2-S-BENZYLSUBSTITUTED PYRIMIDINES AS CRTH2 ANTAGONISTS Russian patent published in 2013 - IPC C07D239/38 A61K31/505 A61P37/08 A61P11/06 A61P19/02 A61P1/00 A61P29/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new 2-S-benzylpyrimidine derivatives having CRTH2 receptor antagonist activity. In formula 1: R¹ means -CO₂H; R^4a and R^4b mean hydrogen; W means -C(O)NR⁷-; R² and R³, each independently mean F; Cl; Br;-NR¹⁰R¹¹ or (C₁-C₆)alkoxy, optionally substituted by 1-3 halogen atoms; R⁵ means hydrogen; R⁶ means (C₁-C₆)alkyl; (C₆-C₁₉)aryl or (5-15)-member heteroaryl containing nitrogen, oxygen or sulphur atoms as heteroatoms, wherein above aryl and heteroaryl are optionally substituted by one or more substitutes specified in a group consisting of halogen; (C₁-C₆)alkyl optionally substituted by 1-3 halogen atoms; and (C₁-C₆)alkoxy optionally substituted by one, two or three halogen atoms; R⁷ means hydrogen; R¹⁰ and R¹¹, each independently mean (C₁-C₆)alkyl; or R¹⁰ and R¹¹, together with N, whereto attached form a 3-8- member saturated or unsaturated ring optionally containing one or more O or S atoms, or one or more additional N atoms in the ring; k is equal to 0; m is equal to 1.

EFFECT: invention also refers to using the above compounds for preparing a drug for treating allergic and inflammatory diseases mediated by CRTH2 receptor activity, such as asthma, atopic dermatitis, allergic conjunctivitis, Churg-Strauss disease, sinusitits, basophilic leukaemia, and recurrent urticaria.

27 cl