Patents Assigned to Rigel Pharmaceuticals, Inc.
  • Publication number: 20210002236
    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: January 7, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
  • Publication number: 20210002237
    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: January 7, 2021
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
  • Publication number: 20200407332
    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: December 31, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
  • Patent number: 10858335
    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. The compounds inhibit signaling by a member of the TGF-? superfamily such as Nodal or Activin.
    Type: Grant
    Filed: January 16, 2019
    Date of Patent: December 8, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Donald Payan, Marina Gelman, Todd Kinsella
  • Publication number: 20200377518
    Abstract: A method of preventing or treating thrombosis in a patent is disclose, wherein the method comprises administering to the patient an amount of fostamatinib or a form or metabolite thereof effective to prevent or treat the thrombosis, respectively.
    Type: Application
    Filed: May 29, 2020
    Publication date: December 3, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Esteban Masuda
  • Patent number: 10851093
    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 R1, X, Y1, Y2, Y3 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: May 29, 2019
    Date of Patent: December 1, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ihab Darwish, Jiaxin Yu, Rao Kolluri, Sacha Holland
  • Patent number: 10844040
    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: December 20, 2019
    Date of Patent: November 24, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Patent number: 10822337
    Abstract: Disclosed are pyrazole 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, X, Z, m, p, and R2 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: Grant
    Filed: March 30, 2016
    Date of Patent: November 3, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Marina Gelman, Todd Kinsella, Somasekhar Bhamidipati, Ihab Darwish, Rajinder Singh, Jiaxin Yu
  • Publication number: 20200339556
    Abstract: Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) 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: July 14, 2020
    Publication date: October 29, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
  • Publication number: 20200339678
    Abstract: Provided herein are antigen binding molecules that bind to TIGIT, including antibodies and antigen binding fragments thereof.
    Type: Application
    Filed: July 10, 2020
    Publication date: October 29, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Ramesh R. Bhatt, Todd Kinsella, Wei Li
  • Patent number: 10815206
    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: Grant
    Filed: May 2, 2019
    Date of Patent: October 27, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
  • Patent number: 10792282
    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: March 12, 2018
    Date of Patent: October 6, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
  • Publication number: 20200299276
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or produg 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 5, 2020
    Publication date: September 24, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 10774066
    Abstract: Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs 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 prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: September 15, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Beth Fernandez, Gary Park, Ihab Darwish
  • Patent number: 10774076
    Abstract: Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) 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: August 7, 2018
    Date of Patent: September 15, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
  • Patent number: 10759855
    Abstract: Provided herein are antigen binding molecules that bind to TIGIT, include antibodies and antigen binding fragments thereof.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: September 1, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ramesh R. Bhatt, Todd Kinsella, Wei Li
  • Publication number: 20200270271
    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: March 2, 2020
    Publication date: August 27, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Patent number: 10710983
    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: Grant
    Filed: June 26, 2017
    Date of Patent: July 14, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 10709703
    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: November 21, 2019
    Date of Patent: July 14, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Publication number: 20200216431
    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.
    Type: Application
    Filed: January 3, 2020
    Publication date: July 9, 2020
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh