发明公开
- 专利标题: SOLUBLE MTOR COMPLEXES AND MODULATORS THEREOF
- 专利标题(中): MTOR复合物调节剂
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申请号: EP09820914.1申请日: 2009-10-16
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公开(公告)号: EP2350053A2公开(公告)日: 2011-08-03
- 发明人: GRAY, Nathanael , CHANG, Jae, Won , ZHANG, Jianming , THOREEN, Carson, C. , KANG, Seong Woo, Anthony , SABATINI, David, M. , LIU, Qingsong
- 申请人: Whitehead Institute For Biomedical Research , Dana-Farber Cancer Institute Inc.
- 申请人地址: Nine Cambridge Center Cambridge, MA 02142 US
- 专利权人: Whitehead Institute For Biomedical Research,Dana-Farber Cancer Institute Inc.
- 当前专利权人: Whitehead Institute For Biomedical Research,Dana-Farber Cancer Institute Inc.
- 当前专利权人地址: Nine Cambridge Center Cambridge, MA 02142 US
- 代理机构: Chapman, Paul William
- 优先权: US185923P 20090610; US196772P 20081020; US106411P 20081017
- 国际公布: WO2010044885 20100422
- 主分类号: C07D401/14
- IPC分类号: C07D401/14 ; C07D403/14 ; C07D487/04 ; C07D487/02 ; A61K31/4162 ; A61P3/00 ; A61P3/04
摘要:
The present invention relates to small molecule modulators of mTORCl and mT0RC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORCl, mT0RC2, and PI3K-related proteins. Novel methods of providing soluble mTORCl and mT0RC2 complexes are discussed, as well as methods of using the soluble complexes in a high- throughput manner to screen for inhibitory compounds.
公开/授权文献
- EP2350053B1 Modulators of MTOR Complexes 公开/授权日:2013-12-11
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