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1. 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.

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

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：

4. 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。

5. 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.

6. 发明申请

WO2002081730A2 TRAC1: MODULATORS OF LYMPHOCYTE ACTIVATION 审中-公开
标题翻译： TRAC1：淋巴细胞激活的调节剂
公开(公告)号：WO2002081730A2
公开(公告)日：2002-10-17
申请号：PCT/US2002/011205
申请日：2002-04-08
申请人： RIGEL PHARMACEUTICALS, INC. , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , ZHAO, Haoran
发明人： CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , ZHAO, Haoran
IPC分类号： C12Q
CPC分类号： G01N33/573 , C07K14/4702 , G01N33/505 , G01N2333/9015 , G01N2500/04
摘要： The present invention relates to regulation of lymphocyte activation. More particularly, the present invention is directed to nucleic acids encoding TRAC1, which is involved in modulation of lymphocyte activation. The invention further relates to methods for identifying and using agents, including small organic molecules, peptides, circular peptides, antibodies, lipids, antisense nucleic acids, RNAi, and ribozymes, that modulate lymphocyte activation via modulation of TRAC1; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression.
摘要翻译：本发明涉及淋巴细胞活化的调节。更具体地，本发明涉及编码TRAC1的核酸，其涉及淋巴细胞活化的调节。本发明还涉及用于鉴定和使用通过调节TRAC1来调节淋巴细胞活化的试剂，包括小有机分子，肽，环状肽，抗体，脂质，反义核酸，RNAi和核酶的试剂; 以及在与淋巴细胞活化和抑制相关的诊断和治疗中使用表达谱和组合物。

7. 发明申请

WO2003029280A3 GRB7: NOVEL REGULATOR OF LYMPHOCYTE SIGNALING 审中-公开
公开(公告)号：WO2003029280A3
公开(公告)日：2003-04-10
申请号：PCT/US2002/031622
申请日：2002-10-02
申请人： RIGEL PHARMACEUTICALS, INC. , PARDO, Jorge , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , ZHAO, Haoran
发明人： PARDO, Jorge , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , ZHAO, Haoran
IPC分类号： C12Q1/68
摘要： The present invention relates to regulation of T lymphocyte activation. More particularly, the present invention is directed to nucleic acids encoding GRB7, which is involved in modulation of T lymphocyte activation and TCR signaling. The invention further relates to methods for identifying and using agents, including small organic molecules, peptides, circular peptides, antibodies, lipids, antisense nucleic acids, RNAi, and ribozymes, that modulate lymphocyte activation and TCR signaling via modulation of GRB7; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression.

8. 发明申请

WO2003029277A2 MODULATORS OF LYMPHOCYTE ACTIVATION AND MIGRATION 审中-公开
标题翻译：淋巴细胞活化和迁移的调节剂
公开(公告)号：WO2003029277A2
公开(公告)日：2003-04-10
申请号：PCT/US2002/031618
申请日：2002-10-02
申请人： RIGEL PHARMACEUTICALS, INC. , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , ZHAO, Haoran
发明人： CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , ZHAO, Haoran
IPC分类号： C07K
CPC分类号： G01N33/505 , G01N2500/00
摘要： The present invention relates to regulation of lymphocyte activation and migration. More particularly, the present invention is directed to nucleic acids encoding the nucleic acids and proteins listed in Figure 7, which are involved in modulation of lymphocyte activation and migration, e.g., A-raf-1, Lck, Zap70, Syk, PLCγ1, PAG, SHP/PTP1C, CSK, nucleolin, SLAP, PAK2, TRAC1, TCPTP/PTPN2, EDG1, IL10-Rα, integrinα2, Enolase 1a, PRSM1, CLN2, P2X5b, 6PFKL, DUSP1, KIAA0251, GG2-1, GRB7, SH2-B, STAT1, TCF19, HFP101S, RERE, SudD, Ku70, SCAMP2, Fibulin-5, KIAA1228, Est from clone 2108068, vimentin, filamin A α, centractin α, moesin, TIMP3, and RNH. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, siRNA, and ribozymes, that modulate lymphocyte activation or migration; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression, and lymphocyte migration.
摘要翻译：本发明涉及淋巴细胞活化和迁移的调控。更具体地，本发明涉及编码图7所列核酸和蛋白质的核酸，其涉及淋巴细胞活化和迁移的调节，例如A-raf-1，Lck，Zap70，Syk，PLCγ1 ，PAG，SHP / PTP1C，CSK，核仁素，SLAP，PAK2，TRAC1，TCPTP / PTPN2，EDG1，IL10-Rα，整合素α2，烯醇化酶1a，PRSM1，CLN2，P2X5b，6PFKL，DUSP1，KIAA0251，GG2-1 ，GRB7，SH2-B，STAT1，TCF19，HFP101S，RERE，SudD，Ku70，SCAMP2，Fibulin-5，KIAA1228，来自克隆2108068的Est，波形蛋白，丝氨酸Aα，中心素α，moesin，TIMP3和RNH。本发明还涉及用于鉴定和使用调节淋巴细胞活化或迁移的试剂（包括小有机分子，抗体，肽，环肽，核酸，反义核酸，siRNA和核酶）的方法; 以及在与淋巴细胞活化和抑制以及淋巴细胞迁移相关的诊断和治疗中使用表达谱和组合物。

9. 发明申请

WO2002085290A2 EDG : MODULATORS OF LYMPHOCYTE ACTIVATION AND MIGRATION 审中-公开
标题翻译： EDG：淋巴细胞活化和迁移的调节剂
公开(公告)号：WO2002085290A2
公开(公告)日：2002-10-31
申请号：PCT/US2002/012342
申请日：2002-04-18
申请人： RIGEL PHARMACEUTICALS, INC. , CHU, Peter , JIANG, Yingping , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , SPENCER, Colin , ZHAO, Haoran
发明人： CHU, Peter , JIANG, Yingping , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , PARDO, Jorge , SPENCER, Colin , ZHAO, Haoran
IPC分类号： A61K
CPC分类号： C07K14/705 , G01N33/56972 , G01N2333/4703 , G01N2500/10
摘要： The present invention relates to regulation of lymphocyte activa tion 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.
摘要翻译：本发明涉及淋巴细胞活化和迁移的调节。更具体地，本发明涉及编码EDG家族GPCR蛋白质的核酸，例如涉及淋巴细胞活化和迁移调节的EDG-1,2,3,4,5,6,7或8。本发明还涉及用于鉴定和使用通过调节EDG GPCR和EDG来调节淋巴细胞活化或迁移的包括小有机分子，抗体，肽，环肽，核酸，反义核酸，鞘脂类似物和核酶的试剂的方法相关信号转导; 以及在与淋巴细胞活化和抑制以及淋巴细胞迁移相关的诊断和治疗中使用表达谱和组合物。

10. 发明申请

WO2003029280A2 GRB7: NOVEL REGULATOR OF LYMPHOCYTE SIGNALING 审中-公开
标题翻译： GRB7：LYMPHOCYTE信号的新型调节剂
公开(公告)号：WO2003029280A2
公开(公告)日：2003-04-10
申请号：PCT/US2002/031622
申请日：2002-10-02
申请人： RIGEL PHARMACEUTICALS, INC. , PARDO, Jorge , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , ZHAO, Haoran
发明人： PARDO, Jorge , CHU, Peter , LI, Congfen , LIAO, X., Charlene , MASUDA, Esteban , ZHAO, Haoran
IPC分类号： C07K
CPC分类号： C07K14/4713 , G01N33/505 , G01N2333/4706 , G01N2500/10
摘要： The present invention relates to regulation of T lymphocyte activation. More particularly, the present invention is directed to nucleic acids encoding GRB7, which is involved in modulation of T lymphocyte activation and TCR signaling. The invention further relates to methods for identifying and using agents, including small organic molecules, peptides, circular peptides, antibodies, lipids, antisense nucleic acids, RNAi, and ribozymes, that modulate lymphocyte activation and TCR signaling via modulation of GRB7; as well as to the use of expression profiles and compositions in diagnosis and therapy related to lymphocyte activation and suppression.
摘要翻译：本发明涉及T淋巴细胞活化的调控。更具体地，本发明涉及编码GRB7的核酸，其涉及T淋巴细胞活化和TCR信号传导的调节。本发明还涉及用于鉴定和使用通过调节GRB7来调节淋巴细胞活化和TCR信号的试剂，包括小有机分子，肽，环状肽，抗体，脂质，反义核酸，RNAi和核酶的方法; 以及在与淋巴细胞活化和抑制相关的诊断和治疗中使用表达谱和组合物。

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