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:
August 7, 2018
Publication date:
December 6, 2018
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
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.
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:
May 24, 2018
Publication date:
September 20, 2018
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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 2, 2016
Date of Patent:
September 4, 2018
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
Abstract: Disclosed are sulfonamidoquinoline compounds, as well as pharmaceutical compositions and methods of use. 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 and R4 are as described herein. In certain embodiments, a compound disclosed herein inhibits ubiquitination, and can be used to treat disease by blocking the degradation of tumor suppressors.
Type:
Grant
Filed:
August 14, 2015
Date of Patent:
August 7, 2018
Assignee:
RIGEL PHARMACEUTICALS, INC.
Inventors:
David Carroll, Arvinder Sran, Rajinder Singh, Jianing Huang, Lyuben Tsvetkov, Sarkiz Issakani, Donald Payan, Simon Shaw
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:
March 22, 2018
Publication date:
July 26, 2018
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
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:
March 23, 2018
Publication date:
July 26, 2018
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
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:
May 5, 2017
Date of Patent:
June 26, 2018
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, Ryan Kelley
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:
Grant
Filed:
January 30, 2017
Date of Patent:
June 26, 2018
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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:
February 8, 2018
Publication date:
June 14, 2018
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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:
Application
Filed:
July 17, 2017
Publication date:
June 7, 2018
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
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:
April 22, 2016
Date of Patent:
May 29, 2018
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
Abstract: Disclosed are 2,2?-bipyridyl 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, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.
Type:
Grant
Filed:
February 15, 2016
Date of Patent:
May 29, 2018
Assignees:
RIGEL PHARMACEUTICALS, INC, BRISTOL-MYERS SQUIBB COMPANY
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:
Application
Filed:
January 19, 2018
Publication date:
May 24, 2018
Applicant:
Rigel Pharmaceuticals, Inc.
Inventors:
Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
Abstract: A construct system for expressing a reporter protein, as well as a transgenic animal and a screening method employing the same, are provided. In certain embodiments, the construct system is a three component system in which expression of a reporter protein from a reporter construct is induced by a transcription factor that is produced using two other constructs, each producing a different part of the transcription factor. The parts of the transcription factor are ligated together. Expression of the reporter only occurs in tissues in which both of the parts of the transcription factor are produced.
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:
February 22, 2017
Date of Patent:
March 20, 2018
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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.
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 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:
May 14, 2015
Date of Patent:
March 13, 2018
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rao Kolluri, Esteban Masuda, Kin Tso, Salvador Alvarez, Thilo Heckrodt, Sacha Holland, Ryan Kelley, Matthew Duncton, Rajinder Singh, Darren McMurtrie
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:
July 8, 2016
Date of Patent:
March 13, 2018
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
Abstract: Embodiments of topical formulations for administering compound I or a pharmaceutically acceptable salt or solvate thereof are disclosed. Embodiments of methods for using the topical formulations in the treatment of dermatological disorders such as cutaneous collagen vascular diseases, e.g., cutaneous lupus, also are disclosed.