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PAK1-Activation Blocking Compounds, Preparation Thereof and Methods of Use
专利权人:
Hiroshi Maruta
发明人:
Hiroshi Maruta,Hideaki Takahashi,Yoshihiro Uto,Binh Cao Quan Ngyuen,Pham Thi Be Tu,Shinkichi Tawata
申请号:
US15364416
公开号:
US20170224830A1
申请日:
2016.11.30
申请国别(地区):
US
年份:
2017
代理人:
摘要:
The present invention relates to a PAK1 blocking compound having a much higher bioavailability and cell permeability than traditional herbal PAK1 blockers or synthetic PAK1 blockers, and the uses thereof for treating cancer or other PAK1 dependent diseases or disorders. This PAK1 blocking compound comprises an ester of an acidic PAK1 blocker, or a pharmaceutically acceptable salt thereof. This PAK1-blocking ester may be prepared by esterifying a PAK1 blocker starting material with an alcohol; and treating the esterified PAK1 blocker with an aromatic azide to generate a 1,2,3-triazolyl derivative.
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