LOW-MOLECULAR WEIGHT Trp-p8 ACTIVITY MODULATORS Russian patent published in 2014 - IPC C07D235/26 C07D213/40 C07D405/04 C07D403/04 C07C323/40 A61K31/4184 A61K31/167 A61K31/416 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I

or a pharmaceutically acceptable salt thereof, where R₁ is H or R₁ and R₂ together with a nitrogen group can form where A, B, C and D are independently selected from a group consisting of CR_1a and N; where at least one of A, B, C and D is CR_1a; where R_1a is selected from a group consisting of H, -ORⁱ, -SRⁱⁱ, -S(O)Rⁱⁱⁱ, -C(O)NR^vR^vi and CF₃, where Rⁱ is selected from a group consisting of methyl, ethyl, propyl, hydroxyethyl, hydroxypropyl, 2-oxo-2-phenylethyl, butyl, acetonitrile and benzyl; Rⁱⁱ, Rⁱⁱⁱ and R^iv denote methyl; R^v and R^vi are independently selected from a group consisting of H, methyl, ethyl, hydroxyethyl, hydroxypropyl, diethyalminoethyl, phenyl, pyridinyl, methoxyethyl, hydroxyethoxyethyl, benzyl, phenylethyl, 2-hydroxy-1-hydroxymethyl-2-phenylethyl and carbomoylethyl, or R^v and R^Vi together form morpholine or ethyl ester of piperazine; R₂ is selected from a group consisting of phenyl, naphthyl, pyrazolyl and C₁-C₈alkylene phenyl; R₃ is C₁-C₈alkylene; R₄ is selected from a group consisting of H, C₁-C₈alkyl and -C=NH(NH₂). The invention also relates to compounds of formulae I-A

I-B I-C

I-D I-E

values of radicals of which are given in the claim; a method of treating said pathological conditions, a pharmaceutical composition based on said compounds, a method of identifying a Trp-p8 agonist and specific compounds.

EFFECT: obtaining compounds which are useful as Trp-p8 modulators.

25 cl, 19 dwg, 8 tbl, 17 ex