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, -C1-6-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 C1-6-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 C1-2-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
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Authors
Dates
2023-06-05—Published
2019-02-06—Filed