公开(公告)号：US20100099686A1

公开(公告)日：2010-04-22

申请号：US12448258

申请日：2007-12-14

申请人： Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

发明人： Jean-Damien Charrier ,  Ronald Knegtel ,  David Kay

IPC分类号： A61K31/4985 ,  C07D487/12 ,  C12N9/99 ,  A61P35/00

CPC分类号： C07D475/00

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：US07625913B2

公开(公告)日：2009-12-01

申请号：US10026992

申请日：2001-12-19

申请人： David Bebbington ,  Jean-Damien Charrier ,  Julian Golec ,  Andrew Miller ,  Ronald Knegtel

发明人： David Bebbington ,  Jean-Damien Charrier ,  Julian Golec ,  Andrew Miller ,  Ronald Knegtel

IPC分类号： C07D403/12 ,  A61K31/506

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

摘要： This invention describes novel pyrazole compounds of formula IIIc: wherein R1 is T—Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2, and R2′ 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.

摘要翻译： 本发明描述了式IIIc的新型吡唑化合物：其中R1是T环D，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; Rx，Ry，R2和R2'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Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。

公开(公告)号：US20090281128A1

公开(公告)日：2009-11-12

申请号：US12464380

申请日：2009-05-12

申请人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

发明人： Ronald Knegtel ,  Michael Mortimore ,  John Studley ,  David Millan

IPC分类号： A61K31/472 ,  C07D217/24 ,  C07D239/88 ,  A61K31/517

CPC分类号： C07D239/90 ,  C07D217/24

摘要： The present invention relates to compounds of formula I: useful as inhibitors of caspases. The present invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for preparing the compounds, and methods of using the compounds and compositions in the treatment of various diseases, conditions, or disorders.

摘要翻译： 本发明涉及式I化合物：可用作半胱天冬酶的抑制剂。 本发明还提供包含所述化合物的药学上可接受的组合物，制备化合物的方法，以及使用该化合物和组合物治疗各种疾病，病症或病症的方法。

公开(公告)号：US07531536B2

公开(公告)日：2009-05-12

申请号：US10632428

申请日：2003-08-01

申请人： David Bebbington ,  Jean-Damien Charrier ,  Julian Golec ,  Andrew Miller ,  Ronald Knegtel

发明人： David Bebbington ,  Jean-Damien Charrier ,  Julian Golec ,  Andrew Miller ,  Ronald Knegtel

IPC分类号： C07D403/14 ,  A61K31/4155

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

摘要： This invention describes novel pyrazole compounds of formula IIIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx, Ry, R2; and R2′ 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.

摘要翻译： 本发明描述了式IIIa的新型吡唑化合物：其中R1是T环D，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; Rx，Ry，R2; 和R2'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Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。

公开(公告)号：US07390815B2

公开(公告)日：2008-06-24

申请号：US10692355

申请日：2003-10-23

申请人： Robert Davies ,  David Bebbington ,  Ronald Knegtel ,  Marion Wannamaker ,  Pan Li ,  Cornelia Forster ,  Albert Pierce

发明人： Robert Davies ,  David Bebbington ,  Ronald Knegtel ,  Marion Wannamaker ,  Pan Li ,  Cornelia Forster ,  Albert Pierce

IPC分类号： C07D401/14 ,  C07D471/04 ,  A61K31/517 ,  A61P35/00

CPC分类号： 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

摘要： This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2′ are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.

摘要翻译： 本发明描述了式II的新型吡唑化合物：其中环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，R 2， SUP> 2'，R“x”和“R”如说明书中所述。 环C具有邻位取代基，并且在非邻位任选被取代。 R 2和R 2'任选地与它们的插入原子一起形成稠环体系，例如吲唑环; 并且R x和R y可以任选地与它们的插入原子一起形成稠环体系，例如喹唑啉环。 这些化合物可用作蛋白激酶抑制剂，特别是GSK-3的抑制剂，用于治疗诸如糖尿病和阿尔茨海默病的疾病。

公开(公告)号：US20070219205A1

公开(公告)日：2007-09-20

申请号：US11656876

申请日：2007-01-23

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

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

IPC分类号： A61K31/519 ,  A61K31/498 ,  A61K31/4745 ,  C07D487/04 ,  C07D471/02

CPC分类号： C07D471/04 ,  C07D487/04

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：US20070179156A1

公开(公告)日：2007-08-02

申请号：US11511086

申请日：2006-08-28

申请人： Jean-Damien Charrier ,  Sharn Ramaya ,  Steven Durrant ,  Juan-Miguel Jimenez ,  Guy Brenchley ,  Ronald Knegtel ,  Michael Mortimore

发明人： Jean-Damien Charrier ,  Sharn Ramaya ,  Steven Durrant ,  Juan-Miguel Jimenez ,  Guy Brenchley ,  Ronald Knegtel ,  Michael Mortimore

IPC分类号： A61K31/497 ,  A61K31/4709 ,  A61K31/444 ,  C07D401/14 ,  C07D403/14

CPC分类号： C07D213/64 ,  C07D401/14 ,  C07D417/14

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.

公开(公告)号：US07179826B2

公开(公告)日：2007-02-20

申请号：US10389709

申请日：2003-03-14

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

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

IPC分类号： A01N43/78 ,  C07D271/02 ,  C07D253/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： The present invention relates to compounds useful as 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.

公开(公告)号：US20060258658A1

公开(公告)日：2006-11-16

申请号：US11492450

申请日：2006-07-25

申请人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian Golec ,  Pan Li ,  Jean-Damien Charrier

发明人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian Golec ,  Pan Li ,  Jean-Damien Charrier

IPC分类号： C07D403/14 ,  A61K31/53 ,  A61K31/497 ,  A61K31/506

CPC分类号： 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

摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least 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; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

公开(公告)号：US07041687B2

公开(公告)日：2006-05-09

申请号：US10350806

申请日：2003-01-23

申请人： Hayley Binch ,  Guy Brenchley ,  Julian M. C. Golec ,  Ronald Knegtel ,  Michael Mortimore ,  Sanjay Patel ,  Alistair Rutherford

发明人： Hayley Binch ,  Guy Brenchley ,  Julian M. C. Golec ,  Ronald Knegtel ,  Michael Mortimore ,  Sanjay Patel ,  Alistair Rutherford

IPC分类号： A61K31/41

CPC分类号： C07D417/12 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

摘要： The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.

摘要翻译： 本发明提供式I化合物或其药学上可接受的衍生物，其中R 1，R 2，V 1，V SUP > 2 和V 3 3如说明书中所述。 这些化合物是蛋白激酶的抑制剂，特别是AKT，PKA，PDK1，p70S6K或ROCK激酶的抑制剂，涉及增殖性和神经变性疾病的哺乳动物蛋白激酶。 本发明还提供包含本发明化合物的药物组合物和利用这些组合物治疗各种疾病的方法。