发明名称 POSITIVE ALLOSTERIC MODULATORS (PAM)
摘要 FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to novel derivatives of phenylethinyl of formula (I) or to their pharmaceutically acceptable acid addition salts, possibly, in the form of a racemic mixture, or an enantiomer, that corresponds to it, and/or an optic isomer, and/or a stereoisomer. The compounds possess properties of positive allosteric modulators (PAM) of metabotropic glutamate receptors of subtype 5 (mGluR5) and can be used in the treatment of schizophrenia or cognitive disorders. In formula (I)Rrepresents hydrogen, halogen, lower alkyl or a lower alkyl, substituted with halogen; Rrepresents hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl, substituted with hydroxyl; X represents N, CF or CH; L represents -NR-, -NHC(R)-, -O-, -OC(R)-, -CRR-; Rrepresents hydrogen or lower alkyl, R/Rindependently on each other represent hydrogen or lower alkyl; cyc represents cycloalkyl or heterocycloalkyl, or represents a non-aromatic bicycle, selected from 7-oxa-bicyclo [2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n represents 1, 3 or 3.EFFECT: obtaining novel phenylethinyl derivatives.23 cl, 1 tbl, 44 ex
申请公布号 RU2561920(C2) 申请公布日期 2015.09.10
申请号 RU20120120307 申请日期 2010.10.25
申请人 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
分类号 C07D213/74;A61K31/44;A61K31/4427;A61K31/505;A61K31/506;A61P25/18;A61P25/28;C07D239/34;C07D239/42;C07D401/06;C07D405/12;C07D413/06;C07D493/08 主分类号 C07D213/74
代理机构 代理人
主权项
地址