JAESCHKE,GEORG,JOLIDON,SYNESE,LINDEMANN,LOTHAR,RICCI, ANTONIO,RUEHER, DANIEL,STADLER,HEINZ,VIEIRA, ERIC
申请号：
MYPI 2013003816
公开号：
MY161403A
申请日:
2012.04.17
申请国别(地区):
MY
年份:
2017
代理人:
摘要：
THE PRESENT INVENTION RELATES TO ETHYNYL DERIVATIVES OF FORMULA I WHEREIN Y IS N OR C-R3； AND R3 IS HYDROGEN, METHYL, HALOGEN OR NITRILE； R1 IS PHENYL OR PYRIDINYL, WHICH ARE OPTIONALLY SUBSTITUTED BY HALOGEN, LOWER ALKYL OR LOWER ALKOXY； R2/R2’ ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN, LOWER ALKYL OR LOWER ALKYL SUBSTITUTED BY HALOGEN, OR R2 AND R2’ MAY FORM TOGETHER WITH THE N-ATOM TO WHICH THEY ARE ATTACHED A MORPHOLINE RING, A PIPERIDINE RING OR AN AZETIDINE RING, WHICH ARE UNSUBSTITUTED OR SUBSTITUTED ONE OR MORE SUBSITUENTS SELECTED FROM LOWER ALKOXY, HALOGEN, HYDROXY OR METHYL； R4/R4’ ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN OR LOWER ALKYL, OR R4 AND R4’ 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 NOW, SURPRISINGLY BEEN FOUND THAT THE COMPOUNDS OF GENERAL FORMULA I ARE POSITIVE ALLOSTERIC MODULATORS (PAM) OF THE METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE 5 (MGLUR5). (NO SUITABLE FIGURE)
