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公开(公告)号：US20110060013A1
公开(公告)日：2011-03-10
申请号：US12601026
申请日：2009-11-20
申请人： Michael Paul Mortimore , Christopher John Davis , Julian M.C. Golec , John Studley , Daniel David Robinson
发明人： Michael Paul Mortimore , Christopher John Davis , Julian M.C. Golec , John Studley , Daniel David Robinson
IPC分类号： A61K31/4439 , C07D401/14 , C07D417/14 , A61P35/00
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译： 本发明涉及可用作Aurora蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US20110046104A1
公开(公告)日：2011-02-24
申请号：US12598277
申请日：2009-10-30
IPC分类号： A61K31/506 , C07D417/14 , C07D403/14 , C07D401/14
CPC分类号： C07D403/12 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
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公开(公告)号：US20100215772A1
公开(公告)日：2010-08-26
申请号：US12598276
申请日：2009-10-30
IPC分类号： A61K33/24 , C07D239/46 , A61K31/495 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/513 , A61P35/00
CPC分类号： C07D403/12 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译： 本发明涉及可用作Aurora蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US20130089624A1
公开(公告)日：2013-04-11
申请号：US13631730
申请日：2012-09-28
IPC分类号： C07D413/14 , A61K33/24 , C07D267/10 , C07D413/10 , C07D413/04 , A61K31/5377 , C07D265/30
CPC分类号： A61K31/5377 , A61K33/24 , C07D265/30 , C07D267/10 , C07D401/04 , C07D413/04 , C07D413/10 , C07D413/14
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 formula I: wherein the variables are as defined herein.Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
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：其中变量如本文所定义。 此外，本发明还涉及用于生产各种基于morpoholine的中间体的新方法。
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公开(公告)号：US08569337B2
公开(公告)日：2013-10-29
申请号：US12670989
申请日：2010-01-27
申请人： Juan-Miguel Jimenez , John Studley , Ronald Knegtel , Luca Settimo , Christopher John Davis , Damien Fraysse , Philip N. Collier , Guy Brenchley , Dean Boyall , Andrew Miller , Heather Twin , Stephen Young
发明人： Juan-Miguel Jimenez , John Studley , Ronald Knegtel , Luca Settimo , Christopher John Davis , Damien Fraysse , Philip N. Collier , Guy Brenchley , Dean Boyall , Andrew Miller , Heather Twin , Stephen Young
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , A61K31/496 , A61K31/506 , C07D239/24 , C07D241/10 , C07D519/00
摘要： The present invention relates to compounds of tri-cyclic pyrazolopyridine useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions containing such 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： 本发明涉及可用作蛋白激酶抑制剂的三环吡唑并吡啶化合物。 本发明还提供含有这些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。
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公开(公告)号：US08455507B2
公开(公告)日：2013-06-04
申请号：US12595703
申请日：2009-10-13
申请人： John Studley , Stephen Young
发明人： John Studley , Stephen Young
IPC分类号： C07D403/14 , A61K31/4155
CPC分类号： C07D403/14 , C07D401/14 , C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
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公开(公告)号：US20100317641A1
公开(公告)日：2010-12-16
申请号：US12598275
申请日：2009-10-30
IPC分类号： A61K31/4439 , C07D417/14 , C07D401/14 , C12N9/99 , A61P35/00 , A61P35/02
CPC分类号： C07D417/14 , C07D401/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译： 本发明涉及可用作Aurora蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US20070155718A1
公开(公告)日：2007-07-05
申请号：US11489939
申请日：2006-07-20
IPC分类号： A61K31/55 , A61K31/5513 , A61K31/503 , A61K31/517 , A61K31/513 , A61K31/4745 , A61K31/424 , C07D491/04
CPC分类号： C07D498/04
摘要： This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.
摘要翻译： 本发明涉及包含呋喃并[3,2-d]恶唑啉-5-酮部分的胱天蛋白酶抑制剂的前体药物，其在特定条件下可转化为生物活性化合物，特别是胱天蛋白酶抑制剂。 本发明还涉及制备这些半胱天冬酶抑制剂前药的方法。 本发明还涉及包含所述前药的药物组合物及其用于治疗与炎性或退行性疾病相关的疾病的用途。
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公开(公告)号：US08637511B2
公开(公告)日：2014-01-28
申请号：US12796297
申请日：2010-06-08
申请人： Hayley Binch , Michael Mortimore , Chris Davis , Dean Boyall , Simon Everitt , Daniel Robinson , Sham Ramaya , Damien Fraysse , John Studley , Andrew Miller , Michael O'Donnell , Alistair Rutherford , Joanne Pinder
发明人： Hayley Binch , Michael Mortimore , Chris Davis , Dean Boyall , Simon Everitt , Daniel Robinson , Sham Ramaya , Damien Fraysse , John Studley , Andrew Miller , Michael O'Donnell , Alistair Rutherford , Joanne Pinder
IPC分类号： A61K31/506 , A61K31/5355 , A61P29/00 , A61P19/08 , A61P3/00 , A61P25/28 , A61P35/00 , A61P9/00 , A61P37/08
CPC分类号： C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。
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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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