JAESCHKE, GEORG,LINDEMANN, LOTHAR,RICCI, ANTONIO,RUEHER, DANIEL,STADLER, HEINZ,VIEIRA, ERIC
申请号：
CA2847096
公开号：
CA2847096A1
申请日:
2012.10.04
申请国别(地区):
CA
年份:
2013
代理人:
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).
