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1. 发明授权

US08946410B2 Automated radiosynthesis 有权
标题翻译：自动放射合成
公开(公告)号：US08946410B2
公开(公告)日：2015-02-03
申请号：US13394655
申请日：2010-10-08
申请人： John Woodcraft , L Clare Jones , Alessandra Gaeta , John William Trigg , Alexander Paul Jones , Stuart Plant , Alexander Jackson
发明人： John Woodcraft , L Clare Jones , Alessandra Gaeta , John William Trigg , Alexander Paul Jones , Stuart Plant , Alexander Jackson
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlab™. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.
摘要翻译：本发明提供了获得用于体内成像GABA A受体的放射性氟化化合物的方法。本发明的方法是高产量的，并且可以方便地在诸如Fastlab TM的自动合成仪上进行。本发明的另一方面是适用于实施本发明的自动合成方法的盒。还提供了可用于本发明方法的新型前体化合物，以及通过本发明的方法获得的多种新型化合物。

2. 发明申请

US20120190843A1 AUTOMATED RADIOSYNTHESIS 有权
标题翻译：自动放射治疗
公开(公告)号：US20120190843A1
公开(公告)日：2012-07-26
申请号：US13394655
申请日：2010-10-08
申请人： John Woodcraft , L. Clare Jones , Alessandra Gaeta , John William Trigg , Alexander Paul Jones , Stuart Plant , Alexander Jackson
发明人： John Woodcraft , L. Clare Jones , Alessandra Gaeta , John William Trigg , Alexander Paul Jones , Stuart Plant , Alexander Jackson
IPC分类号： C07D487/04 , B01L3/00
CPC分类号： C07D487/04
摘要： The present invention provides a method to obtain radiofluorinated compounds useful for in vivo imaging GABAA receptors. The method of the invention is high-yielding and may conveniently be carried out on an automated synthesizer such as Fastlab™. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention. Novel precursor compounds useful in the method of the invention are also provided, as are a number of novel compounds obtained by the method of the invention.
摘要翻译：本发明提供了获得用于体内成像GABA A受体的放射性氟化化合物的方法。本发明的方法是高产量的，并且可以方便地在诸如Fastlab TM的自动合成仪上进行。本发明的另一方面是适用于实施本发明的自动合成方法的盒。还提供了可用于本发明方法的新型前体化合物，以及通过本发明的方法获得的多种新型化合物。

3. 发明申请

US20120189547A1 [18F] LABELLED ANALOGUES OF FLUMAZENIL AS IN VIVO IMAGING AGENTS 审中-公开
标题翻译： [18F]维生素成像剂中氟马西林的标记类似物
公开(公告)号：US20120189547A1
公开(公告)日：2012-07-26
申请号：US13394639
申请日：2010-10-08
申请人： John Woodcraft , Clare L. Jones , Alessandra Gaeta , William John Trigg , Paul Alexander Jones , Stuart Plant
发明人： John Woodcraft , Clare L. Jones , Alessandra Gaeta , William John Trigg , Paul Alexander Jones , Stuart Plant
IPC分类号： A61K51/04 , B01J19/00 , C07D487/02
CPC分类号： C07D487/04 , A61K51/047
摘要： The present invention provides radiofluorinated compounds useful for in vivo imaging GABAA receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.
摘要翻译：本发明提供了可用于体内成像GABA A受体的放射性氟化化合物。本发明还提供了本发明的放射性氟化合物的合成方法，特别是一种自动合成方法。本发明的另一方面是适用于实施本发明的自动合成方法的盒。

4. 发明申请

US20110129419A1 IN VIVO IMAGING AGENTS 审中-公开
标题翻译：在VIVO成像代理
公开(公告)号：US20110129419A1
公开(公告)日：2011-06-02
申请号：US12519398
申请日：2007-12-19
申请人： Anthony Eamon Storey , Julie Davis , Erik Arstad , Benedicte Guilbert , Alessandra Gaeta
发明人： Anthony Eamon Storey , Julie Davis , Erik Arstad , Benedicte Guilbert , Alessandra Gaeta
IPC分类号： A61K51/04 , C07C235/56 , C07D401/12 , C07D401/04 , C07D211/58 , C07D405/12 , C07D211/48 , C07D471/10
CPC分类号： A61K51/0406 , A61K51/04 , A61K51/0455 , C07B59/002 , C07B2200/05 , C07C235/56 , C07D211/62 , C07D401/04 , C07D401/14 , C07D405/12 , C07D471/10
摘要： The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
摘要翻译：本发明涉及医学成像领域，特别涉及与趋化因子受体5（CCR5）的上调相关的疾病状态的成像。提供了成像剂，前体和方法，其可用于成像这样的疾病状态。

5. 发明申请

US20130236395A1 HETEROCYCLIC COMPOUNDS AS IMAGING PROBES OF TAU PATHOLOGY 有权
标题翻译：杂环化合物作为TAU病理学的成像探针
公开(公告)号：US20130236395A1
公开(公告)日：2013-09-12
申请号：US13885466
申请日：2011-11-07
申请人： Clare Jones , Amanda Ewan , Duncan Wynn , Alessandra Gaeta , James Nairne
发明人： Clare Jones , Amanda Ewan , Duncan Wynn , Alessandra Gaeta , James Nairne
IPC分类号： A61K51/04
CPC分类号： A61K51/0455 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/36 , C07D295/067 , C07D401/04 , C07D401/12
摘要： Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
摘要翻译：描述了用作阿尔茨海默氏病Tau病理学成像探针的式（I）的杂环化合物。还描述了制备这种化合物的组合物和方法。

6. 发明授权

US09040021B2 Heterocyclic compounds as imaging probes of tau pathology 有权
标题翻译：杂环化合物作为tau病理学的成像探针
公开(公告)号：US09040021B2
公开(公告)日：2015-05-26
申请号：US13885466
申请日：2011-11-07
申请人： Clare Jones , Amanda Ewan , Duncan Wynn , Alessandra Gaeta , James Nairne
发明人： Clare Jones , Amanda Ewan , Duncan Wynn , Alessandra Gaeta , James Nairne
IPC分类号： A61K51/00 , A61M36/14 , A61K51/04 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/36 , C07D295/067 , C07D401/04 , C07D401/12
CPC分类号： A61K51/0455 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/36 , C07D295/067 , C07D401/04 , C07D401/12
摘要： Heterocyclic compounds of formula (I) useful as imaging probes of Tau pathology in Alzheimer's disease are described. Compositions and methods of making such compounds are also described.
摘要翻译：描述了用作阿尔茨海默氏病Tau病理学成像探针的式（I）的杂环化合物。还描述了制备这种化合物的组合物和方法。

7. 发明申请

US20080200520A1 Iron Modulators 审中-公开
标题翻译：铁调制器
公开(公告)号：US20080200520A1
公开(公告)日：2008-08-21
申请号：US11886879
申请日：2006-03-31
申请人： Robert Charles Hider , Alessandra Gaeta , Zu Dong Liu
发明人： Robert Charles Hider , Alessandra Gaeta , Zu Dong Liu
IPC分类号： A61K31/4412 , C07D213/24 , A61P25/00
CPC分类号： C07D213/81
摘要： Iron modulator compounds of formula (I) are provided for treating amyloidoses wherein R1 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl, R2 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl and C6-10 aralykyl in which the aryl group of the aralkyl group is optionally substituted by hydroxy, halo or C1-4 alkyl R3 is selected from H, C1-6 alkyl, C1-6 alkenyl and C1-12 acyl; R4 is selected from H and C1-3 alkyl R5, R6 and R7 are independently selected from H, C1-6 alkyl, C3-7 aryl, and C1-10 aralkyl; the alkyl, aryl and aralkyl groups being optionally substituted by one or more halo, hydroxy and nitro groups or R5 and R7 together with the nitrogen atom to which they are bonded form a heterocyclic ring optionally substituted by one or more hydroxyl groups or a pharmaceutically acceptable tautomer, ester or addition salt thereof.
摘要翻译：提供式（I）的铁调节剂化合物用于治疗淀粉样变性，其中R 1选自H，C 1-6烷基，C 1-6 - 亚烷基，C 1-6 - 羟基烷基，C 1-6 - 羟基烯基，R 2选自H，C 1〜 C 1-6烷基，C 1-6链烯基，C 1-6 1-6羟基烷基，C 1-6 1-6羟基烯基和C 1 -C 6 - 芳烷基的芳基任选被羟基，卤代或C 1-4烷基取代的6-10芳烷基R 3选自H，C 1-6 C 1-6烷基，C 1-6 - 烯基和C 1-12酰基; R 4选自H和C 1-3烷基R 5，R 6和R 6， 7个独立地选自H，C 1-6烷基，C 3-7芳基和C 1-10烷基 ; 烷基，芳基和芳烷基任选被一个或多个卤素，羟基和硝基或R 5和R 7与它们所键合的氮原子一起取代形成任选被一个或多个羟基取代的杂环或其药学上可接受的互变异构体，酯或其加成盐。

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