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公开(公告)号：US20120178756A1
公开(公告)日：2012-07-12
申请号：US13106167
申请日：2011-05-12
申请人： Jean-Damien Charrier , Steven John Durrant , Ronald Marcellus Alphonsus Knegtel , Joanne Pinder , Stephen Young , Philip Michael Reaper
发明人： Jean-Damien Charrier , Steven John Durrant , Ronald Marcellus Alphonsus Knegtel , Joanne Pinder , Stephen Young , Philip Michael Reaper
IPC分类号： A61K31/5377 , C07D401/04 , C07D401/12 , C07D409/06 , C07D401/06 , A61N5/00 , C07D413/12 , C07D403/06 , C07D403/10 , A61K31/4965 , A61K31/497 , A61P35/00 , C07D241/20 , C07D405/12
CPC分类号： C07D241/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/06
摘要： The present invention relates to pyrazine and pyridine 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 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: wherein the variables are as defined herein.
摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪和吡啶化合物。 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：其中变量如本文所定义。
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公开(公告)号：US08188281B2
公开(公告)日：2012-05-29
申请号：US12273799
申请日：2008-11-19
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及蛋白激酶抑制剂。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US07507826B2
公开(公告)日：2009-03-24
申请号：US11093821
申请日：2005-03-30
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及蛋白激酶抑制剂。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US20070043063A1
公开(公告)日：2007-02-22
申请号：US11093821
申请日：2005-03-30
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang
IPC分类号： A61K31/506 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及蛋白激酶抑制剂。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US08501446B2
公开(公告)日：2013-08-06
申请号：US13441287
申请日：2012-04-06
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： C12N9/99 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：US20090176763A1
公开(公告)日：2009-07-09
申请号：US12273799
申请日：2008-11-19
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： A61K31/55 , C07D401/14 , A61K31/506 , C07D243/08 , A61K31/551 , C07D403/14 , A61K31/496 , C07D471/02 , A61K31/437 , C07D413/14 , A61K31/5377 , A61P37/00 , A61P29/00 , A61P25/00 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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公开(公告)号：US08841308B2
公开(公告)日：2014-09-23
申请号：US12642447
申请日：2009-12-18
申请人： Jean-Damien Charrier , David Kay , Ronald Knegtel , Somhairle MacCormick , Michael O'Donnell , Joanne Pinder , Philip Michael Reaper
发明人： Jean-Damien Charrier , David Kay , Ronald Knegtel , Somhairle MacCormick , Michael O'Donnell , Joanne Pinder , Philip Michael Reaper
IPC分类号： A61K31/4965
CPC分类号： C07D413/14 , A61P35/00 , C07D241/28 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to pyrazine 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: wherein the variables are as defined herein.
摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪化合物。 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：其中变量如本文所定义。
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公开(公告)号：US20120258958A1
公开(公告)日：2012-10-11
申请号：US13441287
申请日：2012-04-06
申请人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
发明人： Francesco Salituro , Luc Farmer , Randy Bethiel , Edmund Harrington , Jeremy Green , John Court , Jon Come , David Lauffer , Alex Aronov , Hayley Binch , Dean Boyall , Jean-Damien Charrier , Simon Everitt , Damien Fraysse , Michael Mortimore , Francoise Pierard , Daniel Robinson , Jian Wang , Joanne Pinder , Tiansheng Wang , Albert Pierce
IPC分类号： A61K31/551 , A61K31/55 , A61P37/08 , A61P11/06 , C12N9/99 , A61P29/00 , A61P25/00 , A61P25/28 , A61P35/00 , A61K31/506 , A61P37/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0805
摘要： The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及蛋白激酶抑制剂。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US08962631B2
公开(公告)日：2015-02-24
申请号：US13106173
申请日：2011-05-12
申请人： Jean-Damien Charrier , Steven John Durrant , Ronald Marcellus Alphonsus Knegtel , Michael O'Donnell , Philip Michael Reaper
发明人： Jean-Damien Charrier , Steven John Durrant , Ronald Marcellus Alphonsus Knegtel , Michael O'Donnell , Philip Michael Reaper
IPC分类号： A61K31/4965 , A61K31/497 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D411/14 , C07D413/04 , C07D241/24 , C07D417/04
CPC分类号： C07D403/04 , C07D241/24 , C07D403/12 , C07D417/04
摘要： The present invention relates to pyrazine 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 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 II: wherein the variables are as defined herein.
摘要翻译： 本发明涉及可用作ATR蛋白激酶抑制剂的吡嗪化合物。 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II：其中变量如本文所定义。
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公开(公告)号：US20130184292A1
公开(公告)日：2013-07-18
申请号：US13631759
申请日：2012-09-28
申请人： Jean-Damien Charrier , John Studley , Francoise Yvonne Theodora Marie Pierard , Steven John Durrant , Benjamin Joseph Littler , Robert Michael Hughes , David Andrew Siesel , Paul Angell , Armando Urbina , Yi Shi
发明人： Jean-Damien Charrier , John Studley , Francoise Yvonne Theodora Marie Pierard , Steven John Durrant , Benjamin Joseph Littler , Robert Michael Hughes , David Andrew Siesel , Paul Angell , Armando Urbina , Yi Shi
IPC分类号： C07D413/04 , C07D413/14 , C07D241/20 , C07C251/48
CPC分类号： C07D413/04 , C07C251/48 , C07D241/20 , C07D413/14
摘要： The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also 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 or II: wherein the variables are as defined herein.
摘要翻译： 本发明涉及制备用作ATR激酶抑制剂的化合物的方法和中间体，例如氨基吡嗪 - 异恶唑衍生物和相关分子。 本发明还涉及可用作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。 本发明的化合物具有式I或II：其中变量如本文所定义。
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