4-SUBSTITUTED-2-PHENOXYPHENYLAMINE MODULATORS OF DELTA-OPIOID RECEPTORS Russian patent published in 2015 - IPC C07D205/04 C07D207/09 C07D211/56 C07D401/12 C07D405/12 C07D409/12 C07D413/12 C07D451/04 C07D453/02 C07C217/90 A61K31/397 A61K31/40 A61K31/444 A61K31/4245 A61K31/4025 A61P29/00 A61P25/24 A61P25/32 A61P25/36 A61P25/16 A61P9/00 A61P11/00 A61P1/04 A61P13/08 A61P1/12 A61P15/08 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R₁ is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C_1-4alkyl, C_1-4alcoxy, C_1-4alkylthio, hydroxyl, di(C_1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C_1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C_1-4alkyl, C_1-4alcoxy, C_1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C_1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R₁ represents optionally substituted phenyl, where substituent represents C_1-4alcoxy; R₂ represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C_1-4alkyl, C_1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R₂ represents phenyl, substituted with one aminocarbonyl, di(C_1-4alkyl)aminocarbonyl, C_1-4alcoxycarbonyl or carboxysubstituent; R₃ is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R₃ together with R_a and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C_1-4alkyl; R_a represents hydrogen, 2-(N-methylamino)ethyl or C_1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex