11,13-MODIFIED SAXITOXINS FOR PAIN TREATMENT Russian patent published in 2022 - IPC C07D487/14 A61K31/519 A61P25/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the Formula (I) or to its pharmaceutically acceptable salt, where X² is -C(R⁴)(R^4a)- or -N(R⁸)-; R⁴ and R^4a, in each case, are hydrogen; R⁷ is hydrogen; R^7a is phenyl, naphthyl, tetrahydronaphthyl, 6,7,8,9-tetrahydro-5H-benzo[7]annulenyl or indanyl; each of which is optionally substituted with 1 or 2 groups independently selected from halo, C_1-6alkyl, and C_1-6alkoxy; or R^7a is bicyclic heterocycle containing one or two heteroatoms, which are oxygen, where heterocycle is optionally substituted with 1 or 2 R^7b; R^7b, in each case, if present, is independently halo, C_1-6alkyl, or C_1-6alkoxy; and R⁸ is oxygen; C_1-6alkyl; carboxy-C_1-6-alkyl; halo-C_1-6-alkyl; hydroxy-C_1-6-alkyl; C₃-C₈-cycloalkyl; or unsubstituted phenyl; or stereoisomer, or tautomer. The invention also relates to a method for the production of the specified compound of the Formula (I) and a pharmaceutical composition for use in the treatment of a condition associated with a function of potential-controlled sodium channels based on it.

EFFECT: new compounds and a pharmaceutical composition based on them are obtained, which can be used in medicine for the treatment of pain, cough, itching or discomfort related to a dry eye syndrome.

35 cl, 2 tbl, 2 ex