TRICYCLIC INDOLE DERIVATIVES AS PBR LIGANDS Russian patent published in 2014 - IPC C07D209/80 C07D209/88 A61K51/04 

FIELD: chemistry.

SUBSTANCE: invention relates to novel in vivo visualising agents of formula I, where R¹stands for C_1-3alkyl, C_1-3fluorinealkyl; R² stands for H, OH, halogeno, C_1-3alkyl, C_1-3alkoxy, C_1-3fluoroalkyl, C_1-3fluoroalkoxy; R³ and R⁴ independently stand for C_1-3alkyl, C₇-C₁₀aralkyl or R³ and R⁴ together with nitrogen atom, to which they are bound, form nitrogen-containing C_4-6aliphatic ring; Y¹ stands for CH₂; Y² stands for CH₂, CH₂-CH₂, CH(CH₃)-CH₂ or CH₂-CH₂-CH₂; and where formula I, as it is determined, contains atom, which represents radioactive isotope, suitable for visualisation in vivo, selected from ¹¹C, ¹⁸F, ⁷⁷Br, ¹²³I, ¹²⁴I and ¹³¹I. Claimed compounds bind with PBR with high affinity, have good absorption in brain after introduction. Described is method of obtaining in vivo visualising agent and set for claimed method realisation.

EFFECT: radio-pharmaceutical composition, which contains in vivo visualising agent, is described.

21 cl, 13 dwg, 18 ex