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    POLYMER-CYCLODEXTRIN-LIPID CONJUGATES
    2.
    发明申请
    POLYMER-CYCLODEXTRIN-LIPID CONJUGATES 审中-公开
    聚合物 - 环糊精 - 脂质混合物

    公开(公告)号：US20160375150A1

    公开(公告)日：2016-12-29

    申请号：US15184015

    申请日：2016-06-16

    Applicant: Nian Wu

    Inventor： Nian Wu

    IPC: A61K47/48

    CPC classification number: A61K47/6851 ,  A61K9/08 ,  A61K31/05 ,  A61K31/337 ,  A61K31/496 ,  A61K31/506 ,  A61K31/57 ,  A61K31/7068 ,  A61K47/48969 ,  A61K47/542 ,  A61K47/554 ,  A61K47/60 ,  A61K47/6951 ,  C07J9/00 ,  C07J41/0055 ,  C08B37/0012 ,  C08B37/0015

    Abstract: The invention comprises compounds, methods of making, and methods of using. A group of polymer-cyclodextrin-lipid conjugates having a center backbone and three or four appended functional groups are disclosed, wherein one of the hydrophilic components is cyclodextrin. The compounds may have a backbone with three or four appended functional groups: one or two lipophilic compounds including sterols or “fat soluble” vitamins or fatty acids, one or two hydrophilic polymer and one cyclodextrin. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. Typical coupling reaction of the conjugates may involve one or more or combinations or in series of alkylation including N-alkylation or O-alkylation, etherification, esterification and amidation chemical processes. A variety of linkers between the center backbone and functional groups may also be selected to modify the carriers or center backbones for the coupling reactions and optimize performance of the conjugates.

    Abstract translation: 本发明包括化合物，制备方法和使用方法。 公开了一组具有中心主链和三个或四个附加官能团的聚合物 - 环糊精 - 脂质缀合物，其中亲水组分之一是环糊精。 化合物可以具有带有三个或四个附加官能团的骨架：一种或两种亲脂性化合物，包括甾醇或“脂溶性”维生素或脂肪酸，一种或两种亲水性聚合物和一种环糊精。 可以在配制药物，化妆品，营养品等中的特定应用中选择特定的官能团。 缀合物的典型偶联反应可以包括一种或多种或组合或串联烷基化，包括N-烷基化或O-烷基化，醚化，酯化和酰胺化学过程。 还可以选择中心骨架和官能团之间的各种连接体，以修饰偶联反应的载体或中心骨架，并优化缀合物的性能。

    HIGHLY MONODISPERSE BRANCHED PEG-LIPID CONJUGATES
    3.
    发明申请
    HIGHLY MONODISPERSE BRANCHED PEG-LIPID CONJUGATES 审中-公开
    高度单体分支的PEG-脂质结合体

    公开(公告)号：US20120232169A1

    公开(公告)日：2012-09-13

    申请号：US13412676

    申请日：2012-03-06

    Applicant: Nian Wu ,  Brian Charles Keller

    Inventor： Nian Wu ,  Brian Charles Keller

    IPC: A61K47/14 ,  C07C59/58

    CPC classification number: A61K47/14 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0095 ,  A61K9/4858 ,  A61K31/7052 ,  A61K38/13 ,  A61K47/28 ,  A61K47/60 ,  A61K47/6911

    Abstract: (PEG)-lipid conjugates and methods of preparation are disclosed herein. Methods of preparation may involve stepwise addition of small PEG oligomers to a glycerol backbone until a desired chain size is attained. Polymers resulting from the syntheses may be highly monodisperse. The resulting polymers may comprise branched polyethyleneglycol (PEG)-lipid conjugates. The present disclosure may provide several advantages such as simplified synthesis, high product yield and low cost for starting materials. The present synthesis method may be suitable for preparing a wide range of conjugates such as PEG lipid conjugates having a glycerol-like central backbone covalently attached to two or more monodisperse PEG chains and a lipid comprising a range of diesters made from fatty acids or bile acids.

    Abstract translation: （PEG）脂质偶联物和制备方法在本文中公开。 制备方法可以包括将小PEG低聚物逐步添加到甘油骨架中，直至达到所需的链尺寸。 由合成得到的聚合物可能是高度单分散的。 所得聚合物可以包含支链聚乙二醇（PEG） - 脂质缀合物。 本公开可以提供几个优点，例如简化的合成，高产率和起始材料的低成本。 本发明的合成方法可适用于制备宽范围的缀合物，例如具有共价连接到两个或更多个单分散PEG链的甘油样中心骨架的PEG脂质缀合物和包含由脂肪酸或胆汁酸制成的一系列二酯​​的脂质 。

    Pure PEG-lipid conjugates
    5.
    发明申请
    Pure PEG-lipid conjugates 审中-公开
    纯PEG-脂质缀合物

    公开(公告)号：US20110040113A1

    公开(公告)日：2011-02-17

    申请号：US12802197

    申请日：2010-06-01

    Applicant: Nian Wu ,  Brian Charles Keller

    Inventor： Nian Wu ,  Brian Charles Keller

    IPC: C07C55/00 ,  C07C41/00

    CPC classification number: C08G65/329 ,  A61K47/60 ,  A61K47/6911 ,  C08L2203/02

    Abstract: Syntheses of polyethyleneglycol (PEG)-lipid conjugates are disclosed. Such syntheses involve stepwise addition of small PEG oligomers to a glycerol backbone until the desired chain size is attained. Polymers resulting from the syntheses are highly monodisperse. The present invention provides several advantages such as simplified synthesis, high product yield and low cost for starting materials. The present synthesis method is suitable for preparing a wide range of conjugates.In another aspect, the invention comprises PEG lipid conjugates having a glycerol backbone covalently attached to one or two monodisperse PEG chains and one or two lipids. These conjugates are especially useful for pharmaceutical formulations.

    Abstract translation: 公开了聚乙二醇（PEG）脂质缀合物的合成。 这种合成包括将小PEG低聚物逐步加入到甘油骨架中，直到达到所需的链尺寸。 由合成产生的聚合物是高度单分散的。 本发明提供了诸如简化合成，高产品收率和起始材料成本低等优点。 本合成方法适用于制备宽范围的共轭物。 在另一方面，本发明包括具有共价连接到一个或两个单分散PEG链和一个或两个脂质的甘油主链的PEG脂质缀合物。 这些缀合物对于药物制剂特别有用。

    POLYMER-CARBOHYDRATE CONJUGATES FOR DRUG DELIVERY TECHNOLOGY
    8.
    发明申请
    POLYMER-CARBOHYDRATE CONJUGATES FOR DRUG DELIVERY TECHNOLOGY 审中-公开
    聚合物 - 碳水化合物用于药物输送技术

    公开(公告)号：US20150157721A1

    公开(公告)日：2015-06-11

    申请号：US14561219

    申请日：2014-12-05

    Applicant: Nian Wu

    Inventor： Nian Wu

    IPC: A61K47/26 ,  A61K47/28

    CPC classification number: A61K47/26 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0095 ,  A61K9/08 ,  A61K31/05 ,  A61K31/337 ,  A61K31/506 ,  A61K47/28 ,  C08G2650/26 ,  C08L71/02 ,  C08L2203/02

    Abstract: The invention comprises compounds, methods of making, and methods of using. The compounds may have a linear or cylic backbone and three or four appended functional groups: one or two lipohilic compounds including sterols or “fat soluble” vitamins, one or two hydrophilic polymer, and one or two carbohydrate. A group of polymer-carbohydrate conjugates having a central backbone and three appended functional groups are disclosed wherein one lipophilic compound is void of both steroid acids. The conjugate may have fatty acids as the primary lipophilic carrier, one hydrophilic polymer, and one carbohydrate. Specific functional groups may be selected for specific applications in formulating pharmaceuticals, cosmetics, nutriceuticals, and the like. Typical coupling reaction of the conjugates may involve one or more or combinations or in series of alkylation including N-alkylation or O-alkylation, etherification, esterification and amidation chemical processes. A variety of linkers between the backbone and functional groups may also be selected to modify the carriers or center backbones for the coupling reactions and optimize performance of the conjugates.

    Abstract translation: 本发明包括化合物，制备方法和使用方法。 所述化合物可以具有线性或环状主链和三个或四个附加的官能团：一种或两种脂肪酸化合物，包括甾醇或“脂溶性”维生素，一种或两种亲水性聚合物和一种或两种碳水化合物。 公开了一组具有中心骨架和三个附加官能团的聚合物 - 碳水化合物缀合物，其中一种亲脂性化合物不含类固醇酸。 缀合物可以具有脂肪酸作为主要的亲脂性载体，一种亲水性聚合物和一种碳水化合物。 可以在配制药物，化妆品，营养品等中的特定应用中选择特定的官能团。 缀合物的典型偶联反应可以包括一种或多种或组合或串联烷基化，包括N-烷基化或O-烷基化，醚化，酯化和酰胺化学过程。 骨架和官能团之间的各种接头也可以被选择以修饰耦合反应的载体或中心骨架并优化共轭物的性能。

    Method of treatment with rapamycin
    9.
    发明申请
    Method of treatment with rapamycin 审中-公开
    雷帕霉素治疗方法

    公开(公告)号：US20110105387A1

    公开(公告)日：2011-05-05

    申请号：US12924038

    申请日：2010-09-18

    Applicant: Nian Wu ,  Brian Charles Keller

    Inventor： Nian Wu ,  Brian Charles Keller

    IPC: A61K38/13 ,  A61K31/436 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06

    CPC classification number: A61K31/436 ,  A61K9/0019 ,  A61K9/1273

    Abstract: The invention comprises a method of treatment using an oral capsule dose of rapamycin formulated with PEG-lipids. Two types of PEG-lipids are used in the formulation. A solubilizing agent dissolves the rapamycin, and solidifying agent is used to convert the solution of rapamycin/solubilizing agent to a more solid form.

    Abstract translation: 本发明包括使用PEG-脂质配制的口服胶囊剂量的雷帕霉素的治疗方法。 在制剂中使用两种类型的PEG-脂质。 增溶剂溶解雷帕霉素，并且使用固化剂将雷帕霉素/增溶剂的溶液转化成更固体的形式。

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