Patents Assigned to Rigel Pharmaceuticals, Inc.
  • Patent number: 11963958
    Abstract: Disclosed herein are methods for treating a subject afflicted with a cancer having an activating RET alteration by administering an effective amount of a selective RET inhibitor, e.g., Compound 1 or pharmaceutically acceptable salts thereof, including, e.g., administering an amount of 60 mg to 400 mg of the selective RET inhibitor once daily.
    Type: Grant
    Filed: October 2, 2020
    Date of Patent: April 23, 2024
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Erica Evans Raab, Beni B. Wolf
  • Patent number: 11939317
    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: November 9, 2022
    Date of Patent: March 26, 2024
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
  • Publication number: 20230399326
    Abstract: Disclosed herein are embodiments of a pyrazole compound according to formula I. Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and/or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and/or composition. The compound and/or composition may be useful to inhibit an IRAK protein and/or to ameliorate, treat and/or prevent an IRAK-associated disease or condition in a subject.
    Type: Application
    Filed: August 24, 2023
    Publication date: December 14, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Lu Chou, Matt Duan, Ihab S. Darwish, Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor, Yan Chen, Dazhong Fan, Zhushou Luo
  • Patent number: 11827628
    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: November 2, 2021
    Date of Patent: November 28, 2023
    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
  • Publication number: 20230312568
    Abstract: Disclosed embodiments concern compounds according to Formula I In some embodiments, the compounds are useful as kinase inhibitors, such as interleukin receptor associated kinases (IRAK) inhibitors. Also disclosed are compositions comprising such inhibitors, and 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: March 30, 2023
    Publication date: October 5, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Zhushou Luo, Simon Shaw, Ihab Darwish, Estaban Masuda, Chrystelle Lamagna
  • Publication number: 20230303555
    Abstract: Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitor compounds and compositions comprising such compounds. The compounds may have a structure according to Formula I 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: March 22, 2023
    Publication date: September 28, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Jack Maung, Yan Chen, Simon Shaw, David Sweeny, Esteban Masuda
  • Patent number: 11672791
    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 2, 2021
    Date of Patent: June 13, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Sacha Holland, Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Rao Kolluri, Ihab Darwish, Esteban Masuda, Jiaxin Yu
  • Patent number: 11667611
    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: Grant
    Filed: May 6, 2019
    Date of Patent: June 6, 2023
    Assignee: 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
  • Patent number: 11667643
    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: June 25, 2021
    Date of Patent: June 6, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Simon Shaw, Ihab Darwish, Jiaxin Yu, Rao Kolluri, Vanessa Taylor, Esteban Masuda, Mark Irving
  • Publication number: 20230123591
    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: Application
    Filed: October 7, 2022
    Publication date: April 20, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Marina Gelman, Todd Kinsella, Somasekhar Bhamidipati, Ihab Darwish, Rajinder Singh, Jiaxin Yu
  • Publication number: 20230115275
    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: November 9, 2022
    Publication date: April 13, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
  • Publication number: 20230095835
    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: November 16, 2022
    Publication date: March 30, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Publication number: 20230062818
    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: Application
    Filed: September 27, 2022
    Publication date: March 2, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Ryan Kelley, Darren McMurtrie, Kin Tso, Vanessa Taylor, Rajinder Singh, Rose Yen, Jack Maung
  • Patent number: 11584758
    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: April 2, 2021
    Date of Patent: February 21, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ihab Darwish, Zhushou Luo, Vanessa Taylor
  • Patent number: 11578078
    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 compounds may have a structure according to Formula I 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: November 6, 2020
    Date of Patent: February 14, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Jiaxin Yu, Simon Shaw, Ihab Darwish, Vanessa Taylor, Somasekhar Bhamidipati, Zhushou Luo, Rao Kolluri
  • Patent number: 11564930
    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: September 4, 2020
    Date of Patent: January 31, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Ihab Darwish, Vanessa Taylor, Rao Kolluri, Yan Chen, Simon Shaw, Somasekhar Bhamidipati, Zhushou Luo
  • Publication number: 20230012676
    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: Application
    Filed: September 2, 2021
    Publication date: January 19, 2023
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Sacha Holland, Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Rao Kolluri, Ihab Darwish, Esteban Masuda, Jiaxin Yu
  • Patent number: 11530194
    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: February 24, 2021
    Date of Patent: December 20, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
  • Patent number: 11524955
    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: Grant
    Filed: June 5, 2020
    Date of Patent: December 13, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 11492349
    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: February 24, 2021
    Date of Patent: November 8, 2022
    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