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1. 发明授权

US09017724B2 Catalytic radiofluorination 有权
公开(公告)号：US09017724B2
公开(公告)日：2015-04-28
申请号：US12638606
申请日：2009-12-15
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K9/14 , C07F9/54 , A61K51/04 , C07D295/073 , A61B6/00 , C07B39/00
CPC分类号： A61K51/0459 , A61B6/507 , A61K51/04 , A61K51/0489 , C07B39/00 , C07B2200/05 , C07D295/073 , C07F9/5442
摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.

2. 发明申请

US20080206135A1 Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权
标题翻译：用放射性标记的链烷酸监测组织中血流和代谢摄取的方法
公开(公告)号：US20080206135A1
公开(公告)日：2008-08-28
申请号：US11974139
申请日：2007-10-11
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K51/04
CPC分类号： A61K51/0402
摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.
摘要翻译：本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换在2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

3. 发明授权

US5716594A Biotin compounds for targetting tumors and sites of infection 失效
标题翻译：用于靶向肿瘤和感染部位的生物素化合物
公开(公告)号：US5716594A
公开(公告)日：1998-02-10
申请号：US725060
申请日：1996-10-02
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup , John W. Babich
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup , John W. Babich
IPC分类号： A61K51/04 , A61K51/00 , A01N43/50 , A61K35/00 , C07D235/02
CPC分类号： A61K51/0497 , A61K47/48146 , A61K51/0495 , A61K2121/00 , A61K2123/00
摘要： Novel biotin amide analogs that are useful for targeting therapeutic and imaging agents to sites of infection and tumors in vivo are disclosed.
摘要翻译：公开了可用于将治疗和显像剂靶向感染部位和体内肿瘤的新型生物素酰胺类似物。

4. 发明授权

US08092782B2 Polybiotin compounds of magnetic resonance imaging and drug delivery 有权
标题翻译：用于磁共振成像和药物递送的多生物素化合物
公开(公告)号：US08092782B2
公开(公告)日：2012-01-10
申请号：US12208025
申请日：2008-09-10
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
IPC分类号： A61B5/055 , A61B5/05 , C07F5/00 , C07D255/02 , C07D235/02
CPC分类号： C07D519/00 , A61B5/0059 , A61B5/055 , A61B5/412 , A61B5/4839 , A61K47/557 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/124 , A61K51/0446 , A61K51/0497 , G01R33/5601
摘要： The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.
摘要翻译：本发明一般涉及可用作成像剂和药物递送剂的含生物素的化合物。本发明的另一方面涉及上述与金属原子螯合的化合物。在优选的实施方案中，金属原子是钆。本发明的另一方面涉及包含三个生物素部分和共价结合到杂环核心的药剂的化合物。在某些实施方案中，药剂是抗生素，抗病毒剂或放射性核素。本发明的另一方面涉及一种治疗涉及将哺乳动物施用本发明化合物的疾病的方法。本发明的另一方面涉及使用本发明化合物获得磁共振图像的方法。

5. 发明申请

US20110236308A1 Aryl Bidentate Isonitriles and Their Uses 审中-公开
标题翻译：芳基二异丁腈及其用途
公开(公告)号：US20110236308A1
公开(公告)日：2011-09-29
申请号：US12297513
申请日：2007-04-17
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman , Bhaskar C. Das
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman , Bhaskar C. Das
IPC分类号： A61K51/04 , C07C255/33 , C07C255/51 , C07F13/00 , A61K47/48 , A61P43/00
CPC分类号： A61K51/0478 , A61K49/0002 , A61K49/0019
摘要： The present invention relates generally to chelation compounds, radionuclide metal chelate compounds, i.e., complexes, and radiolabeled targeting moieties, i.e., conjugates, formed therefrom, and methods of using these compounds, complexes and conjugates for diagnostic and therapeutic purposes. This invention is more particularly related to aryl bidentate isonitrile metal complexes generated by a chemical interaction of a metal salt oxide or weak complex of the metal with aryl isonitrile bidentate ligands.
摘要翻译：本发明一般涉及螯合化合物，即放射性核素金属螯合物，即络合物和放射性标记的靶向部分，即由其形成的缀合物，以及用于诊断和治疗目的的这些化合物，复合物和缀合物的使用方法。本发明更特别涉及通过金属盐氧化物或金属与芳基异腈二齿配体的弱络合物的化学相互作用产生的芳基二齿异腈金属络合物。

6. 发明授权

US08558003B2 Imaging tracers for early detection and treatment of amyloid plaques caused by Alzheimer's disease and related disorders 有权
标题翻译：用于早期检测和治疗由阿尔茨海默病和相关疾病引起的淀粉样斑块的成像示踪剂
公开(公告)号：US08558003B2
公开(公告)日：2013-10-15
申请号：US12854625
申请日：2010-08-11
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
IPC分类号： A61K31/428 , A61K51/04 , A61K49/00 , C07D277/66
CPC分类号： C07D277/66 , A61K51/0446 , A61K51/0453
摘要： The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4′-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.
摘要翻译：本发明涉及用于成像和治疗阿尔茨海默病或淀粉样变性相关病理状况的化合物和方法，其利用新型淀粉样蛋白成像示踪剂来检测患有这些病症的受试者中的淀粉样蛋白沉积物。在某些实施方案中，本发明涉及[N-2 [18F]氟丙基] -2-（4' - （甲基氨基） - 苯基）-6-羟基苯并噻唑（F-18MHT）及其二聚体。

7. 发明授权

US08257680B1 Catalytic radiofluorination 有权
标题翻译：催化放电氟化
公开(公告)号：US08257680B1
公开(公告)日：2012-09-04
申请号：US11506603
申请日：2006-08-18
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/04 , A61B6/507 , A61K9/0021 , A61K49/0433 , A61K51/00 , A61K51/0459 , A61K51/0489 , C07B2200/05 , C07C209/74 , C07C211/64 , C07C381/12 , C07D241/04 , C07D295/073 , C07F9/5442
摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
摘要翻译：本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。在优选的实施方案中，使用氟化钾-18。本发明的另一方面涉及可用作成像剂的含氟-18的芳基铵化合物。在某些实施方案中，铵化合物是四芳基铵盐。本发明的另一方面涉及可用作成像剂的含有氟-18的芳基锍化合物。在某些实施方案中，锍化合物是三芳基锍盐。本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

8. 发明申请

US20100298389A1 Novel Imaging Tracers for Early Detection and Treatment of Amyloid Plaques Caused by Alzheimer's Disease and Related Disorders 有权
标题翻译：用于早期检测和治疗阿尔茨海默病和相关疾病引起的淀粉样斑块的新型成像追踪仪
公开(公告)号：US20100298389A1
公开(公告)日：2010-11-25
申请号：US12854625
申请日：2010-08-11
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
IPC分类号： A61K31/428 , C07D277/66 , C07D417/12 , A61P25/28
CPC分类号： C07D277/66 , A61K51/0446 , A61K51/0453
摘要： The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4′-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.
摘要翻译：本发明涉及用于成像和治疗阿尔茨海默病或淀粉样变性相关病理状况的化合物和方法，其利用新型淀粉样蛋白成像示踪剂来检测患有这些病症的受试者中的淀粉样蛋白沉积物。在某些实施方案中，本发明涉及[N-2 [18F]氟丙基] -2-（4' - （甲基氨基） - 苯基）-6-羟基苯并噻唑（F-18MHT）及其二聚体。

9. 发明授权

US07790142B2 Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权
标题翻译：用放射性标记的链烷酸监测组织中血流和代谢摄取的方法
公开(公告)号：US07790142B2
公开(公告)日：2010-09-07
申请号：US11974139
申请日：2007-10-11
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/0402
摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.
摘要翻译：本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换在2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

10. 发明授权

US07632485B2 Catalytic radiofluorination 有权
标题翻译：催化放电氟化
公开(公告)号：US07632485B2
公开(公告)日：2009-12-15
申请号：US11065345
申请日：2005-02-24
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K51/00 , A61M36/14 , C07F5/00
CPC分类号： A61K51/04 , A61B6/507 , A61B6/508 , C07B59/00 , C07B2200/05 , C07D241/04
摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
摘要翻译：本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。在优选的实施方案中，使用氟化钾-18。本发明的另一方面涉及可用作成像剂的含有氟-18的哌嗪化合物。在某些实施方案中，哌嗪化合物含有季胺。本发明的另一方面涉及可用作成像剂的含有氟-18的芳基鏻化合物。在某些实施方案中，鏻化合物是四芳基鏻盐。本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

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