公开(公告)号：US20200270271A1

公开(公告)日：2020-08-27

申请号：US16806541

申请日：2020-03-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

IPC: C07D498/04 ,  C07F9/6574 ,  C07F9/6561 ,  C07F9/6558 ,  A61K31/5383 ,  A61K31/675

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.

公开(公告)号：US10709703B2

公开(公告)日：2020-07-14

申请号：US16691352

申请日：2019-11-21

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Ankush Argade ,  Donald Payan ,  Susan Molineaux ,  Sacha J. Holland ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Catherine Sylvain ,  Hui Li ,  Alexander B. Rossi

IPC: A61K31/505 ,  A61K31/519 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D239/48 ,  C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D498/04 ,  C07D265/36 ,  A61K31/5395 ,  C07D495/04 ,  C07F5/02 ,  C07D498/14 ,  C07D407/14

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.

公开(公告)号：US20200216431A1

公开(公告)日：2020-07-09

申请号：US16733571

申请日：2020-01-03

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

IPC: C07D413/12 ,  C07D451/02 ,  A61K31/635 ,  A61K31/5415 ,  C07F9/6558 ,  C07D498/04 ,  C07D487/10 ,  C07D471/04 ,  C07D413/14 ,  A61K31/675 ,  A61K31/55 ,  A61K31/538 ,  C07D491/08 ,  C07D487/04 ,  C07D471/08 ,  C07D419/14 ,  A61K45/06 ,  A61K31/551 ,  A61K31/541 ,  A61K31/54 ,  A61K31/5383 ,  A61K31/5377 ,  A61K31/506 ,  C07D487/08 ,  C07D413/04 ,  C07D403/12 ,  C07D401/14 ,  A61K31/155

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.

公开(公告)号：US20200216412A1

公开(公告)日：2020-07-09

申请号：US16723881

申请日：2019-12-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/04 ,  C07D257/04 ,  C07D255/02 ,  C07D249/12

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.

公开(公告)号：US20200181130A1

公开(公告)日：2020-06-11

申请号：US16551393

申请日：2019-08-26

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： 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

IPC: C07D413/12 ,  C07F7/08 ,  C07D417/12 ,  C07D401/14 ,  A61K45/06 ,  C07F7/10 ,  C07D498/04 ,  A61K39/395 ,  A61K38/13 ,  A61K31/695 ,  A61K31/541 ,  A61K31/5383 ,  A61K31/538 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/505 ,  A61K31/436 ,  A61K31/343 ,  C07D239/48 ,  C07D413/14 ,  C07D403/12 ,  C07D401/12 ,  C07D239/42 ,  C07D403/04

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.

公开(公告)号：US20200078348A1

公开(公告)日：2020-03-12

申请号：US16575852

申请日：2019-09-19

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rajinder Singh ,  Somasekhar Bhamidipati ,  Pingyu Ding ,  Rao Kolluri ,  Ihab Darwish ,  Esteban Masuda ,  Jiaxin Yu

IPC: A61K31/4545 ,  A61K31/519 ,  C07D519/00 ,  C07D471/04

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.

公开(公告)号：US10556891B2

公开(公告)日：2020-02-11

申请号：US15988920

申请日：2018-05-24

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Vanessa Taylor ,  Hui Li ,  Rajinder Singh

IPC: A61K31/506 ,  C07D413/12 ,  A61K31/155 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D487/08 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D419/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  A61K31/538 ,  A61K31/55 ,  A61K31/675 ,  C07D413/14 ,  C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07F9/6558 ,  A61K31/5415 ,  A61K31/635 ,  C07D451/02

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.

公开(公告)号：US10421752B2

公开(公告)日：2019-09-24

申请号：US15637833

申请日：2017-06-29

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： 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

IPC: A61K31/506 ,  C07D413/12 ,  C07D403/04 ,  C07D239/42 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/395 ,  C07D498/04 ,  C07F7/10 ,  A61K45/06 ,  C07D401/14 ,  C07D417/12 ,  C07F7/08 ,  C07D285/22

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.

公开(公告)号：US10369148B2

公开(公告)日：2019-08-06

申请号：US15366931

申请日：2016-12-01

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： 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

IPC: A61K31/505 ,  A61K31/519 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/06 ,  C07D498/04 ,  C07D265/36 ,  A61K31/5395 ,  C07D495/04 ,  C07F5/02 ,  C07D498/14 ,  C07D407/14

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.

公开(公告)号：US10166216B2

公开(公告)日：2019-01-01

申请号：US15147669

申请日：2016-05-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Dane Goff ,  Jing Zhang ,  Catherine Sylvain ,  Rajinder Singh ,  Sacha Holland ,  Jiaxin Yu ,  Thilo J. Heckrodt ,  Pingyu Ding

IPC: C07D249/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  A61K31/635 ,  A61K31/519 ,  A61K31/517 ,  A61K31/506 ,  A61K31/502 ,  A61K31/501 ,  A61K31/498 ,  A61K31/497 ,  A61K31/454 ,  A61K31/428 ,  A61K31/4196 ,  C07D401/04 ,  C07D491/048 ,  A61K31/4355 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377

Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.