公开(公告)号：US20150158824A1

公开(公告)日：2015-06-11

申请号：US14624301

申请日：2015-02-17

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D239/50 ,  C07D417/12 ,  A61K45/06 ,  A61K31/505 ,  A61K31/506 ,  C07D409/12 ,  C07D401/12

CPC classification number: C07D239/50 ,  A61K31/505 ,  A61K31/506 ,  A61K45/06 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

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.

Abstract translation: 本发明包括具有式I的化合物和使用这些化合物的组合物和方法用于治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制在治疗上有用的条件。

公开(公告)号：US20140314785A1

公开(公告)日：2014-10-23

申请号：US14315073

申请日：2014-06-25

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Sambaiah Thota ,  David Carroll ,  Ankush Argade ,  Kin Tso ,  Arvinder Sran ,  Jeffrey Clough ,  Holger Keim ,  Somasekhar Bhamidipati ,  Venessa Taylor ,  Robin Cooper ,  Rajinder Singh ,  Brian Wong

IPC: C07D239/48 ,  A61K31/505 ,  C07F7/08 ,  A61K31/695 ,  A61K31/506 ,  A61K31/541 ,  C07D401/12 ,  C07D401/14 ,  A61K31/5377 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K45/06 ,  C07D403/12

CPC classification number: C07D413/12 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/3955 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D285/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07F7/0812 ,  C07F7/10

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.

Abstract translation: 本发明包括具有式I-V的化合物和使用这些化合物的组合物和方法，用于治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制可能是治疗上有用的条件。

公开(公告)号：US20140275055A1

公开(公告)日：2014-09-18

申请号：US14209997

申请日：2014-03-13

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

IPC: C07D471/04 ,  C07D498/04

CPC classification number: A61K31/506 ,  C07D471/04 ,  C07D498/04 ,  Y02A50/411

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.

Abstract translation: 本公开涉及可用作蛋白激酶C（PKC）的抑制剂的化合物，因此可用于治疗通过PKC的活性介导或维持的多种疾病和病症。 本公开还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：US08815848B2

公开(公告)日：2014-08-26

申请号：US13750632

申请日：2013-01-25

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: C07D239/48 ,  C07D285/22 ,  A61K31/506

CPC classification number: C07D413/12 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/3955 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D285/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07F7/0812 ,  C07F7/10

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.

Abstract translation: 本发明包括具有式I-V的化合物和使用这些化合物的组合物和方法，用于治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制可能是治疗上有用的条件。

公开(公告)号：US20140221352A1

公开(公告)日：2014-08-07

申请号：US14250329

申请日：2014-04-10

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/14 ,  C07D413/12 ,  C07D419/14 ,  C07D498/04 ,  A61K31/55 ,  A61K31/538 ,  C07D471/04 ,  A61K31/506 ,  A61K31/5415

CPC classification number: C07D413/12 ,  A61K31/155 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/551 ,  A61K31/635 ,  A61K31/675 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/14 ,  C07D419/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D498/04 ,  C07F9/65583

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：US20130210810A1

公开(公告)日：2013-08-15

申请号：US13718632

申请日：2012-12-18

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Hui Li ,  Haoran Zhao ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu ,  Carlos Valdez ,  Jing Zhang ,  Emily Stauffer ,  Matthew Duncton ,  Salvador Alvarez

IPC: A61K31/506 ,  A61K31/55 ,  A61K31/538 ,  A61K31/5377

CPC classification number: A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

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：US11993594B2

公开(公告)日：2024-05-28

申请号：US17953570

申请日：2022-09-27

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

CPC classification number: 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：US20220098181A1

公开(公告)日：2022-03-31

申请号：US17517428

申请日：2021-11-02

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 ,  C07D403/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D239/48 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  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

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：US11198689B2

公开(公告)日：2021-12-14

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: C07D403/04 ,  C07D413/12 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D239/48 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  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：US11174251B2

公开(公告)日：2021-11-16

申请号：US16656461

申请日：2019-10-17

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/12 ,  C07F9/6558 ,  C07B59/00

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.