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    • 2. 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。
    • 3. 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。
    • 5. 发明申请
    • DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY
    • 具有增强放大和内部功能的聚合物聚合物
    • WO2006115547A8
    • 2007-02-15
    • PCT/US2005047635
    • 2005-12-21
    • DENDRITIC NANOTECHNOLOGIES INCTOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDYHEINZELMANN JOSEPH RSVENSON SONKEREYNA LORI AZHURAVEL MICHAEL ACHAUHAN ABHAY SINGHDEMATTEI CORDELL R
    • TOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDYHEINZELMANN JOSEPH RSVENSON SONKEREYNA LORI AZHURAVEL MICHAEL ACHAUHAN ABHAY SINGHDEMATTEI CORDELL R
    • A61K48/00A61K31/785C12N15/87
    • C12N15/87A61K47/59A61K47/593A61K47/595A61K48/00A61K49/0002B82Y5/00B82Y10/00C08G83/003C08L101/005C09B67/0013
    • 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,更容易扩展到商业尺寸,新的材料范围和更低的成本。 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,热稳定性和更少或没有反向迈克尔反应),并在较低代次达到包封表面密度。 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,例如药物递送,转染和诊断,这些树枝状聚合物具有用于承载材料的附加性能。
    • 6. 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。
    • 9. 发明申请
    • DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY
    • 具有增强放大和内部功能的聚合物聚合物
    • WO2006065266A2
    • 2006-06-22
    • PCT/US2005013864
    • 2005-04-20
    • DENDRITIC NANOTECHNOLOGIES INCTOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDY
    • TOMALIA DONALD ASWANSON DOUGLAS RHUANG BAOHUAPULGAM VEERA REDDY
    • C08F20/02
    • 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)结合使用分支细胞反应物以受控的方式制备,以快速和精确地构建树枝状聚合物结构,一代代,具有更清洁化学物质的精确结构 ,通常是单一产品,较低的反应物过剩,较低的稀释水平,更高的容量方法,更容易扩展到商业尺寸,新的材料范围和较低的成本。 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或没有反向迈克尔斯反应,并且在较低代次下达到包封表面密度。 出乎意料的是,具有多官能表面的多功能分支细胞试剂的这些反应不产生胶凝材料。 这种树枝状聚合物可用作油/水乳液的破乳剂,制造纸中的湿强剂,质子清除剂,电子显微镜校准标准品,制备尺寸选择性膜,以及用于改进水性配方如油漆中的粘度的试剂。 当这些树枝状聚合物具有与其表面和/或内部相关的载体材料时,由于树枝状聚合物的独特特征,这些树枝状结构具有额外的性质。