公开(公告)号：EP2350053B1

公开(公告)日：2013-12-11

申请号：EP09820914.1

申请日：2009-10-16

申请人： Whitehead Institute For Biomedical Research ,  Dana-Farber Cancer Institute, Inc.

发明人： GRAY, Nathanael ,  CHANG, Jae, Won ,  ZHANG, Jianming ,  THOREEN, Carson, C. ,  KANG, Seong Woo, Anthony ,  SABATINI, David, M. ,  LIU, Qingsong

IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D487/02 ,  A61K31/4162 ,  A61P3/00 ,  A61P3/04 ,  C07D498/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D498/04 ,  C07D519/00

公开(公告)号：EP2350053A2

公开(公告)日：2011-08-03

申请号：EP09820914.1

申请日：2009-10-16

申请人： Whitehead Institute For Biomedical Research ,  Dana-Farber Cancer Institute Inc.

发明人： GRAY, Nathanael ,  CHANG, Jae, Won ,  ZHANG, Jianming ,  THOREEN, Carson, C. ,  KANG, Seong Woo, Anthony ,  SABATINI, David, M. ,  LIU, Qingsong

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  C07D487/02 ,  A61K31/4162 ,  A61P3/00 ,  A61P3/04

CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D498/04 ,  C07D519/00

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.