NEW SUBSTITUTED 8-HETEROARYLXANTINES AND BASED PHARMACEUTICAL COMPOSITION Russian patent published in 2009 - IPC C07D473/06 C07D519/00 C07D473/08 A61K31/519 A61K31/522 A61P11/06 

FIELD: chemistry.

SUBSTANCE: present invention refers to substituted 8-heteroarylzantines of general formula where R represents hydrogen, (C₁-C₅)alkyl or halogen(C₁-C₈)alkyl; R¹ is chosen from (C₃-C₆)cycloalkyl or (C₃-C₆)cycloalkyl(C₁-C₄)alkyl-; R² is chosen from (C₁-C₈)alkyl, (C₃-C₈)alkenyl, (C₃-C₈)alkinyl, (C₃-C₈)cycloalkyl, (C₃-C₈)cycloalkyl(C₁-C₈)alkyl- or (C₆-C₁₀)aryl(C₁-C₈)alkyl-; X represents 3-pyridyl substituted in 6th position with Z; Z represents -NR⁴R⁵ or (C₄-C₁₀)heterocycle where heterocycle is optionally substituted with 1, 2, 3 or 4 substitutes independently chosen from (C₁-C₈)alkyl; each Z¹ independently represents halogen or -NR⁷R⁸; R⁵ is chosen from -C(O)R⁶, -CO₂R⁶ or -C(O)NHR⁷; R⁴ is chosen from hydrogen, (C₁-C₈)alkyl, (C₃-C₈)cycloalkyl, (C₃-C₈)cycloalkyl(C₁-C₈)alkyl-, (C₃-C₁₀)heterocycle(C₁-C₈)alkyl-, (C₆-C₁₀)aryl, (C₆-C₁₀)aryl(C₁-C₈)alkyl-, (C₅-C₁₀)heteroaryl, (C₅-C₁₀)heteroaryl(C₁-C₈)alkyl-, -((CH₂)_2-4)Y)q-(CH₂)_2-4-X¹, -C(O)R⁶, -CO₂R⁶ or -C(O)NR⁷R⁸; or R⁴ and R⁵ together with atoms whereto attached form saturated mono-or bicyclic ring with 5, 6, 7 or 8 ring atoms and optionally containing 1 or 2 heteroatoms chosen of non-peroxide oxy (-0-) and amine -N(R⁹)- in the ring where the ring is optionally substituted by 1, 2, 3 or 4 substitutes independently chosen from -C(O)R^a and -C(O)NR^bR^c; X¹ represents -OR⁶; and Y represents oxy (-O-); where alkyl, alkenyl, cycloalkyl, alkinyl, aryl, heterocyclic or hetero aryl groups from R¹, R², R³, R⁴ and R⁵ groups are optionally substituted by one or more substitutes independently chosen from (C₁-C₈)alkyl, -OR^a, (C₆-C₁₀)aryl, hydroxy(C₁-C₈)alkyl and R^bR^cN(C₁-C₈)alkyl; where R⁶ represents (C₁-C₈)alkyl or (C₄-C₁₀)heteroaryl; where heteroaryl is optionally substituted by 1, 2, 3 or 4 substitutes independently chosen from halogen, -OR^a and halogen(C₁-C₈)alkyl; where R₇, R₈ and R₉ independently represent (C₁-C₈)alkyl, R^aO(C₁-C₈)alkyl, (C₆-C₁₀)aryl or (C₄-C₁₀)heteroaryl; where heteroaryl or aryl are optionally substituted by 1, 2, 3 or 4 substitutes independently chosen from halogen and -OR^a; Ra represents hydrogen or (C₁-C₆)alkyl; each R^b and R^c independently represents hydrogen or (C₆-C₁₀)aryl; and where n is equal to 0, 1 or 2; and q is equal to 1; or its pharmaceutically acceptable salt. In addition, the invention concerns pharmaceutical composition based on compound of formula I.

EFFECT: new substituted 8-heteroarylxantines are selective antagonists of A_2B adenosine receptors.

38 cl, 1 tbl, 1 ex