MACROCYCLIC PYRIDAZINONE DERIVATIVES Russian patent published in 2018 - IPC C07D471/18 C07D487/08 C07D487/18 C07D487/22 C07D498/18 A61K31/504 A61P35/00 A61P37/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to compounds of formula (I) and pharmaceutically acceptable salts and stereoisomers thereof, which are inhibitors of IRAK. In the formula (I), R1 and R3, each independently of one another, mean H, (CH₂)_pCON(R5)₂, OA, Hal, COOH, COOA, (CH₂)_pNHCOA, (CH₂)_PHet1, (CH₂)_pNR2R5 or OH; R2 is H or a linear or branched alkyl of 1, 2 or 3 carbon atoms; R4 is H or A; R5 is H or a linear or branched alkyl of 1, 2 or 3 carbon atoms; Z is absent or means Ar-diyl or Het-diyl; L is (CH₂)_n, where one or two CH₂ groups can be replaced by O and/or CH=CH groups and/or where one or two H atoms can be replaced by OR2 or NR2R5; Ar-diyl is 1,2-, 1,3- or 1,4-phenylene optionally substituted by 1 to 5 groups independently selected from Hal, OH, OA, Het2 and/or A; Het-diyl means an unsaturated, saturated or aromatic 5- or 6-membered heterocycle having from 1 to 2 N, O and/or S atoms which may be unsubstituted or mono-, di- or trisubstituted by O-A and/or A; A is a linear or branched alkyl having from 1 to 10 carbon atoms in which one or two non-adjacent CH₂ groups can be replaced by O; Het1 is morpholinyl; Het2 is morpholinyl; Hal is F, Cl, Br, I; n is 1, 2, 3, 4, 5, or 6; p means 0, 1 or 2. (I).

EFFECT: invention also relates to particular compounds of formula (I), a pharmaceutical composition containing said compounds, and a method of synthesizing them.

13 cl, 1 tbl, 45 ex