President And Fellows Of Harvard College;Shanghai Institute Of Organic Chemistry
发明人:
Dawei MA,Junli Liu,Junyng Yuan,Lihong Zhang
申请号:
BR112012001316
公开号:
BR112012001316A2
申请日:
2010.07.21
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity. (I)