公开(公告)号：US20210179601A1

公开(公告)日：2021-06-17

申请号：US17184182

申请日：2021-02-24

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC: C07D413/14 ,  A61P29/00

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.

公开(公告)号：US10941140B2

公开(公告)日：2021-03-09

申请号：US16444093

申请日：2019-06-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC: C07D413/14 ,  A61P29/00

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.

公开(公告)号：US10828301B2

公开(公告)日：2020-11-10

申请号：US16402912

申请日：2019-05-03

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 ,  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：US10414753B2

公开(公告)日：2019-09-17

申请号：US15793743

申请日：2017-10-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Kin Tso ,  Hui Li ,  Yan Chen ,  Rose Yen ,  Vanessa Taylor ,  Thilo Heckrodt ,  Rajinder Singh ,  Simon Shaw

IPC: C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D403/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

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.

公开(公告)号：US20190256476A1

公开(公告)日：2019-08-22

申请号：US16404481

申请日：2019-05-06

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ankush Argade ,  Arvinder Sran ,  David Carroll ,  Jeffrey Clough ,  Kin Tso ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Rajinder Singh ,  Vanessa Taylor ,  Hui Li ,  Esteban Masuda

IPC: C07D239/48 ,  C07D417/12 ,  C07D413/12 ,  C07D407/12 ,  C07D403/12 ,  A61K31/505 ,  C07D401/12 ,  C07D498/04 ,  C07D413/14 ,  C07D405/12 ,  C07D401/14

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.

公开(公告)号：US10370367B2

公开(公告)日：2019-08-06

申请号：US15793770

申请日：2017-10-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC: C07D413/14 ,  A61P29/00

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.

公开(公告)号：US10314840B2

公开(公告)日：2019-06-11

申请号：US15443145

申请日：2017-02-27

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：US20190153006A1

公开(公告)日：2019-05-23

申请号：US16259685

申请日：2019-01-28

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Ryan Kelley ,  Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC: C07F9/6558 ,  C07D413/04 ,  C07D417/14 ,  C07D405/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/04

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.

公开(公告)号：USRE47396E1

公开(公告)日：2019-05-21

申请号：US14918353

申请日：2015-10-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Thilo J. Heckrodt ,  Yan Chen ,  Darren John McMurtrie ,  Vanessa Taylor ,  Rajinder Singh ,  Pingyu Ding ,  Rose Yen

IPC: A61K31/505 ,  A61K31/675 ,  C07D413/12 ,  C07F9/02 ,  C07B59/00 ,  C07D239/02 ,  C07F9/6558

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.

公开(公告)号：US10005777B2

公开(公告)日：2018-06-26

申请号：US15588410

申请日：2017-05-05

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： 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

IPC: C07D471/04 ,  C12Q1/48 ,  A61K31/506 ,  A61K31/538 ,  C12N9/12 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  C12N9/12 ,  C12Q1/485 ,  C12Y207/11013

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.