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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Authors
Dates
2022-12-05—Published
2018-10-11—Filed