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1. 发明申请

US20190231903A1 IMAGING SYSTEMS AND METHODS FOR PARTICLE-DRIVEN, KNOWLEDGE-BASED, AND PREDICTIVE CANCER RADIOGENOMICS 审中-公开
公开(公告)号：US20190231903A1
公开(公告)日：2019-08-01
申请号：US16315401
申请日：2017-06-28
申请人： Memorial Sloan Kettering Cancer Center , Cornell University
发明人： Michelle S. Bradbury , Cameron Brennan , Mithat Gonen , Mohan Pauliah , Ulrich Wiesner
IPC分类号： A61K49/00 , A61B5/00 , A61K51/12 , A61B5/055 , A61B6/03 , A61B6/00 , A61K51/08 , A61K49/18 , G01R33/56 , G01R33/563 , G01R33/48 , G01T1/164 , G01T1/29 , G06T7/00 , G06T7/40
CPC分类号： A61K49/0002 , A61B1/00009 , A61B5/0035 , A61B5/0042 , A61B5/055 , A61B5/1072 , A61B5/1075 , A61B5/4842 , A61B5/4848 , A61B6/03 , A61B6/037 , A61B6/4417 , A61B6/481 , A61B6/501 , A61B6/5217 , A61B6/5247 , A61B8/085 , A61B8/4416 , A61B8/481 , A61B8/5223 , A61B8/5261 , A61K49/1818 , A61K51/082 , A61K51/088 , A61K51/1244 , G01R33/481 , G01R33/4812 , G01R33/4814 , G01R33/5601 , G01R33/56341 , G01T1/1642 , G01T1/2985 , G06T7/0012 , G06T7/40 , G06T2207/10072 , G06T2207/10088 , G06T2207/30096
摘要： Described herein are particle-driven radiogenomics systems and methods that can be used to identify imaging features for prediction of intratumoral and interstitial nanoparticle distributions in cancers (e.g., in low grade and/or high-grade brain cancers (e.g., gliomas, e.g., primary gliomas)). In certain embodiments, the systems and methods described herein extract and combine quantitative multi-dimensional data generated from structural, functional, and/or metabolic imaging. In certain embodiments, the combined multidimensional data is linked to intratumoral and interstitial nanoparticle distributions. For example, this linked data can be used to determine quantitative functional-metabolic multimodality particle-based imaging features and to predict treatment efficacy. These techniques provide an improved quantitative ability to measure treatment response and determine tumor progressions compared to traditional size-based imaging methods.

2. 发明申请

US20180193410A1 COMPOSITIONS AND METHODS FOR INHIBITING CELLULAR ADHESION OR DIRECTING DIAGNOSTIC OR THERAPEUTIC AGENTS TO RGD BINDING SITES 审中-公开
公开(公告)号：US20180193410A1
公开(公告)日：2018-07-12
申请号：US15867101
申请日：2018-01-10
申请人： Allegro Pharmaceuticals, Inc
发明人： Michael John Mackel , John Park
IPC分类号： A61K38/12 , A61K47/64 , A61K38/07 , A61K51/08 , A61L31/04 , C07K7/00 , A61K51/06 , A61K38/17 , A61K9/08
CPC分类号： A61K38/12 , A61K9/06 , A61K9/08 , A61K38/07 , A61K38/1709 , A61K47/64 , A61K51/065 , A61K51/082 , A61K51/088 , A61L27/227 , A61L31/043 , A61L2300/252 , C07K7/00
摘要： Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

3. 发明授权

US09981050B2 Bispecific peptide conjugate and radioactive bispecific peptide imaging agent 有权
公开(公告)号：US09981050B2
公开(公告)日：2018-05-29
申请号：US15157905
申请日：2016-05-18
申请人： Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan, R.O.C.
发明人： Hung-Man Yu , Jyun-Hong Chen , Kun-Liang Lin , Chien-Jen Chen , Wuu-Jyh Lin
IPC分类号： A61K38/00 , A61K51/08 , C07K7/08 , C07K5/09
CPC分类号： A61K51/082 , A61K51/088 , C07K5/0817 , C07K7/08 , C07K2319/33
摘要： Disclosed herein is a bispecific peptide conjugate comprising an epidermal growth factor receptor (EGFR) targeting peptide, an αvβ3 integrin targeting peptide, and a linker, where the linker is conjugated respectively to the EGFR targeting peptide and the αvβ3 integrin targeting peptide.

4. 发明授权

US09872886B2 Compositions and methods for inhibiting cellular adhesion or directing diagnostic or therapeutic agents to RGD binding sites 有权
公开(公告)号：US09872886B2
公开(公告)日：2018-01-23
申请号：US14696250
申请日：2015-04-24
申请人： Allegro Pharmaceuticals, Inc.
发明人： Michael John Mackel , John Park
IPC分类号： A61K38/08 , A61K38/12 , C07K7/00 , A61K9/08 , A61K38/17 , A61K51/06 , A61K51/08 , A61L27/22 , A61L31/04 , A61K38/07 , A61K47/64 , A61K9/06
CPC分类号： A61K38/12 , A61K9/06 , A61K9/08 , A61K38/07 , A61K38/1709 , A61K47/64 , A61K51/065 , A61K51/082 , A61K51/088 , A61L27/227 , A61L31/043 , A61L2300/252 , C07K7/00
摘要： Compounds comprising R-G-Cysteic Acid (i.e., R-G-NH—CH(CH2—SO3H)COOH or Arg-Gly-NH—CH(CH2—SO3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

5. 发明申请

US20170267699A1 NITROGEN-CONTAINING MACROCYCLIC CONJUGATES AS RADIOPHARMACEUTICALS 审中-公开
公开(公告)号：US20170267699A1
公开(公告)日：2017-09-21
申请号：US15612185
申请日：2017-06-02
申请人： THE UNIVERSITY OF MELBOURNE
发明人： Paul Stephen DONNELLY , Michelle Therese MA , Denis Bernard SCANLON
IPC分类号： C07D521/00 , A61K51/04 , A61K51/08
CPC分类号： C07D521/00 , A61K49/06 , A61K49/08 , A61K49/10 , A61K49/101 , A61K51/00 , A61K51/02 , A61K51/04 , A61K51/0482 , A61K51/082 , A61K51/088
摘要： The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.

6. 发明申请

US20170189567A1 Cage-Like Bifunctional Chelators, Copper-64 Radiopharmaceuticals and PET Imaging Using the Same 审中-公开
公开(公告)号：US20170189567A1
公开(公告)日：2017-07-06
申请号：US15194425
申请日：2016-06-27
申请人： UNIVERSITY OF SOUTHERN CALIFORNIA
发明人： Peter S. Conti , Hancheng Cai , Zibo Li , Shuanglong Liu
IPC分类号： A61K51/04 , A61K51/10 , A61K51/08 , C07D487/04
CPC分类号： A61K51/0474 , A61K51/0482 , A61K51/082 , A61K51/088 , A61K51/1093 , C07D487/04 , C07D487/08 , C07K5/1021 , C07K7/086
摘要： Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

7. 发明授权

US09625456B2 Fluorescent silica-based nanoparticles 有权
公开(公告)号：US09625456B2
公开(公告)日：2017-04-18
申请号：US13381209
申请日：2010-07-02
申请人： Michelle Bradbury , Ulrich Wiesner , Oula Penate Medina , Hoosweng Ow , Andrew Burns , Jason Lewis , Steven Larson
发明人： Michelle Bradbury , Ulrich Wiesner , Oula Penate Medina , Hoosweng Ow , Andrew Burns , Jason Lewis , Steven Larson
IPC分类号： G01N33/543 , A61K49/00 , A61K51/08 , A61K51/12 , B82Y5/00 , B82Y15/00 , G01N33/58
CPC分类号： A61K51/1244 , A61K9/5115 , A61K9/5146 , A61K9/5169 , A61K49/0019 , A61K49/0032 , A61K49/0054 , A61K49/0056 , A61K49/0093 , A61K51/08 , A61K51/082 , A61K51/086 , A61K51/1255 , B82Y5/00 , B82Y15/00 , G01N33/54346 , G01N33/552 , G01N33/574 , G01N33/582 , G01N33/587 , G01N33/60 , Y10S977/773 , Y10S977/927
摘要： The present invention provides a fluorescent silica-based nanoparticle that allows for precise detection, characterization, monitoring and treatment of a disease such as cancer The nanoparticle has a fluorescent compound positioned within the nanoparticle, and has greater brightness and fluorescent quantum yield than the free fluorescent compound To facilitate efficient urinary excretion of the nanoparticle, it may be coated with an organic polymer, such as polyethylene glycol) (PEG) The small size of the nanoparticle, the silica base and the organic polymer coating minimizes the toxicity of the nanoparticle when administered in vivo The nanoparticle may further be conjugated to a ligand capable of binding to a cellular component associated with the specific cell type, such as a tumor marker A therapeutic agent may be attached to the nanoparticle Radionuclides/radiometals or paramagnetic ions may be conjugated to the nanoparticle to permit the nanoparticle to be detectable by various imaging techniques.

8. 发明授权

US09463255B1 Radiolabeled alpha-melanocyte stimulating hormone hybrid peptide for melanoma targeting 有权
标题翻译：用于黑素瘤靶向的放射性标记的α-黑素细胞刺激激素杂交肽
公开(公告)号：US09463255B1
公开(公告)日：2016-10-11
申请号：US13617042
申请日：2012-09-14
申请人： Yubin Miao
发明人： Yubin Miao
IPC分类号： A61K51/00 , A61M36/14 , A61K51/08
CPC分类号： A61K51/086 , A61K38/00 , A61K38/17 , A61K51/082 , C07K7/56
摘要： The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue, suggesting favorable selective activity of compounds according to the present invention, which can be used as effective therapeutic agents against melanoma, including metastatic melanoma. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are useful to initiate therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic and therapeutic tools for a number of conditions and diseases states, especially melanoma.
摘要翻译：本发明涉及用于成像癌症的新型非侵入性诊断工具/化合物，特别是黑素瘤，包括体内转移性黑素瘤。本发明化合物在癌细胞和组织中表现出增强的摄取，表明根据本发明的化合物的有利选择性活性，其可以用作抗黑素瘤（包括转移性黑素瘤）的有效治疗剂。根据本发明的化合物代表使用非侵入性分子成像技术在黑色素瘤的诊断和治疗中的进展，包括转移性黑素瘤。本发明的新型探针可用于开始黑色素瘤的治疗以及监测患者对化疗治疗的反应以及用于治疗黑素瘤/转移性黑色素瘤的其它干预或治疗。根据本发明的化合物可用作许多病症和疾病状态的诊断和治疗工具，特别是黑素瘤。

9. 发明申请

US20160251378A1 Transmetalation Methods for the Synthesis of PET and SPECT Imaging Agents 审中-公开
标题翻译：用于合成PET和SPECT成像剂的转化方法
公开(公告)号：US20160251378A1
公开(公告)日：2016-09-01
申请号：US15055203
申请日：2016-02-26
申请人： Hans F. Schmitthenner , Anne M. Sweeney-Jones , Scott Williams
发明人： Hans F. Schmitthenner , Anne M. Sweeney-Jones , Scott Williams
IPC分类号： C07F5/00 , B01D15/38 , B01D15/42 , C07F1/08
CPC分类号： C07F5/00 , A61K51/082 , A61K51/088 , B01D15/325 , B01D15/3857 , B01D15/426 , C07F1/005 , C07F1/08 , C07F5/003
摘要： A process for the preparation of a radionuclide imaging agent includes providing an imaging agent including a chelated place-holder metal; loading the imaging agent onto an acid stable stationary phase; replacing the chelated place-holder metal of the imaging agent loaded on the stationary phase with a replacement radioactive metal under mild reaction conditions; and eluting the imaging agent including the chelated replacement radioactive metal from the stationary phase to provide a radionuclide imaging agent suitable for positron emission tomography (PET) or single-photon emission computed tomography (SPECT). The imaging agent can include a targeting agent that is directly conjugated to the imaging agent or by means of a linker. The process may also apply to other metals that are non-radioactive but used as diluent metals or other metals that are strongly bound to DOTA.
摘要翻译：一种制备放射性核素成像剂的方法包括提供包含螯合位置保持金属的成像剂; 将成像剂加载到酸稳定的固定相上; 在温和的反应条件下用置换的放射性金属代替负载在固定相上的成像剂的螯合的载体金属; 并从固定相中洗脱包含螯合置换放射性金属的成像剂，以提供适用于正电子发射断层摄影（PET）或单光子发射计算机断层摄影（SPECT）的放射性核素显像剂。成像剂可以包括直接与成像剂结合的靶向剂或借助于接头。该方法也可以应用于其它非放射性但用作稀释金属或与DOTA强烈结合的其它金属的金属。

10. 发明授权

US09403875B2 Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same 有权
标题翻译：笼状双功能螯合剂，铜64放射性药物和使用其的PET成像
公开(公告)号：US09403875B2
公开(公告)日：2016-08-02
申请号：US12695125
申请日：2010-01-27
申请人： Peter S. Conti , Hancheng Cai , Zibo Li , Shuanglong Liu
发明人： Peter S. Conti , Hancheng Cai , Zibo Li , Shuanglong Liu
IPC分类号： A61K51/00 , A61M36/14 , C07K7/08 , A61K51/04 , A61K51/08 , C07D487/08 , C07K5/113
CPC分类号： A61K51/0474 , A61K51/0482 , A61K51/082 , A61K51/088 , A61K51/1093 , C07D487/04 , C07D487/08 , C07K5/1021 , C07K7/086
摘要： Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.
摘要翻译：公开了一类通用的基于Sarcophagine的双功能螯合剂（BFC），其包含用于用具有成像，治疗或对比应用放射性标记的金属进行标记的六氮杂笼，以及一种或多种接头（A）和（B）。所述化合物具有通式，其中A是选自胺，羧酸，酯，羰基，硫醇，叠氮化物和烯烃的官能团，B是选自以下的官能团：的氢，胺，羧酸和酯，羰基，硫醇，叠氮化物和烯烃。还公开了BFC和靶向部分的缀合物，其可以是肽或抗体。还公开了可用作放射性药物，成像剂或造影剂的BFC /靶向部分缀合物的金属络合物。

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