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1. 发明申请

WO2013043960A1 COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE 审中-公开
标题翻译：化合物作为氯霉素激酶的抑制剂有用
公开(公告)号：WO2013043960A1
公开(公告)日：2013-03-28
申请号：PCT/US2012/056474
申请日：2012-09-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , EVERITT, Simon , KNEGTEL, Ronald , MORTIMORE, Michael , RUTHERFORD, Alistair
发明人： EVERITT, Simon , KNEGTEL, Ronald , MORTIMORE, Michael , RUTHERFORD, Alistair
IPC分类号： C07D453/00 , A61K31/496 , A61P7/00 , A61K31/439 , A61P35/00 , A61P9/00 , A61K31/4545 , A61P37/00 , A61P13/00 , A61K31/538 , A61P1/00 , A61P25/00 , A61K31/444 , A61P3/00 , A61P29/00
CPC分类号： C07D453/02 , A61K31/439 , A61K31/498 , A61K31/538 , A61K45/06 , C07D453/00 , Y02A50/411
摘要： The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及可用作胆碱激酶抑制剂的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

2. 发明申请

WO2014143240A1 FUSED PYRAZOLOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：用作ATR激酶抑制剂的熔融的吡唑并吡啶衍生物
公开(公告)号：WO2014143240A1
公开(公告)日：2014-09-18
申请号：PCT/US2013/073468
申请日：2013-12-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： CHARRIER, Jean-Damien , DAVIS, Chris , DURRANT, Steven , JARDI, Gorka, Etxebarria I , FRAYSSE, Damien , KAY, David , KNEGTEL, Ronald , PIERARD, Francoise , PINDER, Joanne , STORCK, Pierre-Henri
IPC分类号： C07D471/14 , A61K31/519 , A61P35/00
CPC分类号： C07D471/14
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have the formula I:Additionally, the compounds of this invention have the formula I-A:or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物具有式I：另外，本发明的化合物具有式I-A：或其药学上可接受的盐，其中变量如本文所定义。

3. 发明申请

WO2014055756A1 METHOD FOR MEASURING ATR INHIBITION MEDIATED INCREASES IN DNA DAMAGE 审中-公开
标题翻译：用于测量ATR抑制介导的DNA损伤增加的方法
公开(公告)号：WO2014055756A1
公开(公告)日：2014-04-10
申请号：PCT/US2013/063254
申请日：2013-10-03
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： FALCON, Susanna , REAPER, Philip , POLLARD, John , CURTIN, Nicola, Jane , CHEN, Tao , MIDDLETON, Fiona, Kay
IPC分类号： G01N33/68
CPC分类号： G01N33/6875 , G01N33/5047 , G01N33/573 , G01N33/68 , G01N2333/4703 , G01N2333/912 , G01N2440/14
摘要： The present relates to methods for detecting DNA damage in subjects treated with an ATR inhibitor. More specifically, this invention relates to a method for measuring changes in levels of γΗ2ΑΧ and/or pChkl Ser345 in, e.g., surrogate tissue cells, following ex vivo stimulation with a DNA damaging agent.
摘要翻译：本发明涉及用ATR抑制剂治疗的受试者中DNA损伤检测方法。更具体地说，本发明涉及一种测量γ＆EEgr; 2＆Agr＆amp; KHgr水平变化的方法。和/或pChklSer345在例如替代组织细胞中，在用DNA损伤剂离体刺激之后。

4. 发明申请

WO2015195740A1 METHOD FOR TREATING CANCER USING A COMBINATION OF CHK1 AND ATR INHIBITORS 审中-公开
标题翻译：使用CHK1和ATR抑制剂组合治疗癌症的方法
公开(公告)号：WO2015195740A1
公开(公告)日：2015-12-23
申请号：PCT/US2015/036137
申请日：2015-06-17
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： HELLEDAY, Thomas , SANJIV, Kumar
IPC分类号： A61K45/00 , A61P35/00
CPC分类号： A61K31/519 , A61K31/4535 , A61K31/4709 , A61K31/4965 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , A61K2300/00
摘要： The present invention relates to methods of treating cancer in a patient by administering a compound useful as an inhibitor of ATR protein kinase in combination with a compound useful as an inhibitor of Chkl protein kinase. The aforementioned combination displays a surprising synergistic effect in treating cancer despite the targeted protein kinases being within the same biological pathway. Moreover, the present invention also relates to methods of treating cancer by administering a compound useful as an inhibitor of ATR protein kinase; administering a compound useful as an inhibitor of Chkl protein kinase; as well as administering a DNA damaging agent to a patient. The compounds utilized in this invention are represented by formula (I) and formula (II): wherein the variables are as defined herein.
摘要翻译：本发明涉及通过将可用作ATR蛋白激酶抑制剂的化合物与可用作Chk1蛋白激酶抑制剂的化合物组合施用于治疗患者癌症的方法。尽管目标蛋白激酶位于相同的生物学途径内，但是上述组合在治疗癌症中表现出惊人的协同效应。此外，本发明还涉及通过施用可用作ATR蛋白激酶抑制剂的化合物来治疗癌症的方法; 施用可用作Chk1蛋白激酶抑制剂的化合物; 以及向患者施用DNA损伤剂。用于本发明的化合物由式（I）和式（II）表示：其中变量如本文所定义。

5. 发明申请

WO2015187451A1 RADIOLABELLED DERIVATIVES OF A 2-AMINO-6-FLUORO-N-[5-FLUORO-PYRIDIN-3-YL]- PYRAZOLO[1,5-A]PYRIMIDIN-3-CARBOXAMIDE COMPOUND USEFUL AS ATR KINASE INHIBITOR, THE PREPARATION OF SAID COMPOUND AND DIFFERENT SOLID FORMS THEREOF 审中-公开
标题翻译：用于ATR激酶抑制剂的2-氨基-6-氟-N- [5-氟-2-吡啶-3-基] - 吡唑并[1,5-A]嘧啶-3-羰氧基化合物的放射性衍生物，制备化合物化合物和不同的固体形式
公开(公告)号：WO2015187451A1
公开(公告)日：2015-12-10
申请号：PCT/US2015/032879
申请日：2015-05-28
申请人： VERTEX PHARMACETUCALS INCORPORATED
发明人： AHMAD, Nadia , CHARRIER, Jean-Damien , DAVIS, Chris , ETXEBARRIA I JARDI, Gorka , FRAYSSE, Damien , KNEGTEL, Ronald , PANESAR, Maninder , PIERARD, Francoise , PINDER, Joanne , STORCK, Pierre-Henri , STUDLEY, John
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula (I-l) or (I-A); wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 和本发明化合物的固体形式。本发明化合物具有式（I-1）或（I-A）; 其中变量如本文所定义。

6. 发明申请

WO2014143241A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2014143241A1
公开(公告)日：2014-09-18
申请号：PCT/US2013/073471
申请日：2013-12-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BRENCHLEY, Guy , CHARRIER, Jean-damien , DAVIS, Chris , DURRANT, Steven , JARDI, Gorka, Etxebarria I , FRAYSSE, Damien , JIMENEZ, Juan-miguel , KAY, David , KNEGTEL, Ronald , PIERARD, Francoise , PINDER, Joanne , SHAW, David , STORCK, Pierre-henri , STUDLEY, John , TWIN, Heather
IPC分类号： C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D487/04 , A61K31/36 , A61K31/4188 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/7068 , A61K33/24 , A61K45/06 , A61N5/1028 , A61N5/1077 , A61N2005/1087 , A61N2005/1089 , A61N2005/109 , C07D453/02 , C07D471/08 , C07D491/107 , C07D519/00 , C12N9/12 , C12Y207/11001
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I) or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物具有式（I）或其药学上可接受的盐，其中变量如本文所定义。

7. 发明申请

WO2014081689A1 COMPOUNDS USEFUL AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE 审中-公开
标题翻译：化合物作为INDOLEAMINE 2,3-DIOXYGENASE的抑制剂有用
公开(公告)号：WO2014081689A1
公开(公告)日：2014-05-30
申请号：PCT/US2013/070693
申请日：2013-11-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BOYALL, Dean , DAVIS, Christopher , DODD, James , EVERITT, Simon , MILLER, Andrew , WEBER, Peter , WESTCOTT, James , YOUNG, Stephen
IPC分类号： C07D403/12 , C07D401/12 , C07D413/12 , C07D249/10 , A61K31/4192 , A61P35/00
CPC分类号： C07D249/04 , A61K31/4192 , A61K31/4439 , A61K45/06 , C07D249/10 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications.. The compounds of this invention have formula I-A; wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作吲哚胺2,3-双加氧酶（IDO）抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用该化合物的方法。本发明的化合物具有式I-A; 其中变量如本文所定义。

8. 发明申请

WO2014062604A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2014062604A1
公开(公告)日：2014-04-24
申请号：PCT/US2013/064920
申请日：2013-10-15
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： CHARRIER, Jean-Damien , PINDER, Joanne , STORCK, Pierre-Henri
IPC分类号： C07D413/14 , C07D413/04 , A61K31/496 , A61P35/00
CPC分类号： C07D413/14 , C07D413/04 , C07D413/12
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I); or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明化合物具有式（I）; 或其药学上可接受的盐，其中变量如本文所定义。

9. 发明申请

WO2013043961A1 COMPOUNDS USEFUL AS INHIBITORS OF CHOLINE KINASE 审中-公开
标题翻译：可用作胆碱激酶抑制剂的化合物
公开(公告)号：WO2013043961A1
公开(公告)日：2013-03-28
申请号：PCT/US2012/056476
申请日：2012-09-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , MORTIMORE, Michael , EVERITT, Simon , RUTHERFORD, Alistair , KNEGTEL, Ronald
发明人： MORTIMORE, Michael , EVERITT, Simon , RUTHERFORD, Alistair , KNEGTEL, Ronald
IPC分类号： C07D453/02 , A61K31/439 , A61P35/00 , A61P33/06
CPC分类号： C07D453/02 , A61K31/439 , A61K31/496 , A61K31/5377 , A61K45/06
摘要： The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及用作胆碱激酶抑制剂的化合物。本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。本发明还提供了制备本发明化合物的方法。

10. 发明申请

WO2015084384A1 COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
标题翻译：化合物作为ATR激酶的抑制剂有用
公开(公告)号：WO2015084384A1
公开(公告)日：2015-06-11
申请号：PCT/US2013/073482
申请日：2013-12-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BOYALL, Dean , CHARRIER, Jean-Damien , DAVIS, Chris , DURRANT, Steven , ETXEBARRIA I JARDI, Gorka , FRAYSSE, Damien , KAY, David , KNEGTEL, Ronald , PINDER, Joanne
IPC分类号： C07D471/04 , C07D487/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention are represented by formula (I-A) and formula (I-B); or a pharmaceutically acceptable salt, wherein the variables are as defined herein.
摘要翻译：本发明涉及可用作ATR蛋白激酶抑制剂的化合物。本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。本发明的化合物由式（I-A）和式（I-B）表示; 或其药学上可接受的盐，其中变量如本文所定义。

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