发明名称 PYRIMIDINE COMPOUNDS FOR USE AS DELTA-OPIOID RECEPTOR MODULATORS
摘要 FIELD: chemistry.SUBSTANCE: invention relates to novel compounds of formula I, having the capacity to modulate delta-opioid receptors. In compounds of formula IRis selected from a group consisting of i) phenyl, optionally substituted with one or two substitutes independently selected from a group consisting of Calkyl, Calkoxy, Calkythio, hydroxy, chloro and fluoro; or a phenyl optionally substituted with one amino, Calkylamino, di(Calkyl)amino, di(Calkyl)aminocarbonyl, Calkylaminocarbonyl, hydroxy(C)alkyl, aminocarbonyl, Calkylcarbonylamino, cyano, trifluoromethoxy, Calkylsulphonyl, nitro, trifluoromethyl, phenyl or formamide; ii) pyrimidinyl optionally substituted with one or two substitutes independently selected from a group consisting of Calkyl, Calkoxy, Calkylthio and hydroxy; or pyrimidinyl optionally substituted with one amino, Calkylamino, di(Calkyl)amino, cyano, piperazin-1-yl, which is optionally substituted with 4-Calkyl, morpholin-4-yl; iii) pyridinyl optionally substituted with one or two substitutes independently selected from a group consisting of Calkyl, Calkoxy, Calkylthio, hydroxy, fluoro, chloro and cyano; or pyridinyl optionally substituted with one hydroxymethyl, amino, Calkylamino, di(Calkyl)amino, Calkylsulphonyl, Calkylcarbonylamino; 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
申请公布号 RU2568434(C2) 申请公布日期 2015.11.20
申请号 RU20120122191 申请日期 2010.10.28
申请人 JANSSEN FARMATSEVTIKA NV 发明人 KOUTS STIVEN DZH.;BIAN KHAJAN;KONNOLLI PITER DZH.;BIN'JAN ZHILL';TSAJ CHAOCHZHUN;DAKS SKOTT L.;DE KORT BART L.;LIN' SHU-CHEHN';LJU LI;MEHSILAG MARK DZH.;PITIS FILIP M.;CHZHAN JUEH-MEHJ;CHZHU BIN';KHE VEJ
分类号 C07D401/14;A61K31/506;A61P25/04;C07D403/12;C07D403/14;C07D413/14;C07D417/14 主分类号 C07D401/14
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