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：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：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.

公开(公告)号：US09982000B2

公开(公告)日：2018-05-29

申请号：US15136508

申请日：2016-04-22

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

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：US20160102084A1

公开(公告)日：2016-04-14

申请号：US14974143

申请日：2015-12-18

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 ,  C07D417/12

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.

公开(公告)号：US09040543B2

公开(公告)日：2015-05-26

申请号：US14247878

申请日：2014-04-08

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/12 ,  C07D239/42 ,  C07D239/48 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K45/06 ,  C07D401/14 ,  C07D405/12 ,  C07D491/052

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/052 ,  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 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在治疗JAK途径调节或JAK激酶抑制在治疗上有用的情况下的组合物和方法。

公开(公告)号：US20140234333A1

公开(公告)日：2014-08-21

申请号：US14247878

申请日：2014-04-08

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D239/48 ,  A61K31/505 ,  C07D403/12 ,  A61K31/506 ,  C07D401/12 ,  C07D401/14 ,  C07D498/04 ,  A61K31/5383 ,  C07D471/04 ,  C07D405/12 ,  A61K31/5377 ,  C07D417/12 ,  A61K31/54 ,  C07D491/052 ,  A61K45/06

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D491/052 ,  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 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在治疗JAK途径调节或JAK激酶抑制在治疗上有用的情况下的组合物和方法。

公开(公告)号：US20130331374A1

公开(公告)日：2013-12-12

申请号：US13857028

申请日：2013-04-04

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 ,  C07D519/00

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.