发明名称 ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
摘要 The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH; with the proviso that Y can only be CH, if at least on of U, V or W are N; U is N or C-R4; V and W are independently N or CH; with the proviso that only one of U, V or W can be simultaneously nitrogen; R4 is hydrogen, methyl or halogen; R1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, lower alkoxy, CF3 or S-lower alkyl; are independently from each other hydrogen, lower alkyl or lower alkoxy; or R3 and R3 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 been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
申请公布号 CA2847096(A1) 申请公布日期 2013.04.11
申请号 CA20122847096 申请日期 2012.10.04
申请人 F. HOFFMANN-LA ROCHE AG 发明人 JAESCHKE, GEORG;LINDEMANN, LOTHAR;RICCI, ANTONIO;RUEHER, DANIEL;STADLER, HEINZ;VIEIRA, ERIC
分类号 C07D237/22;A61K31/44;A61K31/50;A61K31/505;C07D239/42 主分类号 C07D237/22
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