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 23, 1997
Date of Patent:
July 25, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Lekhanh O. Tran, Steven D. Young
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
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.
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.
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.
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:
December 14, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, Theresa M. Williams
Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
Type:
Grant
Filed:
September 9, 1997
Date of Patent:
December 7, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Dong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Jenny M. Wai
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 21, 1997
Date of Patent:
November 9, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, George D. Hartman
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
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 chemotherpeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Abstract: The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs 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:
October 29, 1997
Date of Patent:
October 26, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Jeffrey M. Bergman, S. Jane deSolms, Chrisopher J. Dinsmore, Robert P. Gomez, Suzanne C. MacTough, Kelly M. Solinsky, Theresa M. Williams
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.
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 21, 1997
Date of Patent:
October 19, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, George D. Hartman
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:
October 12, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Samuel L. Graham, Theresa M. Williams, John S. Wai
Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
Type:
Grant
Filed:
October 14, 1997
Date of Patent:
September 7, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Victor M. Garsky, Deborah Defeo-Jones, Dong-Mei Feng
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:
August 17, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Kelly M. Solinsky
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 22, 1997
Date of Patent:
August 17, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Samuel L. Graham, Lekhanh O. Tran, Ian M. Bell, S. Jane deSolms, Robert P. Gomez, Michelle Sparks Kuo, William C. Lumma, Jr., Debra S. Perlow, Anthony W. Shaw, John S. Wai, Steven D. Young
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.
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.
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.