COMPOUNDS AND COMPOSITIONS OF 5-(4-(HALOGENALKOXY)PHENYL)PYRIMIDIN-2-AMINE AS KINASE INHIBITORS Russian patent published in 2012 - IPC C07D239/42 C07D401/12 C07D403/12 C07D413/12 A61K31/505 A61K31/506 A61P1/00 A61P7/04 A61P11/06 

FIELD: medicine, pharmaceutics.

SUBSTANCE: in formula (1): R¹ means haloalkyl containing 1-6 fluorine atoms; R² means C₁-C₆alkyl or halogen; R³ means -L-NR⁴R⁵, -X-NR-C(O)R⁸ or -X-NR-C(O)NR⁴R⁵ wherein L means -X-C(O), -(CR₂)_j, -O(CR₂)_1-4 or and X means (CR₂)_j or [C(R)(CR₂OR)]; R⁴ and R⁵ independently mean H, C₁-C₆alkyl, halogen-substituted C₁-C₆alkyl, hydroxy group-substituted C₁-C₆alkyl, or (CR₂)_k-R⁶; R⁸ independently means (CR₂)_k-R⁶ or C₁-C₆alkyl, or halogen-substituted C₁-C₆alkyl; R⁷ means H; alternatively, R⁴ and R⁵ together with N atom in each NR⁴ R⁵ form a 4-7-member heterocyclic ring containing 1 -2 heteroatoms independently specified in N and O substituted by 0-3 groups R¹¹; R¹¹ means R⁸, (CR₂)_k-OR⁷, CO₂R⁷, (CR₂)_k-C(O)-(CR₂)_k-R⁸, (CR₂)_kC(O)NR⁷R⁷ or (CR₂)_kS(O)_1-2R⁸; each R means H or C₁-C₆alkyl; each k is equal to 0-6; and j and m are independently equal to 0-4; provided R¹ does not mean trifluoromethoxygroup, provided R³ means C(O)NH₂, C(O)NR¹²R¹³; wherein R¹² and R¹³ together form piperazinyl; the values of the radical R⁶ are presented in the patent claim. The invention also refers to the pharmaceutical composition containing said compounds.

EFFECT: producing new 5-(4-(halogenalkoxy)phenyl)pyrimidin-2-amine derivatives showing c-kit, PDGFRα, PDGFRβ kinase inhibitory activity, optionally in the form of isomers or pharmaceutically acceptable salts.

12 cl, 77 ex, 1 tbl