ALAN HASTINGS DRUMMOND,ALAN HORNSBY DAVIDSON,DAVID FESTUS CHARLES MOFFAT,ALISTAIR DAVID GRAHAM DONALD,STEPHEN JOHN DAVIES
申请号:
BRPI0908893
公开号:
BRPI0908893A2
申请日:
2009.02.27
申请国别(地区):
BR
年份:
2015
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.