公开(公告)号：US20100130486A1

公开(公告)日：2010-05-27

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： A61K31/5383 ,  C07D401/14 ,  C07D403/14 ,  C07D265/38 ,  C07D413/14 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61P35/00

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：US20180111923A1

公开(公告)日：2018-04-26

申请号：US15793770

申请日：2017-10-25

申请人： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

发明人： Hui Li ,  Thilo Heckrodt ,  Yan Chen ,  Ryan Kelley ,  Darren McMurtrie ,  Kin Tso ,  Vanessa Taylor ,  Rajinder Singh ,  Rose Yen ,  Jack Maung

IPC分类号： C07D413/14

CPC分类号： C07D413/14 ,  A61P29/00

摘要： Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, such as oxazole compounds, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

公开(公告)号：US20180111917A1

公开(公告)日：2018-04-26

申请号：US15793743

申请日：2017-10-25

申请人： Kin Tso ,  Hui Li ,  Yan Chen ,  Rose Yen ,  Vanessa Taylor ,  Thilo Heckrodt ,  Rajinder Singh ,  Simon Shaw

发明人： Kin Tso ,  Hui Li ,  Yan Chen ,  Rose Yen ,  Vanessa Taylor ,  Thilo Heckrodt ,  Rajinder Singh ,  Simon Shaw

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D403/14 ,  C07D403/12

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： Disclosed embodiments concern novel interleukin receptor associated kinases (IRAK) inhibitors and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.

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：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：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.

公开(公告)号：US08394951B2

公开(公告)日：2013-03-12

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： C07D345/00 ,  C07D517/00

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：US08334297B2

公开(公告)日：2012-12-18

申请号：US12687053

申请日：2010-01-13

申请人： Hui Li ,  Esteban Masuda ,  Stephanie Yung ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso

发明人： Hui Li ,  Esteban Masuda ,  Stephanie Yung ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso

IPC分类号： A01N43/54 ,  A61K31/505

CPC分类号： C07D451/04

摘要： 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same:

摘要翻译： 由式（I）表示的2,4-嘧啶二胺化合物，其制备方法及其用于治疗炎性病症和抑制IL-23产生和/或刺激IL-10产生的方法：

公开(公告)号：US08575165B2

公开(公告)日：2013-11-05

申请号：US12687056

申请日：2010-01-13

申请人： Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Stephanie Yung ,  Hui Li ,  Esteban Masuda

发明人： Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Stephanie Yung ,  Hui Li ,  Esteban Masuda

IPC分类号： A61K31/50 ,  A61K31/505 ,  A61K31/44 ,  A61K31/40 ,  C07D487/04 ,  A01N43/40

CPC分类号： A61K31/506

摘要： Methods for treating an inflammatory disorder and for inhibiting the production of IL-23 using 2,4-pyrimidinediamine compounds represented by formula (I):

摘要翻译： 用式（I）表示的2,4-嘧啶二胺化合物治疗炎性病症和抑制IL-23产生的方法：

公开(公告)号：US20100179164A1

公开(公告)日：2010-07-15

申请号：US12687053

申请日：2010-01-13

申请人： Hui Li ,  Esteban Masuda ,  Stephanie Yung ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso

发明人： Hui Li ,  Esteban Masuda ,  Stephanie Yung ,  Taisei Kinoshita ,  Rongxian Ding ,  Rajinder Singh ,  Tarikere Gururaja ,  Donald G. Payan ,  Kin Tso

IPC分类号： A61K31/497 ,  C07D451/02 ,  A61K31/506 ,  A61P29/00

CPC分类号： C07D451/04

摘要： 2,4-Pyrimidinediamine compounds represented by formula (I), methods for preparing the same and methods for treating an inflammatory disorder and for inhibiting the production of IL-23 and/or stimulating the production of IL-10 using the same:

摘要翻译： 由式（I）表示的2,4-嘧啶二胺化合物，其制备方法及其用于治疗炎性病症和抑制IL-23产生和/或刺激IL-10产生的方法：