GERMANN Jokhannes Kornelius (US),ГЕРМАНН Йоханнес Корнелиус (US),LOURI, DZH. Li Edvin (US),ЛОУРИ, ДЖ. Ли Эдвин (US),LUKAS Metyu S. (US),ЛУКАС Мэтью С. (US),LYUK Kin-Chun Tomas (US),ЛЮК Кин-Чунь Томас,GERMANN Jokhannes Kornelius,ГЕРМАНН Йоханнес Корнелиус,LOURI, DZH. Li Edvin,ЛОУРИ, ДЖ. Ли Эдвин,LUKAS Metyu S.,ЛУКАС Мэтью С.,LYUK Kin-Chun Tomas,PEDILLA Fernando,ПЭДИЛЛА Фернандо,V
申请号：
RU2013145299
公开号：
RU0002610840C2
申请日:
2012.03.26
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmaceutics.SUBSTANCE: invention relates to compound of formula I, where R1 is phenyl optionally including from 1 to 3 of following groups as substitutes: C1-6-haloalkyl, C1-6-alkoxy group, C1-6-alkylsulphonyl or R1'； R1' represents pyrrolidinyl or spiroheterocycloalkyl selected from 8-oxy-3-azabicyclo[3.2.1]octane derivatives or 2-oxy-6-azaspiro[3.3]heptane, each of them optionally contains R1ʺ as substitute； R1ʺ is C1-6-alkyl； B is phenyl, pyridinyl, pyrrolidinyl or piperidinyl； X is OH, C1-6-alkoxy group, NHC(=O)Y, C(=O)NH2, C(=O)NHY, C(=O)X', C(=O)Y, CH2NHY, CH2CH2Y, CF=CHY, CH=CHY, CH2OH, C(=O)NHCH2CH2N(CH3)2 or C(=O)NHCH2CH2Y； X' is OH or C1-6-alkoxy group； Y is heterocycloalkyl, consisting of one ring containing from 5 to 7 ring atoms and containing 1 or 2 N atoms, phenyl or monocyclic or bicyclic heteroaryl containing from 6 to 9 ring atoms, containing at least one aromatic or partially unsaturated ring containing from 5 to 6 ring atoms including 1 or 2 N atoms, each of them optionally contains one or two substitutes Y3； Y3 is hydroxy group, C1-6-alkyl, C1-6-alkoxy group, oxo group, amino group, amide group, C(=O)NH(CH3), C(=O)OH, C(=O)OY4 or heteroaryl, selected from oxadiazolyl or triazolyl, possibly containing one or two C1-6-alkyl groups as substitute, oxo groups or SH； Y4 is C1-6-alkyl； or its pharmaceutically acceptable salts. Invention also relates to pharmaceutical composition with inhibiting activity in relation to splenic tyrosine kinase (SYK), including therapeutically effective amount of compound of formula I, mixed with at least one pharmaceutically acceptable carrier, excipient or thinner.EFFECT: thiazolpyrimidines effective in treating disorders associated with SYK.14 cl, 2 tbl, 68 exИзобретение относится к соединению формулы I, в которой R1 представляет собой фенил, возможно, содержащий в качестве заместителя от 1 до 3-х следующих групп: С1-6-галогеналкил, С1-6-алкоксигруппа, С1-6-алкилсульфонил или R1'； R1' представляет собой пиррол
