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5-(PHENYL/PYRIDINYL-ETHINYL)-2-PYRIDINE/2-PYRIMIDINE-CARBORXAMIDES AS MGLUR5 MODULATORS
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JAESCHKE GEORG,JAESCHKE Georg,JOLIDON SYNESE,JOLIDON Synese,LINDEMANN LOTHAR,LINDEMANN Lothar,RICCI ANTONIO,RICCI Antonio,RUEHER DANIEL,RUEHER Daniel,STADLER HEINZ,STADLER Heinz,VIEIRA ERIC,VIEIRA Eri
申请号:
SI201230200
公开号:
SI2699547T1
申请日:
2012.04.17
申请国别(地区):
SI
年份:
2015
代理人:
摘要:
The present invention relates to ethynyl derivatives of formula I wherein Y is N or C&mdashR3 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&prime are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2&prime 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&prime are each independently hydrogen or lower alkyl, or R4 and R4&prime 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).
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