Alan Hastings Drummond,Alan Hornsby Davidson,David Festus Charles Moffat,Alastair David Graham Donald,Stephen John Davies,Margaret Struthers Drummond
申请号:
US15017853
公开号:
US20160151509A1
申请日:
2016.02.08
申请国别(地区):
US
年份:
2016
代理人:
摘要:
Covalent conjugates of an α,α-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the α,α-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.