Abstract: The present invention relates to methods for preparing indazole compounds of formula I, which are useful as modulators and/or inhibitors of protein kinases. The present invention also relates to intermediate compounds useful in the preparation of compounds of formula I.
Type:
Grant
Filed:
October 31, 2005
Date of Patent:
June 19, 2007
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Brigitte Leigh Ewanicki, Erik Jon Flahive, Annie Judith Kasparian, Mark Bryan Mitchell, Michael David Perry, Stacy Ann O'Neill-Slawecki, Neal William Sach, James Edward Saenz, Bing Shi, Nebojsa Slobodan Stankovic, Jayaram Kasturi Srirangam, Qingping Tian, Shu Yu
Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.
Type:
Grant
Filed:
November 30, 1999
Date of Patent:
May 15, 2007
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
Abstract: The invention relates to compounds represented by Formula (I): and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein each of X1–X5 and R1–R5 are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
Type:
Grant
Filed:
August 26, 2004
Date of Patent:
April 24, 2007
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Jihong Lou, Robert Steven Kania, Mingying He
Abstract: Compounds of the formula: where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
Type:
Grant
Filed:
June 11, 2002
Date of Patent:
February 20, 2007
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Stacie S. Canan Koch, Therese N. Alexander, Benjamin J. Burke, Tanya M. Jewell, David J. Kucera, Maria Angelica Linton, Lennert J. Mitchell, Jr., Siegfried H. Reich, Donald J. Skalitzky, John H. Tatlock, Michael D. Varney, Scott C. Virgil, Stephen E. Webber, Stephen T. Worland, Mark Barvian, Gary Bolton, Frederick Earl Boyer, Jr., Jeffrey J. Machak, Tod Holler, Sean T. Murphy, Michael Melnick, Vara Prasad Josyula
Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Grant
Filed:
September 8, 2003
Date of Patent:
February 20, 2007
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
Abstract: Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
Abstract: The present invention provides compounds of formula (4), and their pharmaceutically acceptable salts and solvates, which are useful as inhibitors of the Hepatitis C virus (HCV) polymerase enzyme and are also useful for the treatment of HCV infections in HCV-infected mammals. The present invention also provides pharmaceutical compositions comprising compounds of formula (4), their pharmaceutically acceptable salts and solvates. Furthermore, the present invention provides intermediate compounds and methods useful in the preparation of compounds of formula (4).
Type:
Grant
Filed:
August 15, 2005
Date of Patent:
December 19, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Angelica Linton, John Howard Tatlock
Abstract: The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
Type:
Grant
Filed:
November 19, 2003
Date of Patent:
December 12, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Allen Borchardt, Javier Gonzalez, Hui Li, Maria Angelica Linton, John Howard Tatlock
Abstract: Indazole 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 and thereby 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 and 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:
August 12, 2003
Date of Patent:
November 28, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Steven Bender, Dana Hu-Lowe, David Ray Shalinsky
Abstract: This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.
Type:
Grant
Filed:
April 26, 2004
Date of Patent:
November 28, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Romuald Gaston Corbau, Charles Eric Mowbray, Manoussos Perros, Paul Anthony Stupple, Anthony Wood
Abstract: Indazole 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 and thereby 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 and 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:
November 18, 2004
Date of Patent:
November 28, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Robert Steven Kania, Steven Lee Bender, Allen J. Borchardt, Stephan James Cripps, Ye Hua, Michael David Johnson, Theodore Otto Johnson, Jr., Hiep The Luu, Cynthia Louise Palmer, Siegfried Heinz Reich, Anna Maria Tempczyk-Russell, Min Teng, Christine Thomas, Michael David Varney, Michael Brennan Wallace, Michael Raymond Collins
Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
Type:
Grant
Filed:
October 14, 2005
Date of Patent:
November 21, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
Abstract: Bicyclic hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integrase and to treat HIV mediated diseases and conditions.
Type:
Grant
Filed:
October 30, 2003
Date of Patent:
November 14, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Qiyue Hu, Ted William Johnson, Atsuo Kuki, Michael Bruno Plewe, Dawn Marie Nowlin, Hai Wang, Junhu Zhang
Abstract: Protein kinase, such as CHK-1, inhibiting tricyclic compounds of the following formula (wherein R2, R3 and R4 are as defined in the specification) pharmaceutical compositions containing effective amounts of said compounds or their salts are useful as a single agent or in combination with an anti-neoplastic agent or therapeutic radiation having an anti-neoplastic effect for treating diseases or conditions such as cancers.
Type:
Grant
Filed:
July 22, 2005
Date of Patent:
November 7, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Suzanne Benedict, Michael Bennett, Sacha Ninkovic, Min Teng, Eugene Rui, Fen Wang, Yong Wang, Jinjiang Zhu
Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Grant
Filed:
January 4, 2005
Date of Patent:
October 24, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
Type:
Grant
Filed:
May 9, 2003
Date of Patent:
October 3, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Allen J. Borchardt, Peter Scott Dragovich, Javier Gonzalez, Tanya Michelle Jewell, Hui Li, Maria Angelica Linton, John Howard Tatlock, Ru Zhou, Thomas Jay Prins, Melwyn A. Abreo
Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
February 10, 2004
Date of Patent:
September 26, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
Type:
Grant
Filed:
April 5, 2002
Date of Patent:
September 19, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
Type:
Grant
Filed:
August 20, 1999
Date of Patent:
September 5, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Mark Brian Anderson, Haresh N. Vazir, David Robert Luthin, Genevieve DeGuzman Paderes, Ved P. Pathak, Lance Christopher Christie, Yufeng Hong, Eileen Valenzuela Tompkins, Haitao Li, James Faust
Abstract: The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibitors of the HIV protease enzyme.
Type:
Grant
Filed:
December 4, 2003
Date of Patent:
August 22, 2006
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
David John Kucera, Robert William Scott