PYRIMIDINE HYDRAZIDE COMPOUNDS AS PGDS INHIBITORS Russian patent published in 2012 - IPC C07D239/28 C07D403/12 C07D403/14 C07D413/12 C07D417/14 A61K31/506 A61P11/06 A61P27/14 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted pyrimidine derivatives having PGDS inhibiting properties. In formula (I): (I), R¹ denotes phenyl or a 5- or 6-member heteroaryl containing 1-3 heteroatoms selected from N, O and S, each optionally having one or more of the following independent substitutes: halogen, (C₁-C₆)-alkyl, or (C₁-C₄)-haloalkyl; R₂ denotes hydrogen or (C₁-C₆)-alkyl, which is optionally substituted with one or more halogens; R³ denotes hydrogen, (C₁-C₆)-alkyl or phenyl; R⁴ denotes C₆-cycloalkyl, phenyl, a 6-member heterocyclyl containing one N heteroatom, a 6-member heteroaryl containing one N heteroatom, -C(=O)-NY¹Y², -C(=S)-NY¹Y², or -C(=O)-R⁵, where the phenyl, 6-member heteroaryl or 6-member heterocyclyl group optionally has one or more independent substitutes R⁶, or R³ and R⁴ together with a nitrogen atom with which they are bonded form a 5- or 6-member heterocyclyl containing one or two heteroatoms selected from N, O and S, a 6-member heterocyclenyl containing two or three N heteroatoms, a 5-member monocyclic or 9-member bicyclic heteroaryl containing one to three N heteroatoms, phenylheterocyclyl, where the heterocyclyl is 5- or 6-membered and contains one or two heteroatoms selected from N and O, each optionally having one or more independent substitutes R⁶. Values of R⁵, R⁶, Y¹, Y² are given in the claim. The invention also relates to a pharmaceutical composition containing said compounds.

EFFECT: improved method.

15 cl, 227 ex