公开(公告)号：US20200155531A1

公开(公告)日：2020-05-21

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

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：US10647697B2

公开(公告)日：2020-05-12

申请号：US15811170

申请日：2017-11-13

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：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：US20180071271A1

公开(公告)日：2018-03-15

申请号：US15711754

申请日：2017-09-21

Applicant: Rigel Pharmaceuticals, Inc.

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

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

CPC classification number: A61K31/4439 ,  A61K31/41 ,  C07D257/04 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  Y02A50/411 ,  Y02A50/414

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：US09701647B2

公开(公告)日：2017-07-11

申请号：US15233676

申请日：2016-08-10

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: C07D257/04 ,  A61K31/41 ,  C07D403/06 ,  C07D403/14 ,  C07D401/12 ,  C07D403/12 ,  C07D401/10 ,  C07D413/10 ,  C07D501/16 ,  C07D401/14 ,  C07J43/00 ,  C07D401/04 ,  C07D487/04 ,  C07D471/04 ,  A61K31/4184 ,  A61K31/4709 ,  A61K31/4245 ,  A61K31/546 ,  A61K31/55 ,  A61K31/496 ,  A61K31/58 ,  A61K31/506 ,  A61K31/519

CPC classification number: C07D257/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/55 ,  A61K31/58 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06 ,  C07D501/16 ,  C07D501/46 ,  C07J9/005 ,  C07J43/003

Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

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：US20170152246A1

公开(公告)日：2017-06-01

申请号：US15261294

申请日：2016-09-09

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Rajinder Singh ,  Kin Tso ,  Jing Zhang ,  Matthew Duncton ,  Salvador Alvarez ,  Rao Kolluri ,  John Ramphal ,  Sacha Holland

IPC: C07D405/14 ,  C07D401/14

CPC classification number: C07D405/14 ,  A61K31/41 ,  A61K31/506 ,  C07D401/14

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：US20160213648A1

公开(公告)日：2016-07-28

申请号：US15005773

申请日：2016-01-25

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Matthew Duncton ,  Rajinder Singh

IPC: A61K31/4155 ,  C07D471/04 ,  A61K31/519 ,  A61K31/517 ,  A61K31/5383 ,  C07D401/12 ,  A61K31/4725 ,  C07D403/10 ,  C07D403/12 ,  C07D498/06

CPC classification number: C07D257/04 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/55 ,  A61K31/58 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/06 ,  C07D501/16 ,  C07D501/46 ,  C07J9/005 ,  C07J43/003

Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Abstract translation: 本公开提供了包含活性剂的羧基的四唑酮衍生物的化合物。 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，以及制备这些化合物的方法。

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。