发明名称 |
POSITIVE ALLOSTERIC MODULATORS (PAM) |
摘要 |
<p>The present invention relates to phenylethynyl derivatives of formula (I) wherein R1 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl substituted by hydroxy; X is N, CF or CH; L is -NR3-, -NHC(R3)2-, -O-, -OC(R3)2-, -CR4R4'-; R3 is hydrogen or lower alkyl; R4/R4' are independently from each other hydrogen or lower alkyl; cyc is cycloalkyl or heterocycloalkyl, or is a non-aromatic bicycle selected from 7-oxa- bicyclo[2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n is 1, 2 or 3; 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). They are useful for the treatment of schizophrenia or cognitive diseases.</p> |
申请公布号 |
WO2011051201(A1) |
申请公布日期 |
2011.05.05 |
申请号 |
WO2010EP66016 |
申请日期 |
2010.10.25 |
申请人 |
F. HOFFMANN-LA ROCHE AG;GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;RICCI, ANTONIO;RUEHER, DANIEL;STADLER, HEINZ;VIEIRA, ERIC |
发明人 |
GREEN, LUKE;GUBA, WOLFGANG;JAESCHKE, GEORG;JOLIDON, SYNESE;LINDEMANN, LOTHAR;RICCI, ANTONIO;RUEHER, DANIEL;STADLER, HEINZ;VIEIRA, ERIC |
分类号 |
C07D213/74;A61K31/44;A61K31/4427;A61K31/505;A61K31/506;C07D239/34;C07D239/42;C07D401/06;C07D405/12;C07D413/06;C07D493/08 |
主分类号 |
C07D213/74 |
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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