Patents Represented by Attorney, Agent or Law Firm David A. Muthard
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5919785
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams, Jeffrey Bergman
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5914341
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: January 29, 1998
    Date of Patent: June 22, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, George D. Hartman
  • Modified pseudomonas exotoxin PE.sub.40
    Patent number: 5912322
    Abstract: Psuedomonas exotoxin 40 is modified by deleting or substituting one or more cysteine residues. Such a modified protein may be incorporated into a fusion protein with TGF.alpha.. The resulting fusion protein exhibits altered biological activities from unmodified TGF.alpha.-PE.sub.40, including decreased cell killing activity and increase receptor-binding activity.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: June 15, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark W. Riemen, Steven M. Stirdivant
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5891889
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: April 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, John S. Wai, Mark W. Embrey, Thorsten E. Fisher
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5885995
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: March 23, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Christopher J. Dinsmore
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5883105
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: March 16, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Biheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5880140
    Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Biheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5874452
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: February 23, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Arylheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5872136
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: February 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Samuel L. Graham
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5872135
    Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogues differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: February 16, 1999
    Assignee: Merk & Co., Inc.
    Inventor: S. Jane deSolms
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5869682
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: February 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: S. Jane deSolms
  • Peptides
    Patent number: 5866679
    Abstract: Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: February 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Deborah DeFeo-Jones, Victor M. Garsky, Dong-Mei Feng, Raymond E. Jones, Allen I. Oliff
  • N-heterocyclic piperazinyl and H-heterocyclic piperazinonyl inhibitors of farnesyl-protein transferase
    Patent number: 5859015
    Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Theresa M. Williams
  • Arylheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5859035
    Abstract: The present invention is directed to compounds which inhibit famesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting famesyl-protein transferase and the famesyl of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5859012
    Abstract: The present invention is directed to piperazine-2,3-dione compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: January 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5856326
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: January 5, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Terrence M. Ciccarone, Christopher J. Dinsmore, Robert P. Gomez, Theresa M. Williams, George D. Hartman
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5854264
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez
  • Biheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5854265
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Genes for the subunits of human farnesyl-protein transferase
    Patent number: 5821118
    Abstract: The present invention relates to an assay useful in determining the farnesyl-protein transferase inhibitory activity of pharmaceutical agents. The assay employs purified human farnesyl-protein transferase which is prepared by gene expression in Escherichia coli.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: October 13, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Charles A. Omer, Ronald E. Diehl, Jackson B. Gibbs, Nancy E. Kohl
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5817678
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: October 6, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone