IMIDAZOQUINOLINE SUBSTITUTED PHOSPHORIC ACID ESTER AS AGONIST, ITS PREPARATION AND USE Russian patent published in 2024 - IPC C07F9/6561 C07F9/6558 A61K31/4745 A61K39/39 A61P31/14 A61P35/00 A61P31/20 A61P17/12 

FIELD: organic chemistry; pharmacology.

SUBSTANCE: group of inventions relates to an imidazoquinoline-substituted phosphoric acid ester as an agonist of toll-like receptors. The following is disclosed: an imidazoquinoline-substituted phosphoric acid ester having the structure of general formula (I), or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R₁ is selected from the group consisting of a C1-C18 alkoxy group, -(CH₂)_nOR₅; R₂ are each the same or different, R₂ independently selected from the group consisting of hydrogen, C1-C18 alkyl; Z represents C1-C18 alkylene; Y represents O; R₅ represents C1-C18 alkyl; X is selected from the group consisting of -P(=O)(X₁R₁₁)(X₃R₁₄R₁₅), -CH₂P(=O)(X₁R₁₁)(X₃R₁₄R₁₅); X₁ represents oxygen; X₃ — nitrogen; R₁₁, R₁₄ and R₁₅ are independently selected from the group with or without substitution consisting of hydrogen, C1-C20 alkyl, C6-C10 aryl, and substitution means substitution with one or more substituents selected from the group consisting of C1-C20-alkyl, halogenated C1-C20-alkyl, C1-C6-alkoxy group, halogen, -COR₁₆, -COOR₁₆, -OCOOR₁₆; R₁₆ is selected from the substituted or unsubstituted group consisting of hydrogen, C1-C18 alkyl, C6-C10 aryl, where substitution means substitution with one or more C6-C10 aryls; x is 0; n is one of the following integers: 0, 1, 2, 3, 4 or 5. In addition, a method of producing these compounds, a pharmaceutical composition based on them, as well as the use of compounds of general formula (I) for the production of TLR7 and/or TLR8 agonists and for the production of medicinal products based on them are disclosed.

EFFECT: invention provides an effective agonistic effect against TLR7 and TLR8.

12 cl, 1 tbl, 25 ex