PHENOXY-SUBSTITUTED PYRIMIDINES FOR APPLICATION AS OPIOID RECEPTOR MODULATORS Russian patent published in 2015 - IPC C07D239/28 C07D239/34 C07D401/12 C07D403/12 C07D413/12 C07D417/12 A61K31/505 A61K31/506 A61P25/04 A61P29/00 A61P25/32 A61P25/36 A61P25/16 A61P9/00 A61P1/04 A61P13/06 A61P15/08 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula

,

possessing properties of binding with delta opioid receptors. In formula I R₁ is selected from the group, consisting of phenyl, pyridinyl and thiazolyl, with R₁ being optionally substituted with one or two substituents, independently selected from the group, consisting of C_1-4alkoxy, fluorine atom, chlorine atom, bromine atom and cyanogroup; in addition, R₁ is optionally substituted with di(C_1-4alkyl)aminocarbonyl; Y represents O, S, H3, vinyl, ethinyl or S(O); R₂ represents a substituent, selected from the group, consisting of hydrogen, C_1-4alkyl, C_1-4alkoxy, C_1-4alkylthio, fluorine atom, chlorine atom, bromine atom and hydroxy; R_a represents hydrogen or methyl; R₃ is selected from the group, consisting of pyrrolidin-2-ylmethyl; pyrrolidin-3-ylmethyl; piperidin-2-ylmethyl, piperidin-3-ylmethyl, piperidin-4-ylmethyl, piperidin-2-ylethyl, piperidin-3-ylethyl, piperidin-4-ylethyl, pyridine-4-yl-(C_1-2)alkyl, azetidin-3-ylmethyl; morpholin-2-ylmethyl, morpholin-3-ylmethyl, imidazolylmethyl, thiazolylmethyl, (amino)-C_3-6cycloalkyl, 3-hydroxy-2-aminopropyl, 8-azabicyclo[3.2.1]octanyl, 1-azabicyclo[2.2.2]octanyl, guanidinylethyl, 4-(imidazol-1-yl)phenylmethyl, 2-(methylamino)ethyl, 2-diethylaminoethyl, 4-diethylaminobut-2-yl, piperidin-3-yl, piperidin-4-yl and pyrrolidin-3-yl; with piperidin-3-yl being optionally substituted on a carbon atom with phenyl; with pyrrolidin-2-yl in pyrrolidin-2-yl-methyl, pyrrolidin-3-yl, piperidin-3-yl and piperidin-4-yl being optionally substituted on a nitrogen atom with methyl, phenylmethyl, phenethyl or methylcarbonyl.

EFFECT: compounds can be used in the treatment of pain, induced by diseases or conditions, such as osteoarthritis, rheumatoid arthritis, migraine, burn, fibromyalgia, cystitis, rhinitis, neuropathic pain, idiopathic neuralgia, toothache, etc.

24 cl, 3 tbl, 19 ex