ALKYL DERIVATIVES OF 1-OXA-4,9-DIAZASPIROOUNDECANE COMPOUNDS HAVING MULTIMODAL ACTIVITY DIRECTED AGAINST PAIN Russian patent published in 2020 - IPC C07D498/10 A61K31/5386 A61P25/04 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a heterocyclic compound of formula (I), optionally in form of one of stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in whatever ratio, or to its corresponding pharmaceutically acceptable salt, where R₁ is unsubstituted C_1-3 alkyl or unsubstituted C_3-6 cycloalkyl; R₂ denotes a substituted or unsubstituted phenyl or substituted or unsubstituted monocyclic heterocyclyl selected from pyridine and thiazole, where phenyl in R₂ during substitution is substituted with one or two substitutes selected from -OR₄, halogen, -CN, halogen-C₁ alkyl, -halogen-OC₁ alkyl, -NR₄R_4''', -NO₂, -NR₄C(O)R_4', -C(O)OR₄, -C(O)NR₄R_4', -NR₄C(O)NR_4'R_4'' and -S(O)₂NR₄R_4'; where the heterocycle in R₂ when substituted is substituted with one substitute selected from -OR₄, halogen, halo-C₁ alkyl and -NR₄R_4"; R₃ denotes a substituted or unsubstituted C_1-3 alkyl, unsubstituted C_2-3 alkenyl, unsubstituted C_2-3 alkynyl, or unsubstituted phenyl bonded to another atom through one group (-CH₂-), where alkyl, as defined in R₃, when substituted with a substitute selected from OH; R_3' is hydrogen or unsubstituted C_1-3 alkyl; alternatively, R₃ and R_3' taken together with the connecting C-atom can form unsubstituted C_3-5 cycloalkyl; R₄, R_4' and R_4" are independently selected from hydrogen or unsubstituted methyl; R_4''' represents hydrogen or -Boc. Invention also relates to a pharmaceutical composition based on the compound of formula (I) and use thereof for preparing a medicament.

(I).

EFFECT: obtaining a novel heterocyclic compound of formula (I) useful for treating pain mediated by double binding activity with sigma-1 receptor and μ-opioid receptor.

12 cl, 95 ex