ALEKTOS TERAPYUTIKS INK.;MERK SHARP END DOME KORP.
发明人:
LYU Kun (US),ЛЮ Кунь (US),SELNIK KHarold Dzh. (US),СЕЛНИК Харолд Дж. (US),CHAN TSzian (CN),ЧАН Цзиан (CN),MAKICHERN Ernest Dzh. (CA),МАКИЧЕРН Эрнест Дж. (CA),MU CHanvej (CN),МУ Чанвэй (CN),SHI Fen (CN,LYU KUN,ЛЮ Кунь,SELNIK KHAROLD DZH.,СЕЛНИК Харолд Дж.,CHAN TSZIAN,ЧАН Цзиан,MAKICHERN ERNEST DZH.,МАКИЧЕРН Эрнест Дж.,MU CHANVEJ,МУ Чанвэй,SHI FEN,ШИ Фэн,VOKADLO DEVID DZH.,ВОКАДЛО Дэвид Дж.,VAN YAODE
申请号：
RU2013126531/04
公开号：
RU0002592285C2
申请日:
2011.11.08
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, where each R represents H； R1 and R2 are independently selected from a group consisting of H, C1-6alkyl, C2-6alkenyl, C1-6alkoxy and -(CH2)n-cyclopropyl, where n equals 1 or 2； or R1 and R2 can be bonded together with a nitrogen atom to which they are bonded to form azetidine, pyrrolidine or isoxazolidine, where said C1-6alkyl is optionally substituted by fluorine or hydroxy； R3 is selected from a group consisting of C1-8alkyl, C2-8alkenyl, C3-6cycloalkyl, phenyl and pyridine, each optionally substituted with 1-3 substitutes selected from fluorine and OH； R4 is selected from a group consisting of H, F or C1-8alkyl； or R3 and R4 and a carbon atom to which they are bonded, can be combined together to form vinyl or 3-7-membered carbocyclic ring, wherein said 3-7-member carbocyclic ring optionally contains a double bond； and R5 is selected from H, F and OH； provided that when R4 represents F while R5 is other than OH. Invention also relates to specific derivatives of pirano[3,2d]thiazole. Disclosed compounds are intended for producing a pharmaceutical composition possessing inhibitory activity on O-GlcNAcase, containing an active ingredient in an effective amount of compound or its pharmaceutically acceptable salt in combination with pharmaceutically acceptable carrier.EFFECT: technical result is a compound for selective inhibition of glycosidase.15 cl, 1 tbl, 218 exИзобретение относится к соединению формулы (I) или его фармацевтически приемлемой соли, где каждый R представляет собой Н； R1 и R2 независимо выбраны из группы, состоящей из Н, С1-6алкила, С2-6алкенила, С1-6алкокси и -(СН2)n-циклопропила, где n равен 1 или 2； или R1 и R2 могут быть соединены вместе с атомом азота, к которому они присоединены, с образованием азетидина, пирролидина или изоксазолидина, где указанный С1-6алкил необязательно замещен фтором или гидрокси； R3 выбран из группы, со
