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11.发明授权Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权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
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。
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公开(公告)号：US07632485B2
公开(公告)日：2009-12-15
申请号：US11065345
申请日：2005-02-24
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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13.发明申请Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 审中-公开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：US20080214853A1
公开(公告)日：2008-09-04
申请号：US11973810
申请日：2007-10-10
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。
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14.发明申请公开(公告)号：US20080213178A1
公开(公告)日：2008-09-04
申请号：US11973925
申请日：2007-10-11
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.
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15.发明授权公开(公告)号：US07060251B1
公开(公告)日：2006-06-13
申请号：US09530818
申请日：1998-09-08
IPC分类号： A61K49/04
CPC分类号： A61K51/088
摘要： The invention provides imaging agents comprising a label in association with a plaque specific targeting molecule. Methods for using the imaging agents to diagnose or monitor plaque formation and growth and kits containing the cardiovascular agents or components suitable for production of the imaging agents are also provided.
摘要翻译： 本发明提供包含与斑块特异性靶向分子相关联的标记物的成像剂。 还提供了使用成像剂诊断或监测斑块形成和生长的方法以及含有适合于生产成像剂的心血管药剂或成分的试剂盒。
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公开(公告)号：US4829051A
公开(公告)日：1989-05-09
申请号：US672167
申请日：1984-11-16
申请人： Joseph H. Cort , Alan J. Fischman
发明人： Joseph H. Cort , Alan J. Fischman
CPC分类号： C07K7/16 , A61K38/00 , Y10S514/807 , Y10S930/15
摘要： Novel analogs of biologically active vasopressin and its synthetic analogs having improved activity are represented by the structural formula: ##STR1## wherein A hydrogen; is hydroxy or lower alkoxy, especially methoxy, B is the peptide residue of phenylalanine (Phe) or isoleucine, Gln represents the peptide residue of glutamine Asn represents the peptide residue of asparagine, E represents the peptide residue of proline (Pro), 4-thioproline (4-thioPro) or 3,4-dehydroproline (3,4-dehydroPro), FNH represents an N-substituted peptide residue of L- or D-lysine (Lys) L or D homolysine (h Lys) or L- or D-orntihine (Orn), X represents a side peptide chain consisting of one or more of Gly, L-Ala, L-Val, L-Leu, or L-Phe, Gly represents the peptide residue of glycine, and G is disulfide (--S--S--) or thioether (--CH.sub.2 S-- or --SCH.sub.2 --).
摘要翻译： 具有改善活性的生物活性加压素及其合成类似物的新型类似物由以下结构式表示：其中A氢; 是羟基或低级烷氧基，特别是甲氧基，B是苯丙氨酸（Phe）或异亮氨酸的肽残基，Gln表示谷氨酰胺的肽残基，Asn代表天冬酰胺的肽残基，E表示脯氨酸（Pro）的肽残基，4- 硫代脯氨酸（4-thioPro）或3,4-脱氢脯氨酸（3,4-脱氢Pro），FNH代表L-或D-赖氨酸（Lys）L或D homolysine（h Lys）或L-或 D-orntihine（Orn），X表示由Gly，L-Ala，L-Val，L-Leu或L-Phe中的一种或多种组成的侧肽链，Gly表示甘氨酸的肽残基，G为二硫键 （-SS-）或硫醚（-CH 2 S-或-SCH 2 - ）。
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17.发明授权公开(公告)号：US08772319B2
公开(公告)日：2014-07-08
申请号：US13396010
申请日：2012-02-14
IPC分类号： A61K31/445 , C07D401/12 , C07D211/18
CPC分类号： C07D295/205 , C07D211/26 , C07D211/58 , C07D213/74 , C07D241/06 , C07D241/08 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/192 , C07D295/21 , C07D295/26
摘要： Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
摘要翻译： 本文描述了可用于治疗以缺乏多巴胺神经元活性为特征的神经变性疾病的哌啶和哌嗪化合物。 这些化合物也可用于成像多巴胺神经元。
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18.发明申请公开(公告)号：US20120208847A1
公开(公告)日：2012-08-16
申请号：US13396010
申请日：2012-02-14
IPC分类号： A61K31/454 , A61P25/36 , C07D401/12 , C07D211/26 , A61K31/445
CPC分类号： C07D295/205 , C07D211/26 , C07D211/58 , C07D213/74 , C07D241/06 , C07D241/08 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/192 , C07D295/21 , C07D295/26
摘要： Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
摘要翻译： 本文描述了可用于治疗以缺乏多巴胺神经元活性为特征的神经变性疾病的哌啶和哌嗪化合物。 这些化合物也可用于成像多巴胺神经元。
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19.发明授权公开(公告)号：US08092782B2
公开(公告)日：2012-01-10
申请号：US12208025
申请日：2008-09-10
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。
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公开(公告)号：US20110236308A1
公开(公告)日：2011-09-29
申请号：US12297513
申请日：2007-04-17
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。
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