F. HOFFMANN-LA ROCHE AG;VIEIRA, Eric;JAESCHKE, Georg;LINDEMANN, Lothar;RUEHER, Daniel;RICCI, Antonio;STADLER, Heinz
发明人:
JAESCHKE, Georg,LINDEMANN, Lothar,RICCI, Antonio,RUEHER, Daniel,STADLER, Heinz,VIEIRA, Eric
申请号：
EPEP2012/069599
公开号：
WO2013/050454A1
申请日:
2012.10.04
申请国别(地区):
EP
年份:
2013
代理人:
摘要：
The present invention relates to ethynyl derivatives of formula (I) wherein U is N or CH, R8 is hydrogen, halogen, lower alkyl or lower alkoxy；Y is –N(R4)-, -O- or –C(R5R5')-； wherein R4 is hydrogen or lower alkyl and R5/R5' are independently hydrogen, hydroxy, lower alkyl or lower alkoxy； V is –N(R6)- or –C(R7R7'), wherein R6 is hydrogen or lower alkyl and R7/R7' are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl； R1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy； m is 0 or 1； in case m is 1, R3/R3' are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl； n is 0 or 1； in case n is 1, R2/R2' are independently from each other hydrogen, lower alkyl, CH2-lower alkoxy or may form together with the carbon atom to which they are attached a C3-C6-cycloalkyl； or if m is 1 and n is 0, R3 and R7 may form together with the carbon atoms to which they are attached a C4-6-cycloalkyl； or if m is 1 and n is 1, R2 and R3 or R3 and R7 may form together with the carbon atoms to which they are attached a C4-6-cycloalkyl； 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 been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).La présente invention concerne des dérivés d'éthynyle de formule (I) où U est un groupe N ou CH, R8 est un groupe hydrogène, halogène, alkyle inférieur ou alcoxy inférieur ； Y est -N(R4)-, -O- ou -C(R5R5')- ； où R4 est un groupe hydrogène ou alkyle inférieur et R5/R5' sont indépendamment un groupe hydrogène, hydroxy, alkyle inférieur ou alcoxy inférieur ； V est -N(R6)- ou -C(R7R7'), où R6 est un groupe h
