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    • 2. 发明授权
    • Dendritic polymers with enhanced amplification and interior functionality
    • 具有增强的扩增和内部功能的树枝状聚合物
    • US07985424B2
    • 2011-07-26
    • US11630044
    • 2005-12-21
    • Donald A. TomaliaDouglas R. SwansonBaohua HuangVeera Reddy PulgamJoseph R. HeinzelmannSonke SvensonLori A. ReynaMichael A. ZhuravelAbhay Singh ChauhanCordell R. DeMattei
    • Donald A. TomaliaDouglas R. SwansonBaohua HuangVeera Reddy PulgamJoseph R. HeinzelmannSonke SvensonLori A. ReynaMichael A. ZhuravelAbhay Singh ChauhanCordell R. DeMattei
    • A61K9/14
    • C08G63/46A01N25/10A61K8/85A61K9/0019A61K9/5146A61Q15/00A61Q17/005C08G83/003H01M4/86H01M8/10Y02P70/56
    • Dendritic polymers with enhanced amplification and interior functionality are disclosed. These dendritic polymers are made by use of fast, reactive ring-opening chemistry (or other fast reactions) combined with the use of branch cell reagents in a controlled way to rapidly and precisely build dendritic structures, generation by generation, with cleaner chemistry, often single products, lower excesses of reagents, lower levels of dilution, higher capacity method, more easily scaled to commercial dimensions, new ranges of materials, and lower cost. The dendritic compositions prepared have novel internal functionality, greater stability (e.g., thermal stability and less or no reverse Michael's reaction), and reach encapsulation surface densities at lower generations. Unexpectedly, these reactions of polyfunctional branch cell reagents with polyfunctional cores do not create cross-linked materials. Such dendritic polymers are useful as demulsifiers for oil/water emulsions, wet strength agents in the manufacture of paper, proton scavengers, polymers, nanoscale monomers, calibration standards for electron microscopy, making size selective membranes, and agents for modifying viscosity in aqueous formulations such as paint. When these dendritic polymers have a carried material associated with their surface and/or interior, then these dendritic polymers have additional properties for carrying materials due to the unique characteristics of the dendritic polymer, such as for drug delivery, transfection, and diagnostics.
    • 公开了具有增强的扩增和内部功能的树枝状聚合物。 这些树枝状聚合物通过使用快速,反应性开环化学(或其他快速反应)结合使用分支细胞试剂以受控方式快速和精确地构建树突状结构,一代代,具有更清洁的化学,通常 单一产品,较低的试剂过量,较低的稀释水平,更高的容量方法,更容易缩放到商业尺寸,新的材料范围以及更低的成本。 制备的树枝状组合物具有新颖的内部功能,更高的稳定性(例如,热稳定性和较少的或没有反向的迈克尔反应),并且在较低的代次下达到包封表面密度。 出乎意料的是,多官能分支细胞试剂与多官能核心的这些反应不产生交联材料。 这种树枝状聚合物可用作油/水乳液的破乳剂,纸张制造中的湿强剂,质子清除剂,聚合物,纳米尺寸单体,用于电子显微镜的校准标准品,制备尺寸选择性膜,以及用于在水性制剂中改性粘度的试剂 作为油漆。 当这些树枝状聚合物具有与其表面和/或内部相关的载体材料时,由于树枝状聚合物的独特特征,例如用于药物递送,转染和诊断,这些树枝状聚合物具有携带材料的附加性质。
    • 4. 发明申请
    • Peham dendrimers as excipients
    • Peham树枝状大分子作为赋形剂
    • US20090324742A1
    • 2009-12-31
    • US12310748
    • 2007-09-07
    • Sonke SvensonAbhay Singh Chauhan
    • Sonke SvensonAbhay Singh Chauhan
    • A61K47/48A61K47/34A61K33/24A61K31/59A61K8/84
    • A61K47/34A61K47/6949B82Y5/00
    • The present invention concerns poly(etherhydroxylamine) PEHAM dendritic polymers wherein they function as excipients for the enhancement of water solubility of poorly water soluble (hydrophobic) Active Materials or enhancement of oil solubility of poorly oil soluble (hydrophilic) Active Materials. These dendritic polymers can have Active Materials associated with them by one or more of the following: (a) by adsorption onto the surface or (b) encapsulation into the interior of the dendritic polymers or (c) a mixture of both where these interactions are driven by one or more of the following (i) electrostatic attraction, (ii) hydrogen bonding between dendritic polymers and Active Material and (iii) hydrophobic or hydrophilic interactions or mixtures of these interactions. Additionally, these associated Active Materials can be associated with dendritic polymers through chemical bonding to the surface or to internal functionalities (IF) of PEHAM dendritic polymers or both. Such bonding is done either directly between PEHAM dendritic polymers and Active Material molecules or via a linker that can have a hydrolysable bond to the Active Material. In addition, a chemical entity with strong interaction to the Active Material and dendritic polymers can be associated with the dendritic polymer prior to adsorption or encapsulation of the Active Material or together with the Active Material.
    • 本发明涉及聚(醚羟胺)PEHAM树枝状聚合物,其中它们用作增强水溶性差(疏水性)活性材料的水溶性的赋形剂,或提高油溶性(亲水性)活性物质的油溶性。 这些树枝状聚合物可以通过一种或多种以下物质与其相关的活性材料:(a)通过吸附到表面上或(b)包封到树枝状聚合物的内部,或(c)两者的混合物,其中这些相互作用是 由以下一个或多个(i)静电吸引,(ii)树枝状聚合物和活性材料之间的氢键和(iii)疏水或亲水相互作用或这些相互作用的混合物驱动。 另外,这些相关的活性材料可以通过与表面的化学键合或PEHAM树枝状聚合物的内部功能(IF)或两者结合而与树枝状聚合物缔合。 这种键合可以直接在PEHAM树枝状聚合物和活性材料分子之间进行,或者通过可以与活性材料具有可水解键的接头进行。 此外,与活性物质和树枝状聚合物具有强相互作用的化学物质在活性物质的吸附或包封之前或与活性物质一起可与树枝状聚合物缔合。