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1. 发明申请

WO2016134164A1 METHODS OF ENHANCING CERENKOV LUMINESCENCE USING NANOPARTICLES, AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：使用纳米颗粒增强CERENKOV发光的方法及其组合物
公开(公告)号：WO2016134164A1
公开(公告)日：2016-08-25
申请号：PCT/US2016/018502
申请日：2016-02-18
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER , CORNELL UNIVERSITY
发明人： PRATT, Edwin , GRIMM, Jan , KIRCHER, Moritz , SHAFFER, Travis M. , WALL, Matthew
IPC分类号： A61K49/00 , G01N21/62 , A61B5/00 , G01T1/164 , A61K51/12 , A61K41/00 , A61K47/48 , A61K49/08 , A61K49/10 , A61K49/18 , A61K51/08 , B82Y5/00 , G01N21/64
CPC分类号： A61B5/0059 , A61K49/0002 , A61K49/0013 , A61K51/1234 , A61K51/1244 , G01T1/22 , G02F2001/374
摘要： Cerenkov luminescence occurs when a charged particle travels through a medium faster than a speed of light in that medium. The luminescence generated depends on the refractive index of the material and the energy of the particle traveling through the dielectric medium. Biomedical applications of Cerenkov luminescence currently utilize radionuclides producing Cerenkov light through interactions with tissue, which has a refractive index range of 1.36-1.41. The present disclosure describes the enhancement of Cerenkov luminescence through coupling various radionuclides to different biocompatible nanoparticles that have refractive indices greater than tissue.
摘要翻译：当带电粒子在该介质中通过介质比光的速度更快地行进时，发生Cerenkov发光。产生的发光取决于材料的折射率和穿过电介质的颗粒的能量。 Cerenkov发光的生物医学应用目前利用放射性核素通过与组织的相互作用产生Cerenkov光，折射率范围为1.36-1.41。本公开描述了通过将各种放射性核素耦合到具有大于组织的折射率的不同生物相容纳米颗粒来增强Cerenkov发光。

2. 发明申请

WO2017044701A1 METHODS AND COMPOSITIONS FOR CANCER TREATMENT 审中-公开
标题翻译：癌症治疗的方法和组成
公开(公告)号：WO2017044701A1
公开(公告)日：2017-03-16
申请号：PCT/US2016/050891
申请日：2016-09-09
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER , WEILL MEDICAL COLLEGE OF CORNELL UNIVERSITY
发明人： GRIMM, Jan , GUZMAN, Monica, L. , KAITTANIS, Charalambos
IPC分类号： A61K33/26 , A61K47/36 , A61K47/40 , A61P35/02
CPC分类号： A61K33/26 , A61K9/0019 , A61K9/5115 , A61K47/02 , A61K2300/00
摘要： A method for treating leukemia is disclosed. The method comprises administering to a subject with leukemia an effective amount of a pharmaceutical composition comprising a naked iron oxide nanoparticle, wherein the composition is not loaded with an active agent. Also disclosed is a method for treating cancer. The method comprises administering an effective amount of a pharmaceutical composition comprising a metal oxide nanoparticle comprising a polymeric coating over a metal oxide core, wherein the nanoparticle is loaded with a reactive oxygen species (ROS)-inducing agent.
摘要翻译：公开了一种治疗白血病的方法。该方法包括向患有白血病的受试者施用有效量的包含裸露的氧化铁纳米颗粒的药物组合物，其中所述组合物未装载活性剂。还公开了一种治疗癌症的方法。该方法包括施用有效量的药物组合物，其包含在金属氧化物核上包含聚合物涂层的金属氧化物纳米颗粒，其中所述纳米颗粒装载有活性氧（ROS）诱导剂。

3. 发明申请

WO2016176462A1 METHODS AND COMPOSITIONS FOR THERANOSTIC NANOPARTICLES 审中-公开
标题翻译：治疗纳米颗粒的方法和组合物
公开(公告)号：WO2016176462A1
公开(公告)日：2016-11-03
申请号：PCT/US2016/029804
申请日：2016-04-28
申请人： UNIVERSITY OF CENTRAL FLORIDA FOUNDATION, INC. , SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE AT LAKE NONA , MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： KHALED, Annette , PEREZ FIGUEROA, Jesus Manuel , SANTRA, Santimukul , KAITTANIS, Charalambos , SANTIESTEBAN, Oscar , GRIMM, Jan , SESSIONS, Hampton
IPC分类号： C07K7/00 , A61P35/00
CPC分类号： A61K47/6869 , A61K38/08 , A61K38/10 , A61K45/06 , A61K47/6935 , A61K51/1072 , A61K51/1244
摘要： Disclosed are compositions and methods for identifying a solid tumor cell target. Compositions and methods for treating prostate cancer are also disclosed. Further, cancer therapeutic compositions comprising CT20p are disclosed. Nanoparticles that are conjugated with a targeting ligand that is a substrate for a solid tumor-specific cell protein are disclosed.
摘要翻译：公开了用于鉴定实体瘤细胞靶的组合物和方法。还公开了用于治疗前列腺癌的组合物和方法。此外，公开了包含CT20p的癌症治疗组合物。公开了与作为固体肿瘤特异性细胞蛋白质的底物的靶向配体缀合的纳米颗粒。

4. 发明申请

WO2016057917A1 PSMA-RELATED THERAPIES 审中-公开
标题翻译： PSMA相关治疗
公开(公告)号：WO2016057917A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054937
申请日：2015-10-09
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： GRIMM, Jan , KAITTANIS, Charalambos
IPC分类号： A61K39/395
CPC分类号： A61K39/395 , A61K31/337 , A61K31/416 , A61K31/4166 , A61K31/47 , A61K31/4745 , A61K31/517 , A61K31/5377 , A61K31/662 , A61K31/69 , A61K31/704 , A61K38/05 , A61K45/06 , A61K2300/00 , G01N2333/705 , G01N2800/52
摘要： The present invention provides methods of treating disease by modulation of PSMA activity. Such modulations can lead to, for example, alterations in cancer tumor metabolism, oxygenation, vascularization, and metastasis. The present invention encompasses the recognition that PSMA, through its role in a complex signaling cascade, can affect cancer progression, angiogenesis, and neovascularization. The present invention provides, among other things, methods of treating cancer, including but not limited to cancer initiation, progression, metastasis, and vascularization by modulation of PSMA activity.
摘要翻译：本发明提供了通过调节PSMA活性来治疗疾病的方法。这种调节可导致例如癌症肿瘤代谢，氧合，血管形成和转移的改变。本发明包括认识到PSMA通过其在复合信号级联中的作用可以影响癌症进展，血管生成和新生血管形成。本发明尤其提供了通过调节PSMA活性来治疗癌症的方法，包括但不限于癌症起始，进展，转移和血管化。

5. 发明申请

WO2018089857A1 SONOPHORE-LABELED PROBES AND RELATED IN VIVO IMAGING TECHNIQUES 审中-公开
标题翻译： SONOPHORE标记的探针和相关的体内成像技术
公开(公告)号：WO2018089857A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/061192
申请日：2017-11-10
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： GRIMM, Jan , REINER, Thomas , BRAND, Christian , HAEDICKE, Katja
IPC分类号： A61K9/107 , C07C245/08 , C07K17/02 , G01N33/53 , G01N33/542
摘要： The present technology provides compositions and nanoemulsions useful in optoacoustic imaging. A composition of the present technology includes at least one contrast agent covalently linked to a targeting agent; where the at least one contrast agent includes a dark quencher; the targeting agent includes an antibody, an antigen, an antigen-targeting ligand, a receptor ligand, or an adhesion peptide; and the at least one contrast agent and targeting agent are covalently linked by a linker of formula (I) X 1 -L 1 -X 2 (I) where X1 is an amino, amide, S, or O of the at least one contrast agent; L 1 is C 1 -C 12 alkylene, C 2 -C 12 alkenylene, C 5 -C 12 cycloalkylene, or C 6 -C 12 arylene; and X 2 is an amino, amide, S, or O of the targeting agent.
摘要翻译：本技术提供了可用于光声成像的组合物和纳米乳液。本技术的组合物包含共价连接至靶向剂的至少一种造影剂; 其中至少一种造影剂包括暗猝灭剂; 靶向剂包括抗体，抗原，靶向抗原的配体，受体配体或粘附肽; 并且所述至少一种造影剂和靶向剂通过式（I）的接头共价连接X 1 -L 1 1 -X 2，（I）其中X 1是所述至少一种造影剂的氨基，酰胺，S或O; L 1为C 1 -C 12亚烷基，C 2 -C 12亚烷基，C 1 -C 12亚烷基，亚烯基，C≡C-C12亚环烷基或C≡C12亚芳基; X 2是靶向剂的氨基，酰胺，S或O.

6. 发明申请

WO2016018896A1 METAL(LOID) CHALCOGEN NANOPARTICLES AS UNIVERSAL BINDERS FOR MEDICAL ISOTOPES 审中-公开
标题翻译：金属（LOID）CHALCOGEN NANOPARTICLES作为医学同位素的通用粘合剂
公开(公告)号：WO2016018896A1
公开(公告)日：2016-02-04
申请号：PCT/US2015/042441
申请日：2015-07-28
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： WALL, Matthew A. , SHAFFER, Travis , HARMSEN, Stefan , GRIMM, Jan , KIRCHER, Moritz F.
IPC分类号： A61K51/12
CPC分类号： A61K51/1244 , A61K51/025 , A61K51/1251 , B82Y15/00
摘要： The present disclosure, among other things, provides new technologies for preparation of medical isotope labeled metal(loid) chalcogen nanoparticles for use in medical imaging and/or therapeutic applications. Provided technologies show a number of advantages as compared with previously available options for preparing and utilizing medical isotopes, including, for example, they utilize metal(loid) chalcogen nanoparticles that serve as universal binders (e.g., via covalent or non-covalent (e.g., chelate) bonds) for medical isotopes to provide medical isotope labeled metal(loid) chalcogen nanoparticles. Surprisingly, the same metal(loid) chalcogen nanoparticles may be used to bind (e.g., covalent or non-covalent e.g., chelation) bonding) a wide variety of different useful medical isotopes without the use of traditional chelating agents.
摘要翻译：本公开尤其提供了用于制备用于医学成像和/或治疗应用的医用同位素标记金属（loid）硫属元素纳米颗粒的新技术。所提供的技术与以前可用于制备和利用医学同位素的选择相比具有许多优点，例如，它们使用用作通用粘合剂的金属（卤素）硫族元素纳米颗粒（例如，通过共价或非共价键（例如，螯合）键），用于医学同位素，以提供医学同位素标记的金属（loid）硫属元素纳米颗粒。令人惊奇的是，相同的金属（卤素）硫族元素纳米颗粒可用于结合（例如共价或非共价例如螯合）键合）各种不同有用的医学同位素，而不使用传统的螯合剂。

7. 发明申请

WO2017019520A1 COMPOSITIONS AND METHODS OF CERENKOV TARGETED AND ACTIVATED IMAGING AND THERAPEUTICS 审中-公开
标题翻译： CERENKOV靶向和活化成像和治疗方法的组合物和方法
公开(公告)号：WO2017019520A1
公开(公告)日：2017-02-02
申请号：PCT/US2016/043601
申请日：2016-07-22
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： GRIMM, Jan , DAS, Sudeep
IPC分类号： A61K47/48 , A61K51/04 , A61P35/00
CPC分类号： A61K51/0495 , A61K47/557
摘要： Described herein are compositions and methods that confine Cerenkov light to a localized area for targeted treatment and/or imaging of tumor cells. In certain embodiments, such compositions include a Cerenkov-activated tagging agent comprising a payload and a covalent binding unit such as an azide. The payload can be an imaging agent, a contrast agent, and/or a therapeutic. In certain embodiments, a radiolabelled biomarker (e.g., 18 F-FDG (fluorodeoxyglucose), 18 F-FLT (fluorothymidine)) or other radiolabelled tumor cell targeting agent that emits Cerenkov luminescence is also administered. Upon local illumination by the Cerenkov luminescence at or near the location of the tumor cells, the payload (the imaging agent, contrast agent, and/or therapeutic) is activated. In this way, activation of the imaging agent, contrast agent, and/or therapeutic agent is limited to the region at or near the location of the tumor cells.
摘要翻译：本文描述了将切伦科夫光限制在局部区域以用于靶向治疗和/或肿瘤细胞成像的组合物和方法。在某些实施方案中，这种组合物包括Cerenkov激活的标记剂，其包含有效负载和共价结合单元如叠氮化物。有效载荷可以是成像剂，造影剂和/或治疗剂。在某些实施方案中，还施用放射性标记的生物标志物（例如18F-FDG（氟脱氧葡萄糖），18F-FLT（氟胸苷））或其他放射性标记的肿瘤细胞靶向剂，其发射Cerenkov发光。当通过Cerenkov发光在肿瘤细胞位置处或附近的局部照射时，有效载荷（成像剂，造影剂和/或治疗剂）被激活。以这种方式，显影剂，造影剂和/或治疗剂的活化限于肿瘤细胞位置处或附近的区域。

8. 发明申请

WO2016134002A1 COMPOSITIONS AND METHODS FOR NANOPARTICLE-BASED DRUG DELIVERY AND IMAGING 审中-公开
标题翻译：用于基于纳米脂的药物递送和成像的组合物和方法
公开(公告)号：WO2016134002A1
公开(公告)日：2016-08-25
申请号：PCT/US2016/018240
申请日：2016-02-17
申请人： MEMORIAL SLOAN KETTERING CANCER CENTER
发明人： GRIMM, Jan , KAITTANIS, Charalambos , SHAFFER, Travis M.
IPC分类号： A61K9/51
CPC分类号： A61K9/5123 , A61K9/5161 , A61K31/195 , A61K31/7028 , Y02A50/411
摘要： Methods and compositions described herein use polysaccharide nanoparticles (or polysaccharide-coated nanoparticles) to retain and deliver unaltered therapeutic agents to sites of disease. The polysaccharide nanoparticles are non-covalently associated with the unaltered therapeutic agent. The polysaccharide is able to retain cargo (drugs, diagnostics, etc.) without chemical modification of the agent. The nanoparticle maintains its association with the agent through non-covalent interactions but releases its agent in response to changes in the microenvironment, e.g., at the site of cancer cells or cancer tissue.
摘要翻译：本文所述的方法和组合物使用多糖纳米颗粒（或多糖包被的纳米颗粒）保留并递送未改变的治疗剂到疾病部位。多糖纳米颗粒与未改变的治疗剂非共价结合。多糖能够保留货物（药物，诊断等），而不会对药剂进行化学修饰。纳米颗粒通过非共价相互作用维持其与药物的结合，但是响应于微环境的变化而释放其药剂，例如在癌细胞或癌组织的位置。

9. 发明申请

WO2014047318A1 DELIVERY OF THERAPEUTIC COMPOUNDS WITH IRON OXIDE NANOPARTICLES 审中-公开
标题翻译：用氧化镍纳米颗粒递送治疗化合物
公开(公告)号：WO2014047318A1
公开(公告)日：2014-03-27
申请号：PCT/US2013/060662
申请日：2013-09-19
申请人： MEMORIAL SLOAN-KETTERING CANCER CENTER
发明人： KAITTANIS, Charalambos , GRIMM, Jan
IPC分类号： A61K47/48
CPC分类号： A61K49/1863 , A61K47/58 , A61K47/61 , A61K47/6923 , A61K47/6929 , A61K49/1854
摘要： The present invention relates to the field of drug delivery, in particular the delivery of unmodified cargo molecules (such as doxorubicin and Taxol®) using iron oxide nanoparticles as therapeutic delivery agents. Specifically described are methods to entrap cargo (i.e. known therapeutics (drugs) and other types of molecules) into the exterior coating of iron oxide nanoparticles, including iron oxide nanoparticles approved for use in humans. Additionally, methods describe the use of such drug- loaded nanoparticles as therapeutic delivery agents. Further, methods include quantifying and visualizing the amount of cargo molecule loading levels when preparing these therapeutic agents and then quantifying and visualizing the amount of delivery (i.e. unloading) of these cargo molecules from these nanoparticles using compact magnetic relaxometers, common NMR instruments and magnetic resonance imaging (MRI) instruments.
摘要翻译：本发明涉及药物递送领域，特别是使用氧化铁纳米颗粒作为治疗递送剂递送未修饰的货物分子（如多柔比星和紫杉醇）。具体描述的是将货物（即已知的治疗剂（药物）和其他类型的分子）捕获到氧化铁纳米颗粒的外部涂层中，包括被批准用于人体的氧化铁纳米颗粒的方法。另外，方法描述了这种药物负载纳米粒子作为治疗递送剂的用途。此外，方法包括在制备这些治疗剂时量化和可视化货物分子负载水平的量，然后使用紧凑型磁性舒张计，常规NMR仪器和磁共振来量化和可视化来自这些纳米颗粒的这些货物分子的递送量（即卸载）量成像（MRI）仪器。

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