Patents Assigned to Agouron Pharmaceuticals, Inc.
  • Fused heteroaryl carboxylic acids as PPAR agonists
    Publication number: 20040209929
    Abstract: Fused heteroarylcarboxylic acids of formula (I): 1
    Type: Application
    Filed: February 19, 2004
    Publication date: October 21, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Donald Skalitzky, Wei-Guo Su, Luke Raymond Zehnder
  • Dual reporter/dye reduction methodology for evaluating antiviral and cytotoxicity of hepatitis C virus inhibitors
    Publication number: 20040209246
    Abstract: Methods are provided for evaluating the antiviral activity and cytotoxicity of a compound in the same population of cells by the use of reporter genes and dye reduction methodology. The dual antiviral activity/cytotoxicity reporter methods are amenable for use in a high-throughput format.
    Type: Application
    Filed: April 5, 2004
    Publication date: October 21, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Mary Brothers, Rohit Duggal, Koleen Herlihy, Amy Patick, Weidong Hao
  • HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
    Publication number: 20040204591
    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, 1
    Type: Application
    Filed: December 4, 2003
    Publication date: October 14, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: David John Kucera, Robert William Scott
  • Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
    Publication number: 20040192735
    Abstract: Indazole compounds that modulate and/or inhibit the ophthalmic diseases and 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 ophthalmic diseases and 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: Application
    Filed: December 15, 2003
    Publication date: September 30, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Allen J. Borchardt, Robert Steven Kania, Cynthia L. Palmer
  • Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
    Publication number: 20040186126
    Abstract: The invention relates to compounds represented by the formula I 1
    Type: Application
    Filed: March 9, 2004
    Publication date: September 23, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Michael Collins, Stephan Cripps, Judith Deal, Robert Steven Kania, Jihong Lou, Mingying He, Cynthia Louise Palmer, William Henry Romines, Ru Zhou
  • Method of treatment with nelfinavir
    Publication number: 20040186066
    Abstract: The invention relates to a method of treating human immunodeficiency virus (HIV) in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of nelfinavir in a pharmaceutical composition, wherein the nelfinavir is administered with food.
    Type: Application
    Filed: February 10, 2004
    Publication date: September 23, 2004
    Applicant: AGOURON PHARMACEUTICALS, INC.
    Inventors: Carolyn Petersen, Edward F.C. Pun
  • Modifications of the VEGF receptor-2 protein and methods of use
    Patent number: 6794146
    Abstract: A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: September 21, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michele A. McTigue, Chris Pinko, Camran V. Parast, Michael R. Gehring, Chen-Chen Kan, Krzysztof Appelt, John A. Wickersham, Richard E. Showalter, Anna M. Tempcyzk-Russell, Barbara Mroczkowski, Jesus E. Villafranca
  • Reporter gene system for use in cell-based assessment of inhibitors of the hepatitis C virus protease
    Patent number: 6790612
    Abstract: A cell-based assay system in which the detection of the reporter gene activity, or secreted alkaline phosphatase (SEAP), is dependent upon the protease activity of the Hepatitis C virus NS3 gene product. This system can be used to assess the activity of candidate protease inhibitors in a mammalian cell-based assay system. The assay system is simpler than previously described assays due to the use of SEAP which allows the reporter gene activity to be quantified by measuring the amount of secreted gene product in the cell media by monitoring the conversion of luminescent or calorimetric alkaline phosphatase substrate.
    Type: Grant
    Filed: July 10, 2002
    Date of Patent: September 14, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Karen Elizabeth Potts, Roberta Lynn Jackson, Amy Karen Patick
  • PIN1 peptidyl-prolyl isomerase polypeptides, their crystal structures, and use thereof for drug design
    Publication number: 20040171019
    Abstract: Polypeptides containing the PIN1 peptidyl-prolyl isomerase domain but not containing the PIN1 WW domain are described. Also described are crystal structures of these polypeptides, including the crystal structure of a PIN1 PPIase:ligand complex. The structure coordinate data derived from these crystals provides a three-dimensional description of the substrate-binding site of PIN1 peptidyl-prolyl isomerase useful in drug discovery and design for the identification and design of modulators of PIN1 peptidyl-prolyl isomerase activity.
    Type: Application
    Filed: December 19, 2003
    Publication date: September 2, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: David Matthews, Eleanor Dagostino, Rose Ann Ferre, Smita Gaur, Chuangxing Guo, Xinjun Hou, Stephen Margosiak, Barbara Mroczkowski, Grace Reiko Nakayama, Hans Parge, Jeff Zhu
  • Modifications of the VEGF Receptor-2 Protein and methods of use
    Patent number: 6784285
    Abstract: A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: August 31, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michele A. McTigue, Chris Pinko, Camran V. Parast, Michael R. Gehring, Chen-Chen Kan, Krzysztof Appelt, John A. Wickersham, Richard E. Showalter, Anna M. Tempcyzk-Russell, Barbara Mroczkowski, Jesus E. Villafranca
  • Efficient synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates
    Patent number: 6774243
    Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.
    Type: Grant
    Filed: October 30, 2001
    Date of Patent: August 10, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Qingping Tian, Naresh K. Nayyar, Srinivasan Babu, Junhua Tao, Terence Jarold Moran, Raymond Dagnino, Jr., Lennert J. Mitchell, Jr., Travis Paul Remarchuk, Michael Joseph Melnick, Steven Lee Bender
  • HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use
    Publication number: 20040147547
    Abstract: Bicyclic hydroxamate compounds represented by the Formula I: 1
    Type: Application
    Filed: October 30, 2003
    Publication date: July 29, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Qiyue Hu, Atsuo Kuki, Michael Bruno Plewe, Dawn Marie Nowlin, Hai Wang, Junhu Zhang
  • Modifications of the VEGF receptor-2 protein and methods of use
    Patent number: 6753416
    Abstract: A 2.4 Å crystal structure of a protein construct containing the catalytic kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2/KDR), a key enzyme in angiogenesis, has been determined in an unliganded, phosphorylated state. This protein construct, contains a modified catalytic linker and has comparable in vitro kinase activity to constructs containing the entire KID. The resulting construct retains comparable in vitro kinase activity to that of the wild-type KID, and more importantly, allows complete crystallization of the protein such that it may be characterized by X-ray crystallography. The present invention further discloses the use of x-ray crystallographic data for identification and construction of possible therapeutic compounds in the treatment of various disease conditions.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: June 22, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michele A. McTigue, Chris Pinko, Camran V. Parast, Michael R. Gehring, Chen-Chen Kan, Krzysztof Appelt, John A. Wickersham, Richard E. Showalter, Anna M. Tempcyzk-Russell, Barbara Mroczkowski, Jesus E. Villafranca
  • Thiazole benzamide derivatives and pharmaceutical compositions for inhibiting cell proliferation
    Patent number: 6720346
    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
  • Metabolites of prinomastat and their synthesis
    Publication number: 20040053922
    Abstract: Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M7); (3S)-2,2-dimethyl-4-[4-(1-oxypyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M8); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M2); and (3S)-2,2-dimethyl-4-[4-(pyridin-4yloxy)-benzenesulfonyl)-thiomorphpline-3-carboxylic acid amide (M3).
    Type: Application
    Filed: June 10, 2003
    Publication date: March 18, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Michael A. Ouellette, Barbara C.M. Potts, Jayaram K. Srirangam, Anthony R. Tibbetts, Kanyin E. Zhang
  • Benzimidazole inhibitors of poly(ADP-ribosyl) polymerase
    Publication number: 20040034078
    Abstract: Compounds of formula I are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used in combination with cytotoxic agents and/or radiation.
    Type: Application
    Filed: June 4, 2003
    Publication date: February 19, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Donald J. Skalitzky, Stephen E. Webber, Brian Eastman
  • Method of making HIV protease inhibitors
    Patent number: 6693199
    Abstract: A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: February 17, 2004
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
  • Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
    Publication number: 20040023958
    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: Application
    Filed: May 9, 2003
    Publication date: February 5, 2004
    Applicant: 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
  • Non-peptide GnRH agents, pharmaceutical compositions and methods for their use
    Publication number: 20040014787
    Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, 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: Application
    Filed: June 11, 2003
    Publication date: January 22, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen Thuy Do, Jun Feng, Yufeng Hong, Haitao Li, Ved P. Pathak, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins
  • Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
    Publication number: 20040009965
    Abstract: The invention relates to compounds represented by the formula I 1
    Type: Application
    Filed: June 11, 2003
    Publication date: January 15, 2004
    Applicant: Agouron Pharmaceuticals, Inc.
    Inventors: Michael Collins, Stephan Cripps, Judith Deal, Robert Steven Kania, Jihong Lou, Mingying He, Cynthia Louise Palmer, William Henry Romines, Ru Zhou