Patents Assigned to Rigel Pharmaceuticals, Inc.
  • Patent number: 11279686
    Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds 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: October 20, 2020
    Date of Patent: March 22, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Publication number: 20220073536
    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 erythematosus and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Application
    Filed: November 19, 2021
    Publication date: March 10, 2022
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Publication number: 20220024907
    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: Application
    Filed: October 5, 2021
    Publication date: January 27, 2022
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 11230554
    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 21, 2019
    Date of Patent: January 25, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Patent number: 11220496
    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: August 26, 2019
    Date of Patent: January 11, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
  • Publication number: 20220000880
    Abstract: Disclosed herein are embodiments of a method and pharmaceutical composition for treating acute myeloid leukemia (AML). In particular, the method embodiments comprise treating AML with 6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one, or a prodrug thereof, alone or in combination with one or more therapeutic agents that themselves are effective for treating AML. Also disclosed are embodiments of a pharmaceutical composition comprising 6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one, or a prodrug thereof, either as the sole therapeutic agent or in combination with one or more therapeutic agents effective for treating AML.
    Type: Application
    Filed: October 31, 2019
    Publication date: January 6, 2022
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Sandra Tong, Vadim Markovtsov, Ann Lowe, Anne-Marie Duliege
  • Patent number: 11198689
    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: August 26, 2019
    Date of Patent: December 14, 2021
    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
  • Patent number: 11174251
    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 17, 2019
    Date of Patent: November 16, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 11174246
    Abstract: Disclosed are benzimidazole 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 R1, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.
    Type: Grant
    Filed: August 15, 2017
    Date of Patent: November 16, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Simon Shaw, Xiang Xu, Sarkiz Issakani, Rajinder Singh, Yasumichi Hitoshi, Matthew Duncton, Nan Lin
  • Publication number: 20210317135
    Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
    Type: Application
    Filed: April 2, 2021
    Publication date: October 14, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Ihab Darwish, Zhushou Luo, Vanessa Taylor
  • Publication number: 20210309655
    Abstract: Disclosed embodiments concern kinase inhibitors, such as 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 a kinase-associated disease or condition, particularly an IRAK-associated disease or condition.
    Type: Application
    Filed: June 8, 2021
    Publication date: October 7, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Vanessa Taylor, Yan Chen, Rose Yen
  • Patent number: 11129819
    Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. 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: October 14, 2019
    Date of Patent: September 28, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
  • Publication number: 20210276982
    Abstract: Disclosed are aryl pyrimidine 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 A, Z, R and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits the activity of one or more members of the TGF-? superfamily, and can be used to treat disease by blocking such activity.
    Type: Application
    Filed: May 19, 2021
    Publication date: September 9, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Marina Gelman, Pingyu Ding, Todd Kinsella, Rajinder Singh, Somasekhar Bhamidipati, Jeffrey Clough
  • Patent number: 11110082
    Abstract: Disclosed are imidazole 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, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.
    Type: Grant
    Filed: September 19, 2019
    Date of Patent: September 7, 2021
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Sacha Holland, Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Rao Kolluri, Ihab Darwish, Esteban Masuda, Jiaxin Yu
  • Publication number: 20210267971
    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, 2021
    Publication date: September 2, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipsti, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 11104737
    Abstract: The present disclosure provides antibodies that specifically bind to and block signaling by ACVR2A, i.e., ACVR2A but not ACVR2B, as well as methods for using the same. The antibodies may be used for the treatment of a number of conditions associated with muscle atrophy, as well as other conditions.
    Type: Grant
    Filed: March 27, 2018
    Date of Patent: August 31, 2021
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Todd M. Kinsella, Ramesh Bhatt, Kristen Baltgalvis
  • Publication number: 20210238153
    Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
    Type: Application
    Filed: September 16, 2020
    Publication date: August 5, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
  • Publication number: 20210214347
    Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
    Type: Application
    Filed: March 23, 2021
    Publication date: July 15, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Vanessa Taylor, Jiaxin Yu, Esteban Masuda, Ihab Darwish, Yan Chen
  • Publication number: 20210214342
    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: February 24, 2021
    Publication date: July 15, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
  • Patent number: RE48898
    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: March 4, 2019
    Date of Patent: January 25, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda