公开(公告)号：US20140221334A1

公开(公告)日：2014-08-07

申请号：US14249614

申请日：2014-04-10

申请人： Vertex Pharmaceuticals Incorporated

发明人： Juan-Miguel Jimenez ,  Guy William Bemis ,  Francois Maltais ,  Tiansheng Wang ,  Ronald Marcellus Alphonsus Knegtel ,  Christopher John Davis ,  Damien Fraysse ,  Dean Boyall ,  Luca Settimo ,  Stephen Young ,  Michael Paul Mortimore

IPC分类号： C07D213/73 ,  C07D401/12 ,  C07D401/04

CPC分类号： C07D213/73 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C07D487/04 ,  C07D487/08

摘要： The present invention relates to compounds useful as inhibitors of protein 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： 本发明涉及可用作蛋白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。

公开(公告)号：US10479784B2

公开(公告)日：2019-11-19

申请号：US15967110

申请日：2018-04-30

申请人： Vertex Pharmaceuticals Incorporated

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Michael Paul Mortimore ,  Michael Edward O'Donnell ,  Joanne Pinder ,  Alistair Rutherford ,  Anisa Nizarali Virani ,  Stephen Clinton Young ,  Philip Michael Reaper

IPC分类号： A61K31/497 ,  C07D403/04 ,  C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D241/28 ,  C07D401/10 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D401/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  A61P35/00

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.

公开(公告)号：US20160311809A1

公开(公告)日：2016-10-27

申请号：US15142286

申请日：2016-04-29

申请人： Vertex Pharmaceuticals Incorporated

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Michael Paul Mortimore ,  Michael Edward O'Donnell ,  Joanne Pinder ,  Alistair Rutherford ,  Anisa Nizarali Virani ,  Stephen Clinton Young ,  Philip Michael Reaper

IPC分类号： C07D413/04

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： 其中变量如本文所定义。

公开(公告)号：US20150376187A1

公开(公告)日：2015-12-31

申请号：US14749070

申请日：2015-06-24

申请人： Vertex Pharmaceuticals Incorporated

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

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

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。