N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS Russian patent published in 2015 - IPC C07D473/00 C07D471/04 C07D519/04 A61K31/52 A61K31/522 A61P35/00 A61P29/00 A61P37/00 A61P19/02 A61P37/06 A61P17/06 A61P3/10 A61P27/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel N-containing heteroaryl derivatives of formula I or II or their pharmaceutically acceptable salts, which possess properties of JAK kinase, in particular JAK3, and can be applied for treating such diseases as asthma and chronic obstructive pulmonary disease (COPD). In formulae A represents carbon and B represents nitrogen or A represents nitrogen and B represents carbon; W represents CH or N; R₁ and R₂, independently represent hydrogen, C_1-4alkyl, halogenC_1-4alkyl, -CN; R₃ represents C_1-4alkyl, R₉-C_1-4alkyl, Cy₁, where Cy₁ is optionally substituted with one or several substituents R₁₀; R₄ represents hydrogen, C_1-4alkyl, R₁₂R₇N-C₀alkyl, where one of R₇ and R₁₂ represents hydrogen, and the other represents C_1-4alkyl or group R₁₃, which is selected from C_1-5alkyl, Cy₂-C₀alkyl; R₅ represents hydrogen; R₆ represents hydrogen, C_1-4alkyl, C_1-4alkoxyC_1-4alkyl, hydroxyC_1-4alkyl, R₁₂R₇N-C_1-4alkyl, R₁₆CO-C₀alkyl, Cy₁; R₇ represents hydrogen or C_1-4alkyl; R₉ represents halogen, -CN, -CONR₇R₁₂, -COR₁₃, CO₂R₁₂, -OR₁₂, -SO₂R₁₃, -SO₂NR₇R₁₂, -NR₇R₁₂, -NR₇COR₁₂; R₁₀ represents C_1-4alkyl or R₉-C_0-4alkyl; R₁₁ represents C_1-4alkyl, halogen, -CN, -NR₇R₁₄; R₁₂ represents hydrogen or R₁₃; R₁₃ represents C_1-5alkyl, hydroxyC_1-4alkyl, cyanoC_1-4alkyl, Cy₂-C₀alkyl or R₁₄R₇N-C_1-4alkyl; where Cy₂ is optionally substituted with one or several constituents R₁₁; R₁₄ represents hydrogen or C_1-4alkyl; R₁₆ represents C_1-4alkyl, halogenC_1-4alkyl, C_1-4alkoxyC_1-4alkyl, hydroxyC_1-4alkyl or cyanoC_1-4alkyl; Cy₁ represents monocyclic carbocyclic unsaturated or saturated ring, selected from C₃-C₆cycloalkyl, phenyl, or saturated monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or partially unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R₁₁, where said ring is bound with the remaining part of molecule via any available C atom, and where one or several ring C or S atoms are optionally oxidised with formation of CO or SO₂; and Cy₂ represents monocyclic carbocyclic unsaturated ring, selected from C₃-C₆cycloalkyl, or aromatic monocyclic 4-6-membered heterocyclic ring, containing from 1 to 2 heteroatoms, selected from N and S, or unsaturated 10-membered bicyclic heterocyclic ring, containing oxygen atom as heteroatom, which can be substituted with group R₁₁, where said ring is bound with the remaining part of molecule via any available atom C or N.

EFFECT: obtaining novel heteroaryl derivatives.

27 cl, 41 ex