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.
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
Abstract: Disclosed embodiments concern kinase inhibitors, such as interleukin receptor associated kinases (IRAK) inhibitors according to Formula 1, 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.
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:
February 24, 2021
Publication date:
June 17, 2021
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
Abstract: Disclosed are aryl pyrimidine compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) 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.
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:
June 19, 2019
Date of Patent:
May 18, 2021
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
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:
Application
Filed:
November 6, 2020
Publication date:
May 13, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Jiaxin Yu, Simon Shaw, Ihab Darwish, Vanessa Taylor, Somasekhar Bhamidipati, Zhushou Luo, Rao Kolluri
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.
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.
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:
Application
Filed:
November 25, 2020
Publication date:
March 18, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Ihab Darwish, Jiaxin Yu, Rao Kolluri, Sacha Holland
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:
August 2, 2019
Date of Patent:
March 16, 2021
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Kin Tso, Hui Li, Yan Chen, Rose Yen, Vanessa Taylor, Thilo Heckrodt, Rajinder Singh, Simon Shaw
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 4, 2020
Publication date:
March 11, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Jiaxin Yu, Simon Shaw, Ihab Darwish, Vanessa Taylor, Somasekhar Bhamidipati, Zhushou Luo, Rao Kolluri
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 4, 2020
Publication date:
March 11, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor
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:
June 25, 2019
Date of Patent:
March 9, 2021
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
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.
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:
June 18, 2019
Date of Patent:
March 9, 2021
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
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 28, 2020
Publication date:
March 4, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Lu Chou, Matt Duan, Ihab Darwish, Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor, Yan Chen, Dazhong Fan, Zhushou Luo
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:
October 16, 2020
Publication date:
February 11, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
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 14, 2021
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Esteban Masuda, Simon Shaw, Vanessa Taylor, Somasekhar Bhamidipati
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:
August 12, 2020
Date of Patent:
January 12, 2021
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Jiaxin Yu, Beth Fernandez, Gary Park, Ihab Darwish