PURINE DERIVATIVES AS A RECEPTOR AGONISTS Russian patent published in 2010 - IPC C07D473/34 C07D473/40 C07D473/16 A61K31/52 A61P11/08 

FIELD: chemistry.

SUBSTANCE: invention relates to novel purine derivatives of general formula I in free form or in form of a pharmaceutically acceptable salt which have A_2A agonist properties. In formula I , R¹ denotes a N-bonded 5-6-member heterocyclic group containing 1-4 nitrogen atoms in the ring, which can be optionally substituted with oxo, phenyl or C_1-8-alkyl, optionally substituted with hydroxy; R² is hydrogen or C₁-C₈-alkyl, optionally substituted with hydroxy or 1-2 phenyls possibly substituted with hydroxy or C₁-C₈-alkoxy; R³ is C₂-C₈-alkynyl or C₁-C₈-alkoxycarbonyl, or R³ is amino substituted with C₃-C₈-cycloalkyl, optionally substituted with amino, hydroxy, benzyloxy or NH-C(=O)-NH-R⁶, or R³ is amino substituted with R⁴, -R⁴-benzyl or C₅-C₁₀-mono- or bicarbocyclic group, optionally substituted with hydroxy or C₁-C₈-alkoxycarbonyl, or R³ is aminocarbonyl optionally substituted with R⁵, or R³ is C₁-C₈-alkylamino optionally substituted with hydroxy, R⁵, NH-C(=O)-C₁-C₈-alkyl, -MH-SO₂-C₁-C₈-alkyl, -NH-C(=O)-NH-R⁶ or phenyl, optionally substituted with phenyloxy, or R³ is a N-bonded 5-member heterocyclic group containing 1 nitrogen atom in the ring which may optionally be substituted with amino, C₁-C₈-alkylamino, di(C₁-C₈-alkyl)amino and other groups.

EFFECT: compounds can be useful in treating conditions mediated by activation of the adenosine A_2A receptor, especially inflammatory or obstructive respiratory tract diseases.

9 cl, 5 tbl, 161 ex