JAESCHKE GEORG,JOLIDON SYNESE,LINDEMANN LOTHAR,STADLER HEINZ,VIEIRA ERIC
申请号：
IN6998/CHENP/2013
公开号：
IN2013CN06998A
申请日:
2013.08.30
申请国别(地区):
IN
年份:
2016
代理人:
摘要：
1233 4466 644 65The present invention relates to ethynyl derivatives of formula I wherein X is N or C R wherein R is hydrogen or halogen G is N or CH with the proviso that maximum one of G or X can be nitrogen R is phenyl or pyridinyl which are optionally substituted by halogen R is hydrogen lower alkyl hydroxy lower alkoxy or C(O)O benzyl R R R R R R are independently from each other hydrogen or lower alkyl or R and R may form together with the carbon atom to which they are attached a C cycloalkyl ring if m is 0 and n is 1 or 2 R is hydrogen or lower alkyl n is 0 1 or 2 m is 0 or 1 with the proviso that n and m are not simultaneously 0 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 may be used for the treatment of schizophrenia or cognitive disorders.
