2-PHENYLIMIDAZO[1,2-A]PYRIMIDINES AS IMAGING AGENTS Russian patent published in 2018 - IPC C07D487/04 A61K31/519 A61P25/28 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of general formula I, their pharmaceutically acceptable acid addition salts, racemic mixtures or corresponding enantiomers that have tau aggregate, beta amyloid aggregate or alpha-synuclein aggregate binding properties. In general formula I R¹ is phenyl optionally substituted with one or two substituents selected from ³H, halogen, lower alkyl, dimethylamino, NHC(O)-lower alkyl, C(O)O-lower alkyl, lower alkoxy, OC(³H)₃, O¹¹CH₃, OCH₂CH₂¹⁸F, lower alkoxy, substituted with halogen, hydroxy, lower alkyl substituted with hydroxy, S-lower alkyl, or a heterocyclyl group, wherein the heterocyclyl group is a 5-6 membered saturated ring with 1 to 2 heteroatoms selected from nitrogen or nitrogen and oxygen; or is benzo[d][1,3]dioxol-5-yl, 2,3-dihydrobenzo[b][1,4]dioxin-6-yl, indolin-2-one, or is a heteroaryl selected from a group consisting of thiophenyl, benzofuranyl, benzothiophenyl, pyrazinyl or benzothiazolyl; R² is hydrogen, lower alkyl or lower alkyl substituted with halogen; R³ is lower alkyl, C(³H)₃, ¹¹CH₃, lower alkyl substituted with halogen, -(CH₂)₂-O-lower alkyl substituted with halogen, or C_3-6-cycloalkyl; or R² and R³ together with the nitrogen atom to which they are attached, form a ring containing -CH₂CH₂CHRCH₂CH₂-, -CH₂CH₂CH₂CH₂-, -CH₂CH₂CH₂-, -CH₂CH₂-NR-CH₂CH₂-, -CH₂CH₂-O-CH₂CH₂-, -CH₂CH₂CHRCH₂-, -CH₂CHRCH₂- or ; R is hydrogen, halogen, lower alkyl substituted with halogen, or lower alkoxy.

EFFECT: compounds can be used in the study and diagnostic imaging of tau aggregates in the brain of a mammal and in patients, for example, with Alzheimer's disease.

14 cl, 1 tbl, 144 ex