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PHENOXY-SUBSTITUTED PYRIMIDINES FOR APPLICATION AS OPIOID RECEPTOR MODULATORS
专利权人:
JANSSEN FARMATSEVTIKA NV
发明人:
KOUTS Stiven Dzh. (US),КОУТС Стивен Дж. (US),ChZhAN Jueh-mehj (US),ЧЖАН Юэ-мэй (US),LIN' Shu-chehn' (US),ЛИНЬ Шу-чэнь (US),LJu Li (US),ЛЮ Ли (US),MISKOVSKI Tamara A. (US),МИСКОВСКИ Тамара А. (US),DAKS,KOUTS STIVEN DZH.,КОУТС Стивен Дж.,CHZHAN JUEH-MEHJ,ЧЖАН Юэ-мэй,LIN SHU-CHEHN,ЛИНЬ Шу-чэнь,LJU LI,ЛЮ Ли,MISKOVSKI TAMARA A.,МИСКОВСКИ Тамара А.,DAKS SKOTT L.,ДАКС Скотт Л.,BRESLIN GENRI,БРЕСЛИН Генри
申请号:
RU2012122196/04
公开号:
RU0002554870C2
申请日:
2010.10.28
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
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 C1-4alkoxy, fluorine atom, chlorine atom, bromine atom and cyanogroup; in addition, R1 is optionally substituted with di(C1-4alkyl)aminocarbonyl; Y represents O, S, H3, vinyl, ethinyl or S(O); R2 represents a substituent, selected from the group, consisting of hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, fluorine atom, chlorine atom, bromine atom and hydroxy; Ra 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-(C1-2)alkyl, azetidin-3-ylmethyl; morpholin-2-ylmethyl, morpholin-3-ylmethyl, imidazolylmethyl, thiazolylmethyl, (amino)-C3-6cycloalkyl, 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 exИзобретение относится к новым соединениям формулы I, обладающим свойствами связывания с д
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