Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
July 15, 2003
Assignee:
Amgen Inc.
Inventors:
Kevin Koch, Andreas Termin, John A. Josey
Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.
Type:
Grant
Filed:
March 21, 2000
Date of Patent:
December 17, 2002
Assignee:
Amgen Inc.
Inventors:
David M. Armistead, Jean E. Bemis, Daniel Elbaum, Gregory J. Habgood, Perry M. Novak, Joseph J. Nunes, Leticia M. Toledo-Sherman
Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
August 17, 2001
Date of Patent:
October 1, 2002
Assignee:
Amgen Inc.
Inventors:
Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
Abstract: The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
August 23, 2000
Date of Patent:
August 27, 2002
Assignee:
Amgen Inc.
Inventors:
Jeffery A. Zablocki, Eugene Tarlton, Jr., James P. Rizzi, Nathan B. Mantlo
Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
February 15, 2000
Date of Patent:
July 16, 2002
Assignee:
Amgen Inc.
Inventors:
Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffery A. Zablocki
Abstract: Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
June 21, 2000
Date of Patent:
June 25, 2002
Assignee:
Amgen Inc.
Inventors:
Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
Abstract: Selected novel substituted pyridine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
August 21, 2000
Date of Patent:
December 25, 2001
Assignee:
Amgen Inc.
Inventors:
Nathan B. Mantlo, Stephen T. Schlachter, John A. Josey
Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
June 7, 2000
Date of Patent:
September 18, 2001
Assignee:
Amgen Inc.
Inventors:
Kevin Koch, Andreas Termin, John A. Josey
Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 6, 1998
Assignee:
G.D. Searle & Co.
Inventors:
Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
March 21, 1995
Date of Patent:
July 15, 1997
Assignee:
Monsanto Company
Inventors:
John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
July 15, 1997
Assignee:
G.D. Searle & Co.
Inventors:
John S. Ng, Claire A. Przybyla, Richard A. Mueller, Michael L. Vazquez, Daniel P. Getman, John J. Freskos, Gary A. DeCrescenzo, Deborah E. Bertenshaw, Robert M. Heintz, Suhong Zhang, Chin Liu, Scott A. Laneman
Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
July 1, 1997
Assignee:
Monsanto Company of St. Louis
Inventors:
John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
January 17, 1996
Date of Patent:
June 17, 1997
Assignee:
G.D. Searle and Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
January 31, 1995
Date of Patent:
February 11, 1997
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
February 2, 1995
Date of Patent:
December 10, 1996
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
August 24, 1993
Date of Patent:
May 28, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.
Type:
Grant
Filed:
December 29, 1992
Date of Patent:
May 7, 1996
Assignee:
Monsanto Company
Inventors:
Deborah E. Bertenshaw, Daniel Getman, Robert M. Heintz, John J. Talley, Kathryn L. Reed
Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
April 23, 1996
Assignee:
G. D. Searle & Co.
Inventors:
Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 23, 1996
Assignee:
G.D. Searle & Co.
Inventors:
John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun