公开(公告)号：US20130309228A1

公开(公告)日：2013-11-21

申请号：US13948342

申请日：2013-07-23

申请人： Rigel Pharmaceuticals, Inc.

发明人： Rajinder Singh ,  Andy Atuegbu ,  John Ramphal ,  Hui Li ,  Marina Gelman ,  Jeffrey Clough ,  Carlos Valdez ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Darren McMurtrie

IPC分类号： A61K31/5383 ,  A61K45/06

CPC分类号： A61K31/5383 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/08 ,  C07D498/04

摘要： Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

公开(公告)号：US09095593B2

公开(公告)日：2015-08-04

申请号：US13760666

申请日：2013-02-06

申请人： Rigel Pharmaceuticals, Inc.

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

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

CPC分类号： C07D498/04 ,  A61K31/5383 ,  C07D498/14

摘要： 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

申请人： RIGEL PHARMACEUTICALS, INC.

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

IPC分类号： A61K31/5383

CPC分类号： C07D498/04 ,  A61K31/5383 ,  C07D498/14

摘要： 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：US09453028B2

公开(公告)日：2016-09-27

申请号：US14754415

申请日：2015-06-29

申请人： Rigel Pharmaceuticals, Inc.

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

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

CPC分类号： C07D498/04 ,  A61K31/5383 ,  C07D498/14

摘要： 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：US20150376203A1

公开(公告)日：2015-12-31

申请号：US14754415

申请日：2015-06-29

申请人： Rigel Pharmaceuticals, Inc.

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

IPC分类号： C07D498/04

CPC分类号： C07D498/04 ,  A61K31/5383 ,  C07D498/14

摘要： 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.

摘要翻译： 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：US09149475B2

公开(公告)日：2015-10-06

申请号：US13718632

申请日：2012-12-18

申请人： Rigel Pharmaceuticals, Inc.

发明人： 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分类号： A61K31/506 ,  A61K31/55 ,  A61K31/538 ,  A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

CPC分类号： A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

摘要： 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：US09040527B2

公开(公告)日：2015-05-26

申请号：US13948342

申请日：2013-07-23

申请人： Rigel Pharmaceuticals, Inc.

发明人： Rajinder Singh ,  Andy Atuegbu ,  John Ramphal ,  Hui Li ,  Marina Gelman ,  Jeffrey Clough ,  Carlos Valdez ,  Somasekhar Bhamidipati ,  Sambaiah Thota ,  Darren McMurtrie

IPC分类号： C07D413/04 ,  C07D498/04 ,  A61K31/5415 ,  A61K31/538 ,  C07D413/14 ,  A61K31/5383 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  A61K45/06

CPC分类号： A61K31/5383 ,  A61K45/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D487/08 ,  C07D498/04

摘要： Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

摘要翻译： 公开的实施方案提供了可用于抑制激酶活性的嘧啶二胺化合物，包括polo样激酶1（PLK1）的活性。 还公开了包含这些化合物的药物组合物和治疗与激酶活性相关的疾病的方法，特别是增强的PLK1催化活性，例如与异常细胞增殖相关的疾病，包括肿瘤性疾病。

公开(公告)号：US20130210810A1

公开(公告)日：2013-08-15

申请号：US13718632

申请日：2012-12-18

申请人： Rigel Pharmaceuticals, Inc.

发明人： 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分类号： A61K31/506 ,  A61K31/55 ,  A61K31/538 ,  A61K31/5377

CPC分类号： A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

摘要： 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.