Abstract: Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described.
These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
Type:
Grant
Filed:
July 5, 2002
Date of Patent:
April 13, 2004
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Shao Song Chu, Larry Andrew Alegria, Ted Michael Bleckman, Wesley Kwan Mung Chong, Rohit K. Duvadie, Lin Li, Siegfried Heinz Reich, William Henry Romines, III, Michael B. Wallace, Yi Yang
Abstract: Diaminothiazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
Type:
Grant
Filed:
February 15, 2001
Date of Patent:
September 16, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Shao Song Chu, Larry Andrew Alegria, Steven Lee Bender, Suzanne Pritchett Benedict, Allen J. Borchardt, Robert Steve Kania, Mitchell David Nambu, Anna Maria Tempczyk-Russell, Sepehr Sarshar, Dilip Bhumralkar, Zhengwei Peng, Michelle Yang
Abstract: Pharmaceutical compositions containing effective amounts of CDK-inhibiting diaminothiazole compounds of the following formula (where R1 and R2 are as defined in the specification) or their salts, or prodrugs or active metabolites of such compounds or salts, are useful for treating disorders and diseases such as cancer:
In preferred embodiments, R1 and R2 are independently unsubstituted or substituted carbocyclic or heterocyclic aryl ring structures. Compounds where R2 is ortho-substituted aryl are especially potent inhibitors of CDKs such as CDK4.
Type:
Grant
Filed:
October 27, 1998
Date of Patent:
May 27, 2003
Assignee:
Agouron Pharmaceuticals Inc.
Inventors:
Wesley K. M. Chong, Shao Song Chu, Lin Li, Rohit K. Duvadie, Yi Yang, Wei Xiao
Abstract: Pyrazole-thiazole compounds that modulate and/or inhibit the activity of cyclin-dependent kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating cyclin-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
Type:
Grant
Filed:
August 8, 2001
Date of Patent:
May 20, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Wesley Kwan Mung Chong, Rohit Kumar Duvadie
Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
Type:
Grant
Filed:
January 18, 2001
Date of Patent:
April 29, 2003
Assignee:
Agouron Pharmaceuticals
Inventors:
Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace