申请人:Hoffmann-La Roche Inc.
公开号:US09227959B2
公开(公告)日:2016-01-05
The present invention relates to ethynyl derivatives of formula I
wherein
Y is N or CH
R1 is fluoro or chloro
R2 is hydrogen or methyl
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 metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
本发明涉及公式I的乙炔衍生物,其中Y为N或CHR1,R1为氟或氯,R2为氢或甲基,或其药学上可接受的酸加成盐,或其外消旋混合物,或其相应的对映体和/或光学异构体和/或立体异构体。现已惊奇地发现,通式I的化合物是代谢型谷氨酸受体拮抗剂(负向变构调节剂),可用于治疗焦虑和疼痛、抑郁症、脆性X综合症、自闭症谱系障碍、帕金森病和胃食管反流病(GERD)。