GREEN, LUKE,GUBA, WOLFGANG,JAESCHKE, GEORG,JOLIDON, SYNESE,LINDEMANN, LOTHAR,RICCI, ANTONIO,RUEHER, DANIEL,STADLER, HEINZ,VIEIRA, ERIC
申请号：
CA2778219
公开号：
CA2778219C
申请日:
2010.10.25
申请国别(地区):
CA
年份:
2017
代理人:
摘要：
The present invention relates to phenylethynyl derivatives of formula (I) wherein R1 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen； R2 is hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl substituted by hydroxy； X is N, CF or CH； L is -NR3-, -NHC(R3)2-, -O-, -OC(R3)2-, -CR4R4'-； R3 is hydrogen or lower alkyl； R4/R4' are independently from each other hydrogen or lower alkyl； cyc is cycloalkyl or heterocycloalkyl, or is a non-aromatic bicycle selected from 7-oxa- bicyclo[2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl； n is 1, 2 or 3； 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 positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
