FAP INHIBITOR Russian patent published in 2023 - IPC C07D401/12 C07D401/14 C07D405/14 A61K31/4709 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, where Q, R and U are absent, each of V, W, Y, Z is individually present or absent, provided that at least three of V, W, Y, Z are present; V is C=O; W is NH; Y is CH₂; Z is C=O; R¹ and R² are independently selected from the group consisting of -H, halo; R³ is selected from the group consisting of -CN; R⁴ is selected from the group consisting of -H, -C_1-6-alkyl; R⁵ and R⁶ are H; R⁷ is , where D is present or absent, while at least A, E and B are present, and, when present: D is a linker selected from the structures specified in claim 1 of the formula; A is selected from the group consisting of NR⁴, O, S and CH₂; E is selected from the group consisting of C_1-6-alkyl and where m is 1, 2 or 3; A and E together form a group selected from: B is selected from the group consisting of a 5–9 membered N-containing aromatic or non-aromatic mono- or bicyclic heterocycle, optionally further containing 1 or 2 heteroatoms selected from N, optionally wherein the N-containing heterocycle is substituted with 1-2 substituents selected from a group consisting of C_1-2-alkyl, C₂-aralkyl; and R⁸ is selected from the group consisting of ¹⁸F, ⁶⁸Ga, ^99mTc, ¹⁸⁶Re, ¹⁸⁸Re, ¹⁵³Sm, ⁹⁰ Y, ¹⁷⁷Lu, ⁶⁴Cu, as well as from the structures specified in paragraph 1 of the formula; is a 10-membered N-containing aromatic bicyclic heterocycle, where there are 2 ring atoms between the N and X atom; and X represents a C atom. The invention also relates to a pharmaceutical composition and a kit based on the compound of formula (I) for the treatment or diagnosis of these diseases, a method for the diagnosis or treatment of these diseases.

EFFECT: effective treatment and diagnosis of diseases characterized by overexpression of fibroblast activation protein (FAP).

13 cl, 57 dwg, 12 tbl, 8 ex