Abstract: The compounds are sulphoxides of heterocyclicthioalkylthioureas, ureas and guanidines which are useful to produce inhibition of histamine H-2 receptors.
Type:
Grant
Filed:
May 24, 1976
Date of Patent:
November 1, 1977
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The compounds are dithiocarbamates and isothioureas which are histamine H.sub.2 -antagonists. Two compounds of the invention are 2-(5-methyl-4-imidazolylmethylthio)ethyl N-methyldithiocarbamate and S-[2-(5-methyl-4-imidazolyl-methylthio)ethyl]-N-cyano-N'-methylisothiourea .
Type:
Grant
Filed:
January 27, 1976
Date of Patent:
November 1, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Thomas Henry Brown, Graham John Durant, Charon Robin Ganellin, Robert John Ife
Abstract: Lower alkyl 4-imidazolecarboxylates are electro-chemically reduced to give the corresponding alcohol and lower alkyl ethers. This mixture is reacted directly with cysteamine to give the important thioamine intermediates.
Abstract: The compounds are 3-((3-substituted amino-2-hydroxypropoxy)-phenyl)-6-hydrazino pyridazines which have .beta.-adrenergic blocking and vasodilator activity.
Type:
Grant
Filed:
June 3, 1975
Date of Patent:
October 11, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
William John Coates, Anthony Maitland Roe, Robert Antony Slater, Edwin Michael Taylor
Abstract: The improved live Newcastle disease virus vaccines of the invention contain a cold or cold and temperature-sensitive strain of Newcastle disease virus obtained by U.V. or nitrous acid mutation. The vaccines are administered to chickens in the form of an aerosol.
Abstract: Piglet colibacillosis vaccine for intramuscular or subcutaneous administration to pregnant sows comprising cell-free heat labile (LT) E. coli enterotoxin with an adjuvant and the method for preventing piglet colibacillosis consisting in administering said vaccine to pregnant sows from 3 to 6 weeks before farrowing.
Abstract: A process for preparing 7-oxo cephalosporins and 6-oxo penicillins by reaction of a 7-amino cephalosporin or 6-amino penicillin with a carbonyl-containing oxidizing agent is disclosed.
Abstract: Pharmaceutical compositions and method of producing anti-Parkinsonism activity by administering internally a nontoxic effective quantity of a benzazepine derivative to an animal.
Type:
Grant
Filed:
August 5, 1975
Date of Patent:
October 4, 1977
Assignee:
SmithKline Corporation
Inventors:
Carl Kaiser, Robert G. Pendleton, Paulette E. Setler
Abstract: Process for preparing N-cyanoguanidines by treating N-(loweralkyl)-N'-cyano-isothioureas with an amine and a heavy metal salt. A specific product is N-cyano-N'-methyl-N"-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]guanidine , useful as a histamine H.sub.2 -antagonist.
Type:
Grant
Filed:
August 20, 1975
Date of Patent:
September 20, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, Charon Robin Ganellin, George Raymond White
Abstract: A process for preparing 5-(alkoxy- and aminoethylthio)methylthiazole compounds via displacement of the trisubstituted phosphonium group from 5-(trisubstituted phosphonium)methylthiazole compounds is disclosed.
Type:
Grant
Filed:
October 29, 1975
Date of Patent:
September 20, 1977
Assignee:
SmithKline Corporation
Inventors:
Bing Lun Lam, Joseph James Lewis, Robert Lee Webb, George Robert Wellman
Abstract: The compounds are heterocyclic thioalkyl-, aminoalkyl- and oxyalkylguanidines which are inhibitors of histamine activity, particularly inhibitors of H-2 histamine receptors.
Type:
Grant
Filed:
March 17, 1976
Date of Patent:
September 20, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Abstract: N-Allyl-benzmorphan compounds having structures distinguished by having either a 4,5 or 6 carbon containing allyl group at the 2- or N-position or various ether derivatives of the 2'-hydroxy group. The compounds are prepared by alkylation of appropriate N-nor bases and have analgetic antagonist activity particularly pronounced in countering the effects of overdosing. Certain N-acyl-2'-hydroxy-5,9-dimethyl-6,7-benzmorphan intermediates are also disclosed.
Abstract: .alpha.-Aminomethyl-4-hydroxy-3-methylsulfonyl benzyl alcohols having .beta.-adrenergic antagonist activity are prepared generally from 4-benzyloxy-3-methylsulfonylacetophenone by, for example, bromination and treatment of the resulting .alpha.-bromo derivative with an N-benzyl secondary amine, followed by catalytic hydrogenation to remove protective benzyl groups and reduce the ketone moiety.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfonic acid or sulfamoyl substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
Abstract: Novel pseudodisaccharide compounds which are related to neamine are prepared. These compounds have a mercapto group or a derivative thereof at position 3 or 4 of the glucose moiety of neamine. The compounds have antibacterial activity and have utility as intermediates to pseudotrisaccharides.
Type:
Grant
Filed:
December 18, 1975
Date of Patent:
September 13, 1977
Assignee:
SmithKline Corporation
Inventors:
David J. Cooper, John R. E. Hoover, Jerry A. Weisbach
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:
November 5, 1975
Date of Patent:
September 6, 1977
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Graham John Durant, John Colin Emmett, Charon Robin Ganellin, Hunter Douglas Prain
Abstract: Cephalosporia compounds having a substituted phenylglycyl substituent at the 7-position and any of a variety of groups at the 3-position are prepared by acylation of a 7-aminocephalosporanic acid. The compounds have anti-bacterial activity.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfoalkyl substituted oxadiazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.