PYRIMIDINE COMPOUNDS FOR USE AS DELTA-OPIOID RECEPTOR MODULATORS Russian patent published in 2015 - IPC C07D401/14 C07D403/12 C07D403/14 C07D413/14 C07D417/14 A61K31/506 A61P25/04 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, having the capacity to modulate delta-opioid receptors. In compounds of formula I R₁ is selected from a group consisting of i) phenyl, optionally substituted with one or two substitutes independently selected from a group consisting of C_1-4alkyl, C_1-4alkoxy, C_1-4alkythio, hydroxy, chloro and fluoro; or a phenyl optionally substituted with one amino, C_1-4alkylamino, di(C_1-4alkyl)amino, di(C_1-4alkyl)aminocarbonyl, C_1-4alkylaminocarbonyl, hydroxy(C_1-4)alkyl, aminocarbonyl, C_1-4alkylcarbonylamino, cyano, trifluoromethoxy, C_1-4alkylsulphonyl, nitro, trifluoromethyl, phenyl or formamide; ii) pyrimidinyl optionally substituted with one or two substitutes independently selected from a group consisting of C_1-4alkyl, C_1-4alkoxy, C_1-4alkylthio and hydroxy; or pyrimidinyl optionally substituted with one amino, C_1-4alkylamino, di(C_1-4alkyl)amino, cyano, piperazin-1-yl, which is optionally substituted with 4-C_1-4alkyl, morpholin-4-yl; iii) pyridinyl optionally substituted with one or two substitutes independently selected from a group consisting of C_1-4alkyl, C_1-4alkoxy, C_1-4alkylthio, hydroxy, fluoro, chloro and cyano; or pyridinyl optionally substituted with one hydroxymethyl, amino, C_1-4alkylamino, di(C_1-4alkyl)amino, C_1-4alkylsulphonyl, C_1-4alkylcarbonylamino; and iv) G is a substitute selected from a group consisting of naphthyl, pyrazolyl, thienyl, benzothiazolyl, benzimidazolyl, quinolinyl, indolyl, thiazolyl, furanyl, dihydrobenzofuranyl, pyrazinyl, isoquinolinyl, quinoxazolinyl, quinazolinyl, isoxazolyl, oxazolyl, pyrrolopyridinyl, benzo[1,3]dioxol-5-yl, benzo[1,2,5]oxadiazolyl, dibenzothiophenyl, 4H-[1,2,4]oxadiazol-5-onyl, benzothiophenyl, indazolyl and 2,3-dihydrobenzo[1,4]dioxynyl. Other values of radicals are given in the claim.

EFFECT: compounds can be used in treating pain in case of opioid receptor-modulated diseases or conditions, such as osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burns, snake bite, spider bite, insect bite, neurogenic bladder etc, as well as when treating diseases or conditions selected from a group consisting of depression, Parkinson's disease, drug addiction, alcohol addiction, gastritis, uroclepsia, premature ejaculation, diarrhoea etc.

29 cl, 25 tbl, 35 ex