公开(公告)号：US20120046295A1

公开(公告)日：2012-02-23

申请号：US13167654

申请日：2011-06-23

申请人： Jean-Damien Charrier ,  Joanne Pinder ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Damien Fraysse ,  Somhairle MacCormick ,  Anisa Nizarali Virani ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Joanne Pinder ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Damien Fraysse ,  Somhairle MacCormick ,  Anisa Nizarali Virani ,  Philip Michael Reaper

IPC分类号： A61K31/4985 ,  C07D495/04 ,  A61P35/00 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

摘要： The present invention relates to pyrrolopyrazines 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咯并吡嗪化合物。 本发明还涉及包含本发明化合物的药用组合物; 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。

公开(公告)号：US08623869B2

公开(公告)日：2014-01-07

申请号：US13167654

申请日：2011-06-23

申请人： Jean-Damien Charrier ,  Joanne Pinder ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Damien Fraysse ,  Somhairle MacCormick ,  Anisa Nizarali Virani ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Joanne Pinder ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Damien Fraysse ,  Somhairle MacCormick ,  Anisa Nizarali Virani ,  Philip Michael Reaper

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D471/04 ,  C07D495/04 ,  A61K2300/00

摘要： The present invention relates to pyrrolopyrazines 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咯并吡嗪化合物。 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。

公开(公告)号：US09096602B2

公开(公告)日：2015-08-04

申请号：US13531464

申请日：2012-06-22

申请人： Simon Everitt ,  Michael Paul Mortimore ,  Jean-Damien Charrier ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Ronald Knegtel ,  Joanne Pinder ,  Steven John Durrant

发明人： Simon Everitt ,  Michael Paul Mortimore ,  Jean-Damien Charrier ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Ronald Knegtel ,  Joanne Pinder ,  Steven John Durrant

IPC分类号： A61K31/4985 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10

摘要： The present invention relates to pyrrolopyrazines 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咯并吡嗪化合物。 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。

公开(公告)号：US20130017273A1

公开(公告)日：2013-01-17

申请号：US13531464

申请日：2012-06-22

申请人： Simon Everitt ,  Michael Paul Mortimore ,  Jean-Damien Charrier ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Ronald Knegtel ,  Joanne Pinder ,  Steven John Durrant

发明人： Simon Everitt ,  Michael Paul Mortimore ,  Jean-Damien Charrier ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Ronald Knegtel ,  Joanne Pinder ,  Steven John Durrant

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/551 ,  A61P35/00 ,  C07D491/113 ,  A61K31/553 ,  A61K33/24 ,  A61K31/7048 ,  C07D487/04 ,  C07D491/08

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K45/06 ,  A61N5/10

摘要： The present invention relates to pyrrolopyrazines 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.

公开(公告)号：US09334244B2

公开(公告)日：2016-05-10

申请号：US13106184

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  Ronald Marcellus Alphonsus Knegtel ,  Anisa Nizarali Virani ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  Ronald Marcellus Alphonsus Knegtel ,  Anisa Nizarali Virani ,  Philip Michael Reaper

IPC分类号： C07D241/06 ,  C07D413/04 ,  C07D239/46

CPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K33/24 ,  C07D239/46 ,  C07D241/24 ,  C07D413/04

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 IV: 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IV：其中变量如本文所定义。

公开(公告)号：US20120122884A1

公开(公告)日：2012-05-17

申请号：US13106184

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  Ronald Marcellus Alphonsus Knegtel ,  Anisa Nizarali Virani ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  Ronald Marcellus Alphonsus Knegtel ,  Anisa Nizarali Virani ,  Philip Michael Reaper

IPC分类号： A61K31/4965 ,  A61P35/00 ,  A61K31/497 ,  C07D241/28 ,  C07D413/04

CPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K33/24 ,  C07D239/46 ,  C07D241/24 ,  C07D413/04

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 IV: 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IV：其中变量如本文所定义。

公开(公告)号：US20130034616A1

公开(公告)日：2013-02-07

申请号：US13531467

申请日：2012-06-22

申请人： Pierre-Henri Storck ,  Jean-Damien Charrier ,  Alistair Rutherford ,  Michael Paul Mortimore ,  Somhairle MacCormick ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant

发明人： Pierre-Henri Storck ,  Jean-Damien Charrier ,  Alistair Rutherford ,  Michael Paul Mortimore ,  Somhairle MacCormick ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/7048 ,  A61K33/24 ,  A61P35/00 ,  C07D487/04 ,  A61K31/551

CPC分类号： C07D487/04

摘要： The present invention relates to pyrrolopyrazines 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.

公开(公告)号：US09309250B2

公开(公告)日：2016-04-12

申请号：US13531467

申请日：2012-06-22

申请人： Pierre-Henri Storck ,  Jean-Damien Charrier ,  Alistair Rutherford ,  Michael Paul Mortimore ,  Somhairle MacCormick ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant

发明人： Pierre-Henri Storck ,  Jean-Damien Charrier ,  Alistair Rutherford ,  Michael Paul Mortimore ,  Somhairle MacCormick ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant

IPC分类号： A61K31/4985 ,  C07D241/38 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention relates to pyrrolopyrazines 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咯并吡嗪化合物。 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。

公开(公告)号：US20130089625A1

公开(公告)日：2013-04-11

申请号：US13631732

申请日：2012-09-28

申请人： Jean-Damien Charrier ,  Pierre-Henri Storck ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Paul Angell ,  Robert Michael Hughes ,  David Andrew Siesel ,  Armando Urbina ,  Carl Zwicker ,  Nicholas LoConte ,  Timothy Barder

发明人： Jean-Damien Charrier ,  Pierre-Henri Storck ,  John Studley ,  Francoise Yvonne Theodora Marie Pierard ,  Steven John Durrant ,  Benjamin Joseph Littler ,  Paul Angell ,  Robert Michael Hughes ,  David Andrew Siesel ,  Armando Urbina ,  Carl Zwicker ,  Nicholas LoConte ,  Timothy Barder

IPC分类号： C07D413/14 ,  A61K45/06 ,  A61N5/10 ,  A61K31/4745 ,  A61K31/7068 ,  A61K31/497 ,  A61K33/24

CPC分类号： C07D413/14 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61N5/10

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; solid forms 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-1: wherein the variables are as defined herein.Additionally, the compounds of this invention have formula II: or a pharmaceutically acceptable salt thereof, 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; 固体形式的本发明化合物; 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-1：其中变量如本文所定义。 此外，本发明的化合物具有式II：或其药学上可接受的盐，其中变量如本文所定义。

公开(公告)号：US08969356B2

公开(公告)日：2015-03-03

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： A61K31/497 ,  A61K31/4965 ,  C07D241/20 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D401/04 ,  C07D401/12 ,  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。