发明名称 Arylethynyl derivatives
摘要 The present invention relates to ethynyl derivatives of formula I; wherein R1 is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl;or to a pharmaceutically acceptable acid addition salt, in enantiomerically pure form with the absolute configuration as shown in formula I.;It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) which show advantageous biochemical-, physicochemical- and pharmacodynamic-properties compared to compounds of prior art.
申请公布号 US9221802(B2) 申请公布日期 2015.12.29
申请号 US201514669653 申请日期 2015.03.26
申请人 Hoffman-La Roche Inc. 发明人 Jaeschke Georg;Lindemann Lothar;Stadler Heinz;Vieira Eric
分类号 C07D413/04 主分类号 C07D413/04
代理机构 代理人 Kale Tamara A.
主权项 1. An ethynyl derivative of formula Iwherein R1 is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl; or a pharmaceutically acceptable acid addition salt in enantiomerically pure form.
地址 Little Falls NJ US