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21. 发明授权

US08323698B2 Polymers for functional particles 有权
标题翻译：功能颗粒聚合物
公开(公告)号：US08323698B2
公开(公告)日：2012-12-04
申请号：US12873692
申请日：2010-09-01
申请人： Frank X. Gu , Omid C. Farokhzad , Robert S. Langer , Benjamin A. Teply
发明人： Frank X. Gu , Omid C. Farokhzad , Robert S. Langer , Benjamin A. Teply
IPC分类号： A61K9/14 , A61K9/51
CPC分类号： C08G63/912 , A61K9/5153 , A61K47/549 , A61K47/593 , A61K47/60 , A61K47/6935 , A61K47/6937 , A61K49/00 , A61K51/1244 , B82Y5/00 , Y10S977/773 , Y10S977/906 , Y10S977/915 , Y10T428/2982
摘要： The present invention generally relates to polymers and macromolecules, in particular, to block polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. The moiety, in some embodiments, may have a molecular weight greater than about 1000 Da; for example, the moiety may include a polypeptide or a polynucleotide, such as an aptamer. The moiety may also be a targeting moiety, an imaging moiety, a chelating moiety, a charged moiety, or a therapeutic moiety. Another aspect of the invention is directed to systems and methods of producing such polymeric conjugates. In some embodiments, a solution containing a polymer is contacted with a liquid, such as an immiscible liquid, to form nanoparticles containing the polymeric conjugate. Other aspects of the invention are directed to methods using such libraries, methods of using or administering such polymeric conjugates, methods of promoting the use of such polymeric conjugates, kits involving such polymeric conjugates, or the like.
摘要翻译：本发明一般涉及聚合物和大分子，特别是阻止可用于颗粒如纳米颗粒的聚合物。本发明的一个方面涉及一种开发具有所需性质的纳米颗粒的方法。在一组实施方案中，该方法包括制备具有高度控制性质的纳米颗粒的文库，其可通过将两种或多种不同比例的大分子混合在一起形成。一个或多个大分子可以是部分与生物相容性聚合物的聚合物缀合物。在一些情况下，纳米颗粒可以含有药物。在一些实施方案中，该部分可具有大于约1000Da的分子量; 例如，该部分可以包括多肽或多核苷酸，例如适体。该部分还可以是靶向部分，成像部分，螯合部分，带电部分或治疗部分。本发明的另一方面涉及制备这种聚合物缀合物的系统和方法。在一些实施方案中，将含有聚合物的溶液与诸如不混溶液体的液体接触以形成含有聚合物缀合物的纳米颗粒。本发明的其它方面涉及使用这种文库的方法，使用或施用这种聚合物缀合物的方法，促进使用这种聚合物缀合物的方法，涉及这种聚合物缀合物的试剂盒等。

22. 发明申请

US20110027172A1 DRUG DELIVERY SYSTEM FOR PHARMACEUTICALS AND RADIATION 审中-公开
标题翻译：用于药物和辐射的药物递送系统
公开(公告)号：US20110027172A1
公开(公告)日：2011-02-03
申请号：US12747040
申请日：2008-12-10
申请人： Zhuang Wang , Omid C. Farokhzad , Liangfang Zhang , Aleksandar Filip Radovic-Moreno , Frank X. Gu , Robert S. Langer
发明人： Zhuang Wang , Omid C. Farokhzad , Liangfang Zhang , Aleksandar Filip Radovic-Moreno , Frank X. Gu , Robert S. Langer
IPC分类号： A61K51/12 , A61K9/14 , A61K9/00 , A61P43/00
CPC分类号： A61K51/1255 , A61K31/337 , A61K47/6937
摘要： The present invention provides a drug delivery system for delivery of an agent and a radiopharmaceutical agent. The drug delivery system may specifically target an organ, tissue, cells, extracellular matrix, or intracellular compartment. Typically, the drug delivery system is a particle. Pharmaceutical compositions comprising the inventive particles are also provided. The present invention provides methods of preparing and using the inventive particles and pharmaceutical compositions. The inventive particles are useful in treating and diagnosing a variety of diseases including cancer. The inventive particles are also useful in tracking particles in vivo.
摘要翻译：本发明提供了用于递送药剂和放射性药剂的药物递送系统。药物递送系统可以特异性地靶向器官，组织，细胞，细胞外基质或细胞内区室。通常，药物递送系统是颗粒。还提供了包含本发明颗粒的药物组合物。本发明提供了制备和使用本发明的颗粒和药物组合物的方法。本发明的颗粒可用于治疗和诊断各种疾病，包括癌症。本发明的颗粒也可用于在体内追踪颗粒。

23. 发明申请

US20100323199A1 POLYMERS FOR FUNCTIONAL PARTICLES 有权
标题翻译：功能颗粒聚合物
公开(公告)号：US20100323199A1
公开(公告)日：2010-12-23
申请号：US12873692
申请日：2010-09-01
申请人： Frank X. Gu , Benjamin A. Teply , Robert S. Langer , Omid C. Farokhzad
发明人： Frank X. Gu , Benjamin A. Teply , Robert S. Langer , Omid C. Farokhzad
IPC分类号： B32B5/00
CPC分类号： C08G63/912 , A61K9/5153 , A61K47/549 , A61K47/593 , A61K47/60 , A61K47/6935 , A61K47/6937 , A61K49/00 , A61K51/1244 , B82Y5/00 , Y10S977/773 , Y10S977/906 , Y10S977/915 , Y10T428/2982
摘要： The present invention generally relates to polymers and macromolecules, in particular, to block polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. The moiety, in some embodiments, may have a molecular weight greater than about 1000 Da; for example, the moiety may include a polypeptide or a polynucleotide, such as an aptamer. The moiety may also be a targeting moiety, an imaging moiety, a chelating moiety, a charged moiety, or a therapeutic moiety. Another aspect of the invention is directed to systems and methods of producing such polymeric conjugates. In some embodiments, a solution containing a polymer is contacted with a liquid, such as an immiscible liquid, to form nanoparticles containing the polymeric conjugate. Other aspects of the invention are directed to methods using such libraries, methods of using or administering such polymeric conjugates, methods of promoting the use of such polymeric conjugates, kits involving such polymeric conjugates, or the like.
摘要翻译：本发明一般涉及聚合物和大分子，特别是阻止可用于颗粒如纳米颗粒的聚合物。本发明的一个方面涉及一种开发具有所需性质的纳米颗粒的方法。在一组实施方案中，该方法包括制备具有高度控制性质的纳米颗粒的文库，其可通过将两种或多种不同比例的大分子混合在一起形成。一个或多个大分子可以是部分与生物相容性聚合物的聚合物缀合物。在一些情况下，纳米颗粒可以含有药物。在一些实施方案中，该部分可具有大于约1000Da的分子量; 例如，该部分可以包括多肽或多核苷酸，例如适体。该部分还可以是靶向部分，成像部分，螯合部分，带电部分或治疗部分。本发明的另一方面涉及制备这种聚合物缀合物的系统和方法。在一些实施方案中，将含有聚合物的溶液与诸如不混溶液体的液体接触以形成含有聚合物缀合物的纳米颗粒。本发明的其它方面涉及使用这种文库的方法，使用或施用这种聚合物缀合物的方法，促进使用这种聚合物缀合物的方法，涉及这种聚合物缀合物的试剂盒等。

24. 发明申请

US20100129439A1 Adjuvant Incorporation in Immunonanotherapeutics 有权
标题翻译：佐剂掺入免疫治疗
公开(公告)号：US20100129439A1
公开(公告)日：2010-05-27
申请号：US12428395
申请日：2009-04-22
申请人： Frank Alexis , Jinjun Shi , Matteo Iannacone , Ashley Moseman , Pamela Basto , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
发明人： Frank Alexis , Jinjun Shi , Matteo Iannacone , Ashley Moseman , Pamela Basto , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
IPC分类号： A61K9/48 , A61K38/20 , A61K38/21 , A61P31/00
CPC分类号： A61K9/14 , A61K38/20 , A61K38/21 , A61K39/00 , A61K39/0002 , A61K39/002 , A61K39/05 , A61K39/08 , A61K39/12 , A61K39/39 , A61K45/06
摘要： The present invention provides compositions and systems for delivery of nanocarriers to cells of the immune system. The invention provides nanocarriers capable of stimulating an immune response in T cells and/or in B cells. The invention provides nanocarriers that comprise an immunofeature surface and an immunostimulatory moiety. In some embodiments, the immunostimulatory moiety is an adjuvant. The invention provides pharmaceutical compositions comprising inventive nanocarriers. The present invention provides methods of designing, manufacturing, and using inventive nanocarriers and pharmaceutical compositions thereof.
摘要翻译：本发明提供用于将纳米载体递送至免疫系统细胞的组合物和系统。本发明提供能够刺激T细胞和/或B细胞中的免疫应答的纳米载体。本发明提供包含免疫表面和免疫刺激部分的纳米载体。在一些实施方案中，免疫刺激部分是佐剂。本发明提供包含本发明纳米载体的药物组合物。本发明提供了设计，制造和使用本发明的纳米载体及其药物组合物的方法。

25. 发明申请

US20100183727A1 Immunonanotherapeutics that Provide IgG Humoral Response Without T-Cell Antigen 有权
标题翻译：提供无T细胞抗原的IgG体液应答的免疫疗法
公开(公告)号：US20100183727A1
公开(公告)日：2010-07-22
申请号：US12428408
申请日：2009-04-22
申请人： Matteo Iannacone , Frank Alexis , Pamela Basto , Ashley Moseman , Jinjun Shi , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
发明人： Matteo Iannacone , Frank Alexis , Pamela Basto , Ashley Moseman , Jinjun Shi , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
IPC分类号： A61K9/14 , A61K39/00 , A61P37/04
CPC分类号： A61K39/00 , A61K39/0002 , A61K39/0013 , A61K39/12 , A61K39/385 , A61K39/39 , A61K2039/55505 , A61K2039/55511 , A61K2039/55555 , A61K2039/6093 , C12N2760/20234
摘要： The present invention provides compositions and systems for delivery of nanocarriers to cells of the immune system. The invention provides synthetic nanocarriers capable of eliciting an immune system response in the form of antibody production, wherein the nanocarriers lack any T cell antigens. In some embodiments, the invention provides nanocarriers that comprise an immunofeature surface, which provides high avidity binding of the nanocarriers to antigen presenting cells. The invention provides pharmaceutical compositions comprising inventive nanocarriers. The present invention provides methods of designing, manufacturing, and using inventive nanocarriers and pharmaceutical compositions thereof.
摘要翻译：本发明提供用于将纳米载体递送至免疫系统细胞的组合物和系统。本发明提供能够以抗体生产形式引发免疫系统应答的合成纳米载体，其中纳米载体缺乏任何T细胞抗原。在一些实施方案中，本发明提供包含免疫表面的纳米载体，其提供纳米载体与抗原呈递细胞的高亲合力结合。本发明提供包含本发明纳米载体的药物组合物。本发明提供了设计，制造和使用本发明的纳米载体及其药物组合物的方法。

26. 发明申请

US20100129392A1 Targeting of Antigen Presenting Cells with Immunonanotherapeutics 有权
标题翻译：用免疫治疗剂靶向抗原呈递细胞
公开(公告)号：US20100129392A1
公开(公告)日：2010-05-27
申请号：US12428381
申请日：2009-04-22
申请人： Jinjun Shi , Frank Alexis , Matteo Iannacone , Ashley Moseman , Pamela Basto , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
发明人： Jinjun Shi , Frank Alexis , Matteo Iannacone , Ashley Moseman , Pamela Basto , Robert Langer , Omid C. Farokhzad , Ulrich von Andrian
IPC分类号： A61K39/00 , A61K39/39
CPC分类号： A61K47/48869 , A61K39/00 , A61K47/6925 , A61K47/6935
摘要： The present invention provides compositions and systems for delivery of nanocarriers to cells of the immune system. The invention provides nanocarriers capable of stimulating an immune response in T cells and/or in B cells. The invention provides nanocarriers that comprise an immunofeature surface. The nanocarriers are capable of targeting antigen presenting cells when administered to a subject. The invention provides pharmaceutical compositions comprising inventive nanocarriers. The present invention provides methods of designing, manufacturing, and using inventive nanocarriers and pharmaceutical compositions thereof.
摘要翻译：本发明提供用于将纳米载体递送至免疫系统细胞的组合物和系统。本发明提供能够刺激T细胞和/或B细胞中的免疫应答的纳米载体。本发明提供了包含免疫电泳表面的纳米载体。当给予受试者时，纳米载体能够靶向抗原呈递细胞。本发明提供包含本发明纳米载体的药物组合物。本发明提供了设计，制造和使用本发明的纳米载体及其药物组合物的方法。

27. 发明授权

US08603532B2 Nanostructures for drug delivery 有权
标题翻译：用于药物输送的纳米结构
公开(公告)号：US08603532B2
公开(公告)日：2013-12-10
申请号：US13122615
申请日：2009-10-20
申请人： Stephen J. Lippard , Shanta Dhar , Omid C. Farokhzad , Frank X. Gu , Nagesh Kolishetti
发明人： Stephen J. Lippard , Shanta Dhar , Omid C. Farokhzad , Frank X. Gu , Nagesh Kolishetti
IPC分类号： A61K9/14 , A61K9/51
CPC分类号： A61K9/48 , A61K9/143 , A61K31/555 , A61K33/24 , A61K47/48092 , A61K47/48869 , A61K47/48915 , A61K47/549 , A61K47/6925 , A61K47/6937 , B82Y5/00
摘要： The present invention provides compositions, preparations, formulations, kits, and methods useful for treating subjects having cancer or at risk of developing cancer. Some embodiments of the invention may comprise a composition comprising a plurality of particles comprising a platinum(IV) therapeutically active precursor.
摘要翻译：本发明提供了可用于治疗患有癌症或有癌症发生危险的受试者的组合物，制剂，制剂，试剂盒和方法。本发明的一些实施方案可以包含包含多个包含铂（IV）治疗活性前体的颗粒的组合物。

28. 发明申请

US20110300219A1 NANOSTRUCTURES FOR DRUG DELIVERY 有权
标题翻译：用于药物递送的纳米结构
公开(公告)号：US20110300219A1
公开(公告)日：2011-12-08
申请号：US13122615
申请日：2009-10-20
申请人： Stephen J. Lippard , Shanta Dhar , Omid C. Farokhzad , Frank X. Gu , Nagesh Kolishetti
发明人： Stephen J. Lippard , Shanta Dhar , Omid C. Farokhzad , Frank X. Gu , Nagesh Kolishetti
IPC分类号： A61K9/14 , A61P35/00 , A61K39/00 , A61K33/00 , A61K31/282
CPC分类号： A61K9/48 , A61K9/143 , A61K31/555 , A61K33/24 , A61K47/48092 , A61K47/48869 , A61K47/48915 , A61K47/549 , A61K47/6925 , A61K47/6937 , B82Y5/00
摘要： The present invention provides compositions, preparations, formulations, kits, and methods useful for treating subjects having cancer or at risk of developing cancer. Some embodiments of the invention may comprise a composition comprising a plurality of particles comprising a platinum(IV) therapeutically active precursor.
摘要翻译：本发明提供了可用于治疗患有癌症或有癌症发生危险的受试者的组合物，制剂，制剂，试剂盒和方法。本发明的一些实施方案可以包含包含多个包含铂（IV）治疗活性前体的颗粒的组合物。

29. 发明授权

US09532956B2 PH sensitive biodegradable polymeric particles for drug delivery 有权
标题翻译： PH敏感的生物可降解聚合物颗粒用于药物递送
公开(公告)号：US09532956B2
公开(公告)日：2017-01-03
申请号：US12762348
申请日：2010-04-18
申请人： Aleksandar Filip Radovic-Moreno , Weiwei Gao , Archana Swami , Gershon Golomb , Robert S. Langer , Omid C. Farokhzad
发明人： Aleksandar Filip Radovic-Moreno , Weiwei Gao , Archana Swami , Gershon Golomb , Robert S. Langer , Omid C. Farokhzad
IPC分类号： A61K47/30 , G01N21/76 , A61K9/51 , A61K48/00 , C12N15/11 , C12N15/115
CPC分类号： A61K9/51 , A61K48/0008 , C12N15/111 , C12N15/115 , C12N2310/11 , C12N2310/14 , C12N2310/16 , C12N2320/32
摘要： The present invention generally relates to polymers and particles, such as nanoparticles. The particles and polymers generally include one or more buffering components. Additionally, the particles and polymers may include two or more components that impart useful properties (functionalities). The particles and polymers, for example, may include a buffering component and a degradable component. As described herein, the particles and polymers may also include a hydrophilic component and/or a cleavable bond component. The particles and polymers described herein have been found to be particularly effective when used for delivery of one or more agents, such as one or more pharmaceutical agents. Other aspects of the invention are directed to methods of using or administering such particles or polymers, kits involving such particles or polymers, and the like. The present invention also relates to particles containing a cleavable bond component and one or more fluorescence resonance energy transfer (FRET) pairs as well as methods of detecting the cleavage of the cleavable bond component of such particles.
摘要翻译：本发明一般涉及聚合物和颗粒，例如纳米颗粒。颗粒和聚合物通常包括一种或多种缓冲组分。此外，颗粒和聚合物可以包括赋予有用性质（功能）的两种或更多种组分。颗粒和聚合物例如可以包括缓冲组分和可降解组分。如本文所述，颗粒和聚合物还可以包括亲水组分和/或可裂解键组分。已经发现本文所述的颗粒和聚合物在用于递送一种或多种试剂如一种或多种药剂时是特别有效的。本发明的其它方面涉及使用或施用此类颗粒或聚合物的方法，涉及这种颗粒或聚合物的试剂等。本发明还涉及含有可切割键组分和一种或多种荧光共振能量转移（FRET）对的颗粒以及检测这些颗粒的可裂解键组分的切割的方法。

30. 发明授权

US09267937B2 System for screening particles 有权
标题翻译：颗粒筛选系统
公开(公告)号：US09267937B2
公开(公告)日：2016-02-23
申请号：US12097118
申请日：2006-12-15
申请人： Omid C. Farokhzad , Aleksandar Filip Radovic-Moreno , Robert S. Langer
发明人： Omid C. Farokhzad , Aleksandar Filip Radovic-Moreno , Robert S. Langer
IPC分类号： C40B30/06 , G01N33/50 , B82Y5/00 , B82Y15/00 , A61K47/48
CPC分类号： G01N33/5088 , A61K47/555 , A61K47/66 , A61K47/6891 , B82Y5/00 , B82Y15/00 , C40B30/06
摘要： Screening of a library of particles in vivo and/or in vitro using Polyplex Iterative Combinatorial Optimization (PICO) allows for the design of particles for targeting a specific organ, tissue (e.g., cancer), or cell. Particles may, for example, include different targeting agents (e.g., aptamers or plurality of aptamers) on their surfaces, and the aptamer or aptamers may be evolved to provide better targeting of the particles. Libraries of particles are enriched in characteristics of particles that have been found to migrate to a tissue of interest, be taken up by cells, etc. The process may be repeated to engineer particles of a desired specificity or biological function.
摘要翻译：使用Polyplex迭代组合优化（PICO）在体内和/或体外筛选粒子库允许设计用于靶向特定器官，组织（例如癌症）或细胞的颗粒。例如，颗粒可以在其表面上包括不同的靶向剂（例如，适体或多个适配体），并且适配体或适体可以进化以提供更好的颗粒靶向。已经发现已经发现迁移到感兴趣的组织，被细胞吸收的颗粒的特征的颗粒的富集等。可以重复该过程来设计具有所需特异性或生物学功能的颗粒。

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