公开(公告)号：US09732070B2

公开(公告)日：2017-08-15

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: C07D401/14 ,  A61K31/506 ,  C07D405/14 ,  A61K31/41

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：US09725419B2

公开(公告)日：2017-08-08

申请号：US13757262

申请日：2013-02-01

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Hui Li ,  Ankush Argade ,  Rajinder Singh ,  Sambaiah Thota ,  David Carroll ,  Kin Tso ,  Vanessa Taylor ,  John McLaughlin ,  Vadim Markovtsov

IPC: C07D403/12 ,  A61K31/505 ,  C07D239/48 ,  A61K31/506 ,  C07D205/12 ,  C07D239/42 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D487/08 ,  C07D295/155 ,  C07D417/12 ,  C07D471/08

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  C07D205/12 ,  C07D239/42 ,  C07D295/155 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  C07D487/08

Abstract: The present disclosure provides 2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.

公开(公告)号：US09321763B2

公开(公告)日：2016-04-26

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 ,  Ryan Kelley

IPC: A61K31/506 ,  A61K31/505 ,  A61K31/535 ,  A61K31/553 ,  C07D471/04 ,  C07D519/00 ,  C07D295/00

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：US20160058760A1

公开(公告)日：2016-03-03

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: 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.

公开(公告)号：US20150306100A1

公开(公告)日：2015-10-29

申请号：US14712748

申请日：2015-05-14

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: A61K31/506 ,  A61K31/5383 ,  A61K31/5377 ,  A61K31/538

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：US09169249B2

公开(公告)日：2015-10-27

申请号：US14209997

申请日：2014-03-13

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 ,  C07D498/04

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：US09095593B2

公开(公告)日：2015-08-04

申请号：US13760666

申请日：2013-02-06

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Haoran Zhao ,  Rao Kolluri ,  Carlos Valdez ,  Kin Tso ,  Rajinder Singh ,  John Ramphal

IPC: C07D345/00 ,  C07D517/00 ,  A61K31/5383 ,  C07D498/04 ,  C07D498/14

CPC classification number: C07D498/04 ,  A61K31/5383 ,  C07D498/14

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：US20130143875A1

公开(公告)日：2013-06-06

申请号：US13760666

申请日：2013-02-06

Applicant: RIGEL PHARMACEUTICALS, INC.

Inventor： Haoran Zhao ,  Rao Kolluri ,  Carlos Valdez ,  Kin Tso ,  Rajinder Singh ,  John Ramphal

IPC: A61K31/5383

CPC classification number: C07D498/04 ,  A61K31/5383 ,  C07D498/14

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.