MACROCYCLIC COMPOUNDS AS IRAK1/4 INHIBITORS AND USE THEREOF Russian patent published in 2020 - IPC C07D471/22 C07D487/18 C07D498/22 C07D513/22 A61K31/395 A61K31/439 A61K31/4523 A61P19/02 A61P35/00 

Abstract RU 2730016 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention refers to a compound of formula I or its pharmaceutically acceptable salt. In formula I ring A is ; ring B is phenyl or pyridinyl; ring C is pyrazolyl, optionally substituted with one substitute selected from methyl, tetrahydropyran-4-yl, piperidin-4-yl, 1-methanesulphonylpiperidin-4-yl, 1-(2,2-difluorocyclopropanecarbonyl) piperidin-4-yl, 1-(N-cyclopropyl)carboxamidopiperidin-4-yl, 1-[2-(dimethylamino)ethyl]piperidin-4-yl, 1-(2-hydroxyethyl)piperidin-4-yl and 1-tert-butoxycarbonylpiperidin-4-yl; X is absent, -CH=CH-, -C≡C-, -O-, -S-, SO2-, SO-, -CO2-, -C(O)N(R)-, OC(O)N(R)- or -N(R)-; Y is absent or is divalent 3–7-member heterocyclic ring containing 1–2 heteroatoms independently selected from nitrogen and oxygen, which is optionally substituted with 1–2 R groups; each R independently represents hydrogen, C1-6 aliphatic group or -OH; Ra is H; Rb is H; n is equal to 1, 2, 3, 4 or 5; p is equal to 0, 1, 2, 3 or 4; and r is equal to 0. Invention also relates to a pharmaceutical composition, to a method for inhibiting IRAK activity, to a method of treating an IRAK related disease.

EFFECT: there are prepared new compounds of formula I possessing properties of IRAK inhibitor.

11 cl, 1 tbl, 40 ex

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RU 2 730 016 C2

Authors

Chen, Xiaoling

Yu, Henry

Lan, Ruoxi

Jorand-Lebrun, Catherine

Johnson, Theresa L.

Goutopoulos, Andreas

Dates

2020-08-14Published

2016-02-05Filed