Patents by Inventor Kenneth G. Holden

Kenneth G. Holden has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Water soluble camptothecin analogs useful for inhibiting the growth of animal tumor cells
    Patent number: 5004758
    Abstract: Water soluble camptothecin analogs, pharmaceutical compositions comprising such analogs, and a method of inhibiting the growth of tumor cells sensitive to such analogs in an animal in need thereof.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: April 2, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Jeffrey C. Boehm, Sidney M. Hecht, Kenneth G. Holden, Randall K. Johnson, William D. Kingsbury
  • Process useful for preparing 7,8-acetamido, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4382029
    Abstract: A chemical process is described for preparing 7,8-acetamido, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines which involves reacting a 7,8-quinone derivative of a 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine with a benzyl or benzhydrylamine followed by hydrolysis of the resulting imine and reaction with acetic anhydride or acetyl chloride.
    Type: Grant
    Filed: August 14, 1981
    Date of Patent: May 3, 1983
    Assignee: SmithKline Beckman Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • Intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4327023
    Abstract: A group of new chemical compounds are described which are intermediates for preparing 7,8-amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines. The intermediates are distinguished in structure by a benzyloxy substituent at either the 7 or 8-position.
    Type: Grant
    Filed: August 7, 1980
    Date of Patent: April 27, 1982
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • 7,8-Amino, hydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4284556
    Abstract: A group of 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines whose structures have amino, hydroxy substituents at the 7,8-positions of the benzazepine nucleus is disclosed. Novel intermediates and routes of synthesis used for preparing them are also described. The end products have pharmacodynamic activity.
    Type: Grant
    Filed: January 31, 1980
    Date of Patent: August 18, 1981
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser, Joseph Weinstock
  • 6-Phenyl thio- and 6-cyclohexyl thio-2,3,4,5-tetrahydro-1H-3-benzazepines
    Patent number: 4265890
    Abstract: Mercapto substituted-2,3,4,5-tetrahydro-1H-3-benzazepines having dopamine receptor blocking activity are prepared from o-quinones or via standard preparative procedures.
    Type: Grant
    Filed: May 17, 1979
    Date of Patent: May 5, 1981
    Assignee: SmithKline Corporation
    Inventors: Kenneth G. Holden, Carl Kaiser
  • 3-Amino-2-hydroxy, halo or mercaptomethyl-4-oxoazetidines
    Patent number: 4257947
    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: March 14, 1979
    Date of Patent: March 24, 1981
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • 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
  • 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 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
  • 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
  • 2,3,4,5-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
  • Methods and intermediates for preparing cis-4-oxoazetidine intermediates
    Patent number: 4166816
    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: August 3, 1977
    Date of Patent: September 4, 1979
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Process for preparing substituted glycines
    Patent number: 4108854
    Abstract: A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
    Type: Grant
    Filed: August 16, 1976
    Date of Patent: August 22, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, Nelson C. F. Yim
  • 8-Oxo-4-thia-1-azabicyclo (4.2.0)-oct-2-ene derivatives
    Patent number: 4103086
    Abstract: Novel bicyclic .beta.-lactams and intermediates useful in their preparation are disclosed. In particular, 7.beta.-acyl-amino- and 7.beta.-amino-8-oxo-4-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acids are prepared. The acylated compounds are antibacterial agents.
    Type: Grant
    Filed: June 8, 1976
    Date of Patent: July 25, 1978
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • 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
  • Process for preparing 7-oxo cephalosporins and 6-oxo penicillins
    Patent number: 4053468
    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.
    Type: Grant
    Filed: February 25, 1976
    Date of Patent: October 11, 1977
    Assignee: SmithKline Corporation
    Inventor: Kenneth G. Holden
  • 3-Substituted-6.beta.-(amino- and acylamino)-7-oxo-1,3-diazabicyclo[3.2.0]- h
    Patent number: 4000154
    Abstract: Novel bicyclic .beta.-lactam penicillin analogs which have antibacterial activity and intermediates for the synthesis thereof are disclosed. In particular, 3-acetyl-7-oxo-6.beta.-phenoxyacetylamino-1,3-diazabicyclo[3.2.0]heptane-2 -carboxylic acid and derivatives thereof are prepared.
    Type: Grant
    Filed: September 3, 1975
    Date of Patent: December 28, 1976
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, William F. Huffman
  • Substituted glycines and intermediates thereof
    Patent number: 3997584
    Abstract: A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
    Type: Grant
    Filed: October 3, 1975
    Date of Patent: December 14, 1976
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, Nelson C. F. Yim
  • Process for preparing substituted glycines
    Patent number: 3994954
    Abstract: A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
    Type: Grant
    Filed: June 24, 1975
    Date of Patent: November 30, 1976
    Assignee: SmithKline Corporation
    Inventors: John G. Gleason, Kenneth G. Holden, Nelson C. F. Yim