Co.
    Inventors: Harold Graboyes, Thomas J. Kasper, Praful D. Vaidya