公开(公告)号：US20190231887A1

公开(公告)日：2019-08-01

申请号：US16255947

申请日：2019-01-24

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Alan Hornsby DAVIDSON ,  Alan Hastings DRUMMOND ,  Lindsey Ann NEEDHAM

IPC: A61K47/54 ,  C07D277/46 ,  C07D471/04 ,  C07C237/22 ,  C07D215/233 ,  C07D213/73

CPC classification number: A61K47/542 ,  A61K47/54 ,  C07C237/22 ,  C07C2601/08 ,  C07D213/73 ,  C07D215/233 ,  C07D277/46 ,  C07D471/04

Abstract: Covalent conjugation of an alpha amino acid ester to 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, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

公开(公告)号：US20210361772A1

公开(公告)日：2021-11-25

申请号：US17326470

申请日：2021-05-21

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Alan Hornsby DAVIDSON ,  Alan Hastings DRUMMOND ,  Lindsey Ann NEEDHAM

IPC: A61K47/54 ,  C07C237/22 ,  C07D213/73 ,  C07D215/233 ,  C07D277/46 ,  C07D471/04

Abstract: Covalent conjugation of an alpha amino acid ester to 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, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.