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31 条记录 (耗时 0.017 秒)

    ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
    2.
    发明公开
    ETHYNYL DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR MODULATORS 有权
    乙酰丙酸甲酯代谢物谷氨酸酶抑制剂

    公开(公告)号：EP2763969A1

    公开(公告)日：2014-08-13

    申请号：EP12772100.9

    申请日：2012-10-04

    申请人： F.Hoffmann-La Roche AG

    发明人： JAESCHKE, Georg ,  LINDEMANN, Lothar ,  RICCI, Antonio ,  RUEHER, Daniel ,  STADLER, Heinz ,  VIEIRA, Eric

    IPC分类号： C07D237/22 ,  C07D239/42 ,  A61K31/44 ,  A61K31/50 ,  A61K31/505

    CPC分类号： C07D213/74 ,  C07D237/22 ,  C07D239/42

    摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH; with the proviso that Y can only be CH, if at least on of U, V or W are N; U is N or C-R
    4 ; V and W are independently N or CH; with the proviso that only one of U, V or W can be simultaneously nitrogen; R
    4 is hydrogen, methyl or halogen; R
    1 is phenyl or heteroaryl, which are optionally substituted by halogen, lower alkyl or lower alkoxy; R is hydrogen or lower alkyl; R
    2 is hydrogen, lower alkyl, lower alkoxy, CF
    3 or S-lower alkyl; are independently from each other hydrogen, lower alkyl or lower alkoxy; or R
    3 and R
    3 form together a C
    3-5 -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. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

    ETHYNYL DERIVATIVES AS MODULATORS OF MGLUR5 RECEPTOR ACTIVITY
    5.
    发明公开
    ETHYNYL DERIVATIVES AS MODULATORS OF MGLUR5 RECEPTOR ACTIVITY 有权
    乙炔基衍生物作为MGLUR5受体活性的调节剂

    公开(公告)号：EP2909179A1

    公开(公告)日：2015-08-26

    申请号：EP13776810.7

    申请日：2013-10-15

    申请人： F.Hoffmann-La Roche AG

    发明人： JAESCHKE, Georg ,  LINDEMANN, Lothar ,  RICCI, Antonio ,  RUEHER, Daniel ,  STADLER, Heinz ,  VIEIRA, Eric

    IPC分类号： C07D213/81 ,  A61K31/44 ,  A61K31/444 ,  A61P25/24 ,  A61P25/16 ,  A61P1/00

    CPC分类号： C07D213/81

    摘要： The present invention relates to ethynyl derivatives of formula (I) 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 metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

    摘要翻译： 本发明涉及式（I）的乙炔基衍生物或其药学上可接受的酸加成盐，外消旋混合物或其相应的对映异构体和/或旋光异构体和/或立体异构体。 现在令人惊讶地发现通式（I）的化合物是用于治疗焦虑和疼痛，抑郁症，脆性X综合症，自闭症谱系障碍，帕金森氏病和 胃食管反流病（GERD）。

    ARYLETHYNYL DERIVATIVES
    7.
    发明公开
    ARYLETHYNYL DERIVATIVES 有权
    芳基乙炔衍生物

    公开(公告)号：EP2875000A1

    公开(公告)日：2015-05-27

    申请号：EP13735315.7

    申请日：2013-07-12

    申请人： F.Hoffmann-La Roche AG

    发明人： JAESCHKE, Georg ,  LINDEMANN, Lothar ,  STADLER, Heinz ,  VIEIRA, Eric

    IPC分类号： C07D209/52 ,  A61K31/403 ,  A61P25/00

    CPC分类号： C07D401/04 ,  C07D209/52

    摘要： The present invention relates to ethynyl derivatives of formula (I) wherein R
    1 is phenyl, which is optionally substituted by 1-2 halogen atoms; selected from fluorine or chlorine; or to a pharmaceutically acceptable acid addition salt in enantiomerically pure form. It has been found that the compounds of general formula (I) are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

    摘要翻译： 本发明涉及式（I）的乙炔基衍生物，其中R 1是苯基，其任选被1-2个卤素原子取代; 选自氟或氯; 或对映体纯形式的药学上可接受的酸加成盐。 已经发现通式（I）的化合物是代谢型谷氨酸受体亚型5（mGluR5）的变构调节剂。