GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人:
DRUMMOND, ALAN HASTINGS,DAVIDSON, ALAN HORNSBY,MOFFAT, DAVID FESTUS CHARLES,DONALD, ALISTAIR DAVID GRAHAM,DAVIES, STEPHEN JOHN
申请号：
CA2934402
公开号：
CA2934402C
申请日:
2009.02.27
申请国别(地区):
CA
年份:
2020
代理人:
摘要：
Covalent conjugates of an .alpha., .alpha.-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 .alpha., .alpha.-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.
