Imidazo[1,2-b]pyridazines, processes, uses, intermediates and compositions
    2.
    发明授权
    Imidazo[1,2-b]pyridazines, processes, uses, intermediates and compositions 有权
    咪唑并[1,2-b]哒嗪,方法,用途,中间体和组合物

    公开(公告)号:US08993562B2

    公开(公告)日:2015-03-31

    申请号:US13282926

    申请日:2011-10-27

    CPC分类号: C07D487/04

    摘要: The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof.Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation.The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

    摘要翻译: 本发明提供式(I)的新型咪唑并[1,2-b]哒嗪及其药学上可接受的盐,多晶型物,水合物,互变异构体,溶剂合物和立体异构体。 式(I)化合物可用于治疗或预防与GABA A受体调节,焦虑,癫痫,包括失眠在内的睡眠障碍以及用于诱导镇静催眠,麻醉,睡眠和肌肉松弛相关的疾病。 本发明还提供了用于制备所述化合物和某些中间体以及中间体本身的合成方法。

    PROCESS FOR PREPARING 4-NITRO-OXY-METHYL-BENZOIC ACID
    4.
    发明申请
    PROCESS FOR PREPARING 4-NITRO-OXY-METHYL-BENZOIC ACID 审中-公开
    制备4-硝基 - 甲基苯甲酸的方法

    公开(公告)号:US20130131378A1

    公开(公告)日:2013-05-23

    申请号:US13509906

    申请日:2010-11-15

    IPC分类号: C07C51/347

    摘要: This invention relates to a new process for preparing 4-nitro-oxy-methyl-benzoic acid, comprising the following steps: a) reaction of 4-chloromethyl-benzoic acid with silver nitrate and in the presence of an acid as a catalyst in acetonitrile at reflux temperature, followed by cooling and adding of a polar aprotic solvent; b) separation of the silver salts by filtration, followed by washout with a polar aprotic solvent; c) precipitation of the 4-nitro-oxy-methyl-benzoic acid with water from the filtrate obtained in step b); and d) drying of the 4-nitro-oxy-methyl-benzoic acid.

    摘要翻译: 本发明涉及一种制备4-硝基 - 氧 - 甲基 - 苯甲酸的新方法,包括以下步骤:a)4-氯甲基 - 苯甲酸与硝酸银的反应,并在乙酸存在下作为催化剂在乙腈 在回流温度下,然后冷却并加入极性非质子溶剂; b)通过过滤分离银盐,然后用极性非质子溶剂洗涤; c)从步骤b)中获得的滤液中用水沉淀4-硝基 - 氧 - 甲基 - 苯甲酸; 和d)4-硝基 - 氧 - 甲基 - 苯甲酸的干燥。