发明名称 ETHYNYL DERIVATIVES
摘要 <p>The present invention relates to ethynyl derivatives of formula (I) wherein X is N or C-R1; Y is N or C-R2; Z is CH or N; R4 is a 6-membered aromatic substituent containing 0, 1 or 2 nitrogen atoms, optionally substituted by 1 to 3 groups, selected from halogen, lower alkyl, lower alkoxy or NRR'; R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, lower hydroxyalkyl, lower cycloalkyl or is heterocycloalkyl optionally substituted with hydroxy or alkoxy; R2 is hydrogen, CN, lower alkyl or heterocycloalkyl; R and R' are independently from each other hydrogen or lower alkyl; or to a pharmaceutically acceptable salt or 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) and they are therefore useful for the treatment of diseases related to this receptor.</p>
申请公布号 WO2011073172(A1) 申请公布日期 2011.06.23
申请号 WO2010EP69593 申请日期 2010.12.14
申请人 F. HOFFMANN-LA ROCHE AG;GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;STADLER, HEINZ;VIEIRA, ERIC 发明人 GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;STADLER, HEINZ;VIEIRA, ERIC
分类号 C07D471/04;A61K31/4162;A61P25/00;C07D487/04 主分类号 C07D471/04
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