PEVARELLO Paolo (IT),ПЕВАРЕЛЛО Паоло (IT),LOHMER Stefan (IT),ЛОМЕР Стефан (IT),LIBERATI Chiara (IT),ЛИБЕРАТИ Кьяра (IT),SENECI Pierfausto (IT),СЕНЕЧИ Пьерфаусто (IT),PESENTI Cristina (IT),ПЕСЕНТИ Крис
申请号：
RU2016131689
公开号：
RU0002701858C1
申请日:
2015.02.04
申请国别(地区):
RU
年份:
2019
代理人:
摘要：
FIELD: medicine； pharmaceuticals.SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, including any stereochemically isomeric form thereof, where n equals 1 or 2； Y is oxygen or sulphur； each of R1 and R2 is independently selected from a group consisting of hydrogen, deuterium, C1-C4alkyl optionally substituted with hydroxy or halogen, such as hydroxymethyl, fluoromethyl, difluoromethyl, trifluoromethyl, C3-C6cycloalkyl optionally substituted with hydroxy or halogen, or C1-C4alkyloxy； each of R3 and R4 is independently selected from a group consisting of hydrogen, halogen, C1-C4alkyl, C1-C4alkyloxy, NR9R10, where R9 and R10 independently represent hydrogen or C1-C4alkyl, or 1,2-thiazolidine-1,1-dione； or two groups R3 or group R3 and R4 together form a six-member heterocyclic ring containing a nitrogen atom； R5 is selected from hydrogen, halogen or represents a heterocyclic ring selected from pyrimidin-2-yl, pyridin-2-yl or pyrazin-2-yl optionally substituted with halogen, C1-C4alkyl； R7 is hydrogen or C1-C4alkyl； radical of formula (a) is optionally substituted azetidine, piperidine, morpholine, oxazepane or 1,2,3,4-tetrahydroisoquinoline ring, where each of R6 is independently selected from a group consisting of hydrogen, halogen, C3-C6 spirocycloalkyl, phenyl, pyrazolyl, phenoxy or benzyloxy, where the phenyl or pyrazolyl group is optionally substituted with halogen, C1-C4alkyl, fluoromethyl, difluoromethyl, trifluoromethyl., (a).EFFECT: compounds of formula (I) have P2X7 receptor antagonist properties.15 cl, 1 dwg, 2 tbl, 26 exИзобретение относится к соединению формулы (I) или его фармацевтически приемлемой соли, включая их любую стереохимически изомерную форму, где n равно 1 или 2； Y представляет собой кислород или серу； каждый из R1 и R2 независимо выбран из группы, состоящей из водорода, дейтерия, С1-С4алкила, возможно замещенного гидрокси или галогеном, такого как гидроксиметил, фторметил, дифторметил, три
