公开(公告)号：WO2012025164A1

公开(公告)日：2012-03-01

申请号：PCT/EP2010/062594

申请日：2010-08-27

Applicant: NOVARTIS AG ,  BROOKS, Clinton, A. ,  CHEN, Christine, Hiu-Tung ,  CHO, Young Shin ,  JIANG, Lei ,  LIU, Gang ,  SHULTZ, Michael

Inventor： BROOKS, Clinton, A. ,  CHEN, Christine, Hiu-Tung ,  CHO, Young Shin ,  JIANG, Lei ,  LIU, Gang ,  SHULTZ, Michael

IPC: C07D207/06 ,  C07D403/06 ,  C07D403/14 ,  C07D407/14 ,  C07D413/06 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4245 ,  A61K31/4015 ,  A61K31/4439 ,  A61K31/4427 ,  A61P29/00 ,  A61P9/00

CPC classification number: C07D413/06 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4245 ,  A61K31/4427 ,  A61K31/4439 ,  C07D207/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D407/14

Abstract: The present teachings relate to compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula (I) and methods of use compounds of Formula (I) in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.

Abstract translation: 本发明涉及式（I）的化合物及其药学上可接受的盐，水合物，酯和前药，其中R 1，R 2，R 3，R 4，R 5，环A和Z如本文所定义。 本教导还提供制备式（I）化合物的方法和使用式（I）化合物治疗全部或部分由脱乙酰酶介导的病理状况或病症的方法。

公开(公告)号：WO2010020675A1

公开(公告)日：2010-02-25

申请号：PCT/EP2009/060793

申请日：2009-08-20

Applicant: NOVARTIS AG ,  ASTEX THERAPEUTICS LTD. ,  BESONG, Gilbert ,  BRAIN, Christopher Thomas ,  BROOKS, Clinton A. ,  CONGREVE, Miles Stuart ,  DAGOSTIN, Claudio ,  HE, Guo ,  HOU, Ying ,  HOWARD, Steven ,  LI, Yue ,  LU, Yipin ,  MORTENSON, Paul ,  SMITH, Troy ,  SUNG, Moo ,  WOODHEAD, Steven ,  WRONA, Wojciech

Inventor： BESONG, Gilbert ,  BRAIN, Christopher Thomas ,  BROOKS, Clinton A. ,  CONGREVE, Miles Stuart ,  DAGOSTIN, Claudio ,  HE, Guo ,  HOU, Ying ,  HOWARD, Steven ,  LI, Yue ,  LU, Yipin ,  MORTENSON, Paul ,  SMITH, Troy ,  SUNG, Moo ,  WOODHEAD, Steven ,  WRONA, Wojciech

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D487/08

Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.

Abstract translation: 所公开的化合物涉及蛋白激酶相关病症的治疗和疗法。 还需要可用于治疗或预防或改善癌症，移植排斥和自身免疫性疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物调节蛋白激酶如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。