Patents Assigned to Rigel Pharmaceuticals, Inc.
  • METHOD AND DEVICE FOR ADMINISTERING XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO[1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3-(METHYLAMINOCARBONYLMETHYLENEOXY)PHENYL]2,4-PYRIMIDINEDIAMINE
    Publication number: 20180064646
    Abstract: Disclosed embodiments concern a device for administering a xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine, or compositions thereof, and a method for making and using the device. Particular disclosed embodiments concern formulating the xinafoate salt for administration via the device.
    Type: Application
    Filed: November 9, 2017
    Publication date: March 8, 2018
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Thomas Sun
  • AMPK-ACTIVATING HETEROCYCLIC COMPOUNDS AND METHODS FOR USING THE SAME
    Publication number: 20180057478
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: May 23, 2017
    Publication date: March 1, 2018
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Compounds and method for treating autoimmune diseases
    Patent number: 9890144
    Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: February 13, 2018
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
  • TGF-beta inhibitors
    Patent number: 9884868
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: February 6, 2018
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Myers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • GDF-8 inhibitors
    Patent number: 9878992
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: January 30, 2018
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS
    Publication number: 20170369476
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Application
    Filed: June 26, 2017
    Publication date: December 28, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Screening assay employing Dex and GDF8
    Patent number: 9845512
    Abstract: Certain aspects of this disclosure relate to a method that comprises contacting a mammalian cell with a glucocorticoid receptor ligand and a myostatin receptor ligand, thereby activating the glucocorticoid receptor and said myostatin receptor. A screening assay employing the same is also provided.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: December 19, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventor: Todd M. Kinsella
  • Nrf2 activating compounds and uses thereof
    Patent number: 9845311
    Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 19, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Kinase inhibitors and their uses
    Patent number: 9834568
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: December 5, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20170298054
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Application
    Filed: June 29, 2017
    Publication date: October 19, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses
    Publication number: 20170291909
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Application
    Filed: November 23, 2016
    Publication date: October 12, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
    Patent number: 9751893
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: September 5, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
    Publication number: 20170246167
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: February 27, 2017
    Publication date: August 31, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossii
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 9737554
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: August 22, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: 9732073
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Protein kinase C inhibitors and uses thereof
    Patent number: 9732070
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Kin Tso, Jing Zhang, Matthew Duncton, Salvador Alvarez, Rao Kolluri, John Ramphal, Sacha Holland
  • Treatment for vitiligo
    Patent number: 9730930
    Abstract: Compounds I and II, as well as prodrugs, hydrates, solvates, N-oxides, salts and pharmaceutical compositions containing them, are useful for treating vitiligo. In certain embodiments, the compounds are provided in topical compositions.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: August 15, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventor: Daniel Magilavy
  • Cycloalkyl substituted pyrimidinediamine compounds and their uses
    Patent number: 9725419
    Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: August 8, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Rajinder Singh, Sambaiah Thota, David Carroll, Kin Tso, Vanessa Taylor, John McLaughlin, Vadim Markovtsov
  • System and method for high-content oncology assay
    Patent number: 9702865
    Abstract: The present invention provides an apparatus, system, method and computer program and computer program product for analyzing cellular samples. One embodiment of the apparatus and method provides a multiparameter assay that provides information with respect to cell proliferation, cell cycling and cell death. The multiparameter assay is particularly useful for assessing and screening candidate compounds for anti-cancer utility.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: July 11, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Susan Catalano, John McLaughlin
  • Tetrazolones as a carboxylic acid bioisosteres
    Patent number: 9701647
    Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: July 11, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh