BENZIMIDAZOLE SULFONAMIDES DERIVATIVES AS INVERSE AGONISTS ASSOCIATED WITH RETINOIDS OF THE ORPHAN RECEPTOR GAMMA ROR GAMMA (T) Russian patent published in 2020 - IPC C07D405/06 C07D413/06 C07D401/06 C07D405/04 C07D401/04 C07D409/06 C07D405/14 C07D403/06 A61K31/4184 A61K31/4439 A61P17/04 A61P17/06 A61P31/10 

Abstract RU 2738843 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to benzimidazole sulfonamides of formula (I), pharmaceutically acceptable addition salts, hydrates thereof and/or solvates thereof, where L is a single bond; X is a following cyclic radical: ; one of elements Y1, Y2, Y3, Y4 and Y5 corresponds to nitrogen atom, and other elements correspond to -CR2group, or each of elements Y1, Y2, Y3, Y4 and Y5 corresponds to -CR2 group; each of elements Q1, Q2 and Q3 corresponds to group -CR2a; R1 is a linear or branched C3-C5alkyl radical or C3-C5cycloalkyl radical; R2 represents a hydrogen atom, a linear or branched C1-C5alkyl radical or C1-C4alkoxy radical; R2a is a hydrogen atom; R3 represents a hydrogen atom or a group (CHR6)n-(Z)o-(CHR'6)p-R7; n, o and p, which can be identical or different, are zero or 1; Z is methylene group -CH2-; R6 and R'6 represent a hydrogen atom; R7 is a non-cationic heterocycloalkyl radical selected from tetrahydropyran, oxabicyclo[3.1.0]hexyl, oxetane, 2-oxo [1,3]dioxolane, 2-oxazolidinone, piperidine and 1,1-dioxo-tetrahydro-2H-thiopyrane, optionally substituted with one halogen atom, one linear or branched C1-C3alkyl group, one group S(=O)2R7a; where R7a is a linear or branched C1-C3alkyl radical; or R7 is a non-cationic unsubstituted heteroaromatic radical selected from pyridine or pyridazine; R5 represents a hydrogen atom or a linear or branched C1-C3alkyl radical. Invention also relates to a pharmaceutical composition based on the compound of formula (I).

.

EFFECT: obtaining novel benzimidazole sulfonamides, useful as reversible agonists associated with retinoids of the orphan gamma receptor (RORγt), in particular, are useful for treating acne, psoriasis, and/or atopic dermatitis.

11 cl, 3 tbl, 22 ex

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RU 2 738 843 C2

Authors

Musicki Branislav

Ouvry Gilles

Thoreau Etienne

Bouix-Peter Claire

Dates

2020-12-17Published

2015-12-18Filed