公开(公告)号：US09630956B2

公开(公告)日：2017-04-25

申请号：US13106476

申请日：2011-05-12

Applicant: 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

Inventor： 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: A61K31/497 ,  A61K33/24 ,  C07D413/14 ,  C07D401/14 ,  C07D241/10

CPC classification number: C07D413/14

Abstract: 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：US08557818B2

公开(公告)日：2013-10-15

申请号：US13356924

申请日：2012-01-24

Applicant: Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

Inventor： Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

IPC: A61K31/519 ,  A61P31/00

CPC classification number: C07D475/00

Abstract: 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.

公开(公告)号：US08524720B2

公开(公告)日：2013-09-03

申请号：US12651639

申请日：2010-01-04

Applicant: David Bebbington ,  Hayley Binch ,  Ronald Knegtel ,  Julian M.C. Golec ,  Sanjay Patel ,  Jean-Damien Charrier ,  David Kay ,  Robert Davies ,  Pan Li ,  Marion Wannamaker ,  Cornelia Forster ,  Albert Pierce

Inventor： David Bebbington ,  Hayley Binch ,  Ronald Knegtel ,  Julian M.C. Golec ,  Sanjay Patel ,  Jean-Damien Charrier ,  David Kay ,  Robert Davies ,  Pan Li ,  Marion Wannamaker ,  Cornelia Forster ,  Albert Pierce

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P25/28 ,  A61P3/10

CPC classification number: C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: This invention describes novel pyrazole compounds of formula IV: wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2′, T, and R3 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract translation: 本发明描述了式IV的新型吡唑化合物：其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R x和R y独立地选自T-R 3，或与它们的插入原子一起形成具有1-3个选自氧，硫或氮的环杂原子的稠合的，不饱和的或部分不饱和的5-8元环; R2，R2'，T和R3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。

公开(公告)号：US08268829B2

公开(公告)日：2012-09-18

申请号：US12436407

申请日：2009-05-06

Applicant: Jean-Damien Charrier ,  Francesca Mazzei ,  David Kay ,  Andrew Miller

Inventor： Jean-Damien Charrier ,  Francesca Mazzei ,  David Kay ,  Andrew Miller

IPC: C07D403/14 ,  A61K31/4155

CPC classification number: C07D403/14 ,  C07D239/34 ,  C07D401/14 ,  C07D403/12 ,  C07D453/02

Abstract: The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions.

Abstract translation: 本发明提供了制备三取代和四取代嘧啶的简便方法。 该方法可用于制备蛋白激酶抑制剂，特别是Aurora激酶。 这些抑制剂可用于治疗或减轻Aurora介导的疾病或病症的严重性。

公开(公告)号：US08201087B2

公开(公告)日：2012-06-12

申请号：US12023903

申请日：2008-01-31

Applicant: David Kay ,  Erland Unruh ,  Gaurav Tandon

Inventor： David Kay ,  Erland Unruh ,  Gaurav Tandon

IPC: G06F17/00

CPC classification number: G06F17/273 ,  G06F3/0237 ,  G06F17/276

Abstract: An adaptation of standard edit distance spell-check algorithms leverages probability-based regional auto-correction algorithms and data structures for ambiguous keypads and other predictive text input systems to provide enhanced typing correction and spell-check features. Strategies for optimization and for ordering results of different types are also provided.

Abstract translation: 标准编辑距离拼写检查算法的适应性利用基于概率的区域自动校正算法和数据结构，用于模糊键盘和其他预测文本输入系统，以提供增强的打字校正和拼写检查功能。 还提供了优化和排序不同类型结果的策略。

公开(公告)号：US20120027874A1

公开(公告)日：2012-02-02

申请号：US13106476

申请日：2011-05-12

Applicant: 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

Inventor： 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: A61K31/497 ,  A61K33/24 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D413/14

Abstract: 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：US08067417B2

公开(公告)日：2011-11-29

申请号：US12796174

申请日：2010-06-08

Applicant: Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

Inventor： Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

IPC: A61K31/495

CPC classification number: C07D487/14

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. 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.

Abstract translation: 本发明涉及可用作结构式（I）表示的蛋白激酶抑制剂的化合物：其中结构式（I）中的变量如本文所述。 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：US20110180005A1

公开(公告)日：2011-07-28

申请号：US12972784

申请日：2010-12-20

Applicant: Stephen Aisthorpe ,  David Kay

Inventor： Stephen Aisthorpe ,  David Kay

IPC: A01K5/01

CPC classification number: A01K5/01 ,  A01K5/0107

Abstract: A housing for animal feedstuff including a base, a roof extending over the base, uprights spaced apart from one another and extending between the base and the roof, and a container locatable between the uprights for containing feedstuff. Livestock, such as cattle, access feedstuff within the container by way of spaces between the uprights. In an embodiment, the uprights are telescopic and the roof can be pivoted between raised and lowered positions relative to the uprights.

Abstract translation: 一种用于动物饲料的壳体，包括基部，在基部上延伸的屋顶，彼此间隔开并在基部和屋顶之间延伸的立柱以及位于用于容纳饲料的立柱之间的容器。 牲畜，如牛，通过立柱之间的空间进入容器内的饲料。 在一个实施例中，立柱是可伸缩的，并且屋顶可以相对于立柱在升高和降低的位置之间枢转。

公开(公告)号：US20100190765A1

公开(公告)日：2010-07-29

申请号：US12569237

申请日：2009-09-29

Applicant: David Kay ,  Ronald Knegtel ,  Jean-Damien Charrier ,  Heather Twin

Inventor： David Kay ,  Ronald Knegtel ,  Jean-Damien Charrier ,  Heather Twin

IPC: A61K31/551

CPC classification number: C07D487/04 ,  A61K31/551 ,  A61K45/06 ,  C07D487/14

Abstract: 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.

Abstract translation: 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：US20090062292A1

公开(公告)日：2009-03-05

申请号：US11786578

申请日：2007-04-12

Applicant: Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

Inventor： Jean-Damien Charrier ,  David Kay ,  Ronald Knegtel

IPC: A61K31/519 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: 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.

Abstract translation: 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。