PROBING PROTEINS OF HENTINGIN PROTEIN Russian patent published in 2020 - IPC A61K51/04 C07D487/04 C07D513/04 C07D513/14 C07B59/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a radiopharmaceutical comprising a compound of formula I

or a pharmaceutically acceptable salt thereof. In formula I: m is equal to 0, 1 or 2; n is 1 or 2; J is C (=O) or -CH₂-; X is S or N; Y is CH or N; Z is CH; W is N or S; each R₁ is independently selected from halogen, C_1-6 alkoxy, hydroxyl group, C_6-12 aryl, 5–10-member heteroaryl containing one or more heteroatoms selected from N, O and S, C_3-10 cycloalkoxy or C_1-6 alkyl, where each C_1-6 alkoxy, C_3-10 cycloalkoxy, C_1-6 alkyl, C_6-12 aryl or 5–10-member heteroaryl is optionally substituted with one, two or three groups independently selected from C_1-6 alkoxy, C_2-6 alkenyl, -NR₄R₅, halogen or 5–10-member heteroaryl containing one or more heteroatoms selected from N, O and S, optionally substituted with one to three C_1-6 alkoxy; R₂ is hydrogen or C_1-6 alkyl; and R₃ is C_1-6 alkyl, C_6-12 aryl, aralkyl, 3–10-member heterocycloalkyl containing one or more heteroatoms selected from N, O and S, 3–10-member heterocycloalkenyl, containing one or more heteroatoms selected from N, O and S, 5–10-member heteroaryl or heteroaralkyl, each of which is optionally substituted with one, two or three groups, independently selected from a hydroxyl group, C_1-6 alkoxy, optionally substituted with C_1-6 alkoxy or halogen, C_1-6 alkyl, optionally substituted with halogen, halogen, 5–10-member heteroaryl, containing one or more heteroatoms selected from N, O and S, -(CH₂)_tNR₄R₅, oxo, cyano, or -C(O)-NR₄R₅, or R₂ and R₃ together with the nitrogen atom, to which they are bonded, form 5–10-member heterocycloalkyl ring, optionally substituted with one, two or three groups independently selected from hydroxy, C_1-6 alkoxy, C_1-6 alkyl, halogen or -C(O)-NR₄R₅; t is equal to 0, 1 or 2; R₄ is independently selected from hydrogen or C_1-6 alkyl; R₅ is independently selected from hydrogen or C_1-6 alkyl. Compound of formula I or its pharmaceutically acceptable salt is labeled (a) by one or more positron-active radionuclides. Also disclosed are a method of producing diagnostic images and compounds of formula I.

EFFECT: compound of formula I possesses kinetics of binding aggregates of HTT protein or aggregates of β-amyloid protein and is suitable for their functioning as effective radiopharmaceuticals.

41 cl, 6 dwg, 23 tbl, 24 ex