公开(公告)号：US20230095835A1

公开(公告)日：2023-03-30

申请号：US17988062

申请日：2022-11-16

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Yan Chen ,  Rose Yen ,  Jiaxin Yu ,  Vanessa Taylor ,  Rajinder Singh

IPC: C07D403/12 ,  C07D239/48 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 μM to 3.7 μM; a TAK1 IC50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.

公开(公告)号：US11530194B2

公开(公告)日：2022-12-20

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：US11492349B2

公开(公告)日：2022-11-08

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：US10947216B2

公开(公告)日：2021-03-16

申请号：US16529995

申请日：2019-08-02

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/14 ,  C07D471/04 ,  C07D405/14 ,  C07D401/12 ,  C07D403/14 ,  C07D403/12 ,  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：US20190060310A1

公开(公告)日：2019-02-28

申请号：US15918929

申请日：2018-03-12

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

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：US20180265503A1

公开(公告)日：2018-09-20

申请号：US15988920

申请日：2018-05-24

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/12 ,  A61K31/155 ,  C07D487/04 ,  C07D451/02 ,  A61K31/635 ,  C07D413/14 ,  C07D498/04 ,  C07D487/08 ,  C07D413/04 ,  C07D403/12 ,  C07D401/14 ,  C07F9/6558 ,  A61K31/55 ,  A61K31/675 ,  C07D471/04 ,  C07D487/10 ,  A61K31/538 ,  A61K31/551 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  C07D491/08 ,  A61K45/06 ,  C07D419/14 ,  C07D471/08 ,  A61K31/5415

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：US09682976B2

公开(公告)日：2017-06-20

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

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：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：US09248132B2

公开(公告)日：2016-02-02

申请号：US14250329

申请日：2014-04-10

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  A61K31/5415 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D487/08 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D413/12 ,  C07D419/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  A61K31/538 ,  A61K31/55 ,  A61K31/675 ,  C07D413/14 ,  C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07F9/6558

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：US20140011770A1

公开(公告)日：2014-01-09

申请号：US14023158

申请日：2013-09-10

Applicant: Rigel Pharmaceuticals, Inc.

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

IPC: C07D413/12 ,  A61K45/06 ,  C07D403/12 ,  C07D471/08 ,  A61K31/5377 ,  C07F9/6558 ,  A61K31/675 ,  C07D487/08 ,  A61K31/551 ,  C07D471/04 ,  C07D413/14 ,  A61K31/541 ,  C07D491/08 ,  C07D487/04 ,  C07D487/10 ,  A61K31/54 ,  C07D419/14 ,  A61K31/55 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/538 ,  A61K31/506

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.

Abstract translation: 公开了式I的化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。