Patents Assigned to Rigel Pharmaceuticals
  • Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses
    Publication number: 20190292197
    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 28, 2018
    Publication date: September 26, 2019
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: 10421752
    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: June 29, 2017
    Date of Patent: September 24, 2019
    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
  • 2,3-Disubstituted Pyridine Compounds as TGF-Beta Inhibitors and Methods of Use
    Publication number: 20190284155
    Abstract: The invention described herein comprises compounds and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer.
    Type: Application
    Filed: January 16, 2019
    Publication date: September 19, 2019
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Donald Payan, Marina Gelman, Todd Kinsella
  • Amide compounds and method for making and using
    Patent number: 10414753
    Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: September 17, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
  • Compounds and method for treating autoimmune diseases
    Patent number: 10414758
    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: January 19, 2018
    Date of Patent: September 17, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20190256476
    Abstract: The invention encompasses compounds having formula I 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, are therapeutically useful.
    Type: Application
    Filed: May 6, 2019
    Publication date: August 22, 2019
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Ankush Argade, Arvinder Sran, David Carroll, Jeffrey Clough, Kin Tso, Somasekhar Bhamidipati, Sambaiah Thota, Rajinder Singh, Vanessa Taylor, Hui Li, Esteban Masuda
  • 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
    Publication number: 20190255047
    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: May 3, 2019
    Publication date: August 22, 2019
    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. Rossi
  • AMPK-activating heterocyclic compounds and methods for using the same
    Patent number: 10377742
    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: Grant
    Filed: May 23, 2017
    Date of Patent: August 13, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • 2,4-pyrimidinediamine compounds and their uses
    Patent number: 10369148
    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: Grant
    Filed: December 1, 2016
    Date of Patent: August 6, 2019
    Assignee: 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. Rossi
  • IRAK inhibitors and method for making and using
    Patent number: 10370367
    Abstract: Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: August 6, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Ryan Kelley, Darren McMurtrie, Kin Tso, Vanessa Taylor, Rajinder Singh, Rose Yen, Jack Maung
  • Prodrugs of 2,4-pyrimidinediamine compounds and their uses
    Patent number: 10357505
    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: July 17, 2017
    Date of Patent: July 23, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
  • 2,4-pyrimidinediamine compounds and their uses
    Patent number: 10314840
    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: Grant
    Filed: February 27, 2017
    Date of Patent: June 11, 2019
    Assignee: 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. Rossi
  • Mode of action screening method
    Patent number: 10311214
    Abstract: Certain aspects of this disclosure relate to a screening method. In general terms, the screening assay comprises contacting test cells with a test compound to provide contacted test cells, obtaining values for a plurality of cytological attributes of the contacted test cells, and scoring the cells using the values to provide a likelihood score for at least one of a plurality of classifiers, where the plurality of classifiers are defined using values for cytological attributes obtained from cells that have been contacted with compounds of known mode of action.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: June 4, 2019
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: John McLaughlin, Zachary Pincus, Jim Bernstein
  • PYRAZOLE COMPOUNDS AND METHODS FOR MAKING AND USING THE COMPOUNDS
    Publication number: 20190153006
    Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Application
    Filed: January 28, 2019
    Publication date: May 23, 2019
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Ryan Kelley, Hui Li, Thilo Heckrodt, Yan Chen, Darren McMurtrie, Kin Tso, Vanessa Taylor, Rajinder Singh, Rose Yen, Jack Maung
  • TGF-? inhibitors
    Patent number: 10287295
    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: January 2, 2018
    Date of Patent: May 14, 2019
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Meyers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
    Patent number: 10259826
    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 lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: April 16, 2019
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use
    Patent number: 10233170
    Abstract: The invention described herein comprises compounds of formula (IV) and a method of treating cancer comprising administering to a subject having cancer one of the compounds in conjunction with another therapeutic treatment of cancer. The compounds (IV) inhibit signaling by a member of the TGF-? superfamily such as Nodal or Activin.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: March 19, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Donald Payan, Marina Gelman, Todd Kinsella
  • Pyrazole compounds and method for making and using the compounds
    Patent number: 10208074
    Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: February 19, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ryan Kelley, Hui Li, Thilo Heckrodt, Yan Chen, Darren McMurtrie, Kin Tso, Vanessa Taylor, Rajinder Singh, Rose Yen, Jack Maung
  • Pyrazole compounds and method for making and using the compounds
    Patent number: 10208075
    Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: February 19, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ryan Kelley, Hui Li, Thilo Heckrodt, Yan Chen, Darren McMurtrie, Kin Tso, Vanessa Taylor, Rajinder Singh, Rose Yen, Jack Maung
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: RE47396
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: May 21, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen