Patents Represented by Attorney William H. Edgerton

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  • 7 -Acylamino-3-(3-sulfomethyl-1,2,4-triazol-5-ylthiomethyl)-3-cephem-4-carb oxylic acids
    Patent number: 4083975
    Abstract: New semisynthetic cephalosporins characterized by having structures with a 3-sulfomethyl-1,2,4-triazol-5-ylthiomethyl group at position 3. Exemplary is the antibacterially effective 7-D-mandelamido-3-(3-sulfomethyl-1,2,4-triazol-5-ylthiomethyl)-3-cephem-4- carboxylic acid disodium salt.
    Type: Grant
    Filed: September 24, 1976
    Date of Patent: April 11, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Pharmacologically active compounds
    Patent number: 4084001
    Abstract: The compounds are substituted S-(aminoalkyl)isothioureas which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are S-[6-(N'-methylthioureido)hexyl]isothiourea and S-[5-(N'-cyano-N"-methylguanidino)pentyl]isothiourea.
    Type: Grant
    Filed: November 23, 1976
    Date of Patent: April 11, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin, Robert John Ife
  • Substituted aurones
    Patent number: 4083952
    Abstract: Substituted aurones useful as inhibitors of certain antigen-antibody reactions, particularly in alleviating allergic manifestations such as asthma, are prepared by reaction of a 3-coumaranone with an appropriately substituted benzaldehyde followed by treatment with aqueous mineral acid and an alkanol.
    Type: Grant
    Filed: May 17, 1976
    Date of Patent: April 11, 1978
    Assignee: SmithKline Corporation
    Inventors: Kenneth M. Snader, Chester R. Willis
  • 3-(3-(3-Substituted amino-2-hydroxypropoxy)phenyl)-6-hydrazino pyridazines and their use as vasodilators and .beta.-adrenergic blocking agents
    Patent number: 4082843
    Abstract: The compounds are 3-(3-(3-substituted amino-2-hydroxypropoxy)phenyl)-6-hydrazino pyridazines which have .beta.-adrenergic blocking and vasodilator activity.
    Type: Grant
    Filed: December 15, 1975
    Date of Patent: April 4, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: William John Coates, Anthony Maitland Roe, Robert Antony Slater, Edwin Michael Taylor
  • Pyridyl-alkylaminoethylene compounds
    Patent number: 4080459
    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-[2-((4-methyl-5-imidazolyl)methylthio)ethylamino]2-[2-((3-chloro -2-pyridyl)methylthio)ethylamino]ethylene.
    Type: Grant
    Filed: November 19, 1976
    Date of Patent: March 21, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, John Colin Emmett, Charon Robin Ganellin, Hunter Douglas Prain
  • Process using alkali fusion for decyanation of tert.-nitriles
    Patent number: 4079061
    Abstract: An improvement in the decyanation of tertiary nitriles comprises the alkali fusion of the nitriles. Exemplary are the preparation of chlorpheniramine and brompheniramine by heating the respective nitriles in liquid sodium or potassium hydroxide at from 100.degree.-200.degree..
    Type: Grant
    Filed: June 21, 1976
    Date of Patent: March 14, 1978
    Assignee: SmithKline Corporation
    Inventors: Charles E. Berkoff, Donald E. Rivard
  • 7-Acylamino-3-(5-sulfomethyl-1,3,4-thiadiazol-2-y lthiomethyl)-3-cephem-4-carboxylic acids
    Patent number: 4079134
    Abstract: New semisynthetic cephalosporins characterized by having structures with a 5-sulfomethyl-1,3,4-thiadiazol-2-ylthiomethyl group at position 3. Exemplary is the anti-bacterially effective 7-D-mandelamido-3-(5-sulfomethyl-1,3,4-thiadiazol-2-ylthiomethyl)-3-cephem -4-carboxylic acid disodium salt.
    Type: Grant
    Filed: September 24, 1976
    Date of Patent: March 14, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Uricosuric composition and method of producing uricosuria and hypouricemia
    Patent number: 4076839
    Abstract: Uricosuric compositions containing 2,3-dichloro-4-carboxyphenoxyacetic acid or its alkali metal salts and methods of producing uricosuria and hypouricemia by administering said compounds.
    Type: Grant
    Filed: June 27, 1977
    Date of Patent: February 28, 1978
    Assignee: SmithKline Corporation
    Inventor: Alfred Roland Maass
  • Substituted acetamidocephalosporins
    Patent number: 4075338
    Abstract: Novel cephalosporins with the trifluoroethylmercaptoacetamido, trifluoroethylsulfinylacetamido, and trifluoroethylsulfonylacetamido groups at position 7 are prepared. These compounds have antibacterial activity.
    Type: Grant
    Filed: December 3, 1976
    Date of Patent: February 21, 1978
    Assignee: SmithKline Corporation
    Inventor: Robert M. DeMarinis
  • Piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and dibenzoxepins and antipsychotic use thereof
    Patent number: 4073912
    Abstract: Novel piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and dibenzoxepins administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.
    Type: Grant
    Filed: October 12, 1976
    Date of Patent: February 14, 1978
    Assignee: SmithKline Corporation
    Inventors: Carl Kaiser, John J. Lafferty
  • Certain guanidine compounds, and their use as inhibitors of histamine activity
    Patent number: 4072748
    Abstract: The compounds are guanidines, for example N-benzenesulphonyl-N'-[2-((4-methyl-5-imidazolyl)-methylthio)ethyl]guanidi ne, which are inhibitors of histamine activity.
    Type: Grant
    Filed: September 24, 1976
    Date of Patent: February 7, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Cis-4-oxoazetidine intermediates and methods of preparing them
    Patent number: 4072674
    Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
    Type: Grant
    Filed: June 14, 1976
    Date of Patent: February 7, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Guanidino, thioureido, isothioureido and nitrovinylamino derivatives of pyridine
    Patent number: 4070472
    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: April 20, 1976
    Date of Patent: January 24, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, Charon Robin Ganellin
  • Pharmacologically active guanidine compounds as H-2 histamine receptor inhibitors
    Patent number: 4070475
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl-, and oxyalkyl-guanidines which are inhibitors of histamine activity.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: January 24, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, John Colin Emmett, Charon Robin Ganellin
  • Preparation of trifluoromethylthioacetic acid and its esters
    Patent number: 4069243
    Abstract: A new method of preparing trifluoromethylthioacetic acid using a tertiary phosphine in a sulfur extrusion of lower alkyl trifluoromethyldithioacetate with optional is situ alkaline hydrolysis of said acetate using a biphasic hydrolysis system in the presence of a phase transfer catalyst.
    Type: Grant
    Filed: May 24, 1976
    Date of Patent: January 17, 1978
    Assignee: SmithKline Corporation
    Inventor: Robert Michael DeMarinis
  • Pharmacologically active thiourea and urea compounds as inhibitors of H-2 histamine receptors
    Patent number: 4069327
    Abstract: The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
    Type: Grant
    Filed: January 5, 1977
    Date of Patent: January 17, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, John Colin Emmett, Charon Robin Ganellin
  • Intermediates for preparing 7-acyl-3-(sulfoalkyl substituted oxadiazolylthiomethyl)cephalosporins
    Patent number: 4067880
    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.
    Type: Grant
    Filed: April 25, 1977
    Date of Patent: January 10, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Pyridylbutylamino ethylene compounds
    Patent number: 4067984
    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-[4-(3-chloro-2-pyridyl)butylamino]ethylene.
    Type: Grant
    Filed: October 4, 1976
    Date of Patent: January 10, 1978
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham John Durant, John Colin Emmett, Charon Robin Ganellin, Hunter Douglas Prain
  • Pharmaceutical compositions of .alpha.-amino-.alpha.-(ureidophenyl)acetamidocephalosporins
    Patent number: 4067978
    Abstract: Cephalosporins with a .alpha.-amino-(ureidophenyl)acetamido substituent at position 7 are prepared by acylation of a 7-aminocephalosporin with a derivative of .alpha.-amino-p(or m)-ureidophenylacetic acid. These compounds are antibacterial agents.
    Type: Grant
    Filed: October 1, 1976
    Date of Patent: January 10, 1978
    Assignee: SmithKline Corporation
    Inventors: John Russel Eugene Hoover, Jerry Arnold Weisbach
  • 7-Amino intermediates for preparing 7-acyl-3-(ureidoalkyl substituted tetrazolylthiomethyl)-cephalosporins
    Patent number: 4068073
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and an ureidoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
    Type: Grant
    Filed: December 22, 1976
    Date of Patent: January 10, 1978
    Assignee: SmithKline Corporation
    Inventor: David A. Berges