注册 登录  
 加关注
   显示下一条  |  关闭
温馨提示!由于新浪微博认证机制调整,您的新浪微博帐号绑定已过期,请重新绑定!立即重新绑定新浪微博》  |  关闭

zliming2004的博客

新药研发与药物合成

 
 
 

日志

 
 
 
 

Dinaciclib  

2015-06-19 14:13:45|  分类: 合成化学 |  标签: |举报 |字号 订阅

  下载LOFTER 我的照片书  |

Dinaciclib - zliming2004 - zliming2004的博客
 CDK5/p25 Inhibitors
CDK1/Cyclin B Inhibitors
CDK9/Cyclin T1 Inhibitors
CDK2/Cyclin A Inhibitors
SCH-727965 is an apoptosis inducer currently in phase III clinical trials at Merck & Co. for the treatment of refractory chronic lymphocytic leukemia. Phase II clinical trials at Merck & Co. for the treatment of advanced breast cancer, non-small cell lung cancer (NSCLC), acute lymphocytic leukemia, acute myeloid leukemia and for the treatment of mantle cell lymphoma. The National Cancer Institute is also investigating the drug candidate in early clinical trials for the treatment of stage IV melanoma and for the treatment of relapsed or refractory multiple myeloma.

The compound is a novel pyrazolo (1,5-a) pyrimidine which potently and selectively inhibits the cyclin-dependent kinases CDK1, CDK2, CDK5 and CDK9. Inhibition of CDK2/CDK1 in tumor cells leads to cell cycle arrest and apoptosis. To date, SCH-727965 demonstrated activity against a broad panel of tumor cell lines including breast, small cell and non-small cell lung, colon and prostate cancers.

In 2011, orphan drug designation was assigned in the U.S. for the treatment of chronic lymphocytic leukemia.

Phase Organization Condition
Phase IIIMerck & Co.Leukemia, chronic lymphocytic
Phase IINational Cancer Institute (NCI)Melanoma, metastatic
Phase IINational Cancer Institute (NCI)Multiple myeloma

Dinaciclib - zliming2004 - zliming2004的博客
 

Patent NumberApplicantTitleConditionSubject Matter
US 2004209878
US 7119200
JP 2007522220
WO 2005077954
EP 1720882
JP 2010215675
 
Schering Corp.  Pyrazolopyrimidine-derivatives as cyclin dependent kinase inhibitorsDinaciclib - zliming2004 - zliming2004的博客  
Cancer
Dinaciclib - zliming2004 - zliming2004的博客  
Drug Substances
 
EP 2051963
JP 2010501487
US 7786306
WO 2008021509
US 2008051579
 
Schering Corp.  Process for resolving chiral piperidine alcohol and process for synthesis of pyrazolo[1,5-a]pyrimidine derivatives using sameDinaciclib - zliming2004 - zliming2004的博客  
Cancer
Dinaciclib - zliming2004 - zliming2004的博客  
Processes
 
US 2008058518
EP 2057166
JP 2010502607
US 8076479
WO 2008027220
 
Schering Corp.  Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivativesDinaciclib - zliming2004 - zliming2004的博客  
Cancer
Dinaciclib - zliming2004 - zliming2004的博客  
Synthesis
 
  评论这张
 
阅读(105)| 评论(0)
推荐 转载

历史上的今天

在LOFTER的更多文章

评论

<#--最新日志,群博日志--> <#--推荐日志--> <#--引用记录--> <#--博主推荐--> <#--随机阅读--> <#--首页推荐--> <#--历史上的今天--> <#--被推荐日志--> <#--上一篇,下一篇--> <#-- 热度 --> <#-- 网易新闻广告 --> <#--右边模块结构--> <#--评论模块结构--> <#--引用模块结构--> <#--博主发起的投票-->
 
 
 
 
 
 
 
 
 
 
 
 
 
 

页脚

网易公司版权所有 ©1997-2017