Patents Assigned to SmithKline Corporation
  • Alkylthio-7,8-dihdroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having dopaminergic activity
    Patent number: 4206210
    Abstract: A new series of lower alkylthio-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines having potent central dopaminergic activity of utility in treating Parkinson's disease. The 6-and 9-methylthio compounds are particularly of use.
    Type: Grant
    Filed: June 2, 1978
    Date of Patent: June 3, 1980
    Assignee: SmithKline Corporation
    Inventor: Kenneth G. Holden
  • Bis[triethylphosphine)aurio]sulfonium sugars
    Patent number: 4201775
    Abstract: A new series of gold containing sugars having anti-arthritic activity are characterized by the presence of a bis[(triethylphosphine)aurio]sulfonium salt moiety at the 1-position of the glucopyranoside. The compounds are prepared by reacting a 1-S-triethylphosphinegold-1-thio-glucopyranoside with a triethylphosphinegold halide.
    Type: Grant
    Filed: March 23, 1979
    Date of Patent: May 6, 1980
    Assignee: SmithKline Corporation
    Inventors: John J. Filan, Walter W. Holl, George R. Wellman
  • Substituted azetidinones
    Patent number: 4200572
    Abstract: Substituted azetidine intermediates for preparing novel bicyclic .beta.-lactam penicillin analogs which have antibacterial activity are disclosed.
    Type: Grant
    Filed: May 1, 1978
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Method for preparing auranofin
    Patent number: 4200738
    Abstract: A new synthesis of auranofin comprising reacting 2,3,4,6-tetra-O-acetyl-.alpha.-D-glucopyranosyl bromide with a S-(triethylphosphineaurous)thiouronium salt.
    Type: Grant
    Filed: April 21, 1977
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: David T. Hill, Blaine M. Sutton, Ivan Lantos
  • Method for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
    Patent number: 4200754
    Abstract: A novel process for preparing 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline by cyclizing N-acetyl-2,3-dichlorobenzylaminoacetaldehyde dimethyl acetal with a Lewis acid, reducing, and hydrolyzing the resulting acylated isoquinoline is disclosed.
    Type: Grant
    Filed: February 2, 1979
    Date of Patent: April 29, 1980
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl D. Perchonock
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 1-(2-Sulfamidoethyl)-1,4-dihydro-5H-tetrazole-5-thione
    Patent number: 4174323
    Abstract: Novel cephalosporins having various acyl substituents at the 7-position and a sulfamidoethyl substituted tetrazolylthiomethyl 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
  • 2,3,4,5-Tetrahydro-1H-3-benzazepine-7,8-diones
    Patent number: 4172890
    Abstract: Novel benzazepine derivatives having central and peripheral dopaminergic activity useful in treating Parkinson's and cardiovascular diseases. The compounds have additional use as intermediates for the synthesis of other benzazepines with similar useful properties. The 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-dione derivatives are particularly useful.
    Type: Grant
    Filed: May 11, 1978
    Date of Patent: October 30, 1979
    Assignee: SmithKline Corporation
    Inventor: Kenneth G. Holden