SID-NUNES KHOSE MARIJA,СИД-НУНЬЕС Хосе Мария,TRABANKO-SUARES ANDRES AVELINO,ТРАБАНКО-СУАРЕС Андрес Авелино,MAKDONALD GREGOR DZHEJMS,МАКДОНАЛЬД Грегор Джеймс
申请号：
RU2011120816/04
公开号：
RU0002512283C2
申请日:
2009.11.24
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: invention relates to novel derivatives of indole and benzoxazine, possessing positive allosteric modulating activity with respect to mGluR2 receptor. In formula (I) R1 represents C1-3alkyl, substituted with trifluoromethyl, R2 represents cyano or halogeno, R3 represents hydrogen, C1-3alkyl, C1-3alkyl, substituted with C3-7cycloalkyl, pyridinyl, hydroxy C2-4alkyl, C1-3alkyloxyC2-4alkyl, 4-tetrahydropyranyl, 4-(hydroxy)-cyclohexanyl, 4-(hydroxy)-4-(C1-3alkyl)cyclohexanyl, phenyl, pyridinyl methyl, pyridinyl methyl, substituted with one C1-3alkyl group, or phenyl or pyridinyl, substituted with one or two substituents, selected from group, consisting of halogeno and C1-3alkyl, R4 represents hydrogen or halogeno, A represents radical of formula -CH=CH-(a) or -CH2-CH2-O-(b), where one or two hydrogen atoms can be substituted with C1-3alkyl. Invention also relates to pharmaceutical composition, containing claimed compounds, and to compound for application in treatment or prevention of central nervous system disorder, selected from the group: anxiety disorders, psychotic disorders, personality disorders, mood disorders, migraine, epilepsy or convulsive disorders, cognitive disorders, attention deficit/hyperactivity syndrome, nervous anorexia, neurogenic bulimia, neurodegeneration, neurotoxicity, ischemia, alcohol addiction, cocaine addiction, nicotine addiction, opioid addiction.EFFECT: obtaining novel indole and benzoxazine derivatives.15 cl, 3 tbl, 6 exИзобретение относится к новым производным индола и бензоксазина, обладающим положительной аллостерической модулирующей активностью в отношении mGluR2 рецептора. В формуле (I) R1 представляет собой С1-3алкил, замещенный трифторметилом, R2 представляет собой циано или галогено, R3 представляет собой водород, С1-3алкил, С1-3алкил, замещенный С3-7циклоалкилом, пиридинил, гидроксиС2-4алкил, С1-3алкилоксиС2-4алкил, 4-тетрагидропиранил, 4-(гидрокси)-циклогексанил, 4-(гидрокси)-4-(С1-3алкил)циклогексани
