HETEROAROMATIC MODULATORS OF RETINOL-BOUND ORPHAN GAMMA RECEPTOR Russian patent published in 2022 - IPC C07D413/14 C07D413/12 C07D417/14 C07D241/04 A61K31/496 A61P17/04 

Abstract RU 2771280 C2

FIELD: medicine.

SUBSTANCE: invention relates to a compound corresponding to the general formula (I), where X is N, CH; R1 is selected from a group including -CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7-element)heterocycloalkyl containing 1-2 heteroatoms selected from nitrogen, oxygen, (5-element) heteroaryl containing 1-3 heteroatoms selected from nitrogen, oxygen, sulfur, where the specified (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7-element)heterocycloalkyl, (5-element)heteroaryl is optionally substituted with one or more substituents independently selected from R6; R2 is selected from a group including halogen, (C1-C4)alkyl and (C3-C7)cycloalkyl, where the specified (C1-C4)alkyl and (C3-C7)cycloalkyl are optionally substituted with one or two substituents independently selected from halogen; R3 is selected from a group including (C1-C4)alkyl; R4 is selected from a group including (C1-C4)alkyl; R5 is selected from a group including (C1-C6)alkyl, (C3-C7)cycloalkyl, phenyl and -ORa, where the specified (C1-C6)alkyl, (C3-C7)cycloalkyl, phenyl and -ORa are optionally substituted with one or more substituents independently selected from R7; R6 is a group including -OH, -CN, halogen, =O, -S(O)2Rb, -NRcRd, -C(O)Rb, (C1-C4)alkyl, hydroxy(C1-C4)alkyl, ORb, (C3-C6)cycloalkyl; R7 is a group including halogen, (C1-C4)alkyl; Ra is (C1-C6)alkyl; Rb is (C1-C6)alkyl; each Rc and Rd is independently H, (C1-C6)alkyl; or its pharmaceutically acceptable salts. The invention also relates to compounds of the general formula (II) and (IX), where R2 is selected from a group including halogen and (C1-C4)alkyl, where the specified (C1-C4)alkyl is optionally substituted with one or two substituents independently selected from halogen; R3 is selected from (C1-C4)alkyl; R4 is selected from a group of (C1-C4)alkyl; R5 is selected from a group including (C1-C6)alkyl, (C3-C7)cycloalkyl, phenyl and -ORa, where the specified (C1-C6)alkyl, (C3-C7)cycloalkyl, phenyl and -ORa are optionally substituted with one or more substituents independently selected from halogen; Ra is selected from (C1-C6)alkyl. The invention relates to a pharmaceutical composition with a modulating effect of ROR-gamma, containing effective amount of the compound of the formula (I), together with a pharmaceutically acceptable base or auxiliary substance or a pharmaceutically acceptable carrier(s).

EFFECT: heteroaromatic compounds for use in the treatment of a disease, disorder or condition, where the disease, disorder or condition is sensitive to ROR-gamma modulation.

20 cl, 2 tbl, 83 ex

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RU 2 771 280 C2

Authors

Jessiman, Alan Stuart

Johnson, Patrick Stephen

Maansson, Kristoffer

Sorensen, Morten Dahl

Dates

2022-04-29Published

2017-07-11Filed