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PIPERIDIN-4-ILAZETIDINDIAMIDES AS MONOACYLGLYCERINLIPASE INHIBITORS
专利权人:
ЯНССЕН ФАРМАЦЕВТИКА НВ (BE)
发明人:
КОННОЛЛИ Питер Дж. (US),БИАН Хайан (US),ЛИ Сюнь (US),ЛЮ Ли (US),МЭСИЛАГ Марк Дж. (US),МАКДОННЕЛЛ Марк Е. (US)
申请号:
RU2013123275/04
公开号:
RU2013123275A
申请日:
2011.10.20
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. The compound of formula (I) formula (I) where Y and Z are independently selected from group a) or group b) such that one of the elements (Y or Z) is selected from group a) and the other from group b); group a) is i) C-aryl not substituted or substituted by a substituent selected from the group consisting of fluoro, chloro, C-alkyl, C-alkoxyl, cyano and trifluoromethyl; or ii) an unsubstituted heteroaryl selected from the group consisting of thiazolyl, isothiazolyl and 1H-pyrrolyl; group b) is i) C-aryl; ii) a heteroaryl selected from the group consisting of benzoxazolyl, benzothiazolyl, benzimidazolyl, benzothienyl, indazolyl and indolyl; iii) phenylmethylphenyl in which the phenyl group of the phenylmethyl has no substituent or is substituted with trifluoromethyl or fluorine; or iv) 1,3-dihydro-3H-benzimidazol-2-onyl; wherein members of group b) other than phenylmethylphenyl have no substituents or are substituted with one or two substituents independently selected from the group consisting of bromine, chlorine, fluorine, iodine, C-alkyl, C-alkoxyl and R; subject to the presence of not more than one substituent R; and R is selected from the group consisting of trifluoromethyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, 4,4-difluorocyclohexyl, thienyl, pyridinyl and phenyl; moreover, these thienyl, pyridinyl and phenyl in R do not have substituents or are substituted by one or two substituents independently selected from the group consisting of trifluoromethyl, methyl, chlorine, cyano and fluorine; R is hydrogen or hydroxy; and also its enantiomers, diastereomers, solvates and pharmaceutically acceptable salts. 2. The compound according to claim 1, in which group a) is non-substituted phenyl or non-substituted�1. Соединение формулы (I)формула (I)гдеY и Z независимо выбраны из группы a) или группы b) таким образом, что один из элементов (Y или Z) выбран из группы a), а другой - из группы b);группа a) представляет собойi) C-арил, не имеющий заместителя или замеще
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