Patents by Inventor Ta-Sen Chou

Ta-Sen Chou 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).

  • Patent number: 5945547
    Abstract: The compound 2-deoxy-2,2-difluoro-D-erythro-pentofuranos-1-ulose-3,5-dibenzoate is described and claimed.
    Type: Grant
    Filed: March 19, 1997
    Date of Patent: August 31, 1999
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath
  • Patent number: 5821357
    Abstract: A stereoselective glycosylation process for preparing beta-anomer enriched 2'-deoxy-2',2'-difluoropurine and triazole nucleosides and 2'-deoxy-2'-fluoropurine and triazole nucleosides which involves reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least a molar equivalent of a nucleobase derivative in a low freezing inert solvent.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: October 13, 1998
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Charles D. Jones
  • Patent number: 5744597
    Abstract: A stereoselective anion glycosylation process for preparing beta- and alpha-anomer enriched 2', 2'-difluoro-2'-deoxynucleosides and 2'-deoxy-2'-fluoronucleosides by reacting an alpha- or beta-anomer enriched 2-deoxy-2-fluorocarbohydrate or 2-deoxy-2,2-difluorocarbohydrate with at least a molar equivalent of a salt of a nucleobase derivative in an inert solvent.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 28, 1998
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Cora S. Grossman, Larry Wayne Hertel, Richard E. Holmes, Charles D. Jones, Thomas E. Mabry
  • Patent number: 5648473
    Abstract: A stereoselective glycosylation process for preparing beta-anomer enriched 2'-deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides which involves reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least a molar equivalent of a pyrimidine nucleobase derivative in a low freezing inert solvent.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: July 15, 1997
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5606048
    Abstract: A stereoselective glycosylation process for preparing beta- and alpha-anomer enriched 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides by reacting a concentrated alpha- or beta-anomer enriched 2 -deoxy-2,2-difluorocarbohydrate or 2-deoxy-2 -fluorocarbohydrate with at least a molar equivalent of a nucleobase derivative in a high boiling inert solvent.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: February 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Laurie M. Poteet, Douglas P. Kjell
  • Patent number: 5594124
    Abstract: A stereoselective glycosylation process for preparing beta-anomer enriched 2'-deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides which involves reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least a molar equivalent of a pyrimidine nucleobase derivative in a low freezing inert solvent.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: January 14, 1997
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5453499
    Abstract: A stereoselective process for preparing an alpha-anomer enriched 1-.alpha.-halo-2-deoxy-2,2-difluoro-D-ribofuranosyl derivatives involving contacting a 3,5-hydroxy protected-2-deoxy-2,2-difluoro-D-ribofuranosyl-1-.beta.-sulfonate with a halide source in an inert solvent.
    Type: Grant
    Filed: July 29, 1993
    Date of Patent: September 26, 1995
    Inventors: Ta-Sen Chou, Charles D. Jones, Thomas E. Mabry
  • Patent number: 5434254
    Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.
    Type: Grant
    Filed: April 19, 1993
    Date of Patent: July 18, 1995
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath, Lawrence E. Patterson
  • Patent number: 5401838
    Abstract: A stereoselective fusion glycosylation process for prearing beta-anomer enriched 2'-deoxy-2',2'-difluoronucleotides and 2'-deoxy-2'-fluoronucleosides by reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorcarbohydrate with at least a 3 molar equivalent of a nucleobase derivative at a temperature sufficient to melt the carbohydrate and nucleobase derivative.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: March 28, 1995
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5401861
    Abstract: A stereoselective process for preparing alpha-anomer enriched 2-deoxy-2,2-difluoro-D-ribofuranosyl sulfonates by contacting a lactol with an amine base in an inert solvent, adjusting the temperature and adding a sulfonating reagent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: March 28, 1995
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5371210
    Abstract: A stereoselective fusion glycosylation process for preparing beta-anomer enriched 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides is provided which requires reacting an alpha-anomer enriched 2-deoxy-2,2-difluorocarbohydrate or 2-deoxy-2-fluorocarbohydrate with at least 3 molar equivalents of a nucleobase derivative at a temperature sufficient to fuse the carbohydrate and nucleobase; in the absence of a catalyst and a solvent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: December 6, 1994
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 5256798
    Abstract: A process for providing an alpha-anomer enriched ribofuranosyl sulfonate from a beta-anomer ribofuranosyl sulfonate; comprising treating a beta-anomer ribofuranosyl sulfonate or anomeric mixture thereof with a conjugate anion of a sulfonic acid source at elevated temperatures in an inert solvent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 26, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Charles D. Jones
  • Patent number: 5256797
    Abstract: A process for separating an anomeric mixture of alpha and beta 2-deoxy-2,2-difluoro-D-ribofuranosyl-1-alkylsulfonates by contacting the anomeric mixture with a solvent; heating; adding a countersolvent; and lowering the temperature.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 26, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Timothy J. McCarthy
  • Patent number: 5252756
    Abstract: A stereoselective process for preparing 2-deoxy-2,2-difluoro-D-ribofuranosyl beta-anomer enriched aryl sulfonates or substituted arylsulfonates involving reacting a lactol with an acid scavenger and a sulfonating reagent in an inert solvent.
    Type: Grant
    Filed: June 22, 1992
    Date of Patent: October 12, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Charles D. Jones
  • Patent number: 5223608
    Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.
    Type: Grant
    Filed: July 12, 1990
    Date of Patent: June 29, 1993
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath
  • Patent number: 4965374
    Abstract: The present invention provides a process for preparing lactone intermediates to 2',2'-difluoronucleosides whereby reversion back to the lactone's open chain precursor is minimized and the desired erythro enantiomer can be selectively isolated from an enantiomeric mixture of erythro and threo lactones in crystalline form. Also provided is a process for producing 2'-deoxy-2',2'-difluoronucleosides in about a 1:1 .alpha./.beta. anomeric ratio, and processes for selectively isolating .beta.-2'-deoxy-2',2'-difluorocytidine, or an organic or inorganic acid addition salt thereof, from the 1:1 .alpha./.beta. mixture.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: October 23, 1990
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath, Lawrence E. Patterson
  • Patent number: 4665168
    Abstract: 7-Amino-3-pyridiniummethyl (and substituted pyridiniummethyl)-3-cephem-4-carboxylic acid hydrothiocyanate salts and a process for the preparation thereof are provided. The salts are useful for recovering the pyridinium nuclei from reaction mixtures in which they are formed or used.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: May 12, 1987
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath
  • Patent number: 4616080
    Abstract: Ceftazidime pentahydrate in crystalline form is provided in a one-step process comprising acidic removal of protecting groups from an amino-protected and carboxy-protected ceftazidime, separation of aqueous phase after addition of a water-immiscible organic solvent, and precipitation of pentahydrate by adjusting pH of aqueous phase from about 3.5 to about 4.5.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: October 7, 1986
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Robert E. Lakin
  • Patent number: 4537959
    Abstract: Ceftazidime bishydrobromide crystalline monohydrates are provided and are useful for preparing crystalline ceftazidime pentahydrate.
    Type: Grant
    Filed: March 26, 1984
    Date of Patent: August 27, 1985
    Assignee: Eli Lilly and Company
    Inventor: Ta-Sen Chou
  • Patent number: 4525587
    Abstract: (6R,7R)-7-[(Z)-2-(2-triphenylmethylaminothiazol-4-yl)-2-(2-tert.-butoxycarb onylprop-2-oxyimino)acetamido]-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylat e is isolated by formation of N,N-dimethylacetamide solvates.
    Type: Grant
    Filed: February 3, 1984
    Date of Patent: June 25, 1985
    Assignee: Eli Lilly and Company
    Inventors: Ta-Sen Chou, Perry C. Heath