发明名称 5-(PHENYL/PYRIDINYL-ETHINYL)-2-PYRIDINE/2-PYRIMIDINE-CARBORXAMIDES AS MGLUR5 MODULATORS
摘要 <p>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).</p>
申请公布号 SI2699547(T1) 申请公布日期 2015.06.30
申请号 SI20120030200T 申请日期 2012.04.17
申请人 F. HOFFMANN-LA ROCHE AG 发明人 JAESCHKE GEORG;JOLIDON SYNESE;LINDEMANN LOTHAR;RICCI ANTONIO;RUEHER DANIEL;STADLER HEINZ;VIEIRA ERIC
分类号 主分类号
代理机构 代理人
主权项
地址