Georg Jaeschke;Daniel Rueher;Eric Vieira;Antonio Ricci;Lothar Lindemann;Heinz Stadler;Synese Jolidon
发明人:
Georg Jaeschke,Synese Jolidon,Lothar Lindemann,Antonio Ricci,Daniel Rueher,Heinz Stadler,Eric Vieira
申请号：
US13443911
公开号：
US20120270852A1
申请日:
2012.04.11
申请国别(地区):
US
年份:
2012
代理人:
摘要：
The present invention relates to ethynyl derivatives of formula IwhereinY is N or C—R3；R3 is hydrogen, methyl, halogen or nitrile；R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy；R2/R2′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl；R4/R4′ are each independently hydrogen or lower alkyl, or R4 and R4′ together form 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. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
