Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
October 17, 2000
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Scott R. Hambaugh, Randall W. Hungate
Abstract: The present invention relates to assays and kits using porcine carotid arteries for screening compounds to identify modulators of angiogenesis. In particular, an assay for rapidly screening compounds that inhibit angiogenesis is provided.
Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
October 15, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
Abstract: The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
October 1, 2002
Assignee:
Merck & Co., Inc.
Inventors:
H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
Abstract: The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic 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:
September 7, 2000
Date of Patent:
August 27, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ian M. Bell, Douglas C. Beshore, Steven N. Gallicchio, C. Blair Zartman
Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
July 16, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, George D. Hartman, Randall W. Hungate
Abstract: The instant invention is directed to a process for synthesizing substituted prolines, in particular, optically pure substituted prolines, which comprises the steps of:
a) adding an unsubstituted or substituted proline alkali salt and an alkali halide to a solution of dialkylacylamidomalonate; and
b) adding &agr;, &bgr; unsaturated aldehyde to produce an adduct.
Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, 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 a prenyl-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 a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
S. Jane deSolms, John H. Hutchinson, Anthony W. Shaw, Samuel L. Graham, Terrence M. Ciccarone