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：US20120040020A1

公开(公告)日：2012-02-16

申请号：US13104291

申请日：2011-10-27

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Haley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Haley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

IPC分类号： A61K33/24 ,  C07D401/14 ,  C07D413/14 ,  A61K31/551 ,  A61K31/497 ,  A61K31/5377 ,  C07D417/14 ,  A61K31/541 ,  C07D405/14 ,  C07D471/04 ,  C07D491/113 ,  A61K31/506 ,  C07D513/04 ,  C07D409/14 ,  C07D487/04 ,  A61K31/4985 ,  C07D487/10 ,  A61K38/16 ,  A61K31/704 ,  A61K31/675 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/706 ,  A61K38/12 ,  A61P17/06 ,  A61P35/00 ,  A61P31/18 ,  A61P1/16 ,  A61P31/20 ,  C07D403/14

CPC分类号： C07D403/14 ,  A61K31/497 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/113

摘要： The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; 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.

摘要翻译： 本公开涉及式I的吡嗪化合物：其中L，n，R 1和R 2如说明书中所述。 这些化合物可用作ATR蛋白激酶的抑制剂。 本公开还涉及包含本公开内容的化合物的药学上可接受的组合物; 使用本公开的化合物治疗各种疾病，病症和病症的方法; 制备本公开的化合物的方法; 用于制备本公开的化合物的中间体; 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。

公开(公告)号：US08410112B2

公开(公告)日：2013-04-02

申请号：US13104291

申请日：2011-10-27

申请人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

发明人： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

IPC分类号： A61K31/4965 ,  C07D403/00

CPC分类号： C07D403/14 ,  A61K31/497 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/113

摘要： The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; 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.

摘要翻译： 本公开涉及式I的吡嗪化合物：其中L，n，R 1和R 2如说明书中所述。 这些化合物可用作ATR蛋白激酶的抑制剂。 本公开还涉及包含本公开内容的化合物的药学上可接受的组合物; 使用本公开的化合物治疗各种疾病，病症和病症的方法; 制备本公开的化合物的方法; 用于制备本公开的化合物的中间体; 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。

公开(公告)号：US09630956B2

公开(公告)日：2017-04-25

申请号：US13106476

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

发明人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

IPC分类号： A61K31/497 ,  A61K33/24 ,  C07D413/14 ,  C07D401/14 ,  C07D241/10

CPC分类号： C07D413/14

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.

公开(公告)号：US20120027874A1

公开(公告)日：2012-02-02

申请号：US13106476

申请日：2011-05-12

申请人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

发明人： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

IPC分类号： A61K31/497 ,  A61K33/24 ,  A61P35/00 ,  C07D413/14

CPC分类号： C07D413/14

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.

公开(公告)号：US20130095193A1

公开(公告)日：2013-04-18

申请号：US13440981

申请日：2012-09-04

申请人： Jean-Damien Charrier ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Joanne Pinder ,  Michael Edward O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Stephen Clinton Young ,  Philip Michael Reaper ,  Steven John Durrant ,  Heather Clare Twin ,  Christopher John Davis

发明人： Jean-Damien Charrier ,  David Kay ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Joanne Pinder ,  Michael Edward O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Stephen Clinton Young ,  Philip Michael Reaper ,  Steven John Durrant ,  Heather Clare Twin ,  Christopher John Davis

IPC分类号： C07D413/14 ,  A61K31/5377 ,  C07D453/00 ,  C07D495/04 ,  A61K31/7068 ,  A61K45/06 ,  A61K31/501 ,  A61K31/55 ,  A61K31/7048 ,  A61K31/497 ,  A61K33/24

CPC分类号： C07D413/14 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/555 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  C07D453/00 ,  C07D453/02 ,  C07D495/04 ,  A61K2300/00

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.

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。

公开(公告)号：US08877759B2

公开(公告)日：2014-11-04

申请号：US13440981

申请日：2012-09-04

申请人： Jean-Damien Charrier ,  David Kay ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Joanne Pinder ,  Michael Edward O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Stephen Clinton Young ,  Philip Michael Reaper ,  Steven John Durrant ,  Heather Clare Twin ,  Christopher John Davis

发明人： Jean-Damien Charrier ,  David Kay ,  Somhairle MacCormick ,  Pierre-Henri Storck ,  Joanne Pinder ,  Michael Edward O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Stephen Clinton Young ,  Philip Michael Reaper ,  Steven John Durrant ,  Heather Clare Twin ,  Christopher John Davis

IPC分类号： A61K31/4965 ,  C07D403/00 ,  A61K31/501 ,  A61K45/06 ,  A61K31/55 ,  A61K31/5377 ,  A61K31/7068 ,  C07D413/14 ,  C07D495/04 ,  A61K31/7048 ,  A61K33/24 ,  A61K31/497 ,  C07D453/00

CPC分类号： C07D413/14 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/555 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  C07D453/00 ,  C07D453/02 ,  C07D495/04 ,  A61K2300/00

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.

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。

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：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。