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1. 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。

2. 发明申请

WO2005028432A1 HYPERBRANCHED (PAMAM) POLYMERS VIA A ONE POT PROCESS 审中-公开
标题翻译：高分子（PAMAM）聚合物通过一个工艺过程
公开(公告)号：WO2005028432A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/029384
申请日：2004-09-10
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： C07C381/00
CPC分类号： C08F220/18 , C07C229/16 , C07C233/36 , C08G83/005
摘要： Methods of providing hyperbranched polymers by polymerization of appropriate AB 2 monomers derived from the reaction of tris-(2-aminoethyl) amine and various other materials, namely, succinic anhydride, methyl acrylate, and dimethyl itaconate.
摘要翻译：通过聚合衍生自三 - （2-氨基乙基）胺和各种其他材料即琥珀酸酐，丙烯酸甲酯和衣康酸二甲酯的各种其他材料的合适的AB2单体提供超支化聚合物的方法。

3. 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。

4. 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。

5. 发明申请

WO2008054466A2 DELIVERY OF BIOLOGICALLY ACTIVE MATERIALS USING CORE-SHELL TECTO (DENDRITIC POLYMERS) 审中-公开
标题翻译：使用核壳TECTO（树枝状聚合物）交付生物活性材料
公开(公告)号：WO2008054466A2
公开(公告)日：2008-05-08
申请号：PCT/US2007/005681
申请日：2007-03-03
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , DEMATTEI, Cordell, R. , HUANG, Baohua , REYNA, Lori, A. , SVENSON, Sonke , SWANSON, Douglas, R. , TOMALIA, Donald, A. , ZHURAVEL, Michael, A. , PULGAM, Veera, Reddy
发明人： DEMATTEI, Cordell, R. , HUANG, Baohua , REYNA, Lori, A. , SVENSON, Sonke , SWANSON, Douglas, R. , TOMALIA, Donald, A. , ZHURAVEL, Michael, A. , PULGAM, Veera, Reddy
IPC分类号： A61K48/00
CPC分类号： A61K48/00 , A61K9/5146 , A61K47/59 , A61K47/595 , A61K47/60 , C08G83/003 , Y02A50/463
摘要： The present invention concerns core-shell tecto (dendritic polymers) that are associated with biologically active materials (such as nucleic acids for use for RNAi and in transfection). Also included are formulations for their use. The constructs are useful for the delivery of drugs to an animal or plant and may be in vivo , in vitro or ex vivo .
摘要翻译：本发明涉及与生物活性物质（例如用于RNAi和转染的核酸）相关的核 - 壳结构（树状聚合物）。还包括它们的使用配方。该构建体可用于将药物递送至动物或植物，并且可以在体内，体外或离体。 >

6. 发明申请

WO2006115547A2 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：WO2006115547A2
公开(公告)日：2006-11-02
申请号：PCT/US2005/047635
申请日：2005-12-21
申请人： DENDRITIC NANOTECHNOLOGIES, INC. , TOMALIA, Donald, A. , SWANSON, Douglas, R. , HUANG, Baohua , PULGAM, Verra, 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, Verra, 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
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，热稳定性和较少或没有反向迈克尔反应），并且在较低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。

7. 发明申请

WO2006105043A2 JANUS DENDRIMERS AND DENDRONS 审中-公开
标题翻译： JANUS DENDRIMERS和DENDRONS
公开(公告)号：WO2006105043A2
公开(公告)日：2006-10-05
申请号：PCT/US2006/011160
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： A61K48/00
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结构连接在核心处（具有或不具有连接基团），并且其中至少两个树枝状突起具有不同的功能。那些Janus树枝状大分子是首选的，其中至少有一个树突是PEHAM树突。因此，这些Janus树枝状大分子是异性双功能的，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。

8. 发明申请

WO2006065266A3 DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY 审中-公开
公开(公告)号：WO2006065266A3
公开(公告)日：2006-06-22
申请号：PCT/US2005/013864
申请日：2005-04-20
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： C08J3/00 , C08J9/32 , C08J9/40 , C08K9/00
摘要： 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.

9. 发明授权

EP1171507B1 CORE-SHELL TECTODENDRIMERS 有权
标题翻译： CORE-SHELL TECTODENDRIMERE
公开(公告)号：EP1171507B1
公开(公告)日：2010-04-14
申请号：EP00911801.9
申请日：2000-02-15
申请人： Dendritic Nanotechnologies, Inc.
发明人： TOMALIA, Donald, A. , SWANSON, Douglas, R. , UPPULURI, Srinivas , BROTHERS, Herbert, M., II
IPC分类号： C08G69/02 , C08G69/48 , C08L77/06 , C08G83/00 , C08L101/00 , C08G81/00 , A61K47/48
CPC分类号： C08G83/003 , C08G69/02 , C08G69/04 , C08G69/48 , Y10S424/16 , Y10S977/754 , Y10S977/788 , Y10S977/835
摘要： Core-shell tecto(dendrimers) useful in biomedicine, pharmaceuticals, personal care products, and in other ways analogous to the known uses for dendrimers, hypercomb branched polymers, and other dendritic polymers are the reaction product of a core dendritic polymer molecule having a plurality of terminal functional groups of a first type which are not reactive with each other, and a plurality of shell dendritic polymer molecules having a plurality of terminal functional groups of a second type which are not reactive with each other, but which are reactive with the terminal functional groups of the first type. Each of the shell dendritic polymer molecules is chemically bonded to the core dendritic polymer molecule by a reaction of at least one of the terminal functional groups of the second type with at least one of the terminal functional groups of the first type.

10. 发明公开

EP1877103A2 DENDRITIC POLYMERS WITH ENHANCED AMPLIFICATION AND INTERIOR FUNCTIONALITY 审中-公开
标题翻译：具有改进的扩增和内部官能团树枝状聚合物
公开(公告)号：EP1877103A2
公开(公告)日：2008-01-16
申请号：EP05857843.6
申请日：2005-12-21
申请人： Dendritic Nanotechnologies, Inc.
发明人： TOMALIA, Donald, A. , SWANSON, Douglas, R. , HUANG, Baohua , PULGAM, Verra, Reddy , HEINZELMANN, Joseph, R. , SVENSON, Sonke , REYNA, Lori, A. , ZHURAVEL, Michael, A. , CHAUHAN, Abhay, Singh , DeMATTEL, Cordell, R.
IPC分类号： A61K48/00 , A61K31/785
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.

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