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1. 发明申请

US20080221300A1 Janus Dendrimers and Dendrons 失效
标题翻译：珍珠树枝和树枝
公开(公告)号：US20080221300A1
公开(公告)日：2008-09-11
申请号：US11885244
申请日：2006-03-27
申请人： Donald A. Tomalia , Veera Reddy Pulgam , Douglas R. Swanson , Baohua Huang
发明人： Donald A. Tomalia , Veera Reddy Pulgam , Douglas R. Swanson , Baohua Huang
IPC分类号： C08G75/00
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。

2. 发明授权

US07985424B2 Dendritic polymers with enhanced amplification and interior functionality 有权
标题翻译：具有增强的扩增和内部功能的树枝状聚合物
公开(公告)号：US07985424B2
公开(公告)日：2011-07-26
申请号：US11630044
申请日：2005-12-21
申请人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam , Joseph R. Heinzelmann , Sonke Svenson , Lori A. Reyna , Michael A. Zhuravel , Abhay Singh Chauhan , Cordell R. DeMattei
发明人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam , Joseph R. Heinzelmann , Sonke Svenson , Lori A. Reyna , Michael A. Zhuravel , Abhay Singh Chauhan , Cordell R. DeMattei
IPC分类号： A61K9/14
CPC分类号： C08G63/46 , A01N25/10 , A61K8/85 , A61K9/0019 , A61K9/5146 , A61Q15/00 , A61Q17/005 , C08G83/003 , H01M4/86 , H01M8/10 , Y02P70/56
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。

3. 发明申请

US20100086482A1 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） - 分散的DENDRONS和DENDRIMERS的多重合成
公开(公告)号：US20100086482A1
公开(公告)日：2010-04-08
申请号：US12448513
申请日：2007-12-28
申请人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam
发明人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam
IPC分类号： A61K49/00 , C07D487/00 , C07D491/00 , A61K31/395 , C07D245/00 , A61K31/495 , A61K31/16 , G01N33/566
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。

4. 发明授权

US07981444B2 Dendritic polymers with enhanced amplification and interior functionality 有权
标题翻译：具有增强的扩增和内部功能的树枝状聚合物
公开(公告)号：US07981444B2
公开(公告)日：2011-07-19
申请号：US10594776
申请日：2005-04-20
申请人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam
发明人： Donald A. Tomalia , Douglas R. Swanson , Baohua Huang , Veera Reddy Pulgam
IPC分类号： A61K9/14
CPC分类号： C08G83/003 , C08G59/1477 , C08G59/32 , C08G59/3227 , C08G59/5026
摘要： Poly(ester-acrylate) and poly(ester/epoxide) dendrimers. These materials can be synthesized by utilizing the so-called “sterically induced stoichiometric” principles. The preparation of the dendrimers is carried out by reacting precursor amino/polyamino-functional core materials with various branch cell reagents. The branch cell reagents are dimensionally large, relative to the amino/polyamino-initiator core and when reacted, produce generation=1 dendrimers directly in one step. There is also a method by which the dendrimers can be stabilized and that method is the reaction of the dendrimers with surface reactive molecules to pacify the reactive groups on the dendrimers.
摘要翻译：聚（酯 - 丙烯酸酯）和聚（酯/环氧化物）树枝状大分子。这些材料可以通过利用所谓的“空间诱导化学计量”原理来合成。树枝状大分子的制备通过使前体氨基/聚氨基官能的核心材料与各种分支细胞试剂反应来进行。分支细胞试剂相对于氨基/聚氨基 - 引发剂核心在尺寸上是大的，并且当反应时，在一个步骤中直接产生生成= 1个树枝状大分子。还有一种树枝状聚合物可以稳定的方法，该方法是树枝状聚合物与表面反应性分子的反应，以平衡树枝状聚合物上的反应性基团。

5. 发明申请

US20090012033A1 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）递送生物活性材料
公开(公告)号：US20090012033A1
公开(公告)日：2009-01-08
申请号：US12224644
申请日：2007-03-03
申请人： Cordell R. DeMattei , Baohua Huang , Lori A. Reyna , Sonke Svenson , Douglas R. Swanson , Donald A. Tomalia , Michael A. Zhuravel , Veera Reddy Pulgam
发明人： Cordell R. DeMattei , Baohua Huang , Lori A. Reyna , Sonke Svenson , Douglas R. Swanson , Donald A. Tomalia , Michael A. Zhuravel , Veera Reddy Pulgam
IPC分类号： A61K48/00 , C08G73/02 , C08G63/08 , C12Q1/68 , A61P43/00 , C12N15/63 , C08G63/91 , A61K31/7052
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（树枝状聚合物）。还包括其使用的配方。所述构建体可用于将药物递送至动物或植物，并且可以在体内或体外进行。

6. 发明申请

US20080112891A1 Encapsulated (Chelate or Ligand) Dendritic Polymers 审中-公开
标题翻译：封装（螯合或配体）树枝状聚合物
公开(公告)号：US20080112891A1
公开(公告)日：2008-05-15
申请号：US11795091
申请日：2006-02-15
申请人： Donald A. Tomalia , Baohua Huang
发明人： Donald A. Tomalia , Baohua Huang
IPC分类号： A61K49/10 , A61K31/787 , C08G63/91 , C08G63/48
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，治疗或递送该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。

7. 发明申请

US20100158850A1 DENDRIMER BASED MODULAR PLATFORMS 审中-公开
标题翻译：基于DENDRIMER的模块化平台
公开(公告)号：US20100158850A1
公开(公告)日：2010-06-24
申请号：US12645081
申请日：2009-12-22
申请人： James R. Baker, JR. , Mark M. Banaszak Holl , Xue-min Cheng , Baohua Huang , Daniel McNemy , Douglas G. Mullen , Thommey Thomas
发明人： James R. Baker, JR. , Mark M. Banaszak Holl , Xue-min Cheng , Baohua Huang , Daniel McNemy , Douglas G. Mullen , Thommey Thomas
IPC分类号： A61K31/74 , C08G69/00
CPC分类号： A61K31/74 , A61K31/00 , A61K45/06 , A61K47/551 , A61K47/59 , A61K47/595 , C08G73/0206 , C08G73/028 , C08G81/00 , C08G83/003 , C08L79/02 , C08L101/005 , A61K2300/00
摘要： The present invention relates to novel therapeutic and diagnostic dendrimer based modular platforms (e.g., drug delivery platforms). In particular, the dendrimer based modular platforms are configured such that two or more dendrimers (e.g., PAMAM dendrimers) are coupled together (e.g., via a cycloaddition reaction) wherein each of the coupled dendrimers is functionalized (e.g., functionalized for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy). In some embodiments, the present invention provides dendrimer based modular platforms having coupled dendrimers (e.g., two or more coupled dendrimers) wherein each dendrimer is conjugated to one or more functional groups (e.g., therapeutic agent, imaging agent, targeting agent, triggering agent) (e.g., for specific targeting and/or therapeutic use of the dendrimer based modular platform). In some embodiments, the functional groups are conjugated to the dendrimers via a linker and/or a triggering agent. In addition, the present invention is directed to methods of synthesizing dendrimer based modular platforms, compositions comprising the dendrimer based modular platforms, as well as systems and methods utilizing the dendrimer based modular platforms (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).
摘要翻译：本发明涉及新颖的基于树枝状大分子的模块化平台（例如药物递送平台）。特别地，基于树枝状聚合物的模块化平台被配置为使得两个或更多个树枝状聚合物（例如，PAMAM树枝状聚合物）偶联在一起（例如，通过环加成反应），其中每个偶联的树枝状聚合物被官能化（例如，功能化用于靶向，成像，感测和/或提供治疗或诊断材料和/或监测对治疗的响应）。在一些实施方案中，本发明提供了具有结合的树枝状大分子（例如两个或更多个偶联的树枝状大分子）的树枝状大分子模块化平台，其中每个树枝状聚合物与一个或多个官能团（例如，治疗剂，成像剂，靶向剂，引发剂）（例如，用于基于树枝状聚合物的模块化平台的特异性靶向和/或治疗用途）。在一些实施方案中，官能团通过接头和/或引发剂与树枝状聚合物缀合。此外，本发明涉及基于树枝状聚合物的模块化平台的方法，包含基于树枝状聚合物的模块化平台的组合物以及利用基于树枝状聚合物的模块化平台的系统和方法（例如，在诊断和/或治疗设置（例如，用于递送治疗剂，成像和/或靶向剂（例如，在疾病（例如癌症）诊断和/或治疗中等））。

8. 发明申请

US20070298006A1 Dendritic Polymers With Enhanced Amplification and Interior Functionality 有权
标题翻译：树枝状聚合物具有增强的放大和内部功能
公开(公告)号：US20070298006A1
公开(公告)日：2007-12-27
申请号：US11630044
申请日：2005-12-21
申请人： Donald Tomalia , Douglas Swanson , Baohua Huang , Veera Pulgam , Sonke Svenson , Lori Reyna , Michael Zhuravel , Abhay Chauhan , Cordell DeMattei , Joseph Heinzelmann
发明人： Donald Tomalia , Douglas Swanson , Baohua Huang , Veera Pulgam , Sonke Svenson , Lori Reyna , Michael Zhuravel , Abhay Chauhan , Cordell DeMattei , Joseph Heinzelmann
IPC分类号： A61K31/785 , A61K31/74 , A61K47/30 , A61K48/00 , B05D3/12 , C08G63/48 , C08G65/329 , C08K3/04 , C08K3/22 , C12N15/87
CPC分类号： C08G63/46 , A01N25/10 , A61K8/85 , A61K9/0019 , A61K9/5146 , A61Q15/00 , A61Q17/005 , C08G83/003 , H01M4/86 , H01M8/10 , Y02P70/56
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。

9. 发明申请

US20060160988A1 Heterocycle functionalized dendritic polymers 审中-公开
标题翻译：杂环官能化树枝状聚合物
公开(公告)号：US20060160988A1
公开(公告)日：2006-07-20
申请号：US10543671
申请日：2004-01-29
申请人： Donald Tomalia , Douglas Swanson , Baohua Huang
发明人： Donald Tomalia , Douglas Swanson , Baohua Huang
IPC分类号： C08G69/08
CPC分类号： C08G83/003 , C08G69/02
摘要： Heterocycle terminated dendritic polymers. More specifically, the production of 2-pyrrolidone, 2-piperidone, 2-aza-cycloheptanone or 2-azetidinone-terminated dendritic polymers obtained by reacting precursor primary amine, (e.g., —NH2)-terminated dendritic polymers with certain functionalized methacrylate reagents to produce new and novel dendritic polymers terminated with ester substituted 2-pyrrolidone, 2-piperidone, 2 aza-cycloheptanone or 2-azetidinone groups.
摘要翻译：杂环封端的树枝状聚合物。更具体地说，通过使前体伯胺（例如-NH 2 - ）反应而得到的2-吡咯烷酮，2-哌啶酮，2-氮杂 - 环庚酮或2-氮杂环丁酮封端的树枝状聚合物的制备（例如，-NH 2 - 具有某些官能化甲基丙烯酸酯试剂的树枝状聚合物以产生用酯取代的2-吡咯烷酮，2-哌啶酮，2氮杂 - 环庚酮或2-氮杂环丁酮基团封端的新型和新颖的树枝状聚合物。

10. 发明申请

US20120259098A1 DENDRIMER COMPOSITIONS AND METHODS OF SYNTHESIS 有权
标题翻译： DENDRIMER组合物和合成方法
公开(公告)号：US20120259098A1
公开(公告)日：2012-10-11
申请号：US13502004
申请日：2010-10-07
申请人： James R. Baker, JR. , Baohua Huang
发明人： James R. Baker, JR. , Baohua Huang
IPC分类号： C07K17/02 , C07D311/82 , C07C57/12 , C07K1/04 , C07H1/00 , C07H21/04 , C07D219/08 , B82Y15/00
CPC分类号： A61K47/48207 , A61K47/595 , A61K49/0002 , A61K49/0043 , A61K49/0054 , A61K49/124 , A61K51/065 , C08G73/028
摘要： The present invention relates to novel dendrimer compounds and methods of synthesizing the same. In particular, the present invention is directed to novel polyamidoamine (PAMAM) dendrimers, novel dendrimer branching units, methods for synthesizing such novel PAMAM dendrimers and functionalized dendrimers, as well as systems and methods utilizing the dendrimers (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease diagnosis and/or therapy, etc.))).
摘要翻译：本发明涉及新颖的树枝状大分子化合物及其合成方法。特别地，本发明涉及新颖的聚酰胺胺（PAMAM）树枝状大分子，新型树枝状大分子支化单元，合成这种新型PAMAM树枝状聚合物和官能化树枝状聚合物的方法，以及利用树枝状大分子的系统和方法（例如，在诊断和/或治疗设置（例如，用于递送治疗剂，成像和/或靶向剂（例如，在疾病诊断和/或治疗等中））。

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