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ПРОИЗВОДНЫЕ АРИЛЭТИНИЛА
专利权人:
F.KHOFFMANN-LJA ROSH AG
发明人:
GRIN LJUK,GUBA VOL'FGANG,ESHKE GEORG,ZHOLIDON SINIZ,LINDEMANN LOTAR,RICHCHI ANTONIO,RJUKHER DANIEHL',SHTADLER KHAJNTS,VIEJRA EHRIK,ГРИН Люк,GUBA VOLFGANG,ГУБА Вольфганг,ЕШКЕ Георг,ЖОЛИДОН Синиз,ЛИНДЕМАНН Лотар,РИЧЧИ Антонио,RJUKHER DANIEHL,РЮХЕР Даниэль,SHTADLER
申请号:
RU2012145237
公开号:
RU2573560C2
申请日:
2011.04.11
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a new ethinyl derivative of formula I in the form of a racemic mixture or respective enanthiomer and/or optic isomer and/or stereoisomer or to a pharmaceutically acceptable salt of the above compounds formed by acid addition. The compounds are allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5) and can find application in treating diseases mediated by mGluR5 action, wherein a disease is schizophrenia, cognitive disorders, fragile X syndrome or autism. In formula I,U is N or C(R); V is CH or N; W is CH or N; provided only one of the groups U, V or W is a nitrogen atom, Ris hydrogen, methyl or halogen; Y is -N(R)-, -O-, -C(R)(R)-, -CHO- or -CHS(O)-; Ris hydrogen or lower alkyl, whereas R/Rindependently represent hydrogen, hydroxy group, lower alkyl or lower alkoxy group; Ris phenyl or 5-6-merous heteroaryl containing 1-2 heteroatoms specified in nitrogen atoms, which can contain one or two substitutes specified in halogen or lower alkyl; R/Rindependently represent hydrogen, lower alkyl, hydroxy group, lower alkoxy group, C-C-cycloalkyl, CH-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C-C-cycloalkyl, or a ring containing -CHOCH-; m is equal to 0, 1 or 2; if m is equal to 1, R/Rindependently represent hydrogen, lower alkyl, CH-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C-C-cycloalkyl; or Rand Rtogether with a carbon atom, to which they are attached, can form C-cycloalkyl or a ring containing -(CH)OCH-; n is equal to 0 or 1; if n is equal to 1, R/Rindependently represent hydrogen, lower alkyl, CH-lower alkoxy group or together with a carbon atom, to which they are attached, can form C-C-cycloalkyl; Rand Rtogether with a carbon atom, to which they are attached, can form C-cycloalkyl; or if n is equal to 0, and Y is -N(R)-, then Rand Rtogether with a carbon atom and a nitrogen atom, to which they are
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