发明名称 PHENYL OR PYRIDINYL-ETHYNYL DERIVATIVES
摘要 The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2′are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4′are each independently hydrogen or lower alkyl, or R4 and R4′together form 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. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
申请公布号 US2012270852(A1) 申请公布日期 2012.10.25
申请号 US201213443911 申请日期 2012.04.11
申请人 JAESCHKE GEORG;JOLIDON SYNESE;LINDEMANN LOTHAR;RICCI ANTONIO;RUEHER DANIEL;STADLER HEINZ;VIEIRA ERIC 发明人 JAESCHKE GEORG;JOLIDON SYNESE;LINDEMANN LOTHAR;RICCI ANTONIO;RUEHER DANIEL;STADLER HEINZ;VIEIRA ERIC
分类号 A61K31/506;A61K31/44;A61K31/4427;A61K31/444;A61K31/4545;A61K31/505;A61K31/5377;A61P25/00;A61P25/18;A61P35/00;C07D213/81;C07D213/85;C07D239/28;C07D401/06;C07D403/06;C07D405/12;C07D413/06 主分类号 A61K31/506
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