THIAZOLPYRIMIDINES Russian patent published in 2017 - IPC C07D513/04 A61K31/517 A61P11/06 A61P19/02 A61P29/00 A61P37/00 

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: C_1-6-haloalkyl, C_1-6-alkoxy group, C_1-6-alkylsulphonyl or R^1'; R^1' 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 R^1ʺ as substitute; R^1ʺ is C_1-6-alkyl; B is phenyl, pyridinyl, pyrrolidinyl or piperidinyl; X is OH, C_1-6-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 C_1-6-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, C_1-6-alkyl, C_1-6-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 C_1-6-alkyl groups as substitute, oxo groups or SH; Y⁴ is C_1-6-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 ex