Patents by Inventor Michael Kolb

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: 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of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety.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of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety.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
  • Novel process and intermediates
    Patent number: 5055592
    Abstract: This invention relates to the novel processes for the preparation of a 16-methoxy-16-methyl prostaglandin E.sub.1 derivative and to the novel intermediates useful therefor.
    Type: Grant
    Filed: January 30, 1990
    Date of Patent: October 8, 1991
    Assignee: Merrell Dow Pharmaceuticals
    Inventors: Michael Kolb, Luc Van Hijfte
  • Continuous large-scale production of ethyl 2,2-difluoro-4-pentenoate and 2-fluorinated methyl aminoacetonitriles by use of a flow reactor
    Patent number: 4847401
    Abstract: The large scale preparation of ethyl 2,2-difluoro-4- pentenoate and 2-fluorinated methyl aminoacetonitriles by reaction of 2-H-perfluoroethyl allyl ether and n-butyl lithium and fluoromethylacetonitrile and a Grignard reagent, respectively, is largly unsuccessful because of side reactions which convert intermediate products and reactants to undesired products. Applicants have overcome these problems by performing the reactions with cooling in a continuous manner in a flow reactor with short residence time.
    Type: Grant
    Filed: January 15, 1988
    Date of Patent: July 11, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Fritz Gerhart, Michael Kolb
  • Fluorinated diaminoalkyne derivatives
    Patent number: 4707498
    Abstract: Novel fluorinated diaminoalkyne derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein R represents C.sub.1 -C.sub.4 alkyl, or preferably, hydrogen.
    Type: Grant
    Filed: January 14, 1986
    Date of Patent: November 17, 1987
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Michael Kolb, David A. Kendrick
  • Substituted deoxyadenosine derivatives
    Patent number: 4374128
    Abstract: Novel compounds of the following general Formula I are useful pharmacological agents: ##STR1## wherein: Ado represents 5'-deoxyadenosin-5'-yl;R.sub.1 represents methyl, ethyl or, preferably hydrogen;R.sub.2 represents C.sub.1 -C.sub.8 alkylene;R.sub.4 represents C.sub.1 -C.sub.8 alkylene;R.sub.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl or --R.sub.6 NHR.sub.7 ;R.sub.6 represents C.sub.1 -C.sub.4 alkylene; andR.sub.7 represents hydrogen or C.sub.1 -C.sub.6 alkyl;and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: March 13, 1981
    Date of Patent: February 15, 1983
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Michel Jung, Michael Kolb, Charles Danzin