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    • 2. 发明公开
    • CONVERGENT SELF-BRANCHING POLYMERIZATION
    • KONVERGENTE SELBSTVERZWEIGENDE POLYMERISATION
    • EP0981555A4
    • 2005-01-12
    • EP98906424
    • 1998-02-17
    • TOMALIA DONALD A
    • YIN RUITOMALIA DONALD AQIN DUJIEDUNHAM JAMIE A
    • C08G85/00C08F8/30C08F293/00C08F297/00C08G81/00C08G83/00C08F8/32C08G18/00C08G63/00C08G64/00C08G65/00
    • C08G83/005C08F8/30C08F293/00C08F293/005C08F297/00C08G81/00
    • A method of forming a branched polymer includes forming a plurality of growing linear polymer chains by polymerizing a monomer which is protected against branching and which forms a reactive end group which is in a first condition which is one of electrophilic or nucleophilic, exposing the growing linear polymer chains to a chain transfer agent to cause the reactive end group of at least a first growing linear polymer chain to reverse its electrophilic or nucleophilic character, whereby a non-reversed reactive end group on a second growing linear polymer chain reacts with the reversed reactive end group on the first growing linear polymer chain to create a branched polymer and reverses the electrophilic or nucleophilic character of the reversed reactive end group back to its first condition, whereby it may continue adding monomer in a linear fashion; and quenching the polymerization by adding a compound having multiple reactive sites capable of reacting with the reactive end groups of the polymer chains when they are in the first condition. The method allows the preparation of ultra-high molecular weight dendritic polymers in which the branching junctures are assembled in situ (i.e., are self-branching) in a convergent manner during polymerization of the monomers.
    • 形成支化聚合物的方法包括通过聚合被保护免受支化并且形成处于第一种条件的反应性端基的亲水或亲核性的单体,形成多个生长线性聚合物链,将生长的线性 聚合物链与链转移剂反应以使至少第一生长线型聚合物链的反应性端基反转其亲电或亲核特性,由此第二生长线性聚合物链上的非反转反应性端基与反转反应 在第一生长线性聚合物链上形成末端基团以产生支化聚合物,并将反向反应性端基的亲电或亲核特性逆转回其第一条件,由此其可继续以线性方式加入单体; 并且通过加入具有能够与聚合物链的反应性端基反应的多个反应位点的化合物,当它们处于第一条件时,猝灭聚合反应。 该方法允许制备超高分子量树枝状聚合物,其中分支接合点在单体聚合过程中以会聚方式原位组装(即自分支)。
    • 5. 发明申请
    • JANUS DENDRIMERS AND DENDRONS
    • JANUS DENDRIMERS和DENDRONS
    • WO2006105043A3
    • 2007-10-04
    • PCT/US2006011160
    • 2006-03-27
    • DENDRITIC NANOTECHNOLOGIES INCTOMALIA DONALD APULGAM VEERA REDDYSWANSON DOUGLAS RHUANG BAOHUA
    • TOMALIA DONALD APULGAM VEERA REDDYSWANSON DOUGLAS RHUANG BAOHUA
    • C08G75/00C08G59/68C08G61/00C08G63/44C08G65/04C08G73/00
    • C08G83/003C08G81/00
    • This invention provides a cost effective process and new Janus dendrimers where at least two dendrons are attached at the core (with or without a connector group) and where at least two of the dendrons have different functionality. Preferred are those Janus dendrimers where at least one dendron is a PEHAM dendron. Thus these Janus dendrimers are heterobifunctional in character and use unique ligation chemistry with single site functional dendrons, di-dendrons and multi-dendrons. Also included are Janus dendrons which maybe used as intermediates to make the Janus dendrimers or to further react with another reactive moiety. These Janus dendrimers can provide several new dendrimer moieties, namely: combinatorial libraries of bifunctional structures; combined target director and signaling dendrimers; specific targeting entities for diagnostic and therapeutic applications, such as for example targeted MRI agents, targeted radionuclide delivery for diseases such as cancer, and targeted photosensitive or radiowave sensitive agents.
    • 本发明提供了一种成本有效的方法和新的Janus树枝状大分子,其中至少两个树突状物连接在核心处(具有或不具有连接基团),并且其中至少两个枝状突起具有不同的功能。 那些Janus树枝状大分子是首选,其中至少有一个树突是PEHAM树突。 因此,这些Janus树枝状大分子在性质上是异双功能的,并且使用独特的连接化学物质,其具有单位点功能性树突,二树枝状突起和多枝状突起。 还包括Janus dendron,其可以用作中间体来制备Janus树枝状大分子或进一步与另一反应性部分反应。 这些Janus树枝状大分子可以提供几个新的树枝状大分子部分,即:双功能结构的组合文库; 组合目标主任和信号树枝状大分子; 用于诊断和治疗应用的特异性靶向实体,例如靶向MRI剂,用于诸如癌症的疾病的靶向放射性核素递送,以及靶向感光或无线电波敏感剂。
    • 6. 发明申请
    • ENCAPSULATED(CHELATE OR LIGAND) DENDRITIC POLYMERS
    • 包封(CHELATE或LIGAND)DENDRITIC POLYMERS
    • WO2006088958A8
    • 2007-07-26
    • PCT/US2006005334
    • 2006-02-15
    • DENDRITIC NANOTECHNOLOGIES INCTOMALIA DONALD AHUANG BAOHUA
    • TOMALIA DONALD AHUANG BAOHUA
    • A61K51/00A61M36/14
    • C08G83/003
    • An encapsulated chelate dendritic polymer and an encapsulated ligand dendritic polymer are disclosed which have unique properties. These encapsulated chelate dendritic polymers may have associated with its dendritic polymer surface target directors, proteins, DNA, RNA (including single strands) or any other moieties that will assist in diagnosis, therapy or delivery of this encapsulated chelate dendritic polymer. These encapsulated dendritic polymers are suitable as contrast agents for use in imaging in an animal, for other imaging techniques, for EPR, and as scavenger agents for chelant therapy. Formulations for these uses are also included within the scope of this invention.
    • 公开了包封的螯合树枝状聚合物和包封的配体树枝状聚合物,其具有独特的性质。 这些包封的螯合树枝状聚合物可能与其树突状聚合物表面靶向导体,蛋白质,DNA,RNA(包括单链)或将有助于诊断,治疗或递送这种包封的螯合树枝状聚合物的任何其它部分相关联。 这些包封的树突状聚合物适合作为用于动物成像的对比剂,其它成像技术用于EPR,以及用作螯合剂治疗的清除剂。 这些用途的制剂也包括在本发明的范围内。
    • 8. 发明申请
    • DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY
    • 具有增强放大和内部功能的树枝状聚合物
    • WO2006065266A9
    • 2006-12-21
    • PCT/US2005013864
    • 2005-04-20
    • DENDRITIC NANOTECHNOLOGIES INCTOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDY
    • TOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDY
    • C08J3/00C08J9/32C08J9/40C08K9/00
    • C08G83/003C08G59/1477C08G59/32C08G59/3227C08G59/5026
    • Dendritic polymers with enhanced amplification and interior functionality are disclosed. These dendritic polymer are made by use of fast, reactive ring opening chemistry (or other fast reactions) combined with the use of branch cell reagants in a controlled way to rapidly and precisely build dendrimer structures, generation by generation, with precise structures with cleaner chemistry, typically single products, lower excesses of reagants, lower levels of dilution, higher capacity method, more easily scale to commercial dimensions, new ranges of materials, and lower cost. The dendrimer composition prepared have novel internal functionality, greater stability, e.g., thermal stability and less or no reverse Michaels reaction, and which reach encapsulation surface densities at lower generations. Unexpectedly, these reactions of poly-functional branch cell reagents with polyfunctional surfaces do not create gelled materials. Such dendritic polymers are useful as demulsifiers for oil/water emulsions, wet strength agents in the manufacture of paper, proton scavengers, 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 have additional properties due to the unique characteristics of the dendritic polymer.
    • 公开了具有增强的放大和内部功能的树枝状聚合物。 这些树状聚合物是通过使用快速,反应性开环化学(或其他快速反应),并结合使用分子细胞反应物,以可控的方式快速精确地构建树枝状聚合物结构,逐代生成,具有精确的结构和更清洁的化学 ,通常是单一产品,更低的稀料过量,更低的稀释水平,更高的产能方法,更容易扩展到商业规模,新的材料范围和更低的成本。 所制备的树枝状聚合物组合物具有新的内部官能团,更高的稳定性,例如热稳定性和更少的或不反向的迈克尔斯反应,并且在较低代时达到包封表面密度。 出乎意料的是,多功能分支细胞试剂与多功能表面的这些反应不会产生胶凝材料。 这种树枝状聚合物可用作油/水乳剂的破乳剂,制造纸中的湿强度剂,质子清除剂,电子显微镜的校准标准品,制备尺寸选择膜和用于改变水性制剂如油漆中粘度的试剂。 当这些树枝状聚合物具有与其表面和/或内部相关的携带材料时,由于树枝状聚合物的独特特性,这些树枝状聚合物具有附加性能。