PYRIMIDINE DERIVATIVES WITH ANTAGONIST PROPERTIES TOWARDS CRTH2(VERSIONS) Russian patent published in 2009 - IPC C07D239/42 C07D401/12 C07D405/12 C07D403/12 C07D403/04 C07D403/14 C07D413/04 C07D239/48 A61K31/505 A61K31/506 A61K31/5377 A61P11/06 A61P27/14 A61P37/08 

FIELD: chemistry.

SUBSTANCE: invention relates to new pyrimidine derivatives with general formula (I), their tautomeric or stereoisomeric form, in free form, in form of pharmaceutically acceptable salt or C_1-6alkyl ester which are effective antagonists of CRTH2 (G-protein-associated chemoattractant receptor, ex prone on Th2 cells) and can be used for preventing and treating diseases related to CRTH2 activity, particularly in treatment of allergic diseases such as asthma, allergic rhinitis, atopic dermatitis, diseases related to eosinophil. In formula (I) R¹ is hydrogen, or in which n is an integer from 0 to 6; -Q₁- is -NH-, -N(C_1-6alkyl)- or -O; Y is hydrogen, C_1-6alkyl, C_3-6cycloalkyl, optionally substituted with C_1-6alkyl, C_3-6cycloalkyl, condensed with a benzene ring, phenyl, naphthyl or 5-6-member heteroaryl, possibly condensed with a benzene ring, and containing at least one heteroatom, chosen from a group consisting of oxygen and nitrogen, where the said phenyl, naphthyl or heteroaryl are optionally substituted on the displaceable position with one or several substitutes, chosen from a group consisting of cyano, halogen, nitro, guanidine, pyrroyl, sulfamoyl, phenyloxy, phenyl, di(C_1-6)alkylamino, C_1-6alkanoylamino, C_1-6alkyl, optionally mono-, di- or tri-substituted with halogen, C_1-6alkoxy, optionally mono-, di- or tri-substituted with halogen and C_1-6alkylthio, optionally mono-, di- or tri-substituted with halogen; or phenyl, condensed with 1,3-dioxolane; R² is hydrogen or C_1-6alkyl; R³ is a halogen, C_1-6alkoxy, optionally mono-, di- or tri-substituted with halogen, or , R^3a and R^3b are independently C_3-8cycloalkyl or C_1-6alkyl, this C_1-6alkyl is optionally substituted with hydroxyl, carboxy, C_3-6cycloalkylcarbamoyl, C_5-6heterocyclocarbonyl containing a heteroatom in form of nitrogen, or C_1-6alkoxy, q is an integer from 1 to 3; R^3c is hydrogen, hydroxyl or carboxy; Xa is -O-; R⁴ is hydrogen, halogen, di(C_1-6alkyl) amino or C_1-6alkyl, optionally substituted C_1-6alkoxy or mono- , di- or tri-substituted with halogen; R⁵ is hydrogen or C_1-6alkyl; and R⁶ is carboxy, carboxamide, nitrile or tetrazolyl.

EFFECT: wider field of use of compounds.

32 cl, 9 tbl, 13 ex