The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 02, 2017
Filed:
Feb. 08, 2016
Enzyme and receptor modulation using covalent conjugates of alpha,alpha-disubstituted glycine esters
Glaxosmithkline Intellectual Property Development Limited, Brenford, Middlesex, GB;
Alan Hornsby Davidson, Abingdon, GB;
David Festus Charles Moffat, Abingdon, GB;
Alastair David Graham Donald, Oxfordshire, GB;
Stephen John Davies, Abingdon, GB;
GlaxoSmithKline Intellectual Property Development Limited, Brentford, Middlesex, GB;
Abstract
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, as in the following compound: