PYRIDONAMIDES AS SODIUM CHANNELS MODULATORS Russian patent published in 2023 - IPC C07D213/75 C07D401/12 A61K31/44 A61P29/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a process for the preparation of a compound of formula I or a pharmaceutically acceptable salt thereof. In formula (I): R¹ is H, halogen, CN, or C₁-C₆ alkyl, where the said C₁-C₆ alkyl is substituted with 0–6 halogens, and where up to two non-adjacent CH₂ units of the said C₁-C₆ alkyl may be substituted on -O-; R² is H, halogen, CN, or C₁-C₆ alkyl, where the said C₁-C₆ alkyl is substituted with 0–6 halogens, where up to two non-adjacent CH₂ units of the said C₁-C₆ alkyl may be replaced by -O-; R³ is H, halogen, CN or C₁-C₆ alkyl, where the said C₁-C₆ alkyl is substituted with 0–6 halogens, where up to two non-adjacent CH₂ units of the said C₁-C₆ alkyl may be replaced by -O-; R⁴ is H, halogen, CN, or C₁-C₆ alkyl, where the said C₁-C₆ alkyl is substituted with 0–6 halogens, where up to two non-adjacent CH₂ units of the said C₁-C₆ alkyl may be replaced by -O-; R⁵ is H, halogen, CN or -XR^x; R^5' is H, halogen, CN or -XR^x; R⁶ is H, halogen, CN or -XR^x; R^6' is H, halogen, CN or -XR^x; R⁷ is H, halogen, CN or -XR^x; X is a bond or C₁-C₆ alkyl, where the said C₁-C₆ alkyl is substituted with 0–6 halogens, where up to two non-adjacent CH₂ units of the said C₁-C₆ alkyl may be replaced by -O-; and R^x is absent or is H or C₃-C₈ cycloaliphatic group, where up to two non-adjacent CH₂ units of the specified C₃-C₈ cycloaliphatic group can be replaced by -O-, and where the said C₃-C₈ cycloaliphatic group substituted with 0–3 substituents selected from halo and C₁-C₄ alkyl. The method includes the following: reaction of a compound of formula A with a compound of formula B in the presence of a first base to give a compound of formula I, and optional reaction of a compound of formula I with an acid or a second base to give a pharmaceutically acceptable salt. A compound of formula A and a compound of formula C are also provided. The invention makes it possible to obtain pyridonamide compounds of formula I or pharmaceutically acceptable salts thereof that can be used as sodium channel inhibitors.

EFFECT: obtaining pyridonamides as sodium channels modulators.

30 cl, 4 tbl, 30 ex