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    PREPARATION OF PURIFIED PHOSPHORODIAMIDITE
    1.
    发明申请
    PREPARATION OF PURIFIED PHOSPHORODIAMIDITE 审中-公开
    纯化磷酸二钙的制备

    公开(公告)号：WO2015107110A1

    公开(公告)日：2015-07-23

    申请号：PCT/EP2015/050669

    申请日：2015-01-15

    Applicant: RHODIA OPERATIONS

    Inventor： GARY, Woodward

    IPC: C07F9/24

    CPC classification number: C07F9/2412 ,  C07F9/2408 ,  C07F9/2458

    Abstract: The instant invention relates to a method of phosphorodiamidite production that comprises: (E1 ) preparing a purified solution of a dialkylamine in a polar solvent as follows: - the dialkylamine dissolved in a polar solvent is contacted with a quantity of phosphorus trihalide that is sufficient to react with the alcohol impurities contained in the dialkylamine but sufficiently low to leave a major part of the dialkylamine unreacted, whereby a mixture is obtained that contains the dialkylamine in the polar solvent and reaction products of the impurities with the phosphorous trihalide; - the unreacted dialkylamine and polar solvent present in the mixture obtained in step (E1.1.) are extracted from the solution S by their difference of volatility, typically by distillation, whereby the purified solution of the dialkylamine in the polar solvent is obtained; (E2) the purified solution of dialkylamine in a polar solvent as obtained in step (E1) is reacted with a phosphorus trihalide, whereby an intermediate compound is formed; (E3) the intermediate compound obtained in step (E2) is reacted with a hydroxyalkyl compound in the presence of a non-polar co-solvent.

    Abstract translation: 本发明涉及一种磷二亚铁矿生产方法，其包括：（E1）如下制备极性溶剂中的二烷基胺纯化溶液： - 将溶解在极性溶剂中的二烷基胺与一定量的三卤化磷接触， 与二烷基胺中所含的醇杂质反应，但足够低以留下未反应的二烷基胺的主要部分，由此得到在极性溶剂中含有二烷基胺的混合物和杂质与三卤化磷的反应产物; 通过挥发性的差异，通常通过蒸馏从步骤（E1.1。）中获得的混合物中存在的未反应的二烷基胺和极性溶剂存在于溶液S中，由此得到二烷基胺在极性溶剂中的纯化溶液; （E2）将步骤（E1）中得到的极性溶剂中的二烷基胺的纯化溶液与三卤化磷反应，形成中间体化合物; （E3）中，将步骤（E2）中得到的中间体化合物与羟烷基化合物在非极性助溶剂的存在下反应。

    OMEGA-3 FATTY ACID PRODRUG COMPOUNDS AND USES THEREOF
    2.
    发明申请
    OMEGA-3 FATTY ACID PRODRUG COMPOUNDS AND USES THEREOF 审中-公开
    OMEGA-3脂肪酸制剂化合物及其用途

    公开(公告)号：WO2016130417A1

    公开(公告)日：2016-08-18

    申请号：PCT/US2016/016719

    申请日：2016-02-05

    Applicant: OMTHERA PHARMACEUTICALS INC

    Inventor： ZHI, Lin

    IPC: A61K31/202

    CPC classification number: A61K45/06 ,  C07C229/12 ,  C07C233/49 ,  C07C237/06 ,  C07C311/03 ,  C07D207/16 ,  C07D233/58 ,  C07D263/18 ,  C07D285/12 ,  C07D295/215 ,  C07D317/20 ,  C07D317/34 ,  C07D319/06 ,  C07D405/04 ,  C07D407/04 ,  C07D493/04 ,  C07F9/098 ,  C07F9/2412 ,  C07F9/2462 ,  C07F9/2487 ,  C07F9/6533 ,  C07F9/65515 ,  C07F9/6552 ,  C07F9/657154 ,  C07F9/657181 ,  C07F9/65746 ,  C07F9/65846

    Abstract: Provided herein are prodrug compounds, their preparation and their uses, such as treating liver diseases or non-liver diseases via intervening in the molecular pathways in the liver. Novel prodrug compounds of eicosapentaenoic and docosahexaenoic acids, their preparation and their uses are described. Some embodiments are related to novel prodrug compounds that are absorbed in the intestine and taken up via the hepatic portal vein to the liver. Some embodiments are directed to the use of the prodrugs to change eicosapentaenoic and docosahexaenoic acids absorption routes. Another aspect includes the use of prodrugs to treat diseases that benefit from enhanced eicosapentaenoic and docosahexaenoic acids distribution to the liver and like tissues and cells, including but not limited to fatty liver, and metabolic and cardiovascular diseases where the liver is involved in the production and/or the homeostasis control of the biochemical end products, e.g. glucose, cholesterol, fatty acids, triglycerides, lipoproteins, and apolipoproteins.

    Abstract translation: 本文提供前药化合物，其制备及其用途，例如通过介入肝脏中的分子途径来治疗肝脏疾病或非肝脏疾病。 二十碳五烯酸和二十二碳六烯酸的新型前药化合物及其制备方法及用途进行了说明。 一些实施方案涉及被吸收在肠中并通过肝门静脉吸收到肝脏的新型前药化合物。 一些实施方案涉及前体药物改变二十碳五烯酸和二十二碳六烯酸吸收途径的用途。 另一方面包括使用前药来治疗受益于增强的二十碳五烯酸和二十二碳六烯酸分布到肝脏和类似组织和细胞的疾病，包括但不限于脂肪肝以及肝脏参与生产的代谢和心血管疾病，以及 /或生物化学终产物的体内平衡控制，例如 葡萄糖，胆固醇，脂肪酸，甘油三酯，脂蛋白和载脂蛋白。

    PURIFICATION OF SYNTHETIC OLIGOMERS
    7.
    发明申请
    PURIFICATION OF SYNTHETIC OLIGOMERS 审中-公开
    合成低聚物的纯化

    公开(公告)号：WO2008067026A2

    公开(公告)日：2008-06-05

    申请号：PCT/US2007080099

    申请日：2007-10-01

    Applicant: UNIV MICHIGAN TECH ,  FANG SHIYUE

    Inventor： FANG SHIYUE

    IPC: C07F9/06 ,  C07H21/00

    CPC classification number: C07H1/06 ,  C07D207/404 ,  C07D491/16 ,  C07F9/146 ,  C07F9/2408 ,  C07F9/2412 ,  C07F9/5721 ,  C07F9/5728 ,  C07F9/6561 ,  C07K1/02 ,  C07K1/04 ,  C07K1/14

    Abstract: This invention provides a novel method for purifying synthetic oligomers comprising capping, polymerizing and separating any failure sequences produced during oligomer synthesis. Either the failure sequence or the full-length oligmer may be polymerized. Optionally, small molecule impurities may also be incorporated into the polymerized material. The invention provides novel capping agents having a polymerizable functional group. The invention also provides kits comprising at least one composition of the present invention.

    Abstract translation: 本发明提供了一种用于纯化合成低聚物的新方法，其包括封端，聚合和分离低聚物合成期间产生的任何破坏序列。 故障序列或全长寡聚体可以聚合。 任选地，也可以将小分子杂质掺入到聚合材料中。 本发明提供具有可聚合官能团的新型封端剂。 本发明还提供了包含至少一种本发明组合物的试剂盒。

    PHARMACEUTICAL FORMULATIONS
    10.
    发明申请
    PHARMACEUTICAL FORMULATIONS 审中-公开
    药物制剂

    公开(公告)号：WO1998022479A1

    公开(公告)日：1998-05-28

    申请号：PCT/GB1997003203

    申请日：1997-11-21

    Applicant: GOLDSHIELD DEVELOPMENTS LIMITED ,  DOGADINA, Albina Vladimirovna ,  GOUREVITCH, Igor Evgenyevich ,  IONINE, Boris Iosifovich

    Inventor： GOLDSHIELD DEVELOPMENTS LIMITED

    IPC: C07F09/113

    CPC classification number: A61K31/661 ,  A61K31/664 ,  C07F9/113 ,  C07F9/2412 ,  C07F9/2462 ,  C12P9/00

    Abstract: A compound of formula (1), particularly where X = O, Y = NR R , wherein R = R = H and Z = Z = OH, can protect and/or aid the recovery of functionally impaired tissue whose viability is threatened by hypoxia. Typically, the compounds can be used to aid recovery of function of ischaemic tissue during and after open heart surgery. In said formula, X = O or NH, Y = OH, OR , NR R , wherein R and R are independently H, alkyl, alkenyl (except where applied to OR ), cycloalkyl, aryl, or aralkyl.

    Abstract translation: 式（1）的化合物，特别是其中X = O，Y = NR 1 R 2，其中R 1 = R 2 = H且Z 1 = Z 2 = OH， 可以保护和/或辅助其活力受缺氧威胁的功能受损组织的恢复。 通常，该化合物可用于帮助在开心心脏手术期间和之后恢复缺血组织的功能。 在所述式中，X = O或NH，Y = OH，OR 1，NR 1 R 2，其中R 1和R 2独立地为H，烷基，烯基（除非适用于 OR 1），环烷基，芳基或芳烷基。

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