Patents by Inventor Gerald E. Stokker

Gerald E. Stokker 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).

  • Inhibitors of prenyl-protein transferase
    Patent number: 6566385
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: May 20, 2003
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Gerald E. Stokker, Anthony W. Shaw
  • Inhibitors of prenyl-protein transferase
    Patent number: 6562823
    Abstract: The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: May 13, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Samuel L. Graham, Diem N. Nguyen, Gerald E. Stokker, Theresa M. Williams, C. Blair Zartman
  • Inhibitors of prenyl-protein transferase
    Publication number: 20020099007
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Application
    Filed: January 9, 2001
    Publication date: July 25, 2002
    Inventors: S. Jane deSolms, Gerald E. Stokker, Anthony W. Shaw
  • Inhibitors of prenyl-protein transferase
    Publication number: 20020037888
    Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Application
    Filed: March 28, 2001
    Publication date: March 28, 2002
    Applicant: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
  • Inhibitors of prenyl-protein transferase
    Patent number: 6358956
    Abstract: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including-farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, William C. Lumma, Jr., John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Gerald E. Stokker
  • Inhibitors of prenyl-protein transferase
    Patent number: 6358985
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ian M. Bell, Douglas C. Beshore, Terrence M. Ciccarone, S. Jane de Solms, Christopher J. Dinsmore, Gerald E. Stokker
  • Inhibitors of prenyl-protein transferase
    Patent number: 6284755
    Abstract: The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: September 4, 2001
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
  • Biaryl substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
    Patent number: 6080870
    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: October 1, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Gerald E. Stokker, John S. Wai, Theresa M. Williams, Wasyl Halczenko, John H. Hutchinson, Steven D. Young, Kelly M. Solinsky
  • Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
    Patent number: 6063930
    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: October 2, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J Dinsmore, Neville J. Anthony, Gerald E. Stokker, Robert P. Gomez
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5977134
    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: December 4, 1997
    Date of Patent: November 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Wasyl Halczenko, John H. Hutchinson, William C. Lumma, Jr., Gerald E. Stokker, Craig A. Stump, Theresa M. Williams
  • Bisphenyl inhibitors of farnesyl-protein transferase
    Patent number: 5710171
    Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzene and analine analogs, further substituted with a second phenyl ring attached via a bond, a heteroatom linker or an aliphatic linker. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors 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: May 15, 1996
    Date of Patent: January 20, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Suzanne C. MacTough, Gerald E. Stokker, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5661161
    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 antoxidation 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: September 14, 1995
    Date of Patent: August 26, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Terrence M. Ciccarone, S. Jane deSolms, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
  • Heterocycle-containing inhibitors of farnesyl-protein transferase
    Patent number: 5652257
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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: September 21, 1995
    Date of Patent: July 29, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, S. Jane deSolms, Robert P. Gomez, Samuel L. Graham, John H. Hutchinson, Gerald E. Stokker
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5631280
    Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. 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: May 24, 1995
    Date of Patent: May 20, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Christopher J. Dinsmore, Gerald E. Stokker, John S. Wai, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5585359
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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: September 29, 1994
    Date of Patent: December 17, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Breslin, S. J. deSolms, Samuel L. Graham, John H. Hutchinson, Gerald E. Stokker
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5576293
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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: September 29, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Victor M. Garsky, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5523456
    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 the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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: September 29, 1994
    Date of Patent: June 4, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Gerald E. Stokker, Samuel L. Graham
  • Farnesyl pyrophosphate analogs
    Patent number: 5362906
    Abstract: The present invention is directed to farnesyl pyrophosphate analogs 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: June 18, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
  • HMG-CoA reductase inhibitors
    Patent number: RE36481
    Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: January 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta J. Lee, Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker
  • HMG-CoA reductase inhibitors
    Patent number: RE36520
    Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##
    Type: Grant
    Filed: November 4, 1998
    Date of Patent: January 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Wasyl Halczenko, George D. Hartman, Gerald E. Stokker, Edward S. Inamine, Otto D. Hensens, David R. Houck, Ta Jyh Lee