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1. 发明申请

WO2008118822A1 COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY 审中-公开
公开(公告)号：WO2008118822A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/057930
申请日：2008-03-21
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar , RAMPHAL, John , TSO, Kin , SRAN, Arvinder , KEIM, Holger , MARKOVTSOV, Vadim , CARROLL, David , THOTA, Sambaiah , ARGADE, Ankush , CLOUGH, Jeffrey Wayne , SINGH, Rajinder
发明人： LI, Hui , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar , RAMPHAL, John , TSO, Kin , SRAN, Arvinder , KEIM, Holger , MARKOVTSOV, Vadim , CARROLL, David , THOTA, Sambaiah , ARGADE, Ankush , CLOUGH, Jeffrey Wayne , SINGH, Rajinder
IPC分类号： C07D239/48
CPC分类号： C07D239/48
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

WO2006133426A2 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：WO2006133426A2
公开(公告)日：2006-12-14
申请号：PCT/US2006/022590
申请日：2006-06-08
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , THOTA, Sambaiah , CARROLL, David , ARGADE, Ankush , TSO, Kin , SRAN, Arvinder , CLOUGH, Jeffrey , KEIM, Holger , BHAMIDIPATI, Somasekhar , TAYLOR, Vanessa , COOPER, Robin , SINGH, Rajinder , WONG, Brian
发明人： LI, Hui , THOTA, Sambaiah , CARROLL, David , ARGADE, Ankush , TSO, Kin , SRAN, Arvinder , CLOUGH, Jeffrey , KEIM, Holger , BHAMIDIPATI, Somasekhar , TAYLOR, Vanessa , COOPER, Robin , SINGH, Rajinder , WONG, Brian
IPC分类号： A61K31/549 , A61K31/506 , A61K31/505 , C07D417/02 , C07D403/02
CPC分类号： C07D413/12 , A61K31/343 , A61K31/436 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/695 , A61K38/13 , A61K39/3955 , A61K45/06 , C07D239/42 , C07D239/48 , C07D285/22 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07F7/0812 , C07F7/10
摘要： The invention encompasses compounds having formula (I-V) 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, may be therapeutically useful.
摘要翻译：本发明包括具有式（I-V）的化合物以及使用这些化合物在治疗JAK途径调节或JAK激酶，特别是JAK3抑制可能是治疗有用的条件下的组合物和方法。

3. 发明申请

WO2021046407A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：WO2021046407A1
公开(公告)日：2021-03-11
申请号：PCT/US2020/049487
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS, INC. , CHEN, Yan , YU, Jiaxin , SHAW, Simon , DARWISH, Ihab , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar , LUO, Zhushou , KOLLURI, Rao
发明人： CHEN, Yan , YU, Jiaxin , SHAW, Simon , DARWISH, Ihab , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar , LUO, Zhushou , KOLLURI, Rao
IPC分类号： C07D413/14 , C07D413/12 , A61P37/00 , A61K31/553
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

4. 发明申请

WO2018089199A1 OXAZOLE DERIVATIVES FOR USE AS IRAK INHIBITORS AND METHOD FOR THEIR PREPARATION 审中-公开
标题翻译：用作IRAK抑制剂的恶唑衍生物及其制备方法
公开(公告)号：WO2018089199A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/058339
申请日：2017-10-25
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , HECKRODT, Thilo , CHEN, Yan , KELLEY, Ryan , MCMURTRIE, Darren , TSO, Kin , TAYLOR, Vanessa , SINGH, Rajinder , YEN, Rose , MAUNG, Jack
发明人： LI, Hui , HECKRODT, Thilo , CHEN, Yan , KELLEY, Ryan , MCMURTRIE, Darren , TSO, Kin , TAYLOR, Vanessa , SINGH, Rajinder , YEN, Rose , MAUNG, Jack
IPC分类号： C07D413/14 , A61P29/00 , A61K31/422
摘要： Disclosed embodiments concern interleukin receptor associated kinases (IRAK) inhibitors, which are oxazole compounds of formula 1, 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.
摘要翻译：所公开的实施方案涉及作为式1的恶唑化合物的白细胞介素受体相关激酶（IRAK）抑制剂，以及包含这种抑制剂的组合物。还公开了制备和使用该化合物和组合物的方法。公开的化合物和/或组合物可以用于治疗或预防IRAK相关的疾病或病症。

5. 发明申请

WO2018005356A1 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS 审中-公开
标题翻译： 2,4-二氨基嘧啶化合物以及制备和使用该化合物的方法
公开(公告)号：WO2018005356A1
公开(公告)日：2018-01-04
申请号：PCT/US2017/039273
申请日：2017-06-26
申请人： RIGEL PHARMACEUTICALS, INC. , CHEN, Yan , YEN, Rose , YU, Jiaxin , TAYLOR, Vanessa , SINGH, Rajinder
发明人： CHEN, Yan , YEN, Rose , YU, Jiaxin , TAYLOR, Vanessa , SINGH, Rajinder
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61P3/00 , A61P9/00 , A61P11/06 , A61P13/00 , A61P25/00 , A61P31/00 , A61P37/06
摘要： Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R 1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R 2 and R 3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC 50 of from 0.003 μΜ to 3.7 μΜ; a TAK1 IC 50 of from 0.008 μΜ to 132 μΜ; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
摘要翻译：在本发明范围内的化合物具有式1或其盐或其产物，其中环A选自环脂族; 环B是芳基; R 1选自（C 1 -C 10）烷基，（C 3 -C 10）环烷基，卤素，芳基和杂芳基; 和R 2和R 3独立地选自氢和（C 1 -C 6）烷基。公开的化合物可以具有0.003μM至3.7μM的IRAK4IC50; 0.008μM至132μM的TAK1 IC 50; 和/或1至450的IRAK4 / TAK1选择性。特定化合物可具有100至500的IRAK4 / TAK1选择性。可将公开的组合物配制成药物组合物。还公开了使用这些化合物和/或组合物的方法。该方法可以包括向受试者施用有效量的在本发明范围内的化合物，特别是相对于TAK1选择性地抑制IRAK1和/或IRAK4。

6. 发明申请

WO2012015972A1 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：WO2012015972A1
公开(公告)日：2012-02-02
申请号：PCT/US2011/045609
申请日：2011-07-27
申请人： RIGEL PHARMACEUTICALS, INC. , LI, Hui , HECKRODT, Thilo, J. , CHEN, Yan , MCMURTRIE, Darren, John , TAYLOR, Vanessa , SINGH, Rajinder , DING, Pingyu , YEN, Rose
发明人： LI, Hui , HECKRODT, Thilo, J. , CHEN, Yan , MCMURTRIE, Darren, John , TAYLOR, Vanessa , SINGH, Rajinder , DING, Pingyu , YEN, Rose
IPC分类号： C07D413/12 , C07D413/14 , A61K31/506 , A61P27/00 , A61P37/06
CPC分类号： C07D413/12 , C07B59/002 , C07B2200/05 , C07F9/65583
摘要： Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
摘要翻译：公开了式I化合物，含有它们的组合物，以及用于化合物和组合物用于治疗JAK途径的调节或JAK激酶，特别是JAK 2和JAK 3的抑制在治疗上有用的条件的方法。还公开了制备该化合物的方法。

7. 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.

8. 发明申请

WO2021046447A1 HETEROCYCLIC RIP1 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2021046447A1
公开(公告)日：2021-03-11
申请号：PCT/US2020/049540
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS, INC. , SHAW, Simon , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar
发明人： SHAW, Simon , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar
IPC分类号： C07D403/14 , C07D407/14 , C07D413/14 , C07D401/14 , A61P29/00 , A61P37/00 , A61K31/55
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

9. 发明申请

WO2021046382A1 RIP1 INHIBITORY COMPOUNDS AND METHODS FOR MAKING AND USING THE SAME 审中-公开
公开(公告)号：WO2021046382A1
公开(公告)日：2021-03-11
申请号：PCT/US2020/049451
申请日：2020-09-04
申请人： RIGEL PHARMACEUTICALS, INC. , TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar
发明人： TAYLOR, Vanessa , BHAMIDIPATI, Somasekhar
IPC分类号： C07D401/14 , C07D403/12 , C07D405/14 , C07D487/04 , C07D491/107 , A61K31/55 , A61P37/00 , A61P29/00
摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

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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