N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS Russian patent published in 2018 - IPC C07D471/04 A61K31/437 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt or stereoisomer thereof, which have the properties of a Janus kinase inhibitor (JAK). In formula I A is selected from phenyl and heteroaryl; X is independently selected from CH₂ and O, wherein at least one X is other than CH₂; n is equal to 0; m is equal to 0, 1, 2, 3 or 4; p is equal to 2, 3, 4 or 5; R¹ is selected from halogen, oxo (=O), C_0-10alkyliminoC_0-10alkyl, C_1-10alkyl(oxy)_0-1(carbonyl)_0-1C_0-10alkyl, heteroarylC_0-10alkyl(oxy)_0-1(carbonyl)_0-1C_0-10alkyl, (C_3-12)heterocycloalkylC_0-10alkyl(oxy)_0-1(carbonyl)_0-1C_0-10alkyl, C_0-10alkyl(oxy)_0-1(carbonyl)_0-1aminoC_0-10alkyl, C_3-12cycloalkylC_0-10alkyl(oxy)_0-1(carbonyl)_0-1aminoC_0-10alkyl, C_0-10alkylamino(oxy)_0-1(carbonyl)_0-1C_0-10alkyl, C_3-12cycloalkylamino(hydroxy)_0-1(carbonyl)_0-1C_0-10alkyl, C_0-10alkylsulfonylC_0-10alkyl, (C_3-12)heterocycloalkylC_0-10alkylsulfonylC_0-10alkyl, (C_0-10alkyl)_1-2amino, -SO₂NH₂, -SO₂NH(C_1-10alkyl), -SO₂N(C_1-10alkyl)₂, C_1-10alkylsulfinylC_0-10alkyl, thioC_1-10alkyl, hydroxy, -(C_1-10alkyl)OH, -C_0-10alkylalkoxy, cyano, (C_1-6alkyl)cyano and C_1-6haloalkyl. Invention also relates to a pharmaceutical composition containing the above compounds. .

EFFECT: proposed N-(2-cyano heterocyclyl)pyrazolo pyridones as the Janus kinase inhibitors.

7 cl, 10 tbl, 113 ex