PYRAZOLO-HETEROARYL DERIVATIVE, METHOD FOR ITS PREPARATION AND MEDICAL USE Russian patent published in 2021 - IPC C07D471/04 A61K31/395 A61P31/12 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: present invention relates to a new pyrazole-heteroaryl derivative, represented by general formula (I), or its pharmacologically acceptable salt, in which Ring A is a phenyl; G is N; X¹ is CH₂; L¹ is selected from a group consisting of -NR⁴-, -O-, -C(O)-, -N(R⁴)C(O)- and covalent bond; R¹ is C_1-6 alkyl, in which C_1-6 alkyl is optionally substituted with one or more C_1-6 alkoxy; R² is hydrogen or halogen; L² is CH₂; R³ is a 4-6-member saturated monocyclic group, wherein one ring atom is N; R⁴ is hydrogen; and n is 0 or 1. In addition, the invention relates to a compound represented by general formula (I-C), or its pharmacologically acceptable salt, wherein W is p-methoxybenzyl; X is a halogen; Ring A is a phenyl; G is N; X¹ is CH₂; R² is hydrogen or halogen; L² is CH₂; R³ is a 4-6-member saturated monocyclic group, wherein one ring atom is N; n is 0 or 1, and also to the compound represented by general formula (I-E), or its pharmacologically acceptable salt, wherein W is p-methoxybenzyl; Ring A is a phenyl; G is N; X¹ is CH₂; L¹ is selected from a group consisting of -NR⁴-, -O-, -C(O)-, -N(R⁴)C(O)- and covalent bond; R¹ is C_1-6 alkyl, wherein C_1-6 alkyl is optionally substituted with one or more C_1-6 alkoxy; R² is hydrogen or halogen; L² is CH₂; R³ is a 4-6-member saturated monocyclic group, wherein one ring atom is N, R⁴ is hydrogen; n is 0 or 1. In addition, the invention relates to methods for obtaining the presented compounds, a pharmaceutical composition containing the specified derivative, and its use as a therapeutic agent, in particular as a TLR7 agonist.

EFFECT: new compounds that can be used as a therapeutic agent, in particular as a TLR7 agonist, have been obtained and described.

16 cl, 3 tbl