Process for preparing N-phosphonomethylamino carboxylic acids
    4.
    发明授权
    Process for preparing N-phosphonomethylamino carboxylic acids 失效
    制备N-膦酰基甲基氨基羧酸的方法

    公开(公告)号:US5602276A

    公开(公告)日:1997-02-11

    申请号:US674084

    申请日:1996-07-01

    IPC分类号: C07F9/38

    CPC分类号: C07F9/3813

    摘要: A process for preparing N-hydroxyalkylaminomethylphosphonic acid or salts thereof which comprises contacting an alkanolamine, formaldehyde and a dialkyl phosphite in the presence of an alcohol under suitable reaction conditions to produce a reaction mixture, and hydrolyzing the reaction mixture under acidic or basic conditions. In one embodiment, the N-hydroxyalkylaminomethylphosphonic acid or salts thereof is catalytically oxidized to produce an N-phosphonomethylaminocarboxylic acid or salts thereof.

    摘要翻译: 一种N-羟烷基氨基甲基膦酸或其盐的制备方法,其包括在醇的存在下,在合适的反应条件下使链烷醇胺,甲醛和亚磷酸二烷基酯接触以产生反应混合物,并在酸性或碱性条件下水解反应混合物。 在一个实施方案中,N-羟烷基氨基甲基膦酸或其盐被催化氧化以产生N-膦酰基二甲基氨基羧酸或其盐。

    Compositions containing indole-2-carboxylate compounds for treatment of
CNS disorders
    5.
    发明授权
    Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders 失效
    含有吲哚-2-羧酸盐化合物的组合物,用于治疗中枢神经系统疾病

    公开(公告)号:US5229413A

    公开(公告)日:1993-07-20

    申请号:US830108

    申请日:1992-02-03

    IPC分类号: A61K31/405

    CPC分类号: A61K31/405

    摘要: Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.

    摘要翻译: 含有某些吲哚-2-羧酸酯化合物和衍生物的组合物被描述为治疗由神经毒性损伤或神经变性疾病,特别是由缺血事件引起的CNS障碍引起的CNS障碍的治疗有效性。 优选的化合物具有式“IMAGE”,其中R 5和R 6各自独立地选自氢,溴,氯和氟,并且其中R 10和R 12各自独立地选自氢和低级烷基及其药学上可接受的盐。

    ENTERIC COATING COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME
    6.
    发明申请
    ENTERIC COATING COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME 审中-公开
    选择性涂料组合物及其制备方法和使用方法

    公开(公告)号:US20130115285A1

    公开(公告)日:2013-05-09

    申请号:US13578289

    申请日:2011-02-12

    IPC分类号: A61K47/36 A61K47/34

    摘要: An enteric coating composition including about 0.01% to about 10% resin and about 0.01% to about 10% polymer. The enteric coating composition may be applied to a substrate, such as a pharmaceutical, nutraceutical, fruit, vegetable, agricultural product, or industrial product, to form an enteric coating on the substrate. Also provided is a multiple-component system having a first component including a resin and a second component including a polymer, wherein mixing the first component and the second component forms an enteric coating composition having about 0.01% to about 10% resin and about 0.01% to about 10% polymer. Methods for coating a substrate with the enteric coating compositions are also provided.

    摘要翻译: 包括约0.01%至约10%的树脂和约0.01%至约10%的聚合物的肠溶包衣组合物。 肠溶剂组合物可以施用于基质如药物,保健品,水果,蔬菜,农产品或工业产品,以在基材上形成肠溶衣。 还提供了具有包括树脂的第一组分和包含聚合物的第二组分的多组分体系,其中混合第一组分和第二组分形成具有约0.01%至约10%树脂和约0.01% 至约10%的聚合物。 还提供了用肠溶衣组合物涂覆底物的方法。

    Process for Synthesizing Remifentanil
    7.
    发明申请
    Process for Synthesizing Remifentanil 审中-公开
    合成瑞芬太尼的方法

    公开(公告)号:US20080319196A1

    公开(公告)日:2008-12-25

    申请号:US12093517

    申请日:2006-10-23

    申请人: Brian K. Cheng

    发明人: Brian K. Cheng

    IPC分类号: C07D211/56

    CPC分类号: C07D211/66

    摘要: An improved process for synthesizing opiate or opioid analgesics and anesthetics, and intermediates thereof is provided. In particular, processes of synthesizing intermediates for use in the preparation of synthetic opiate or opioid compounds such as, for example, remifentanil, carfentanil, sufentanil, fentanyl, and alfentanil are disclosed. The preparation process requires fewer steps, and results in reduced costs and higher efficiency than processes known in the art for producing remifentanil and carfentanil.

    摘要翻译: 提供了一种用于合成鸦片剂或阿片类止痛剂和麻醉剂的改进方法及其中间体。 特别地,公开了合成用于制备合成阿片剂或阿片样物质的中间体的方法,例如瑞芬太尼,卡芬太尼,舒芬太尼,芬太尼和阿芬太尼。 制备方法需要更少的步骤,并且导致降低成本并且比本领域已知的用于生产瑞芬太尼和卡芬太尼的方法更高的效率。

    Compositions containing indole-2-carboxylate compounds for treatment of
CNS disorders
    8.
    发明授权
    Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders 失效
    含有吲哚-2-羧酸盐化合物的组合物,用于治疗中枢神经系统疾病

    公开(公告)号:US5137910A

    公开(公告)日:1992-08-11

    申请号:US484530

    申请日:1990-03-01

    IPC分类号: A61K31/405

    CPC分类号: A61K31/405

    摘要: Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.

    摘要翻译: 含有某些吲哚-2-羧酸酯化合物和衍生物的组合物被描述为治疗由神经毒性损伤或神经变性疾病,特别是由缺血事件引起的CNS障碍引起的CNS障碍的治疗有效性。 优选的化合物具有式“IMAGE”,其中R 5和R 6各自独立地选自氢,溴,氯和氟,并且其中R 10和R 12各自独立地选自氢和低级烷基及其药学上可接受的盐。

    Process for preparing N-phosphonomethylamino carboxylic acids
    10.
    发明授权
    Process for preparing N-phosphonomethylamino carboxylic acids 失效
    制备N-膦酰基甲基氨基羧酸的方法

    公开(公告)号:US5703273A

    公开(公告)日:1997-12-30

    申请号:US674211

    申请日:1996-07-01

    IPC分类号: C07F9/38

    CPC分类号: C07F9/3813

    摘要: A process for preparing N-hydroxyalkylaminomethyl-phosphonic acid or salts thereof which comprises contacting an alkanolamine, formaldehyde and a trialkyl phosphite under suitable reaction conditions to produce a reaction mixture, and hydrolyzing the reaction mixture under neutral, acidic or basic conditions. In one embodiment, the N-hydroxyalkylaminomethylphosphonic acid or salts thereof is catalytically oxidized to produce an N-phosphonomethylaminocarboxylic acid or salts thereof.

    摘要翻译: 一种N-羟烷基氨基甲基膦酸或其盐的制备方法,其包括在合适的反应条件下使链烷醇胺,甲醛和亚磷酸三烷基酯接触以产生反应混合物,并在中性,酸性或碱性条件下水解反应混合物。 在一个实施方案中,N-羟烷基氨基甲基膦酸或其盐被催化氧化以产生N-膦酰基二甲基氨基羧酸或其盐。