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    Imidazolyl and pyrazolyl ethyne compounds
    2.
    发明申请
    Imidazolyl and pyrazolyl ethyne compounds 审中-公开
    咪唑基和吡唑基乙炔化合物

    公开(公告)号：US20050085523A1

    公开(公告)日：2005-04-21

    申请号：US10874991

    申请日：2004-06-23

    申请人： Nicholas Cosford ,  Theodore Kamenecka ,  Jeffrey Roppe

    发明人： Nicholas Cosford ,  Theodore Kamenecka ,  Jeffrey Roppe

    IPC分类号： C07D213/16 ,  C07D213/30 ,  C07D233/54 ,  C07D233/61 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D285/00 ,  C07D285/01 ,  C07D333/08 ,  A61K31/445 ,  A61K31/416 ,  A61K31/4172 ,  A61K31/4178

    CPC分类号： C07D213/16 ,  C07D213/30 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D285/01 ,  C07D333/08

    摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

    摘要翻译： 根据本发明，提供了一类新的杂环化合物。 本发明的化合物含有包含至少一个氮原子和至少一个碳原子的取代的，不饱和的五，六或七元杂环。 该环另外包括独立地选自碳，氮，硫和氧原子的三个，四个或五个原子。 该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。 该环的强制取代基包括通过碳 - 碳双键，碳 - 碳三键或偶氮基与杂环连接的部分（B）。 强制性取代基位于环氮原子附近。 本发明化合物能够具有多种用途。 例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。 本发明的化合物也可以作为杀虫剂和杀真菌剂。 含有本发明化合物的药物组合物也具有广泛的用途。

    Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5
    10.
    发明申请
    Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5 失效
    代谢型谷氨酸受体-5的二芳基取代三唑调节剂

    公开(公告)号：US20070082067A1

    公开(公告)日：2007-04-12

    申请号：US10552362

    申请日：2004-03-31

    申请人： Nicholas Cosford ,  Jeffrey Roppe ,  Lida Tehrani ,  Bowei Wang

    发明人： Nicholas Cosford ,  Jeffrey Roppe ,  Lida Tehrani ,  Bowei Wang

    IPC分类号： A61K31/444 ,  C07D403/14 ,  A61K31/551 ,  A61K31/485 ,  A61K31/506

    CPC分类号： A61K31/41 ,  A61K31/4192 ,  C07D401/10 ,  C07D401/14

    摘要： Novel triazole compounds represented by Formula (1): (where A, A1, A2, A3, A4, A5, B, R11, W, X, Y and Z are as defined herein) in which the triazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.

    摘要翻译： 由式（1）表示的新型三唑化合物：其中A，A 1，A 2，A 3，A 4， A，B，R 11，W，X，Y和Z如本文所定义），其中三唑直接被取代，或通过桥 ，其中i）包含与杂芳基的连接点相邻的N的杂芳基部分和ii）另外的杂芳基或芳基环，其中至少一个环进一步被另一个环取代，是用于治疗精神病学的mGluR5调节剂 以及情绪障碍，例如精神分裂症，焦虑症，抑郁症，恐慌症和双相性精神障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，药物戒断 ，肥胖等疾病。