Patents Represented by Attorney William H. Edgerton

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  • Thiazole, isothiazole, oxazole and isoxazole compounds
    Patent number: 4197305
    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-(nitrometylene 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)ethyl)isothiour eido]propane. The compounds of this invention are inhibitors of H-2 histamine receptors.
    Type: Grant
    Filed: September 11, 1978
    Date of Patent: April 8, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin
  • 6-Halo-7,8-d ihydroxy-1-(hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4197297
    Abstract: 6-Halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have a hydroxy group substituted on the 1-phenyl ring have potent and specific antihypertensive activity by means of their peripheral dopaminergic effect. The lead compound of the series is 6-chloro-7,8-dihydroxy-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepi ne methane sulfonate.
    Type: Grant
    Filed: March 13, 1978
    Date of Patent: April 8, 1980
    Assignee: SmithKline Corporation
    Inventor: Joseph Weinstock
  • 1,1,1-Trihalo-2-hydroxy-4-(2-hydroxyphenyl)-4-butanones
    Patent number: 4193941
    Abstract: A new synthesis for the preparation of 6-(2-hydrophenyl)-3-pyridazinones whose key reaction is cyclizing a 1,1,1-trihalo-2-hydroxy-4-(2-hydroxyphenyl)-4-butanone with hydrazine. 6-(2-Hydroxyphenyl)-3-pyridazinones are important intermediates for preparing medicinally active compounds especially 3-[2-(3-tert.-butylamino-2-hydroxypropoxy)phenyl]-6-hydrazinopyridazine or its nontoxic acid addition salts. The invention claimed here is the trihalocarbinol intermediates.
    Type: Grant
    Filed: October 5, 1978
    Date of Patent: March 18, 1980
    Assignee: SmithKline Corporation
    Inventors: Sidney H. Levinson, Wilford L. Mendelson
  • 6-Halo-3-lower alkyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4192872
    Abstract: 6-Halo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have a lower alkyl substituted at the 3 or N-position have potent and often specific anti-Parkinsonism activity by means of their central dopaminergic effect. The lead compound of the series is 6-chloro-3-methyl-1-phenyl-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepi ne as the base or its salts such as the hydrochloride, hydrobromide or methane sulfonate.
    Type: Grant
    Filed: March 31, 1978
    Date of Patent: March 11, 1980
    Assignee: SmithKline Corporation
    Inventor: Joseph Weinstock
  • Imidazolyl alkylamino nitroethylene compounds
    Patent number: 4192879
    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: March 31, 1978
    Date of Patent: March 11, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
  • Pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
    Patent number: 4192888
    Abstract: Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using 2-indanamine compounds having 4 and/or 5 substituents.
    Type: Grant
    Filed: April 10, 1978
    Date of Patent: March 11, 1980
    Assignee: SmithKline Corporation
    Inventors: William E. Bondinell, Robert G. Pendleton
  • Isothiourea compounds and pharmacological use
    Patent number: 4191769
    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-imidazolylmethylthio)ethyl]acetamidine, N,N'-bis-[2-(5-methyl-4-imidazolylmethylthio)ethyl]N"-methylguanidine. The compounds of this invention are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: April 17, 1978
    Date of Patent: March 4, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • Amidino and guanidino phosphonates
    Patent number: 4190664
    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]guanidinophosphon ic acid monobenzyl ester, are histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: June 6, 1978
    Date of Patent: February 26, 1980
    Assignee: SmithKline & French Laboratories Limited
    Inventors: Graham J. Durant, Rodney C. Young, Zeav Tashma
  • 3-(o-Hydroxyphenyl)-5-formylhydrazino-.DELTA..sup.2 -pyrazolines
    Patent number: 4189578
    Abstract: New 3-(o-hydroxyphenyl)-5-formylhydrazino-.DELTA..sup.2 -pyrazolines useful in the preparation of 6-(2-hydrophenyl)-3-pyridazinones which are in turn important intermediates for preparing medicinally active compounds especially 3-[2-(3-tert.-butylamino-2-hydroxypropoxy)phenyl]-6-hydrazinopyridazine.
    Type: Grant
    Filed: March 1, 1979
    Date of Patent: February 19, 1980
    Assignee: SmithKline Corporation
    Inventors: Sidney H. Levinson, Wilford L. Mendelson
  • Amidinoformic and amidinosulphinic acids
    Patent number: 4189488
    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: June 12, 1978
    Date of Patent: February 19, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, Charon R. Ganellin, Rodney C. Young
  • 7-Amino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins
    Patent number: 4189573
    Abstract: The compounds of this invention are 7-amino-3-(phosphonoalkyl and esterified phosphonoalkyl substituted tetrazolylthiomethyl)cephalosporins useful as intermediates for preparing antibacterially active 7-acylamino cephalosporins.
    Type: Grant
    Filed: August 14, 1978
    Date of Patent: February 19, 1980
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • 2,2-Alkyldiylbis(thio)bis(imidazoles)
    Patent number: 4188397
    Abstract: New 2,2'-alkyldiylbis(thio)bis(imidazoles) having substituted phenyl groups in the 4- and 5- positions of the imidazole rings are disclosed. These compounds regulate cell-mediated immunity and/or have anti-arthritic activity and are useful to relieve inflammation, for example in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: September 22, 1978
    Date of Patent: February 12, 1980
    Assignee: SmithKline Corporation
    Inventor: David T. Hill
  • Process for preparing oxazine ring compounds
    Patent number: 4187375
    Abstract: A new process for preparing oxazine ring compounds comprises cyclization of an azetidinone-1-hydroxyacetate in the presence of a proton source.
    Type: Grant
    Filed: October 27, 1978
    Date of Patent: February 5, 1980
    Assignee: SmithKline Corporation
    Inventors: Thomas F. Buckley, John G. Gleason
  • Substituted furyl-2,3,4,5-tetrahydro-1H-3-benzazepine compounds and pharmaceutical use
    Patent number: 4187314
    Abstract: A group of 7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepines with structures containing a furyl ring at position 1 which have dopaminergic activity. Particular species of this group include 7,8-dihydroxy-1-(furyl)-2,3,4,5-tetrahydro-1H-3-benzazepine and its dimethyl ether derivative.
    Type: Grant
    Filed: May 24, 1978
    Date of Patent: February 5, 1980
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Nelson C. Yim
  • 2,3-Di(4-substituted phenyl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles
    Patent number: 4186205
    Abstract: New 6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles having substituted phenyl groups in the 2- and 3- positions are disclosed. These compounds regulate cell-mediated immunity and/or have anti-arthritic activity and are useful to relieve inflammation, for example in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: January 8, 1979
    Date of Patent: January 29, 1980
    Assignee: SmithKline Corporation
    Inventor: Paul E. Bender
  • Pharmacologically active triazinones
    Patent number: 4185103
    Abstract: The compounds are substituted 1,2,4-triazin-5-ones which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are 3-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-6-(3-methoxybenzyl)-1,2, 4-triazin-5-one and 3-[2-(5-methyl-4-imidazolylmethylthio)ethylamino]-6-(3-pyridylmethyl)-1,2, 4-triazin-5-one.
    Type: Grant
    Filed: March 13, 1978
    Date of Patent: January 22, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert J. Ife
  • Pharmacologically active compounds as inhibitors of H-2 histamine receptors
    Patent number: 4181730
    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: April 6, 1978
    Date of Patent: January 1, 1980
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Graham J. Durant, John C. Emmett, Charon R. Ganellin
  • Sulfaminoalkyl substituted tetrazole thiol intermediates for preparing cephalosporins
    Patent number: 4178288
    Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfaminoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated cephalosporin compounds have antibacterial activity.
    Type: Grant
    Filed: July 14, 1978
    Date of Patent: December 11, 1979
    Assignee: SmithKline Corporation
    Inventor: David A. Berges
  • Pyridyl substituted 2,3-dihydroimidazo[2,1-b]thiazoles
    Patent number: 4175127
    Abstract: The compounds are 5/6-pyridyl-phenyl-2,3-dihydroimidazo[2,1-b]thiazoles which have utility as intermediates and/or as having antiarthritic activity. A preferred group of compounds is 5-(4-pyridyl)-6-(4-substituted phenyl)-2,3-dihydroimidazo[2,1-b]thiazoles which have significant anti-arthritic activity.
    Type: Grant
    Filed: September 27, 1978
    Date of Patent: November 20, 1979
    Assignee: SmithKline Corporation
    Inventors: Paul E. Bender, Ivan Lantos
  • 3-(Carboxymethyl)thio-1H-1,2,4-triazol-5-thione
    Patent number: 4174324
    Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a carboxymethylthio substituted triazolylthiomethyl group at the 3-position of the cephem nucleus are prepared. These compounds have antibacterial activity.
    Type: Grant
    Filed: July 3, 1978
    Date of Patent: November 13, 1979
    Assignee: Smithkline Corporation
    Inventor: David A. Berges