NEW COMPOUNDS AND THEIR PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF INFLAMMATORY DISEASES Russian patent published in 2022 - IPC C07D471/04 C07D519/00 A61K31/437 A61K31/444 A61K31/4545 A61K31/496 A61K31/501 A61K31/506 A61K31/5377 A61K31/5386 A61P3/00 A61P19/00 A61P29/00 A61P35/00 A61P37/06 A61P37/08 

Abstract RU 2785126 C2

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry and includes a compound of the formula I or its pharmaceutically acceptable salt, as well as a pharmaceutical composition based on them. In the formula I, Cy is phenyl or 5-6-element heteroaryl containing one or two N atoms; L1 is a simple bond, -O-, -C(=O)-, -S(O)2-, -NR6a-, -C(=O)NR6b-, or -S(O)2NR6c-; R1 is H; C1-6 alkyl optionally substituted with one-four substitutes specified in the claims; C3-7 cycloalkyl optionally substituted with one OH or C1-4 alkoxy, octadeuteriomorpholine-4-yl, or 4-9-element monocyclic, or spirobicyclic, or bridged, or condensed bicyclic heterocycloalkyl containing one, or two, or three heteroatoms independently selected from N, S, and O; where heterocycloalkyl is optionally substituted with one-three independently selected R11 groups; R11 is independently: OH, CN, halogen, -NR8aR8b, C3-7 cycloalkyl, C1-4 alkyl optionally substituted with one-three substitutes independently selected from halogen, OH, C1-4 alkoxy, or R9aR9b, C1-4 alkoxy optionally substituted with one C1-4 alkoxy, 4-6-element monocyclic heterocycloalkyl containing one or two heteroatoms independently selected from N and O, -C(=O)OC1-4alkyl, or -NR8cC(=O)OC1-4 alkyl; R2 is halogen or C1-4 alkyl; n is equal to 0 or 1; L2 is O or -NR4-; R3 is C1-6 alkyl optionally substituted with one-four substitutes independently selected from halogen or C3-7 cycloalkyl, phenyl substituted with one R5a group and one or two independently selected R5b groups, 6-element heteroaryl containing one or two N atoms, substituted with one R5a group and one or two independently selected R5b groups, 4-9-element monocyclic or spirobicyclic heterocycloalkyl containing one or two heteroatoms independently selected from N and O, optionally substituted with one, two, or three groups independently selected from R5a and R5b, or 4-10-element monocyclic or bridged cycloalkyl optionally substituted with one, two, or three groups independently selected from R5a and R5b; R4 is H, C1-4 alkyl optionally substituted with one or two substitutes independently selected from OH or C1-4 alkoxy, or C3-7 cycloalkyl; R5a is -CN, -SO2-C1-4 alkyl, or -CF3; each R5b is independently selected from halogen, C1-4 alkyl, and C3-7 cycloalkyl; each R7a and R7b is independently selected from H or C1-4 alkyl optionally substituted with one -NR10aR10b; each R6a, R6b, R6c, R7c, R7d, R8a, R8b, R8c, R9a, R9b, R10a, and R10b is independently selected from H or C1-4 alkyl.

EFFECT: compound of the formula I having inhibitory activity against JAK1, JAK2, JAK3, and TYK2.

14 cl, 1 dwg, 13 tbl, 1 ex

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RU 2 785 126 C2

Authors

Van Der Plas, Steven, Emiel

Mammoliti, Oscar

Martina, Sebastien, Laurent, Xavier

Claes, Pieter, Isabelle, Roger

Coti, Ghjuvanni, Petru, Diunisu

Annoot, Denis, Maurice

Lopez Ramos, Miriam

Galien, Rene, Alexandre

Amantini, David

Brys, Reginald, Christophe, Xavier

Dates

2022-12-05Published

2018-10-11Filed