公开(公告)号：US20120015937A1

公开(公告)日：2012-01-19

申请号：US13242994

申请日：2011-09-23

Applicant: Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

Inventor： Pingyu Ding ,  Ankush Argade ,  Dane Goff ,  Rajinder Singh ,  Esteban Masuda ,  Vanessa Taylor ,  Sacha Holland

IPC: A61K31/52 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/538 ,  C07D409/14 ,  A61K31/551 ,  A61P35/02 ,  A61P37/08 ,  A61P11/06 ,  A61P37/00 ,  A61P37/06 ,  A61P29/00 ,  A61P25/00 ,  A61P17/06 ,  A61P17/00 ,  A61P9/10 ,  A61P11/08 ,  A61P9/12 ,  C12N9/99 ,  C07D473/34

CPC classification number: C07D519/00 ,  A61K31/517 ,  C07D239/94 ,  C07D239/95 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D495/04 ,  C07D495/12

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Abstract translation: 本公开提供了抑制蛋白激酶（例如JAK，Ax1或Syk激酶）的化合物，包含该化合物的组合物和使用该化合物抑制蛋白激酶并治疗和/或预防与不适当激酶活性相关疾病的方法。

公开(公告)号：US20110319613A1

公开(公告)日：2011-12-29

申请号：US13174091

申请日：2011-06-30

Applicant: Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

Inventor： Rajinder Singh ,  Somasekhar Bhamidipati ,  Esteban Masuda ,  Thomas Sun ,  Valentino J. Stella

IPC: C07F9/6561 ,  C07D498/04

CPC classification number: C07D498/04 ,  A61K31/5383 ,  A61K31/675 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65742

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

Abstract translation: 本公开提供了生物活性2,4-嘧啶二胺化合物的前药，包含前体药物的组合物，用于合成前药的中间体和方法以及在各种应用中使用前药的方法。

公开(公告)号：US20100179165A1

公开(公告)日：2010-07-15

申请号：US12687056

申请日：2010-01-13

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

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

IPC: A61K31/506 ,  A61P29/00

CPC classification number: A61K31/506

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

Abstract translation: 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：US20100152172A1

公开(公告)日：2010-06-17

申请号：US12642406

申请日：2009-12-18

Applicant: Jeffrey W. Clough ,  Somasekhar Bhamidipati ,  Rajinder Singh ,  Esteban Masuda ,  Haoran Zhao

Inventor： Jeffrey W. Clough ,  Somasekhar Bhamidipati ,  Rajinder Singh ,  Esteban Masuda ,  Haoran Zhao

IPC: A61K31/5415 ,  A61K31/538 ,  A61K31/506 ,  A61P29/00 ,  A61P37/00 ,  C12N5/00

CPC classification number: C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D498/04

Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.

Abstract translation: 本发明提供式I的3-羟基苯基-2,4-嘧啶二胺化合物，以及用于治疗多种自身免疫疾病的相关组合物和方法。

公开(公告)号：US07659280B2

公开(公告)日：2010-02-09

申请号：US11676096

申请日：2007-02-16

Applicant: Jeffrey Wayne Clough ,  Somasekhar Bhamidipati ,  Rajinder Singh ,  Esteban Masuda ,  Haoran Zhao

Inventor： Jeffrey Wayne Clough ,  Somasekhar Bhamidipati ,  Rajinder Singh ,  Esteban Masuda ,  Haoran Zhao

IPC: C07D403/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61K31/535 ,  A61K31/541 ,  A61P19/02

CPC classification number: C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D498/04

Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.

Abstract translation: 本发明提供式I的3-羟基苯基-2,4-嘧啶二胺化合物，以及用于治疗多种自身免疫疾病的相关组合物和方法。

公开(公告)号：US07521192B2

公开(公告)日：2009-04-21

申请号：US09971228

申请日：2001-10-03

Applicant: X. Charlene Liao ,  Esteban Masuda ,  Peter Chu ,  Jorge Pardo ,  Congfen Li ,  Haoran Zhao ,  Ying-Ping Jiang ,  Collin Spencer

Inventor： X. Charlene Liao ,  Esteban Masuda ,  Peter Chu ,  Jorge Pardo ,  Congfen Li ,  Haoran Zhao ,  Ying-Ping Jiang ,  Collin Spencer

IPC: G01N33/53

CPC classification number: C07K14/705 ,  G01N33/56972 ,  G01N2333/4703 ,  G01N2500/10

Abstract: The present invention relates to regulation of lymphocyte activation and migration. More particularly, the present invention is directed to nucleic acids encoding EDG family GPCR proteins, e.g., EDG-1, 2, 3, 4, 5, 6, 7, or 8, which are involved in modulation of lymphocyte activation and migration. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, sphingolipid analogs, and ribozymes, that modulate lymphocyte activation or migration via modulation of EDG GPCRs and EDG related signal transduction; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression, and lymphocyte migration.

公开(公告)号：US07422867B2

公开(公告)日：2008-09-09

申请号：US11784176

申请日：2007-04-04

Applicant: Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

Inventor： Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

IPC: C12Q1/37

CPC classification number: C07K7/08 ,  A61K38/1709 ,  C07K14/5406 ,  G01N33/6869 ,  G01N2333/5406 ,  G01N2500/00 ,  Y10S435/975

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a CLLD8 protein as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

公开(公告)号：US07378251B2

公开(公告)日：2008-05-27

申请号：US10197962

申请日：2002-07-16

Applicant: Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

Inventor： Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

IPC: G01N33/53

CPC classification number: G01N33/6854 ,  A61K38/00

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a thioredoxin-like 32 kDa protein (TXNL) as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供了能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用硫氧还蛋白样32kDa蛋白（TXNL）作为替代分析物的化合物的方法和试剂盒 以及在各种体外和体外上下文中使用化合物的方法。

公开(公告)号：US20070244033A1

公开(公告)日：2007-10-18

申请号：US11608706

申请日：2006-12-08

Applicant: Esteban MASUDA ,  Todd Kinsella ,  Justin Warner ,  Taisei Kinoshita ,  Mark Bennett ,  David Anderson

Inventor： Esteban MASUDA ,  Todd Kinsella ,  Justin Warner ,  Taisei Kinoshita ,  Mark Bennett ,  David Anderson

IPC: A61K38/00 ,  C07K14/00 ,  C12N5/06 ,  G01N33/53

CPC classification number: C07K14/4703 ,  A61K38/1709 ,  G01N33/6854 ,  G01N2333/5406

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a c-Myc protein as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供了能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用c-Myc蛋白作为替代分析物的这些化合物的方法和试剂盒以及使用 化合物在各种体外，体外和体外上下文中。

公开(公告)号：US07241581B2

公开(公告)日：2007-07-10

申请号：US10222729

申请日：2002-08-16

Applicant: Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

Inventor： Esteban Masuda ,  Todd M. Kinsella ,  Justin E. Warner ,  Taisei Kinoshita ,  Mark K. Bennett ,  David C. Anderson

IPC: G01N33/566 ,  G01N33/53 ,  G01N33/542 ,  A61K38/20 ,  A61K45/00

CPC classification number: C07K14/4703 ,  A61K38/1709 ,  G01N33/6854 ,  G01N2333/5406

Abstract: The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a c-Myc protein as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Abstract translation: 本发明提供了能够调节IL-4受体介导的IgE产生的化合物以及与其相关的IL-4诱导的过程，用于鉴定利用c-Myc蛋白作为替代分析物的这些化合物的方法和试剂盒以及使用 化合物在各种体外，体外和体外上下文中。