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1. 发明申请

US20090023928A1 PHTHALAMIDE-LANTHANIDE COMPLEXES FOR USE AS LUMINESCENT MARKERS 审中-公开
标题翻译：用作紫外线标记物的羟乙基磺酰胺化合物复合物
公开(公告)号：US20090023928A1
公开(公告)日：2009-01-22
申请号：US12202367
申请日：2008-09-01
申请人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
IPC分类号： C07D277/04
CPC分类号： C12Q1/37 , A61K41/0057 , A61K49/0002 , A61K49/0019 , A61K49/103 , A61K49/106 , A61K49/122 , A61K49/124 , A61K51/0478 , A61K51/0482 , A61K51/06 , C07C235/60 , C07D487/08 , C07D487/18 , C07D487/22 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80 , Y10S436/804
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
摘要翻译：本发明提供了包含镧系元素的金属离子的发光镧系元素金属螯合物和包含至少一个邻苯二甲酰亚胺基部分的络合剂。还提供了掺入本发明的邻苯二甲酰氨基配体的探针和利用本发明配体的方法和包含本发明配体的探针。

2. 发明授权

US06864103B2 Phthalamide-lanthanide complexes for use as luminescent markers 有权
标题翻译：邻苯二甲酰镧系配合物用作发光标记
公开(公告)号：US06864103B2
公开(公告)日：2005-03-08
申请号：US09992156
申请日：2001-11-14
申请人： Kenneth N. Raymond , Stephane Petoud , Seth M. Cohen , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Seth M. Cohen , Jide Xu
IPC分类号： G01N33/53 , A61K49/00 , C07C233/00 , C07C235/60 , C07D245/04 , C07D487/08 , C07D487/18 , C07D487/22 , C07F5/00 , C09K11/06 , C12M1/00 , C12N15/09 , C12Q1/25 , C12Q1/68 , G01N21/76 , G01N33/533 , G01N33/542 , G01N33/566 , G01N37/00
CPC分类号： C12Q1/37 , A61K41/0057 , A61K49/0002 , A61K49/0019 , A61K49/103 , A61K49/106 , A61K49/122 , A61K49/124 , A61K51/0478 , A61K51/0482 , A61K51/06 , C07C235/60 , C07D487/08 , C07D487/18 , C07D487/22 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80 , Y10S436/804
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
摘要翻译：本发明提供了包含镧系元素的金属离子的发光镧系元素金属螯合物和包含至少一个邻苯二甲酰亚胺基部分的络合剂。还提供了掺入本发明的邻苯二甲酰氨基配体的探针和利用本发明配体的方法和包含本发明配体的探针。

3. 发明授权

US06406297B1 Salicylamide-lanthanide complexes for use as luminescent markers 有权
标题翻译：用作发光标记的水杨酰胺 - 镧系元素络合物
公开(公告)号：US06406297B1
公开(公告)日：2002-06-18
申请号：US09507599
申请日：2000-02-18
申请人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Seth Cohen , Jide Xu
IPC分类号： C07F500
CPC分类号： C12Q1/37 , C07C235/60 , C07C235/84 , C07C237/34 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one salicylamidyl moiety. Also provided are probes incorporating the salicylamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
摘要翻译：本发明提供了包含镧系元素的金属离子和包含至少一个水杨酰胺基部分的络合剂的发光镧系金属螯合物。还提供了掺入本发明的水杨酰胺基配体的探针和利用本发明配体的方法和包含本发明配体的探针。

4. 发明授权

US4939254A Template synthesis of macrocyclic catecholamide complexes 失效
标题翻译：大环儿茶酚胺复合物的模板合成
公开(公告)号：US4939254A
公开(公告)日：1990-07-03
申请号：US400360
申请日：1989-10-30
申请人： Thomas J. McMurry , Kenneth N. Raymond
发明人： Thomas J. McMurry , Kenneth N. Raymond
IPC分类号： C07D487/08 , C07F15/02 , C07F19/00
CPC分类号： C07D487/08 , C07F15/025 , C07F19/005
摘要： A method is provided for a high yield template synthesis of macrocyclic catecholamide ligands.
摘要翻译：提供了用于大环儿茶酚酰胺配体的高产率模板合成的方法。

5. 发明申请

US20120214843A1 Combination Treatment of Hydroxpyridonate Actinide/Lanthanide Decorporation Agents 审中-公开
标题翻译：羟基吡啶酮锕系元素/镧系元素的组合处理
公开(公告)号：US20120214843A1
公开(公告)日：2012-08-23
申请号：US13291383
申请日：2011-11-08
申请人： Patricia W. Durbin-Heavey , Leonore Frances Heavey , Kenneth N. Raymond , Rebecca J. Abergel , David K. Shuh
发明人： Patricia W. Durbin-Heavey , Leonore Frances Heavey , Kenneth N. Raymond , Rebecca J. Abergel , David K. Shuh
IPC分类号： A61K31/444 , A61P39/04
CPC分类号： A61K31/444
摘要： The invention provides for a method for treating a subject in need of such treatment comprising administering a therapeutically effective amount of one or more pharmaceutical compositions comprising a 1,2-HOPO chelating agent and a 3,2-HOPO chelating agent to a subject in need of such treatment. The use of both 1,2-HOPO and a 3,2-HOPO chelating agents in combination is more effective than using only one chelating agent alone. The invention is especially useful when practiced on a subject that has been exposed to, have been in contact with, or contaminated by one or more known or unknown actinides and/or lanthanides, or a mixture thereof.
摘要翻译：本发明提供了治疗需要这种治疗的受试者的方法，其包括向需要治疗的受试者施用治疗有效量的包含1,2-HOPO螯合剂和3,2-HOPO螯合剂的一种或多种药物组合物的这种治疗。组合使用1,2-HOPO和3,2-HOPO螯合剂比仅使用一种螯合剂更有效。当已经暴露于已经被一种或多种已知或未知的锕系元素和/或镧系元素或其混合物暴露于，已经接触或污染的对象上时，本发明是特别有用的。

6. 发明申请

US20120214253A1 MACROCYCLIC HOPO CHELATORS 有权
标题翻译：大理石叛徒
公开(公告)号：US20120214253A1
公开(公告)日：2012-08-23
申请号：US13392506
申请日：2010-08-24
申请人： Nathaniel G. Butlin , Kenneth N. Raymond , Jide Xu , Anthony D'Aleo
发明人： Nathaniel G. Butlin , Kenneth N. Raymond , Jide Xu , Anthony D'Aleo
IPC分类号： G01N21/76 , C07F5/00 , C07D401/14 , C07D471/22
CPC分类号： G01N33/582 , C07D487/18 , C07D498/22 , G01N21/6428 , G01N33/533 , G01N2021/6432 , G01N2021/6439
摘要： The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds comprise hydroxypyridinonyl moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability.
摘要翻译：本发明提供了一类新的大环化合物以及在金属（例如镧系元素）离子和本发明的化合物之间形成的络合物。优选的配合物在水性介质中表现出高稳定性以及镧系元素离子发光的高量子产率，而不需要第二活化剂。优选的化合物在其大环结构内包含羟基吡啶基部分，其特征在于与多种多肽如抗体和蛋白质具有惊人的低，非特异性结合以及高动力学稳定性。

7. 发明申请

US20090036537A1 AROMATIC TRIAMIDE-LANTHANIDE COMPLEXES 有权
标题翻译：芳香三酰胺 - 兰那肽复合物
公开(公告)号：US20090036537A1
公开(公告)日：2009-02-05
申请号：US10585178
申请日：2004-12-29
申请人： Kenneth N. Raymond , Stephane Petoud , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Jide Xu
IPC分类号： A61K31/16 , C07C233/00 , C07H21/00 , C07H1/00 , C07K2/00 , C07K16/00 , C07K14/00 , C12N9/00 , C07F5/00 , C12Q1/00 , C12Q1/68 , C40B40/16 , C40B40/06 , C40B40/10
CPC分类号： C07C235/60 , C07B2200/11 , C07C271/20 , C07D277/16 , C12Q1/37 , G01N33/533 , G01N33/542 , G01N33/582
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.
摘要翻译：本发明提供了包含镧系元素的金属离子的发光镧系元素金属螯合物和包含至少一个邻苯二甲酰亚胺基部分的络合剂。还提供了掺入本发明的邻苯二甲酰氨基配体的探针和利用本发明配体的方法和包含本发明配体的探针。

8. 发明授权

US06846915B2 Hydroxypyridonate and hydroxypyrimidinone chelating agents 有权
公开(公告)号：US06846915B2
公开(公告)日：2005-01-25
申请号：US10194502
申请日：2002-07-12
申请人： Kenneth N. Raymond , Daniel M. J. Doble , Christopher J. Sunderland , Marlon Thompson
发明人： Kenneth N. Raymond , Daniel M. J. Doble , Christopher J. Sunderland , Marlon Thompson
IPC分类号： A61K49/00 , A61K49/08 , C07C235/60 , C07F5/00
CPC分类号： A61K49/10 , A61K49/085 , A61K49/101 , A61K49/103 , A61K49/126
摘要： The present invention provides hydroxypyridinone and hydroxypyrimidone chelating agents. Also provides are Gd(III) complexes of these agents, which are useful as contrast enhancing agents for magnetic resonance imaging. The invention also provides methods of preparing the compounds of the invention, as well as methods of using the compounds in magnetic resonance imaging applications.

9. 发明授权

US06515113B2 Phthalamide lanthanide complexes for use as luminescent markers 有权
公开(公告)号：US06515113B2
公开(公告)日：2003-02-04
申请号：US09507630
申请日：2000-02-18
申请人： Kenneth N. Raymond , Stephane Petoud , Seth M. Cohen , Jide Xu
发明人： Kenneth N. Raymond , Stephane Petoud , Seth M. Cohen , Jide Xu
IPC分类号： C07F500
CPC分类号： C12Q1/37 , A61K41/0057 , A61K49/0002 , A61K49/0019 , A61K49/103 , A61K49/106 , A61K49/122 , A61K49/124 , A61K51/0478 , A61K51/0482 , A61K51/06 , C07C235/60 , C07D487/08 , C07D487/18 , C07D487/22 , C09K11/06 , C09K2211/1007 , C09K2211/182 , G01N33/582 , G01N2458/40 , Y10S436/80 , Y10S436/804
摘要： The present invention provides luminescent lanthanide metal chelates comprising a metal ion of the lanthanide series and a complexing agent comprising at least one phthalamidyl moiety. Also provided are probes incorporating the phthalamidyl ligands of the invention and methods utilizing the ligands of the invention and probes comprising the ligands of the invention.

10. 发明授权

US5624901A 3-hydroxy-2(1H)-pyridinone chelating agents 失效
标题翻译： 3-羟基-2（1H） - 吡啶酮螯合剂
公开(公告)号：US5624901A
公开(公告)日：1997-04-29
申请号：US285640
申请日：1994-08-02
申请人： Kenneth N. Raymond , Jide Xu
发明人： Kenneth N. Raymond , Jide Xu
IPC分类号： C07D213/81 , C07D405/12 , A61K38/06 , A61K31/44 , A61K38/08 , C07D401/12
CPC分类号： C07D405/12 , C07D213/81
摘要： Disclosed is a series of improved metal chelating agents, which are highly effective upon both injection and oral administration; several of the most effective are of low toxicity. These chelating agents incorporate within their structure 1-hydroxy-2-pyridinone (1,2-HOPO) and 3-hydroxy-2-pyridinone (3,2-HOPO) moieties with a substituted carbamoyl group ortho to the hydroxy or oxo groups of the hydroxypyridinone ring. The electron-withdrawing carbamoyl group increases the acidity of the hydroxypyridinones. In the metal complexes of said chelating agents, the amide protons form very strong hydrogen bonds with its adjacent HOPO oxygen donor, making these complexes very stable at physiological conditions. The terminal N-substituents provides a certain degree of lipophilicity to said 3,2-HOPO, increasing oral activity. Also disclosed is a method of making the chelating agents and a method of producing a known compound, 3-hydroxy-1-alkyl-2(1H)pyridinone, used as a precursor to the chelating agent, safely and in large quantities.
摘要翻译：公开了一系列改进的金属螯合剂，其在注射和口服给药方面都是非常有效的; 几种最有效的是低毒性的。这些螯合剂在它们的结构内引入1-羟基-2-吡啶酮（1,2-HOPO）和3-羟基-2-吡啶酮（3,2-HOPO）部分，与羟基或氧代基邻位的取代的氨基甲酰基羟基吡啶酮环。吸电子氨基甲酰基增加羟基吡啶酮的酸度。在所述螯合剂的金属络合物中，酰胺质子与其相邻的HOPO氧供体形成非常强的氢键，使得这些复合物在生理条件下非常稳定。末端N-取代基对所述3,2-HOPO提供一定程度的亲油性，增加口服活性。还公开了以安全且大量的方式制备螯合剂的方法和用作螯合剂前体的已知化合物3-羟基-1-烷基-2（1H）吡啶酮的方法。

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