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：US20110046104A1

公开(公告)日：2011-02-24

申请号：US12598277

申请日：2009-10-30

申请人： Michael Paul Mortimore ,  Julian M.C. Golec ,  Daniel David Robinson ,  John Studley

发明人： Michael Paul Mortimore ,  Julian M.C. Golec ,  Daniel David Robinson ,  John Studley

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.

公开(公告)号：US08741931B2

公开(公告)日：2014-06-03

申请号：US13442244

申请日：2012-04-09

申请人： 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

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： A61K31/444

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 having formula: which are 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： 本发明涉及具有下式的化合物：其可用作蛋白激酶的抑制剂。 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：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：US20110269732A1

公开(公告)日：2011-11-03

申请号：US12595878

申请日：2009-10-14

申请人： Julian M.C. GOLEC ,  John POLLARD ,  James WESTCOTT ,  Hayley Marie BINCH ,  Michael Paul MORTIMORE ,  Daniel David ROBINSON

发明人： Julian M.C. GOLEC ,  John POLLARD ,  James WESTCOTT ,  Hayley Marie BINCH ,  Michael Paul MORTIMORE ,  Daniel David ROBINSON

IPC分类号： A61K31/397 ,  A61K31/506 ,  C07D403/14 ,  A61K31/496 ,  G06G7/58 ,  A61P35/02 ,  A61P35/04 ,  C12N9/99 ,  C12Q1/48 ,  C07D401/14 ,  A61P35/00

CPC分类号： C07D403/12 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C12Q1/485 ,  G01N2500/04 ,  G16B15/00

摘要： The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.

摘要翻译： 本发明涉及药物发现方法，特别是用于测定化合物作为极光激酶抑制剂的活性的方法。 本发明还涉及描述能够促进蛋白质AuroraB中的构象变化的化合物的药效团，其两步​​法的结合常数以Ki *给出。 最后，本发明还涉及具有药效团特征的化合物。

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：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：US20130018035A1

公开(公告)日：2013-01-17

申请号：US13531461

申请日：2012-06-22

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

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

IPC分类号： A61K31/4985 ,  A61P35/00 ,  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.

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。

公开(公告)号：US08822469B2

公开(公告)日：2014-09-02

申请号：US13531461

申请日：2012-06-22

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

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

IPC分类号： A61K31/4985 ,  C07D241/36

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。