NEW COMPOUND OF BENZIMIDAZOLONE AND ITS PHARMACEUTICAL USE Russian patent published in 2023 - IPC C07D235/26 C07D401/12 C07D405/12 C07D405/14 A61K31/4439 A61K31/45 A61P13/00 A61P25/00 A61P25/04 A61P29/00 

FIELD: organic chemistry and pharmaceuticals.

SUBSTANCE: group of inventions is aimed at providing compounds for the treatment or prevention of a disease in which the Na channel is involved, in particular SCN9A (Nav 1.7). The following is disclosed: a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R^1a and R^1d are independently hydrogen, one of R^1b and R^1c is either C₆ aryl, C₆ aryloxy, 6-membered heteroaryl, or 6-membered heteroaryloxy, wherein aryl and aryl group in aryloxy; and heteroaryl and heteroaryl group in heteroaryloxy may be independently substituted with 1–3 substituents independently selected from the group consisting of halo, methyl optionally substituted with 1–3 substituents independently selected from Substituent Group A, and methoxy optionally substituted with 1–3 substituents independently selected from Substituent Group A; and the other R^1b or R^1c are hydrogen, R⁴ is either hydrogen, methyl or ethyl; m=1, L is CR⁷R⁸, R⁷ and R⁸ are independently hydrogen or methyl, R² and R³ are methyl, or in R², R³ and the hydroxyl group associated with the carbon atom associated with R² and R³, R² and R³ can, together with the carbon atom to which they are attached, form the following group of formula (II) with a hydroxyl group, in formula (II), e and f are 1, V is an oxygen atom, R^5a, R^5b, R^5c and R^5d are hydrogen, or in R², R³, the hydroxyl group associated with the carbon atom associated with R² and R³ and CR⁷ R⁸ in L, R² and R⁷ may together with the carbon atom to which they are attached to form the following group of formula (III) with R³, hydroxyl group and R⁸ in formula (III), m¹ =0, m² = 2, and j= 2, R⁸ and L have the meanings defined above, R^6a, R^6b, R^6c and R^6d are hydrogen, Substituent group A is independently halogen, provided that the following compounds are excluded: 5-(2-butyl-1-oxo-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazin-6-yl)-1-1,3-dihydro-2H-benzimidazol-2-one (2-hydroxyethyl), 3-[3-methyl-2-oxo-1-(3,3,3-trifluoro-2-hydroxypropyl)-2,3-dihydro-1H-benzimidazol-5-yl]pyridine-4-carbonitrile, and -[3-methyl-2-oxo-1-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-2,3-dihydro-1H-benzimidazol-5-yl]pyridine-4-carbonitrile. Besides, the following is described: a pharmaceutical composition for the treatment of a disease in which Nav 1.7 (SCN9A) is involved, containing a therapeutically effective amount of the above compound, a drug for the treatment of a disease in which Nav 1.7 (SCN9A) is involved, the use of this compound or its pharmaceutically acceptable salts to produce a drug; and a method of treating a disease that involves Nav 1.7 (SCN9A).

EFFECT: group of inventions provides effective treatment of the disease using the involved Nav 1.7 (SCN9A).

10 cl, 1 tbl, 28 ex