Core 2 glcnac-t inhibitors

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/704 (2006.01) A61K 31/7048 (2006.01) A61P 9/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2614102

A method of treating a subject in need of therapy for a condition involving detrimental activity of the enzyme core 2 GIcNAc-T is provided, comprising administration of a therapeutically effective amount of an inhibitor of core 2 GIcNAc-T of formula (I) to a patient in need thereof wherein: R1 is H, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6- alkoxy or C1-6 -alkoxy- C1-6-alkyl; R2 is H, - OH or C1-6 alkoxy; S1 and S2 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester thereof.

L'invention concerne un procédé permettant de traiter un patient nécessitant une thérapie d'un état impliquant une activité préjudiciable de l'enzyme GlcNAc-T de structure noyau 2, qui consiste à administrer au patient en question une dose thérapeutiquement efficace d'un inhibiteur de la GlcNAc-T de structure noyau 2 de la formule I, dans laquelle R1 représente H, C1-6alkyle, C1-6 hydroxyalkyle, C1-6- alcoxy ou C1-6 -alcoxy- C1-6-alkyle; R2 représente H, -OH ou C1-6 alcoxy; S1 et S2 sont des fragments de saccharide indépendamment choisis; et Z représente un fragment stéroïde; ou un sel, éther ou ester de celui-ci pharmaceutiquement acceptable.

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