Patents by Inventor H. Michael Kolb

H. Michael Kolb 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).

  • Peptidase inhibitors
    Patent number: 6130315
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: August 24, 1998
    Date of Patent: October 10, 2000
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michael J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • Peptidase inhibitors
    Patent number: 5849866
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: December 15, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michel J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • (S)-4-amino-hepta-5,6-dienoic acid and intermediates therof
    Patent number: 5756762
    Abstract: The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.
    Type: Grant
    Filed: January 9, 1997
    Date of Patent: May 26, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: H. Michael Kolb
  • Processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and intemediates thereof
    Patent number: 5654477
    Abstract: The present invention relates to a novel enantiospecific processes for preparing (S)-4-amino-hepta-5,6-dienoic acid and pharmaceutically acceptable salts thereof, which is useful as an irreversible inhibitor of GABA-T, to novel intermediates thereof, and a process for preparing an intermediate thereof.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: August 5, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventor: H. Michael Kolb
  • Peptidase inhibitors
    Patent number: 5496927
    Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: March 5, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: H. Michael Kolb, Joseph P. Burkhart, Michel J. Jung, Fritz E. Gerhart, deceased, Eugene L. Giroux, Bernhard Neises, Daniel G. Schirlin
  • Difluoroglutamic acid conjugates with folates and anti-folates for the treatment of neoplastic diseases
    Patent number: 5066828
    Abstract: This invention relates to certain conjugates of folates and antifolates with difluoroglutamic acid which are useful in the treatment of patients suffering from certain neoplastic diseases including leukemia, melanomas, carcinomas, sarcomas and mixed neoplasias.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: November 19, 1991
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Philippe Bey, H. Michael Kolb