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1. 发明申请

WO2007098507A3 COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY 审中-公开
公开(公告)号：WO2007098507A3
公开(公告)日：2007-08-30
申请号：PCT/US2007/062753
申请日：2007-02-23
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , ARGADE, Ankush , TSO, Kin , THOTA, Sambaiah , CARROLL, David , SRAN, Arvinder , COOPER, Robin , SINGH, Rajinder , BHAMIDIPATI, Somasekhar , MASUDA, Esteban , TAYLOR, Vanessa
发明人： LI, Hui , ARGADE, Ankush , TSO, Kin , THOTA, Sambaiah , CARROLL, David , SRAN, Arvinder , COOPER, Robin , SINGH, Rajinder , BHAMIDIPATI, Somasekhar , MASUDA, Esteban , TAYLOR, Vanessa
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , A61K31/505 , A61P37/06
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.

2. 发明申请

WO2008079907A1 COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY 审中-公开
标题翻译：用于抑制JAK路径的组合物和方法
公开(公告)号：WO2008079907A1
公开(公告)日：2008-07-03
申请号：PCT/US2007/088241
申请日：2007-12-19
申请人： RIGEL PHARMACEUTICALS, INC. , ARGADE, Ankush , SRAN, Arvinder , CARROLL, David , CLOUGH, Jeffrey Wayne , TSO, Kin , BHAMIDIPATI, Somasekhar , THOTA, Sambaiah , SINGH, Rajinder , TAYLOR, Vanessa , LI, Hui , MASUDA, Esteban
发明人： ARGADE, Ankush , SRAN, Arvinder , CARROLL, David , CLOUGH, Jeffrey Wayne , TSO, Kin , BHAMIDIPATI, Somasekhar , THOTA, Sambaiah , SINGH, Rajinder , TAYLOR, Vanessa , LI, Hui , MASUDA, Esteban
IPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D413/12 , C07D417/12 , A61K31/505 , A61K31/506 , A61P37/06
CPC分类号： C07D239/48 , A61K31/505 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , 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.
摘要翻译：本发明包括具有式（I）的化合物，以及使用这些化合物治疗JAK途径的调节或JAK激酶，特别是JAK3的抑制在治疗上有用的条件的组合物和方法。

3. 发明申请

WO2007070872A1 KINASE INHIBITORS AND THEIR USES 审中-公开
标题翻译：激酶抑制剂及其用途
公开(公告)号：WO2007070872A1
公开(公告)日：2007-06-21
申请号：PCT/US2006/062162
申请日：2006-12-15
申请人： RIGEL PHARMACEUTICALS, INC. , DING, Pingyu , ARGADE, Ankush , GOFF, Dane , SINGH, Rajinder , MASUDA, Esteban , TAYLOR, Vanessa , HOLLAND, Sacha
发明人： DING, Pingyu , ARGADE, Ankush , GOFF, Dane , SINGH, Rajinder , MASUDA, Esteban , TAYLOR, Vanessa , HOLLAND, Sacha
IPC分类号： C07D239/95 , C07D473/16 , C07D487/04 , C07D495/04 , A61K31/52 , A61K31/505 , A61P35/00 , A61P29/00 , A61P25/00 , A61P7/12
CPC分类号： C07D519/00 , A61K31/517 , C07D239/94 , C07D239/95 , C07D471/04 , C07D473/16 , C07D487/04 , C07D495/04 , C07D495/12
摘要： The present disclosure provides compounds that inhibit protein kinases, such as JAK, AxI, 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.
摘要翻译：本公开提供了抑制蛋白激酶（例如JAK，AxI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。

4. 发明申请

WO2010083241A2 2,4-PYRIMIDINEDIAMINE COMPOUNDS FOR TREATMENT OF INFLAMMATORY DISORDERS 审中-公开
标题翻译：用于治疗炎性疾病的2,4-二吡啶二胺化合物
公开(公告)号：WO2010083241A2
公开(公告)日：2010-07-22
申请号：PCT/US2010/020932
申请日：2010-01-13
申请人： RIGEL PHARMACEUTICALS, INC. , GURURAJA, Tarikere , PAYAN, Donald , TSO, Kin , KINOSHITA, Taisei , DING, Rongxian , SINGH, Rajinder , YUNG, Stephanie , LI, Hui , MASUDA, Esteban
发明人： GURURAJA, Tarikere , PAYAN, Donald , TSO, Kin , KINOSHITA, Taisei , DING, Rongxian , SINGH, Rajinder , YUNG, Stephanie , LI, Hui , MASUDA, Esteban
IPC分类号： C07D239/32 , C07D239/30 , C07D403/12 , A61K31/495 , 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 are disclosed.
摘要翻译：公开了由式（I）表示的2,4-嘧啶二胺化合物，其制备方法和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。

5. 发明申请

WO2010083240A2 METHODS FOR TREATING INFLAMMATORY DISORDERS USING 2,4-PYRIMIDINEDIAMINE COMPOUNDS 审中-公开
标题翻译：使用2,4-二吡啶二胺化合物治疗炎症性疾病的方法
公开(公告)号：WO2010083240A2
公开(公告)日：2010-07-22
申请号：PCT/US2010/020931
申请日：2010-01-13
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , MASUDA, Esteban , YUNG, Stephanie , KINOSHITA, Taisei , DING, Rongxian , SINGH, Rajinder , GURURAJA, Tarikere , PAYAN, Donald , TSO, Kin
发明人： LI, Hui , MASUDA, Esteban , YUNG, Stephanie , KINOSHITA, Taisei , DING, Rongxian , SINGH, Rajinder , GURURAJA, Tarikere , PAYAN, Donald , TSO, Kin
IPC分类号： A61K31/506 , A61K31/505 , A61P29/00
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) are disclosed.
摘要翻译：公开了用式（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。

6. 发明申请

WO2008064274A1 PRODRUG SALTS OF 2, 4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES 审中-公开
标题翻译： 2，4-吡啶二胺化合物的制备方法及其用途
公开(公告)号：WO2008064274A1
公开(公告)日：2008-05-29
申请号：PCT/US2007/085313
申请日：2007-11-20
申请人： RIGEL PHARMACEUTICALS, INC. , BHAMIDIPATI, Somasekhar , SINGH, Rajinder , SUN, Thomas , MASUDA, Esteban
发明人： BHAMIDIPATI, Somasekhar , SINGH, Rajinder , SUN, Thomas , MASUDA, Esteban
IPC分类号： C07D498/04 , C07F9/6561 , A61K31/5383 , A61K31/675 , A61P37/00
CPC分类号： A61K31/675 , A61K9/0053 , C07D498/04 , C07F9/6561
摘要： The present disclosure provides prodrugs of biologically active 2,4- pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions. comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications. In particular the claims relate to salts of the phosphate ester of the following structure:
摘要翻译：本公开提供了生物活性的2,4-嘧啶二胺化合物，前药，组合物的盐和水合物的前药。包括用于合成前药的前药，中间体和方法以及在各种应用中使用前药的方法。特别地，权利要求涉及以下结构的磷酸酯的盐：

7. 发明申请

WO2007120980A3 2,4-PYRIMIDINEDIAMINE COMPOUNDS FOR TREATING OR PREVENTING AUTOIMMUNE DISEASES 审中-公开
公开(公告)号：WO2007120980A3
公开(公告)日：2007-10-25
申请号：PCT/US2007/062311
申请日：2007-02-16
申请人： RIGEL PHARMACEUTICALS, INC. , CLOUGH, Jeffrey Wayne , BHAMIDIPATI, Somasekhar , SINGH, Rajinder , MASUDA, Esteban , ZHAO, Haoran
发明人： CLOUGH, Jeffrey Wayne , BHAMIDIPATI, Somasekhar , SINGH, Rajinder , MASUDA, Esteban , ZHAO, Haoran
IPC分类号： C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , A61K31/506 , A61P29/00
摘要： 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.

8. 发明申请

WO2006078846A1 PRODRUGS OF 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES 审中-公开
标题翻译： 2,4-吡啶二胺化合物的制备及其用途
公开(公告)号：WO2006078846A1
公开(公告)日：2006-07-27
申请号：PCT/US2006/001945
申请日：2006-01-19
申请人： RIGEL PHARMACEUTICALS, INC. , SINGH, Rajinder , BHAMIDIPATI, Somasekhar , MASUDA, Esteban
发明人： SINGH, Rajinder , BHAMIDIPATI, Somasekhar , MASUDA, Esteban
IPC分类号： C07F9/6561 , C07D498/04 , A61K31/675 , A61K31/5383 , A61P37/00
CPC分类号： C07D498/04 , A61K31/5383 , A61K31/675 , C07F9/65583 , C07F9/6561 , C07F9/65742
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2012012619A1 PROTEIN KINASE C INHIBITORS AND USES THEREOF 审中-公开
标题翻译：蛋白激酶C抑制剂及其用途
公开(公告)号：WO2012012619A1
公开(公告)日：2012-01-26
申请号：PCT/US2011/044824
申请日：2011-07-21
申请人： RIGEL PHARMACEUTICALS, INC. , HOLLAND, Sacha , KOLLURI, Rao , ALVAREZ, Salvador , DUNCTON, Matthew , SINGH, Rajinder , ZHANG, Jing , MASUDA, Esteban
发明人： HOLLAND, Sacha , KOLLURI, Rao , ALVAREZ, Salvador , DUNCTON, Matthew , SINGH, Rajinder , ZHANG, Jing , MASUDA, Esteban
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14 , A61K31/506 , C12N9/12 , C12Y207/11013
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。

10. 发明申请

WO2012142160A1 METHODS FOR INHIBITING ALLOGRAFT REJECTION 审中-公开
标题翻译：抑制耐药性的方法
公开(公告)号：WO2012142160A1
公开(公告)日：2012-10-18
申请号：PCT/US2012/033123
申请日：2012-04-11
申请人： RIGEL PHARMACEUTICALS, INC. , TAYLOR, Vanessa , MASUDA, Esteban
发明人： TAYLOR, Vanessa , MASUDA, Esteban
IPC分类号： A61K31/397 , A61P37/06
CPC分类号： A61K31/506 , A61K31/436 , A61K31/4545 , A61K38/13 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are methods for treating or inhibiting allograft rejection in a transplant recipient. In some embodiments, the methods include administering to the transplant recipient a first amount of a JAKl/3 inhibitor comprising 5-(2-(4- fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4- ylamino)benzo[ d ]oxazol-2(3H)-one (Compound I) or a prodrug thereof and administering to the transplant recipient a second amount of a non-JAK1/3 inhibitor immunosuppressant, wherein the combined effect of the first amount and the second amount is greater than the effect of the first amount or the second amount individually, wherein the JAK1l/3 inhibitor acts in combination with the non-JAK1/3 inhibitor immunosuppressant to inhibit or treat allograft rejection. In some embodiments at least one of the first amount or the second amount is individually a suboptimal dose for inhibiting or treating allograft rejection. In some examples, the combined effect of the first amount and the second amount to inhibit or treat allograft rejection in the transplant recipient is synergistic.
摘要翻译：本文公开了用于在移植受体中治疗或抑制同种异体移植排斥的方法。在一些实施方案中，所述方法包括向移植受体施用第一量的JAK1 / 3抑制剂，其包含5-（2-（4-氟-3-甲氧基-5-甲基苯基氨基）-5-甲基嘧啶-4-基氨基）苯并 [d]恶唑-2（3H） - 酮（化合物I）或其前药，向移植受体施用第二量的非JAK1 / 3抑制剂免疫抑制剂，其中第一量和第二量的组合效应大于单独的第一量或第二量的作用，其中JAK1 / 3抑制剂与非JAK1 / 3抑制剂免疫抑制剂联合用于抑制或治疗同种异体移植排斥。在一些实施方案中，第一量或第二量中的至少一种量单独为抑制或治疗同种异体移植物排斥反应的次优剂量。在一些实例中，第一量和第二量在移植受体中抑制或治疗同种异体移植物排斥的组合作用是协同的。

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