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    PHENYL OR PYRIDINYL-ETHYNYL DERIVATIVES
    4.
    发明申请
    PHENYL OR PYRIDINYL-ETHYNYL DERIVATIVES 有权
    苯基或吡啶基乙炔衍生物

    公开(公告)号：US20120270852A1

    公开(公告)日：2012-10-25

    申请号：US13443911

    申请日：2012-04-11

    申请人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    发明人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    IPC分类号： A61K31/506 ,  A61K31/44 ,  C07D401/06 ,  A61K31/444 ,  C07D239/28 ,  A61K31/505 ,  C07D405/12 ,  A61K31/4427 ,  C07D413/06 ,  A61K31/5377 ,  A61K31/4545 ,  C07D403/06 ,  C07D213/85 ,  A61P25/00 ,  A61P25/18 ,  A61P35/00 ,  C07D213/81

    CPC分类号： C07D213/56 ,  C07D213/57 ,  C07D239/28 ,  C07D401/06 ,  C07D403/06 ,  C07D407/12 ,  C07D413/06

    摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; 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′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ 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′ are each independently hydrogen or lower alkyl, or R4 and R4′ 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).

    摘要翻译： 本发明涉及式I的乙炔基衍生物，其中Y是N或C-R3; R3是氢，甲基，卤素或腈; R1是苯基或吡啶基，其各自任选被卤素，低级烷基或低级烷氧基取代; R2 / R2'各自独立地为氢，被卤素取代的低级烷基或低级烷基，或R2和R2'与它们所连接的N-原子一起形成吗啉环，哌啶环或氮杂环丁烷环，其中每个 未取代或取代的一个或多个选自低级烷氧基，卤素，羟基和甲基的取代基; R 4 / R 4'各自独立地为氢或低级烷基，或者R 4和R 4'一起形成C 3-5环烷基，四氢呋喃或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。 式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。

    Phenyl or pyridinyl-ethynyl derivatives
    5.
    发明授权
    Phenyl or pyridinyl-ethynyl derivatives 有权
    苯基或吡啶基 - 乙炔基衍生物

    公开(公告)号：US08772300B2

    公开(公告)日：2014-07-08

    申请号：US13443911

    申请日：2012-04-11

    申请人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    发明人： Georg Jaeschke ,  Synese Jolidon ,  Lothar Lindemann ,  Antonio Ricci ,  Daniel Rueher ,  Heinz Stadler ,  Eric Vieira

    IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

    CPC分类号： C07D213/56 ,  C07D213/57 ,  C07D239/28 ,  C07D401/06 ,  C07D403/06 ,  C07D407/12 ,  C07D413/06

    摘要： The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; 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′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ 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′ are each independently hydrogen or lower alkyl, or R4 and R4′ 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).

    摘要翻译： 本发明涉及式I的乙炔基衍生物，其中Y是N或C-R3; R3是氢，甲基，卤素或腈; R1是苯基或吡啶基，其各自任选被卤素，低级烷基或低级烷氧基取代; R2 / R2'各自独立地为氢，被卤素取代的低级烷基或低级烷基，或R2和R2'与它们所连接的N-原子一起形成吗啉环，哌啶环或氮杂环丁烷环，其中每个 未取代或取代的一个或多个选自低级烷氧基，卤素，羟基和甲基的取代基; R 4 / R 4'各自独立地为氢或低级烷基，或者R 4和R 4'一起形成C 3-5环烷基，四氢呋喃或氧杂环丁烷环; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体和/或立体异构体。 式I化合物是代谢型谷氨酸受体亚型5（mGluR5）的正变构调节剂（PAM）。