发明名称 ETHYNYL DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS OF THE mGluR5
摘要 The present invention relates to ethynyl derivatives of formula I wherein X is N or C-R, wherein R is hydrogen or halogen; G is N or CH; with the proviso that maximum one of G or X can be nitrogen; Ris phenyl or pyridinyl, which are optionally substituted by halogen; Ris hydrogen, lower alkyl, hydroxy, lower alkoxy or C(O)O-benzyl; R, R, R, R, R, Rare independently from each other hydrogen or lower alkyl; or Rand Rmay form together with the carbon atom to which they are attached a C-cycloalkyl ring, if m is 0 and n is 1 or 2; Ris hydrogen or lower alkyl; n is 0, 1 or 2; m is 0 or 1; with the proviso that n and m are not simultaneously 0; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They may be used for the treatment of schizophrenia or cognitive disorders.
申请公布号 EA022019(B1) 申请公布日期 2015.10.30
申请号 EA20130091537 申请日期 2012.04.23
申请人 F.HOFFMANN-LA ROCHE AG 发明人 JAESCHKE GEORG;JOLIDON SYNESE;LINDEMANN LOTHAR;STADLER HEINZ;VIEIRA ERIC
分类号 C07D401/04;A61K31/44;A61K31/4406;A61K31/501;A61K31/506;A61K31/55;A61P25/18;A61P25/28;A61P25/30;C07D401/14;C07D403/04 主分类号 C07D401/04
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