发明名称 |
ETHYNYL DERIVATIVES |
摘要 |
<p>The present invention 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'; 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' 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.</p> |
申请公布号 |
WO2011073172(A1) |
申请公布日期 |
2011.06.23 |
申请号 |
WO2010EP69593 |
申请日期 |
2010.12.14 |
申请人 |
F. HOFFMANN-LA ROCHE AG;GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;STADLER, HEINZ;VIEIRA, ERIC |
发明人 |
GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;STADLER, HEINZ;VIEIRA, ERIC |
分类号 |
C07D471/04;A61K31/4162;A61P25/00;C07D487/04 |
主分类号 |
C07D471/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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