公开(公告)号：US08518937B2

公开(公告)日：2013-08-27

申请号：US13610569

申请日：2012-09-11

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

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： C07D498/04 ,  C07D413/04 ,  C07D413/14 ,  A61K31/5415 ,  A61K31/538

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：US08299087B2

公开(公告)日：2012-10-30

申请号：US12902052

申请日：2010-10-11

申请人： Hui Li ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  John Ramphal ,  Kin Tso ,  Arvinder Sran ,  Holger Keim ,  Vadim Markovtsov ,  David Carroll ,  Sambaiah Thota ,  Ankush Argade ,  Jeffrey Wayne Clough ,  Rajinder Singh ,  Robin Cooper

发明人： Hui Li ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  John Ramphal ,  Kin Tso ,  Arvinder Sran ,  Holger Keim ,  Vadim Markovtsov ,  David Carroll ,  Sambaiah Thota ,  Ankush Argade ,  Jeffrey Wayne Clough ,  Rajinder Singh ,  Robin Cooper

IPC分类号： A61K31/505

CPC分类号： A61K31/506 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/5383 ,  C07D239/48 ,  C07D239/49 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D491/04 ,  C07D498/04

摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

公开(公告)号：US20080260754A1

公开(公告)日：2008-10-23

申请号：US12053438

申请日：2008-03-21

申请人： Hui Li ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  John Ramphal ,  Kin Tso ,  Avinder Sran ,  Holger Keim ,  Vadim Markovtsov ,  David Carroll ,  Sambaiah Thota ,  Ankush Argade ,  Jeffrey Wayne Clough ,  Rajinder Singh ,  Robin Cooper

发明人： Hui Li ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  John Ramphal ,  Kin Tso ,  Avinder Sran ,  Holger Keim ,  Vadim Markovtsov ,  David Carroll ,  Sambaiah Thota ,  Ankush Argade ,  Jeffrey Wayne Clough ,  Rajinder Singh ,  Robin Cooper

IPC分类号： A61K39/395 ,  C12N9/12 ,  C07D239/24 ,  A61K31/505 ,  C07D295/00 ,  A61K31/5377 ,  C07D498/02 ,  C12N5/00 ,  A61P37/00 ,  A61K31/5383 ,  C07D403/02 ,  A61K31/496 ,  C07D279/16 ,  A61K31/5415 ,  A61K38/13

CPC分类号： A61K31/506 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/5383 ,  C07D239/48 ,  C07D239/49 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D491/04 ,  C07D498/04

摘要： The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.

公开(公告)号：US06599902B2

公开(公告)日：2003-07-29

申请号：US10157007

申请日：2002-05-30

申请人： Jingrong Cui ,  John Ramphal ,  Congxin Liang ,  Connie Li Sun ,  Chung Chen Wei ,  Peng Cho Tang

发明人： Jingrong Cui ,  John Ramphal ,  Congxin Liang ,  Connie Li Sun ,  Chung Chen Wei ,  Peng Cho Tang

IPC分类号： A61K315377

CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

摘要： The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.

摘要翻译： 本发明涉及抑制激酶，特别是满足激酶的某些5-芳烷基磺酰基-3-（吡咯-2-基 - 亚甲基）-2-二氢吲哚酮衍生物。 还公开了包含这些化合物的药物组合物，使用包含这些化合物的药物组合物治疗由激酶介导的疾病的方法及其制备方法。

公开(公告)号：US08278299B2

公开(公告)日：2012-10-02

申请号：US12649073

申请日：2009-12-29

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

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： C07D413/14 ,  C07D417/14 ,  A61K31/5415 ,  A61K31/538

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

摘要： The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided 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： 本发明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。 还提供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：US20110130415A1

公开(公告)日：2011-06-02

申请号：US12958284

申请日：2010-12-01

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

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

IPC分类号： A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  A61P29/00 ,  A61P17/00 ,  A61P17/06 ,  A61P37/08 ,  A61P1/16 ,  A61P11/00 ,  A61P9/10 ,  A61P25/00 ,  A61P31/18 ,  A61P9/12 ,  A61P3/04 ,  A61P37/06 ,  C12N9/99 ,  C12Q1/48

CPC分类号： C07D405/14 ,  A61K31/41 ,  A61K31/506 ,  C07D401/14

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：US20100204208A1

公开(公告)日：2010-08-12

申请号：US12691607

申请日：2010-01-21

申请人： Rajinder Singh ,  Hui Li ,  Haoran Zhao ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu ,  Carlos Valdez ,  Jing Zhang ,  Emily Stauffer ,  Matthew Duncton ,  Salvador Alvarez

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： A61K31/55 ,  C07D401/14 ,  A61K31/496 ,  A61K31/506 ,  C07D413/14 ,  A61K31/5377 ,  C07D403/14 ,  A61P1/00 ,  A61P27/02 ,  A61P37/00 ,  A61P29/00 ,  A61P17/06 ,  A61P25/28 ,  C12Q1/48

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：US20100184755A1

公开(公告)日：2010-07-22

申请号：US12687054

申请日：2010-01-13

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

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

IPC分类号： A61K31/5383 ,  C07D498/04 ,  C07D498/10 ,  A61P37/00 ,  A61P29/00 ,  A61P27/02 ,  C12N9/99

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：US08993585B2

公开(公告)日：2015-03-31

申请号：US12175441

申请日：2008-07-17

申请人： Rajinder Singh ,  Hui Li ,  Haoran Zhao ,  Donald Payan ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu

发明人： Rajinder Singh ,  Hui Li ,  Haoran Zhao ,  Donald Payan ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu

IPC分类号： C07D401/12 ,  C07D239/48 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

CPC分类号： C07D401/12 ,  C07D239/48 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/04

摘要： The invention encompasses compounds having formula I or II and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.

摘要翻译： 本发明包括具有式I或II的化合物以及使用这些化合物治疗PKC和PKD的抑制在治疗上有用的条件的组合物和方法。

公开(公告)号：US08377924B2

公开(公告)日：2013-02-19

申请号：US12691607

申请日：2010-01-21

申请人： Rajinder Singh ,  Huí Li ,  Haoran Zhao ,  Rao Kolluri ,  Kin Tso ,  John Ramphal ,  Shihai Gu ,  Carlos Valdez ,  Jing Zhang ,  Emily Stauffer ,  Matthew Duncton ,  Salvador Alvarez

发明人： Rajinder Singh ,  Huí 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： A61K31/55 ,  A61K31/497 ,  A61K31/535 ,  A61K31/505 ,  C07D403/10 ,  C07D413/12 ,  C07D401/12

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.