公开(公告)号：US20050004110A1

公开(公告)日：2005-01-06

申请号：US09952878

申请日：2001-09-14

Applicant: David Bebbington ,  Hayley Binch ,  Ronald Knegtel ,  Julian Golec ,  Sanjay Patel ,  Jean- Damien Charrier ,  David Kay ,  Robert Davies

Inventor： David Bebbington ,  Hayley Binch ,  Ronald Knegtel ,  Julian Golec ,  Sanjay Patel ,  Jean- Damien Charrier ,  David Kay ,  Robert Davies

IPC: C07D403/12 ,  A61K31/415 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/00 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P3/14 ,  A61P5/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D239/26 ,  C07D239/36 ,  C07D239/70 ,  C07D239/88 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D475/10 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D491/052 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D521/00 ,  C07

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 compounds of formula III: 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 taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered carbocyclo ring; and 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.

Abstract translation: 本发明描述了式III的新型吡唑化合物：其中环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; R x和R y与它们的插入原子一起形成稠合的，不饱和的或部分不饱和的5-8元碳环; 和R 2和R 2'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：US06653301B2

公开(公告)日：2003-11-25

申请号：US10027001

申请日：2001-12-19

Applicant: David Bebbington ,  Jean-Damien Charrier ,  Robert Davies ,  Julian M. C. Golec ,  David Kay ,  Ronald Knegtel ,  Sanjay Patel

Inventor： David Bebbington ,  Jean-Damien Charrier ,  Robert Davies ,  Julian M. C. Golec ,  David Kay ,  Ronald Knegtel ,  Sanjay Patel

IPC: A61K3133

CPC classification number: 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

Abstract: This invention describes novel pyrazole compounds of formula IIa: 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 and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and 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.

Abstract translation: 本发明描述了式IIa的新型吡唑化合物：其中R 1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; R x和R y与它们的插入原子一起形成具有0-3个杂原子的稠合的，不饱和的或部分不饱和的5-7元环; R 2和R 2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：USD258536S

公开(公告)日：1981-03-10

申请号：US907260

申请日：1978-05-18

Applicant: David Kay

Designer： David Kay

公开(公告)号：US4084442A

公开(公告)日：1978-04-18

申请号：US744895

申请日：1976-11-24

Applicant: David Kay

Inventor： David Kay

IPC: B01F15/00 ,  G01N11/00 ,  G01N33/00 ,  G01N15/00

CPC classification number: B01F15/00207 ,  G01N11/00 ,  G01N2033/0091

Abstract: The end-point of an operation in which the flow properties of particulate material are altered during agitation is determined using a probe inserted into the vessel in which agitation occurs and which deflects when hit by material being agitated and detecting when the amplitude and/or frequency of the deflections of the probe changes to a given level.

Abstract translation: 搅拌期间颗粒材料的流动性质改变的操作的终点是使用插入到容器中的探针来确定的，其中发生搅动，当被搅拌的材料撞击时偏转，并且检测何时振幅和/或频率 探头的偏转变化到给定的水平。