公开(公告)号：US20140329842A1

公开(公告)日：2014-11-06

申请号：US14200951

申请日：2014-03-07

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Sacha Holland ,  Rao Kolluri ,  Salvador Alvarez ,  Matthew Duncton ,  Rajinder Singh ,  Jing Zhang ,  Esteban Masuda

IPC: C07D401/14

CPC classification number: C07D401/14 ,  A61K31/506 ,  C12N9/12 ,  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：US10792282B2

公开(公告)日：2020-10-06

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 ,  C07D471/04 ,  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 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：US20200216412A1

公开(公告)日：2020-07-09

申请号：US16723881

申请日：2019-12-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/04 ,  C07D257/04 ,  C07D255/02 ,  C07D249/12

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate 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：US20180258063A1

公开(公告)日：2018-09-13

申请号：US15811088

申请日：2017-11-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/04 ,  C07D257/04 ,  C07D255/02

CPC classification number: C07D401/04 ,  C07D249/12 ,  C07D255/02 ,  C07D257/04

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate 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：US20160039773A1

公开(公告)日：2016-02-11

申请号：US14815589

申请日：2015-07-31

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Matthew Duncton ,  Somasekhar Bhamidipati ,  Jiaxin Yu ,  Ihab Darwish ,  Rajinder Singh

IPC: C07D257/04 ,  C07D401/04 ,  C07D405/04

CPC classification number: A61K31/4439 ,  A61K31/41 ,  C07D257/04 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06

Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate 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: 本公开的方面包括可用于治疗多种自身免疫性和炎性疾病和病症的化合物。 本公开的实施方案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：US09149475B2

公开(公告)日：2015-10-06

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 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

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：US20140163022A1

公开(公告)日：2014-06-12

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: C07D471/04 ,  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：US11279686B2

公开(公告)日：2022-03-22

申请号：US17075152

申请日：2020-10-20

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/04 ,  C07D249/12 ,  C07D255/02 ,  C07D257/04

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate 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：US11129819B2

公开(公告)日：2021-09-28

申请号：US16600873

申请日：2019-10-14

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Somasekhar Bhamidipati ,  Jiaxin Yu ,  Ihab Darwish ,  Rajinder Singh

IPC: A61K31/41 ,  A61K31/4439 ,  C07D403/12 ,  C07D405/06 ,  C07D257/04 ,  C07D401/04 ,  C07D405/04

Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate 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：US20180051006A1

公开(公告)日：2018-02-22

申请号：US15677809

申请日：2017-08-15

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Simon Shaw ,  Xiang Xu ,  Sarkiz Issakani ,  Rajinder Singh ,  Yasumichi Hitoshi ,  Matthew Duncton ,  Nan Lin

IPC: C07D403/04 ,  C07D235/26 ,  C07D403/14 ,  C07D403/12

CPC classification number: C07D403/04 ,  C07D235/26 ,  C07D403/12 ,  C07D403/14

Abstract: Disclosed are benzimidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.