公开(公告)号：US20220098175A1

公开(公告)日：2022-03-31

申请号：US17500681

申请日：2021-10-13

Applicant: Rigel Pharmaceuticals, Inc.

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

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

公开(公告)号：US20210078969A1

公开(公告)日：2021-03-18

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：US20200339538A1

公开(公告)日：2020-10-29

申请号：US16838699

申请日：2020-04-02

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/14 ,  C07D401/04

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may 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：US20180258070A1

公开(公告)日：2018-09-13

申请号：US15811170

申请日：2017-11-13

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D401/14 ,  C07D401/04

CPC classification number: C07D401/14 ,  C07D401/04

Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may 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：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：US09475781B2

公开(公告)日：2016-10-25

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

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：US09181222B2

公开(公告)日：2015-11-10

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 ,  A61K31/506 ,  C12N9/12

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：US09108990B2

公开(公告)日：2015-08-18

申请号：US14227308

申请日：2014-03-27

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07F5/02

CPC classification number: C07F5/025 ,  Y02P20/55

Abstract: This disclosure concerns a protected cyclopropylboronic acid comprising a substituted cyclopropyl group and a boronic ester group having a protecting group. The protecting group is an N-methyliminodiacetic acid (MIDA) group or MIDA-based group.

Abstract translation: 本公开涉及包含取代的环丙基的保护的环丙基硼酸和具有保护基的硼酸酯基。 保护基是N-甲基亚氨基二乙酸（MIDA）基团或基于MIDA的组。

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.

公开(公告)号：US11174246B2

公开(公告)日：2021-11-16

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: C07D403/10 ,  A61K31/4184 ,  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.