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1. 发明申请

WO2009110971A3 PROCESS FOR CONVERTING MULTIFUNCTIONAL ALIPHATIC ALCOHOLS 审中-公开
公开(公告)号：WO2009110971A3
公开(公告)日：2009-09-11
申请号：PCT/US2009/001163
申请日：2009-02-25
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , PULGAM, Veera, Reddy , SVENSON, Sonke , ZHURAVEL, Michael, A.
发明人： PULGAM, Veera, Reddy , SVENSON, Sonke , ZHURAVEL, Michael, A.
IPC分类号： C07D301/00
摘要： The present invention describes a single-stage process for preparing multifunctional epoxides having at least three hydroxyl groups using epichlorohydrin in the presence of freshly ground KOH, at a temperature between 10-25°C.

2. 发明申请

WO2008082627A1 DIVERGENT SYNTHESIS OF LOOPED POLY (ESTER)-AND POLY (ETHER)- SUBSTITUTED DENDRONS AND DENDRIMERS 审中-公开
标题翻译：循环聚合（ESTER）和聚（醚） - 取代的DENDRONS和DENDRIMERS的多重合成
公开(公告)号：WO2008082627A1
公开(公告)日：2008-07-10
申请号：PCT/US2007/026445
申请日：2007-12-27
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , TOMALIA, Donald, A. , SWANSON, Douglas, R. , HUANG, Baohua , PULGAM, Veera, Reddy
发明人： TOMALIA, Donald, A. , SWANSON, Douglas, R. , HUANG, Baohua , PULGAM, Veera, Reddy
IPC分类号： A61B5/055
CPC分类号： C08G83/003 , Y10T436/143333
摘要： The present invention describes a process for preparing new looped dendrimer and dendron compounds by controlling the molar amount of branch cell reagent monomer that is combined with various cores bearing core- XR functionalities (e.g., primary, or secondary amines, thiol, or epoxy functionalities). These looped, macrocyclic structures are more robust to various conditions, with greater resistance to acid/base hydrolysis. Alternatively, the looped, macrocyclic structure may offer new orientations that would qualify it as a better chelation ligand for metals, and other similar uses.
摘要翻译：本发明描述了通过控制与具有核-XR官能团的各种核心（例如伯，仲胺，硫醇或环氧官能团）组合的分支细胞试剂单体的摩尔量来制备新的环状树枝状聚合物和树枝状化合物的方法，。这些环状的大环结构对各种条件更加坚固，具有较强的抗酸/碱水解的能力。或者，环状的大环结构可以提供新的取向，其将其作为金属的更好的螯合配体和其它类似的用途。

3. 发明申请

WO2007149500A3 FORMULATIONS CONTAINING HYBRID DENDRIMERS 审中-公开
公开(公告)号：WO2007149500A3
公开(公告)日：2007-12-27
申请号：PCT/US2007/014402
申请日：2007-06-20
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , CHAUHAN, Abhay, Singh , SVENSON, Sonke
发明人： CHAUHAN, Abhay, Singh , SVENSON, Sonke
IPC分类号： A61K31/74 , A61K47/48
摘要： The present invention concerns hybrid dendrimers comprising a mixture, at the same or different ratios, of at least two dendritic polymers or dendronized polymers that have at least one difference between them. The surfaces of the dendritic polymer or dendronized polymer may be further modified by known methods. Also included are formulations of hybrid dendrimers wherein the dendritic polymers have the same drug present at either identical or different loading concentrations but have different release profiles. Such formulations of hybrid dendrimers may have different guest molecules present at either identical or different loading concentrations but have different release profiles. Additionally a method of using a hybrid dendrimer for delivery of a drug or guest moiety in order to provide increased solubility to poorly soluble drugs or guest moieties is provided.

4. 发明申请

WO2006105043A3 JANUS DENDRIMERS AND DENDRONS 审中-公开
标题翻译： JANUS DENDRIMERS和DENDRONS
公开(公告)号：WO2006105043A3
公开(公告)日：2007-10-04
申请号：PCT/US2006011160
申请日：2006-03-27
申请人： DENDRITIC NANOTECHNOLOGIES INC , TOMALIA DONALD A , PULGAM VEERA REDDY , SWANSON DOUGLAS R , HUANG BAOHUA
发明人： TOMALIA DONALD A , PULGAM VEERA REDDY , SWANSON DOUGLAS R , HUANG BAOHUA
IPC分类号： C08G75/00 , C08G59/68 , C08G61/00 , C08G63/44 , C08G65/04 , C08G73/00
CPC分类号： C08G83/003 , C08G81/00
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2006088958A8 ENCAPSULATED(CHELATE OR LIGAND) DENDRITIC POLYMERS 审中-公开
标题翻译：包封（CHELATE或LIGAND）DENDRITIC POLYMERS
公开(公告)号：WO2006088958A8
公开(公告)日：2007-07-26
申请号：PCT/US2006005334
申请日：2006-02-15
申请人： DENDRITIC NANOTECHNOLOGIES INC , TOMALIA DONALD A , HUANG BAOHUA
发明人： TOMALIA DONALD A , HUANG BAOHUA
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C08G83/003
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2006115547A3 DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY 审中-公开
标题翻译：具有增强放大和内部功能的聚合物聚合物
公开(公告)号：WO2006115547A3
公开(公告)日：2009-06-04
申请号：PCT/US2005047635
申请日：2005-12-21
申请人： DENDRITIC NANOTECHNOLOGIES INC , TOMALIA DONALD A , SWANSON DOUGLAS R , HUANG BAOHUA , PULGAM VEERA REDDY , HEINZELMANN JOSEPH R , SVENSON SONKE , REYNA LORI A , ZHURAVEL MICHAEL A , CHAUHAN ABHAY SINGH , DEMATTEI CORDELL R
发明人： TOMALIA DONALD A , SWANSON DOUGLAS R , HUANG BAOHUA , PULGAM VEERA REDDY , HEINZELMANN JOSEPH R , SVENSON SONKE , REYNA LORI A , ZHURAVEL MICHAEL A , CHAUHAN ABHAY SINGH , DEMATTEI CORDELL R
IPC分类号： C08J3/00 , C08J9/32 , C08K9/00 , C12N15/87
CPC分类号： C12N15/87 , A61K47/59 , A61K47/593 , A61K47/595 , A61K48/00 , A61K49/0002 , B82Y5/00 , B82Y10/00 , C08G83/003 , C08L101/005 , C09B67/0013
摘要： Dendritic polymers of the macromolecular structure of Figure 1 are disclosed. The dendritic polymers have enhanced amplification and interior functionality. The dendritic polymers are made by use of fact, reactive ring-opening chemistry (or other fast reactions) combined with the use of branch cell reagents in a controlled manner to rapidly and precisely build dendritic structures with cleaner chemistry and often with single products. Additional benefits include lower excesses of regents, lower levels of dilution, higher capacity, more easily scaled to commercial dimensions, new ranges of materials, and lower cost. The compositions prepared have novel internal functionality, including increased thermal stability and no reverse Michael's reaction, and reach encapsulation surface densities at lower generations.
摘要翻译：公开了图1的大分子结构的树枝状聚合物。树枝状聚合物具有增强的扩增和内部功能。树枝状聚合物通过使用事实，反应性开环化学（或其它快速反应）结合使用分支细胞试剂以受控方式快速和精确地构建具有更清洁化学物质的树突状结构并且经常与单一产物一起制备。额外的好处包括摄入量过低，稀释水平降低，容量更大，容易扩展到商业尺寸，新的材料范围以及更低的成本。制备的组合物具有新颖的内部功能，包括增加的热稳定性和没有相反的迈克尔反应，并在较低的代下达到包封表面密度。

7. 发明申请

WO2008013618A1 PROCESS FOR PREPARING ALKYNE INTERMEDIATES FOR DENDRITIC POLYMERS 审中-公开
标题翻译：制备聚合物烯烃中间体的方法
公开(公告)号：WO2008013618A1
公开(公告)日：2008-01-31
申请号：PCT/US2007/014404
申请日：2007-06-20
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , TOMALIA, Donald, A. , SWANSON, Douglas, R.
发明人： TOMALIA, Donald, A. , SWANSON, Douglas, R.
IPC分类号： A01N57/00 , A61K31/66
CPC分类号： C07D295/205 , C07D249/04
摘要： This invention provides a process for preparing alkyne intermediates used for making dendritic polymers. This process concerns alkyne compounds, useful as "clickable intermediates" to produce novel core reagents, branch cell reagents, surface group reagents, dendron reagents, oligomeric extender reagents, dendrimer core reagents, or dendrimer shell reagents suitable for preparing dendritic polymers, which comprises: 1) reacting acetylenic halides ( i.e. chlorides, bromides or iodides) or acetylenic mesylates/tosylates with 2-alkyl/aryl-2-oxazolines or oxazines to produce N-acetylenic-2-oxazolinium or 2-oxazinium cation salts; and 2) reacting N-acetylenic-2-oxazolinium or 2-oxazinium cation salts as catalytic reagents for the polymerization of 2-alkyl/aryl-2-oxazolines or 2-alkyl/aryl-2-oxazines; or 3) reacting propargyl tosylate or propargyl halides with 2-ethyl-2-oxazoline and then polymerizing to alkyne substituted poly(2-ethyl-2-oxazolines) with a degree of polymerization ( i.e. , dp=1-100); or 4) reacting propargyl tosylate with 2-ethyl-2-oxazoline (1:1) in the presence of sodium bromide or sodium iodide in acetonitrile to form N-propargyl-2-oxazolinium bromides/iodides, respectively; or 5) reacting 3-butyne-1,4-ditosylate in the presence of sodium iodide or sodium bromide in acetonitrile to form 3-butyne-1,4-dioxazolinium iodide or bromide, respectively.
摘要翻译：本发明提供了制备用于制备树枝状聚合物的炔烃中间体的方法。该方法涉及可用作“可点击中间体”的炔基化合物，用于制备适用于制备树枝状聚合物的新型核心试剂，支链细胞试剂，表面试剂，树枝状试剂，低聚延伸剂试剂，树枝状聚合物核试剂或树枝状大分子壳试剂，其包括： 1）使炔基卤化物（即氯化物，溴化物或碘化物）或炔丙基甲磺酸酯/甲苯磺酸酯与2-烷基/芳基-2-恶唑啉或恶嗪反应，生成N-炔属-2-恶唑啉鎓或2-恶嗪鎓阳离子盐; 和2）N-炔属-2-恶唑啉鎓或2-恶嗪鎓阳离子盐作为用于2-烷基/芳基-2-恶唑啉或2-烷基/芳基-2-恶嗪的聚合的催化剂; 或3）使炔丙基甲苯磺酸酯或炔丙基卤化物与2-乙基-2-恶唑啉反应，然后聚合成具有聚合度（即dp = 1-100）的炔取代的聚（2-乙基-2-恶唑啉）; 或4）在溴化钠或碘化钠存在下，在乙腈存在下，使甲磺酸炔丙酯与2-乙基-2-恶唑啉（1:1）反应，分别形成N-炔丙基-2-恶唑啉溴化物/碘化物; 或5）在碘化钠或溴化钠存在下在乙腈中的3-丁炔-1,4-二硫酸酯反应，分别形成3-丁炔-1,4-二氧杂环丁烷碘化物或溴化物。

8. 发明申请

WO2007149500A2 FORMULATIONS CONTAINING HYBRID DENDRIMERS 审中-公开
标题翻译：含有混合染料的配方
公开(公告)号：WO2007149500A2
公开(公告)日：2007-12-27
申请号：PCT/US2007014402
申请日：2007-06-20
申请人： DENDRITIC NANOTECHNOLOGIES INC , CHAUHAN ABHAY SINGH , SVENSON SONKE
发明人： CHAUHAN ABHAY SINGH , SVENSON SONKE
IPC分类号： A61K31/785
CPC分类号： A61K31/785
摘要： The present invention concerns hybrid dendrimers comprising a mixture, at the same or different ratios, of at least two dendritic polymers or dendronized polymers that have at least one difference between them. The surfaces of the dendritic polymer or dendronized polymer may be further modified by known methods. Also included are formulations of hybrid dendrimers wherein the dendritic polymers have the same drug present at either identical or different loading concentrations but have different release profiles. Such formulations of hybrid dendrimers may have different guest molecules present at either identical or different loading concentrations but have different release profiles. Additionally a method of using a hybrid dendrimer for delivery of a drug or guest moiety in order to provide increased solubility to poorly soluble drugs or guest moieties is provided.
摘要翻译：本发明涉及混合树枝状大分子，其包含相同或不同比例的至少两种在其间具有至少一个差异的树枝状聚合物或树枝状聚合物的混合物。树枝状聚合物或树枝状聚合物的表面可以通过已知方法进一步修饰。还包括混合树枝状大分子的制剂，其中树状聚合物具有相同的药物，以相同或不同的负载浓度存在但具有不同的释放曲线。混合树枝状大分子的这种配方可以具有以相同或不同负载浓度存在但具有不同释放曲线的不同客体分子。另外，提供了使用混合树枝状大分子递送药物或客体部分以提供对难溶性药物或客体部分的增加的溶解度的方法。

9. 发明申请

WO2006115547A8 DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY 审中-公开
标题翻译：具有增强放大和内部功能的聚合物聚合物
公开(公告)号：WO2006115547A8
公开(公告)日：2007-02-15
申请号：PCT/US2005047635
申请日：2005-12-21
申请人： DENDRITIC NANOTECHNOLOGIES INC , TOMALIA DONALD A , SWANSON DOUGLAS R , HUANG BAOHUA , PULGAM VEERA REDDY , HEINZELMANN JOSEPH R , SVENSON SONKE , REYNA LORI A , ZHURAVEL MICHAEL A , CHAUHAN ABHAY SINGH , DEMATTEI CORDELL R
发明人： TOMALIA DONALD A , SWANSON DOUGLAS R , HUANG BAOHUA , PULGAM VEERA REDDY , HEINZELMANN JOSEPH R , SVENSON SONKE , REYNA LORI A , ZHURAVEL MICHAEL A , CHAUHAN ABHAY SINGH , DEMATTEI CORDELL R
IPC分类号： A61K48/00 , A61K31/785 , C12N15/87
CPC分类号： C12N15/87 , A61K47/59 , A61K47/593 , A61K47/595 , A61K48/00 , A61K49/0002 , B82Y5/00 , B82Y10/00 , C08G83/003 , C08L101/005 , C09B67/0013
摘要： 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.
摘要翻译：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。

10. 发明申请

WO2005019290A2 ULTRA HIGH MOLECULAR WEIGHT HYBRID DENDRIGRAFT ARCHITECTURES 审中-公开
标题翻译：超高分子量混合动力建筑
公开(公告)号：WO2005019290A2
公开(公告)日：2005-03-03
申请号：PCT/US2004/025045
申请日：2004-08-03
申请人： DENDRITIC NANOTECHNOLOGIES, INC.
发明人： TOMALIA, Donald, A. , SWANSON, Douglas, R.
IPC分类号： C08G
CPC分类号： C08G83/002 , C08G83/005
摘要： Mono-reactive dendrigrafts prepared by convergent self-branching polymerization and their subsequent grafting to linear, dendritic, and dendrigraft, branched, and hyper-branched substrates to prepare ultra-high molecular weight dendrigraft architectures using alkyl halides and aryl halides as initiators.
摘要翻译：通过会聚自支化聚合制备的单反应性树枝状体，并且随后将其接枝到线性，树枝状和树枝状，支链和超分支底物，以制备使用烷基卤和芳基卤化物作为引发剂的超高分子量树枝状结构。

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