DERIVATIVES OF HINOLINE, VISUALIZING TAU PROTEIN Russian patent published in 2017 - IPC C07D215/20 C07D215/26 C07D215/38 C07D215/40 C07D401/04 C07D405/12 C07D498/04 A61K31/47 A61K31/4709 A61K31/496 A61K31/5383 A61P25/28 

FIELD: pharmacology.

SUBSTANCE: invention relates to a new quinoline derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is or , R¹ is halogen or , in which R⁴ and R⁵ each independently represents hydrogen, a lower alkyl group, or R⁴, R⁵ and the nitrogen atom to which they are attached together form a 6-member nitrogen-containing aliphatic ring (where the nitrogen atom may be substituted by a lower alkyl group), or R⁴ and the nitrogen atom to which it is attached together with ring A form a 10-membered nitrogen-containing fused bicyclic ring (one carbon atom constituting the nitrogen-containing condensed bicyclic ring can be replaced by the oxygen atom), and R⁵ is a lower alkyl group where a line crossed by a dashed line means a bond of the above general formula with another structural moiety, R² or R³ each independently represents NR^aR^b or -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy groups), ring A is unsubstituted or substituted by R⁶ (where R⁶ is one substituent selected from halogen and an -O-lower alkyl group (each alkyl group may be substituted with 1 to 2 substituents selected from halogen, hydroxy, R^a and R^b each represents hydrogen or a lower alkyl group, m and n denote an integer from 0 to 1, wherein at least one of R², R³ and R⁶ is an -O-lower alkyl group substituted with one hydroxy group and one halogen. The invention also relates to a pharmaceutical composition, a composition for conformational disease diagnosis, treatment or prevention, a diagnostic kit based on a compound of formula (I), a method of treatment, a method for detection or staining of a protein-layer β-structure, a process for preparation of a compound of formula (I) and intermediates.

EFFECT: new compounds are obtained that can be used to diagnose and treat conformational diseases, in particular, a disease having such a cardinal symptom as intracerebral accumulation of tau protein, for example, Alzheimer's disease.

17 cl, 29 dwg, 26 tbl, 2 ex