公开(公告)号：US20050055321A1

公开(公告)日：2005-03-10

申请号：US10889888

申请日：2004-07-13

Applicant: Raya Fratkina ,  Monica Anderson ,  Mark Angel ,  Max Copperman ,  Scott Huffman ,  David Kay ,  Robert Stern ,  Jeffrey Rudy

Inventor： Raya Fratkina ,  Monica Anderson ,  Mark Angel ,  Max Copperman ,  Scott Huffman ,  David Kay ,  Robert Stern ,  Jeffrey Rudy

IPC: G06F17/30 ,  G06N5/04 ,  G06N5/02 ,  G06F7/00 ,  G06F17/00 ,  G06N5/00

CPC classification number: G06F17/30654 ,  G06F17/30873 ,  G06N5/042 ,  Y10S707/99933 ,  Y10S707/99945

Abstract: A method and system are disclosed for retrieving information through the use of a multi-stage interaction with a client to identify particular knowledge content associated with a knowledge map.

Abstract translation: 公开了一种用于通过使用与客户端的多阶段交互来检索信息以识别与知识图相关联的特定知识内容的方法和系统。

公开(公告)号：US06613776B2

公开(公告)日：2003-09-02

申请号：US09952836

申请日：2001-09-14

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

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

IPC: C07D40112

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 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; 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 Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T 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: 本发明描述了包含药学上可接受的载体和式V化合物的新型吡唑组合物：其中Z1是N，CRa或CH，Z2是N或CH，其中Z1和Z2之一是氮; G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; Rx和Ry独立地选自T-R3，或Rx和Ry与它们的插入原子一起形成稠环; R1，R2，R2'，R3和T如说明书所述。 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：US1750778A

公开(公告)日：1930-03-18

申请号：US24028827

申请日：1927-12-15

Applicant: DAVID KAY

Inventor： DAVID KAY

IPC: B64C11/32

CPC classification number: B64C11/32

公开(公告)号：US08877759B2

公开(公告)日：2014-11-04

申请号：US13440981

申请日：2012-09-04

Applicant: 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

Inventor： 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: 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 classification number: 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

Abstract: 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.

Abstract translation: 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：US08394952B2

公开(公告)日：2013-03-12

申请号：US13206638

申请日：2011-08-10

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

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

IPC: C07D401/12

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.

公开(公告)号：US20120040020A1

公开(公告)日：2012-02-16

申请号：US13104291

申请日：2011-10-27

Applicant: 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

Inventor： 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: 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 classification number: 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

Abstract: 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.

Abstract translation: 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：US20110086856A1

公开(公告)日：2011-04-14

申请号：US12967675

申请日：2010-12-14

Applicant: David Bebbington ,  Hayley Binch ,  Jean-Damien Charrier ,  Simon Everitt ,  Juliam M.C. Golec ,  David Kay ,  Ronald Knegtel ,  Andrew Miller ,  Francoise Pierard

Inventor： David Bebbington ,  Hayley Binch ,  Jean-Damien Charrier ,  Simon Everitt ,  Juliam M.C. Golec ,  David Kay ,  Ronald Knegtel ,  Andrew Miller ,  Francoise Pierard

IPC: A61K31/53 ,  A61K31/517 ,  A61K31/519 ,  A61K31/506 ,  A61K31/496 ,  C12N9/99 ,  A61P35/00 ,  A61P35/02 ,  A61P25/00 ,  A61P37/08 ,  A61P11/06 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P19/10 ,  A61P37/06 ,  A61P31/12 ,  A61P19/08 ,  A61P3/10

CPC classification number: C07D403/12

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. 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.

Abstract translation: 本发明涉及可用于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。

公开(公告)号：US07915305B2

公开(公告)日：2011-03-29

申请号：US11656876

申请日：2007-01-23

Applicant: Guy Brenchley ,  Jean-Damien Charrier ,  Steven Durrant ,  David Kay ,  Ronald Knegtel ,  Sharn Ramaya ,  Shazia Sadiq

Inventor： Guy Brenchley ,  Jean-Damien Charrier ,  Steven Durrant ,  David Kay ,  Ronald Knegtel ,  Sharn Ramaya ,  Shazia Sadiq

IPC: A61K31/38

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase represented by formula (I): or a pharmaceutically acceptable salt thereof. 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: 本发明涉及可用作由式（I）表示的蛋白激酶抑制剂的化合物或其药学上可接受的盐。 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：US07863282B2

公开(公告)日：2011-01-04

申请号：US11504528

申请日：2006-08-15

Applicant: David Bebbington ,  Hayley Binch ,  Jean-Damien Charrier ,  Simon Everitt ,  Julian M. C. Golec ,  David Kay ,  Ronald Knegtel ,  Andrew Miller ,  Francoise Pierard

Inventor： David Bebbington ,  Hayley Binch ,  Jean-Damien Charrier ,  Simon Everitt ,  Julian M. C. Golec ,  David Kay ,  Ronald Knegtel ,  Andrew Miller ,  Francoise Pierard

IPC: A01N43/54 ,  A61K31/517 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00

CPC classification number: C07D403/12

Abstract: A compound of formula Ia: or a pharmaceutically acceptable salt thereof.

Abstract translation: 式Ia化合物或其药学上可接受的盐。

公开(公告)号：US20100256170A1

公开(公告)日：2010-10-07

申请号：US12651639

申请日：2010-01-04

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

IPC: A61K31/519 ,  C07D487/04 ,  A61P35/00 ,  A61P25/18 ,  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。