GREEN LUKE,GUBA WOLFGANG,JAESCHKE GEORG,JOLIDON SYNESE,LINDEMANN LOTHAR,STADLER HEINZ,VIEIRA ERIC
申请号：
NZ59955310
公开号：
NZ599553A
申请日:
2010.12.14
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
The present disclosure 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&rsquo；； 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&rsquo； 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. Compounds of the disclosure include: 6-Phenylethynyl-[1,2,3]triazolo[1,5-a]pyridine, 2-tert-Butyl-6-phenylethynyl-pyrazolo[1,5-a]pyridine, 6-Phenylethynyl-2-pyrrolidin-1-yl-[1,2,4]triazolo[1,5-a]pyrimidine, 2-Methyl-2-(6-phenylethynyl-[1,2,4]triazolo[1,5-a]pyridin-2-yl)-propan-1-ol, 2-Cyclobutyl-6-phenylethynyl-pyrazolo[1,5-a]pyrimidine, 2-Isopropyl-6-phenylethynyl-pyrazolo[1,5-a]pyrimidine, 6-(4-Chloro-phenylethynyl)-2-methyl-pyrazolo[1,5-a]pyrimidine and 6-(2-Fluoro-phenylethynyl)-2-methyl-pyrazolo[1,5-a]pyrimidine
