公开(公告)号：US20130210814A1

公开(公告)日：2013-08-15

申请号：US13757262

申请日：2013-02-01

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Ankush Argade ,  Rajinder Singh ,  Sambaiah Thota ,  David Carroll ,  Kin Tso ,  Vanessa Taylor ,  John McLaughlin ,  Vadim Markovtsov

IPC: C07D239/48 ,  C07D401/12 ,  C07D471/08 ,  C07D295/155 ,  C07D403/12 ,  C07D417/12 ,  C07D413/12

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  C07D205/12 ,  C07D239/42 ,  C07D295/155 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  C07D487/08

Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.

Abstract translation: 本公开提供具有抗增殖活性的2,4-嘧啶二胺化合物，包含该化合物的组合物和使用该化合物抑制细胞增殖并治疗增殖性疾病如致瘤性癌症的方法。

公开(公告)号：US11939317B2

公开(公告)日：2024-03-26

申请号：US17983645

申请日：2022-11-09

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 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  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：US11667611B2

公开(公告)日：2023-06-06

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: C07D239/42 ,  C07D239/48 ,  A61K31/505 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/12 ,  C07D417/12 ,  C07D405/12 ,  C07D413/14 ,  C07D498/04

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

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：US11370808B2

公开(公告)日：2022-06-28

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 ,  C07D405/14 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  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：US20210214342A1

公开(公告)日：2021-07-15

申请号：US17184199

申请日：2021-02-24

Applicant: Rigel Pharmaceuticals, Inc.

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

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

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：US10208075B2

公开(公告)日：2019-02-19

申请号：US15934692

申请日：2018-03-23

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: C07D405/14 ,  C07F9/6558 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  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：US10208074B2

公开(公告)日：2019-02-19

申请号：US15928335

申请日：2018-03-22

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: C07D405/14 ,  C07F9/6558 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  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：US09913843B2

公开(公告)日：2018-03-13

申请号：US14712748

申请日：2015-05-14

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rao Kolluri ,  Esteban Masuda ,  Kin Tso ,  Salvador Alvarez ,  Thilo Heckrodt ,  Sacha Holland ,  Ryan Kelley ,  Matthew Duncton ,  Rajinder Singh ,  Darren McMurtrie

IPC: A61K31/506 ,  C07D498/04 ,  C07D455/02 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  C07D455/02 ,  C07D498/04

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.

公开(公告)号：US20180030050A1

公开(公告)日：2018-02-01

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 ,  A61K31/506 ,  A61K31/538 ,  C12N9/12 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00 ,  C12Q1/48 ,  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.

公开(公告)号：US20170298054A1

公开(公告)日：2017-10-19

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