发明名称 5-(PHENYL/PYRIDINYL-ETHINYL)-2-PYRIDINE/ 2-PYRIMIDINE-CARBORXAMID ES AS MGLUR5 MODULATORS.
摘要 The present invention relates to ethynyl derivatives of formula (I), wherein, Y is N or C-R3;and R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2' may form together with the N-atom to which they are attached a morpholine ring, a piperidine ring or an azetidine ring, which are unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy or methyl; R4/R4' are independently from each other hydrogen or lower alkyl, or R4 and R4' form together a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; 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).
申请公布号 MX338631(B) 申请公布日期 2016.04.26
申请号 MX20130012125 申请日期 2012.04.17
申请人 F. HOFFMANN-LA ROCHE AG 发明人 ANTONIO RICCI;GEORG JAESCHKE;SYNESE JOLIDON;LOTHAR LINDEMANN;HEINZ STADLER;ERIC VIEIRA;DANIEL RUEHER
分类号 C07D213/56;A61K31/4427;A61K31/445;A61K31/506;A61P25/00;A61P25/28;C07D213/57;C07D239/28;C07D401/06;C07D403/06;C07D407/12;C07D413/06 主分类号 C07D213/56
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