SELECTIVE GLYCOSIDASE INHIBITORS AND THEIR APPLICATION Russian patent published in 2017 - IPC C07H9/06 C07D513/04 A61K31/7056 C12Q1/34 C12Q1/37 

Abstract RU 2625308 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to compound of formula (I) or to pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent H or F; R3 represents OR5 and R4 represents H, or R3 represents H and R4 represents OR5; each of R5 represents H; R6 represents H or OR5; R7 is selected from the group consisting of H and C1-8-alkyl; R8 is selected from the group consisting of C1-8-alkyl optionally substituted with 1-3 fluorine atoms; and each of R9 is independently selected from the group consisting of H, C1-6-alkyl, or two groups of R9 are linked together with the nitrogen atom to which they are attached to form a 4-membered ring containing 3 carbon atoms. Compounds of formula (I) are intended to produce a drug or a pharmaceutical composition having glycoprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase) inhibitory activity. The invention also relates to a method of glycoprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase) selective inhibition in a subject in need thereof, comprising injection of an effective amount of the compound of formula (I) or pharmaceutically acceptable salt thereof to the subject. Compounds of formula (I) are used to treat diseases mediated by glycoprotein 2-acetamido-2-deoxy-β-D-glucopyranosidase (O-GlcNAcase) inhibition.

EFFECT: selective glycosidase inhibitors.

22 cl, 5 tbl, 49 ex

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RU 2 625 308 C2

Authors

Li Tun-Shuan

Makichern Ernest Dzh.

Vokadlo Devid Dzh.

Chzhou Yuansi

Chzhu Yunbao

Selnik Kharold Dzh.

Dates

2017-07-13Published

2012-06-27Filed