JAESCHKE GEORG,JOLIDON SYNESE,LINDEMANN LOTHAR,RICCI ANTONIO,RUEHER DANIEL,STADLER HEINZ,VIEIRA ERIC
申请号：
NZ61488312
公开号：
NZ614883A
申请日:
2012.04.23
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
The present disclosure relates to ethynyl derivatives of formula I wherein X is N or CH； G is N or CH； with the proviso that maximum one of X or G can be nitrogen； R1 is phenyl or pyridyl, which are optionally substituted by halogen, lower alkyl or lower alkoxy； R2 is hydrogen, lower alkyl or may form together with R4 a C3-C6-cycloalkyl； R3, R3&rsquo；, R4, R4&rsquo； are independently from each other hydrogen, lower alkyl or CF； 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). Examples of compounds of formula (I) are: 2-[6-(2,5-difluoro-phenylethynyl)-pyridazin-3-yl]-5,5-dimethyl-pyrazolidin-3-one； 5,5-dimethyl-2-(5-phenylethynyl-pyrimidin-2-yl)-pyrazolidin-3-one； (RS)-1-(5-phenylethynyl-pyrimidin-2-yl)-tetrahydro-pyrrolo[1,2-b]pyrazol-2-one； 5,5-dimethyl-2-(5-phenylethynyl-pyridin-2-yl)-pyrazolidin-3-one and (RS)-5-isopropyl-2-(5-phenylethynyl-pyridin-2-yl)-pyrazolidin-3-one.
