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АЗОТОСОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ ГЕТЕРОАРИЛОВ
专利权人:
F.KHOFFMANN-LJA ROSH AG
发明人:
BLAJGER KONRAD,FLOR ALEKSANDR,GREBKE TSBINDEN KATRIN,KERNER MATTIAS,KUN BERND,PETERS JENS-UVE,RODRIGEZ SARMIENTO ROZA MARIJA,VIEJRA EHRIK,БЛАЙГЕР Конрад,ФЛОР Александр,ГРЁБКЕ ЦБИНДЕН Катрин,КЁРНЕР Маттиас,КУН Бернд,ПЕТЕРС Йенс-Уве,RODRIGEZ SARM
申请号:
RU2012134306
公开号:
RU2559895C2
申请日:
2011.01.19
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to novel nitrogen-containing heteroaryl derivatives of formula,where Aand Aare independently selected from a group consisting of CH and N, under the condition that Aand Aare simultaneously N; Ris C-C-alkyl, C-C-alkoxy, C-C-alkoxy-C-C-alkyl or cycloalkyl; Rand Rare independently a hydrogen atom or C-C-alkyl; Ris a 6-member heteroaryl containing 2 heteroatoms selected from N; Y is a 5-member heteroaryl selected from a group consisting of:where said heteroaryl is optionally substituted with one substitute selected from a group consisting of C-C-alkyl, which is optionally substituted with 1-3 substitutes selected from a group consisting of aryl, cycloalkyl, a 6-member heterocyclyl 2 heteroatoms selected from O and N, C-C-alkoxy, hydroxyl, halogen atom, amino group, optionally substituted with one or two C-C-alkyl substitutes, cyano and a 5-member heteroaryl containing 2 heteroatoms selected from N, optionally substituted with 1-3 substitutes selected from C-C-alkyl, COO-C-C-alkyl, cycloalkyl and a 6-member heterocyclyl containing 1 heteroatom, selected from O, N, optionally substituted with 1-3 substitutes selected from C-C-alkyl; and Ris phenyl or a 6- or 10-member heteroaryl containing one or two nitrogen atoms, where said phenyl and said heteroaryl are optionally substituted with 1-3 substitutes selected from a group consisting of a halogen atom, C-C-alkoxy, or pharmaceutically acceptable salts thereof.EFFECT: compounds inhibit PDE10A (phosphodiesterase 10A) and can be used as medicinal agents.14 cl, 66 ex, 1 tblИзобретение относится к новым азотсодержащим гетероарильным производным формулы (I),гдеАи Анезависимо выбраны из группы, состоящей из СН и N, при условии, что Аи Аодновременно не представляют собой N; Rпредставляет собой C-С-алкил, C-С-алкокси, C-С-алкокси-C-С-алкил или циклоалкил; Rи Rнезависимо представляют собой атом водорода или C-С-алкил; Rпредставляет собой 6-членный гетероарил, содержащий 2 гетероатома, выб
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