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    Process for the preparation and purification of 1,5-naphthyridine-3-carboxyamides and purification of 1,5-naphthyridine-3-carboxyamides
    3.
    发明申请
    Process for the preparation and purification of 1,5-naphthyridine-3-carboxyamides and purification of 1,5-naphthyridine-3-carboxyamides 审中-公开
    1,5-二氮杂萘-3-羧酰胺的制备和纯化方法及1,5-二氮杂萘-3-羧酰胺的纯化

    公开(公告)号：US20050004364A1

    公开(公告)日：2005-01-06

    申请号：US10852942

    申请日：2004-05-25

    申请人： Michael Castaldi ,  David Ripin ,  Dennis Bourassa

    发明人： Michael Castaldi ,  David Ripin ,  Dennis Bourassa

    IPC分类号： C07D471/02 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A new route for the preparation and purification of substituted 1,5-naphthyridine-3-carboxyamides, useful in the diagnosis and treatment of anxiety, Downs Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness, is provided. These compounds may be readily prepared by treating the corresponding 1,5-naphthyridine-3-carboxylic acids with a primary amine and a 1,1-carbonyldiimidazole. Purification is achieved by converting the substituted 1,5-naphthyridine-3-carboxyamides to a salt with a strong base such as potassium t-butoxide, recrystallizing and acidifying to regenerate the pure carboxyamide.

    摘要翻译： 用于制备和纯化用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍以及用苯二氮卓类药物过量并用于提高警觉性的取代的1,5-二氮杂萘-3-羧酰胺的新途径， 被提供。 这些化合物可以通过用伯胺和1,1-羰基二咪唑处理相应的1,5-二氮杂萘-3-羧酸来容易地制备。 通过将取代的1,5-二氮杂萘-3-羧酰胺与强碱如叔丁醇钾进行转化，重结晶并酸化以再生纯的酰胺来实现纯化。

    Process for the preparation of 1,5-naphthyridine-3-carboxyamides by direct ester amidation
    4.
    发明申请
    Process for the preparation of 1,5-naphthyridine-3-carboxyamides by direct ester amidation 审中-公开
    通过直接酯酰胺化制备1,5-萘啶-3-羧酰胺的方法

    公开(公告)号：US20050038065A1

    公开(公告)日：2005-02-17

    申请号：US10856161

    申请日：2004-05-28

    申请人： Gregory Karrick ,  David Ripin ,  Lulin Wei

    发明人： Gregory Karrick ,  David Ripin ,  Lulin Wei

    IPC分类号： C07D471/04 ,  C07D471/02 ,  A61K31/4745

    CPC分类号： C07D471/04

    摘要： A new route for the preparation of substituted 1,5-naphthyridine-3-carboxyamides, useful in the diagnosis and treatment of anxiety, Downs Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness, is provided. These compounds may be readily prepared by heating the corresponding 1,5-naphthyridine-3-carboxylic acid ester with a primary amine in a polar solvent such as dimethylformamide or dimethylsulfoxide.

    摘要翻译： 提供了一种制备用于诊断和治疗焦虑症，唐氏综合症，睡眠，认知和发作障碍以及用苯二氮卓类药物过量并提高警觉性的取代的1,5-二氮杂萘-3-羧酰胺的新途径 。 这些化合物可以通过在极性溶剂如二甲基甲酰胺或二甲基亚砜中用伯胺加热相应的1,5-二氮杂萘-3-羧酸酯来容易地制备。

    Processes for the preparation of substituted bicyclic derivatives
    5.
    发明申请
    Processes for the preparation of substituted bicyclic derivatives 审中-公开
    制备取代的双环衍生物的方法

    公开(公告)号：US20050026940A1

    公开(公告)日：2005-02-03

    申请号：US10821906

    申请日：2004-04-09

    申请人： David Ripin ,  Michael Vetelino ,  Lulin Wei

    发明人： David Ripin ,  Michael Vetelino ,  Lulin Wei

    IPC分类号： A61K31/517 ,  A61K31/55 ,  C07C271/66 ,  C07D401/12 ,  C07

    CPC分类号： C07D401/12 ,  C07C271/66

    摘要： The invention relates to processes for preparing compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R6, R11, R13, R14, R15, R16, R17, k, l, and m are as defined herein. The compounds of formula 1 are useful intermediates toward preparing compounds that may be used in treating abnormal cell growth in mammals by administering pharmaceutical compositions.

    摘要翻译： 本发明涉及制备式1化合物及其药学上可接受的盐，前药和溶剂化物的方法，其中R 1，R 3，R 4，R 6，R 11，R R 13，R 15，R 16，R 17，k，l和m如本文所定义。 式1的化合物是制备可用于通过施用药物组合物治疗哺乳动物异常细胞生长的化合物的有用中间体。