公开(公告)号：US09566278B2

公开(公告)日：2017-02-14

申请号：US14849376

申请日：2015-09-09

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: C12N9/99 ,  C07D471/04 ,  C07D498/04 ,  A61K31/506

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：US09062068B2

公开(公告)日：2015-06-23

申请号：US14095893

申请日：2013-12-03

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: C07D455/02 ,  C07D498/04

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.

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。 本公开还涉及包括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：US20130142807A1

公开(公告)日：2013-06-06

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

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.

公开(公告)号：US20190300518A1

公开(公告)日：2019-10-03

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：US20180208613A1

公开(公告)日：2018-07-26

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

CPC classification number: C07F9/65586 ,  C07D405/04 ,  C07D405/14 ,  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：US20180208612A1

公开(公告)日：2018-07-26

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

CPC classification number: C07F9/65586 ,  C07D405/04 ,  C07D405/14 ,  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：US20170360786A1

公开(公告)日：2017-12-21

申请号：US15395606

申请日：2016-12-30

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: A61K31/506 ,  C07D498/04 ,  C07D471/04

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.

公开(公告)号：US09481654B2

公开(公告)日：2016-11-01

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

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.

公开(公告)号：US20160257681A1

公开(公告)日：2016-09-08

申请号：US15056535

申请日：2016-02-29

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 ,  A61K31/5383 ,  C07D519/00 ,  C12N9/12 ,  A61K31/5386 ,  A61K31/553 ,  A61K31/5377 ,  C12Q1/48 ,  A61K31/506 ,  A61K31/538

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：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。