PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA Russian patent published in 2018 - IPC C07D473/30 C07D473/28 C07D473/38 C07D473/00 A61K31/52 A61P19/02 A61P11/00 A61P37/00 A61P35/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a novel compound of formula I, or a pharmaceutically acceptable salt or stereoisomer thereof, having properties of a PI3K-alpha inhibitor and relative selectivity for PI3K-delta. In formula I I R¹ is selected from hydrogen, C_1-5alkyl or C_3-8cycloalkyl, where R¹ is optionally substituted with 0, 1 or 2 groups independently selected from hydrogen, fluorine and chlorine; R² is selected from cyclopropyl, isobutyl, 2-methylpropyl, methyl, ethyl, iodine, pyridazinyl, pyrimidinyl, pyrazinyl, pyridinyl, pyrrolidinyl, piperidinyl, ethoxycarbonyl, cyclohexyl, phenyl, quinazolinyl, isoquinolinyl, pyrazolyl, imidazolyl, indolyl, indazolyl, thiazolyl, pyrazolo[1,5-a]pyrimidinyl, 3,6-dihydro-2H-pyranyl, 1H-pyrrolo[2,3-b]pyridinyl, cyclobutyl, 1H-pyrazolo[3,4-b]pyridinyl, pyrrolo[2,3-b]pyridinyl, benzimidazolyl, morpholinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridinyl, 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazolyl, where R² is substituted with 0, 1 or 2 independently selected R³; n is 0, 1, 2, or 3; A is C_3-12cycloalkyl, mono- or bicyclic C_3-7heterocycloalkyl, containing a nitrogen atom as a heteroatom, and C_6-12spirocyclyl containing a nitrogen atom in the ring; L is selected from O, S, SO₂ and -CH₂; K is selected from a bond, O, N((C_1-5)alkyl)_1-2 and -C(O)N(R^b)-(CH₂)_m; R^b is H or C_1-10alkyl; m has the value 0; R³ is independently selected from a fluorine atom, chlorine atom, methyl, ethyl, propyl, methoxy, pyrazolyl, thiazolyl, benzisoxazolyl, pyrazinyl, cyclopropyl, pyridinyl, cyclopropylmethyl, hydroxy, oxo, dimethylamino, morpholinyl, imidazolyl, pyrrolidinyl, piperidinyl, tert-butyl, trifluoromethyl, methoxymethyl, isoxybutylcarboxy, tert-butylcarboxy, phenylcarboxy, hydrogen, methylpropylcarboxy, ethoxycarbonyl and others indicated in the claims, where each R³ is substituted with 0, 1, 2 or 3 substituents R⁴ and each R⁴ is independently selected from methyl, trifluoromethyl, methoxy, amino, dimethylamino, fluorine atom, cyano, oxo, piperazinyl, butenoyl, methylethyl, ethyl, t-butyl, 1,1,3,3-tetramethylbutyl(C_1-10alkyl), chlorine atom, cyclopropyl, difluoromethyl, hydroxymethyl, fluoromethyl, phenyl, tert-butoxycarbonyl, tert-butylcarboxy, ethylcarboxy, pyrazolyl, ethylcarbonyl, thiazolyl and furanyl; R⁴ is substituted with 0, 1 or 2 substituents R⁵ and each substituent R⁵ is independently selected from methyl, hydroxy and fluorine atom.

EFFECT: compounds can be used for the treatment of arthritis, asthma and obstructive airway diseases, autoimmune diseases or disorders, and cancer.

17 cl, 17 tbl, 30 ex