Covalent conjugates of alpha, alpha-disubstituted glycine esters and a modulator of the activity of a target intracellular enzyme or receptor, their preparation and uses thereof
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人:
申请号：
IL20753710
公开号：
IL207537A
申请日:
2010.08.11
申请国别(地区):
IL
年份:
2016
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.
