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    METHOD FOR SYNTHESIZING PIRFENIDONE
    4.
    发明申请
    METHOD FOR SYNTHESIZING PIRFENIDONE 审中-公开
    合成菲尼酮的方法

    公开(公告)号：US20110003863A1

    公开(公告)日：2011-01-06

    申请号：US12792387

    申请日：2010-06-02

    申请人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

    发明人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

    IPC分类号： A61K31/4418 ,  C07D213/64 ,  A61P11/00

    CPC分类号： C07D213/64 ,  A61K31/4412

    摘要： A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenzene is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

    摘要翻译： 公开了一种从具有小于约0.15重量％二溴苯的溴苯合成吡非尼酮的方法。 还公开了在不使用乙酸乙酯或正丁醇的情况下合成吡非尼酮的方法，以及具有受控含量的乙酸乙酯，正丁醇，二（5-甲基-2-吡啶酮）苯和具有特定保留时间的其它杂质的吡非尼酮。 还公开了包括所公开的吡非尼酮的配制剂型。

    Processes for producing triaryl phosphite
    7.
    发明授权
    Processes for producing triaryl phosphite 失效
    生产亚磷酸三芳酯的方法

    公开(公告)号：US06653494B2

    公开(公告)日：2003-11-25

    申请号：US10210922

    申请日：2002-08-02

    申请人： Padiyath Mohammed Akbarali ,  Kuniyil Kulangara Vijay Raj ,  Karabasana T. Gouda ,  Ramachandran Radhakrishnan

    发明人： Padiyath Mohammed Akbarali ,  Kuniyil Kulangara Vijay Raj ,  Karabasana T. Gouda ,  Ramachandran Radhakrishnan

    IPC分类号： C07F902

    CPC分类号： C07F9/145

    摘要： A one pot process for the preparation of sterically hindered triaryl phosphite is provided. It is suitable for large scale commercial production with an advantage of having carried out the reaction at 0-5° C. in a shortest time of 1 hr using pyridine as Lewis base to remove HCl formed in the reaction; thus avoiding the usage of scrubber. The triaryl phosphite is of the formula P(OR)3 and is produced by reacting a di alkyl—substituted phenol of formula ROH with phosphorus trihalide in a presence of a Lewis base, wherein R represents an aryl compound of a formula C6H3RaRb, wherein Ra is tertiary alkyl, Rb is lower alkyl or tertiary alkyl. The process preferably comprises of mixing a stoichiometric amount of 2,4-dialkyl phenol with phosphorous trihalide in methylene chloride with different stoichiometric amounts of pyridine such as the molar equivalent, 10 mol %, 20 mol % and 50 mol % more than the amount of 2,4 dialkyl phenol. The reaction is preferably carried out at 0-5° C. and takes only 1 hr for the completion, followed by a precipitation out of isopropanol.

    摘要翻译： 提供了制备空间位阻亚磷酸三芳酯的一锅法。 适用于大规模商业生产，其优点是使用吡啶作为路易斯碱，在最短时间内在0-5℃下进行反应，以除去反应中形成的HCl; 从而避免了洗涤器的使用。 亚磷酸三芳酯具有式P（OR）3，其通过在路易斯碱存在下使式ROH的二烷基取代酚与三卤化磷反应制备，其中R表示式C 6 H 3 R a R b的芳基化合物，其中R a 是叔烷基，Rb是低级烷基或叔烷基。 该方法优选包括将化学计量量的2,4-二烷基苯酚与三卤化磷在二氯甲烷中混合，其中不同的化学计量量的吡啶如摩尔当量，10摩尔％，20摩尔％和50摩尔％ 2,4-二烷基苯酚。 反应优选在0-5℃进行，完成时间仅为1小时，然后用异丙醇沉淀。

    Corticosteroid inhalation treatment method
    8.
    发明授权
    Corticosteroid inhalation treatment method 失效
    皮质类固醇吸入治疗方法

    公开(公告)号：US5192528A

    公开(公告)日：1993-03-09

    申请号：US444360

    申请日：1989-12-01

    申请人： Ramachandran Radhakrishnan ,  Paul J. Mihalko ,  Robert M. Abra

    发明人： Ramachandran Radhakrishnan ,  Paul J. Mihalko ,  Robert M. Abra

    IPC分类号： A61K9/00 ,  A61K9/127 ,  A61M15/00

    CPC分类号： A61K9/0078 ,  A61K9/127 ,  A61M15/0008 ,  A61M15/009 ,  Y10T428/2984

    摘要： A method for delivering a therapeutic dosage of corticosteroid drug to the lungs, for treating a lung condition or disease. An aqueous suspension of sized liposomes containing the drug in liposome-entrapped form is aerosolized under conditions which produce aerosol particle sizes favoring particle deposition in a selected region of the respiratory tract, and the aerosol is administered in an amount which delivers the thereapeutic dosage level to the selected lung region.

    摘要翻译： 用于将治疗剂量的皮质类固醇药物递送至肺，用于治疗肺部疾病或疾病的方法。 含有脂质体封存形式的药物的大小脂质体的水性悬浮液在产生有利于在呼吸道的选定区域中的颗粒沉积的气溶胶颗粒尺寸的条件下被雾化，并且气雾剂以递送治疗剂量水平的量施用 选择的肺部区域。

    Method for Synthesizing Pirfenidone
    9.
    发明申请
    Method for Synthesizing Pirfenidone 有权
    吡非尼酮合成方法

    公开(公告)号：US20120016133A1

    公开(公告)日：2012-01-19

    申请号：US13244786

    申请日：2011-09-26

    申请人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

    发明人： Sabine M. Pyles ,  Michael Cyr ,  Ramachandran Radhakrishnan

    IPC分类号： C07D213/64

    CPC分类号： C07D213/64 ,  A61K31/4412

    摘要： A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

    摘要翻译： 公开了一种从小于约0.15％（重量）二溴苯的溴苯合成吡非尼酮的方法。 还公开了在不使用乙酸乙酯或正丁醇的情况下合成吡非尼酮的方法，以及具有受控含量的乙酸乙酯，正丁醇，二（5-甲基-2-吡啶酮）苯和具有特定保留时间的其它杂质的吡非尼酮。 还公开了包括所公开的吡非尼酮的配制剂型。