GREEN, LUKE,GUBA, WOLFGANG,JAESCHKE, GEORG,JOLIDON, SYNESE,LINDEMANN, LOTHAR,STADLER, HEINZ,VIEIRA, ERIC
申请号：
SG2012044814
公开号：
SG181779A1
申请日:
2010.12.14
申请国别(地区):
SG
年份:
2012
代理人:
摘要：
The present invention relates to ethynyl derivatives of formula (I) wherein X is N or C-R1； Y is N or C-R2； Z is CH or N； R4 is a 6-membered aromatic substituent containing 0, 1 or 2 nitrogen atoms, optionally substituted by 1 to 3 groups, selected from halogen, lower alkyl, lower alkoxy or NRR'； R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, lower hydroxyalkyl, lower cycloalkyl or is heterocycloalkyl optionally substituted with hydroxy or alkoxy； R2 is hydrogen, CN, lower alkyl or heterocycloalkyl； R and R' are independently from each other hydrogen or lower alkyl； or to a pharmaceutically acceptable salt or 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) and they are therefore useful for the treatment of diseases related to this receptor.
