Enzyme and receptor modulation

Details Enzyme and receptor modulation Enzyme and receptor modulation

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2717020

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.

L'invention concerne des conjugués covalents d'un ester de glycine a,a-disubstitué et un modulateur de l'activité d'un enzyme intracellulaire cible ou d'un récepteur. Le groupe ester du conjugué est hydrolysable par au moins un enzyme carboxylestérase intracellulaire à l'acide correspondant et l'ester de glycine a,a-disubstitué est conjugué au modulateur à une position à distance de l'interface de liaison entre l'inhibiteur et l'enzyme cible ou le récepteur entre dans les cellules et le produit d'hydrolyse acide actif s'accumule dans les cellules.

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