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1. 发明申请

US20110195024A1 ISATIN DERIVATIVES FOR USE AS IN VIVO IMAGING AGENTS 有权
标题翻译：用于VIVO成像剂的ISATIN衍生物
公开(公告)号：US20110195024A1
公开(公告)日：2011-08-11
申请号：US13062064
申请日：2009-09-04
申请人： Eric Ofori Aboabye , Graham Smith , Quang-De Nguyen , Erik Arstad , Matthias Eberhard Glaser
发明人： Eric Ofori Aboabye , Graham Smith , Quang-De Nguyen , Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K49/00 , C07D403/14 , C07D491/113 , A61K31/4192 , A61P43/00
CPC分类号： C07D403/12 , C07D403/14 , C07D405/14
摘要： Isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising the derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing the derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity are disclosed.
摘要翻译：靛红5-磺酰胺衍生物，包含衍生物的药物组合物，其作为分子显像剂的用途，其用于诊断或治疗与凋亡失调相关的疾病或病症的用途，合成衍生物的方法，半胱天冬酶活性的分子成像方法并且公开了细胞凋亡和评估测试物质对胱天蛋白酶活性的治疗效果的方法。

2. 发明授权

US08961930B2 Isatin derivatives for use as in vivo imaging agents 有权
标题翻译：靛红衍生物用作体内成像剂
公开(公告)号：US08961930B2
公开(公告)日：2015-02-24
申请号：US13062064
申请日：2009-09-04
申请人： Eric Ofori Aboagye , Graham Smith , Quang-De Nguyen , Erik Arstad , Matthias Eberhard Glaser
发明人： Eric Ofori Aboagye , Graham Smith , Quang-De Nguyen , Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K49/00 , C07D403/12 , C07D403/14 , C07D405/14 , A61K51/00 , A61M36/14
CPC分类号： C07D403/12 , C07D403/14 , C07D405/14
摘要： Isatin 5-sulfonamide derivatives, pharmaceutical compositions comprising the derivatives, their use as molecular imaging agents, their use for the diagnosis or treatment of diseases or disorders associated with dysregulation of apoptosis, methods for synthesizing the derivatives, methods for the molecular imaging of caspase activity and apoptosis, and methods of assessing the therapeutic effect of a test substance on caspase activity are disclosed.
摘要翻译：靛红5-磺酰胺衍生物，包含衍生物的药物组合物，其作为分子显像剂的用途，其用于诊断或治疗与凋亡失调相关的疾病或病症的用途，合成衍生物的方法，半胱天冬酶活性的分子成像方法并且公开了细胞凋亡和评估测试物质对胱天蛋白酶活性的治疗效果的方法。

3. 发明授权

US08211403B2 Radiolabelling methods 失效
标题翻译：放射性标记方法
公开(公告)号：US08211403B2
公开(公告)日：2012-07-03
申请号：US12305253
申请日：2007-06-20
申请人： Matthias Eberhard Glaser , Erik Arstad
发明人： Matthias Eberhard Glaser , Erik Arstad
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K1/1077 , A61K51/0453 , A61K51/088 , C07B59/008 , C07C17/093 , C07C45/63 , C07D261/08 , C07K1/13 , C07C21/22 , C07C47/55
摘要： The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I): with a compound of formula (II) or, a compound of formula (III): with a compound of formula (IV): in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
摘要翻译：本发明涉及放射性诊断和放射治疗剂，包括用放射性核素标记的生物活性载体。它还涉及标记载体的方法和试剂，所述载体包括式（I）化合物与式（II）化合物或式（III）化合物与式（IV）化合物的反应：）：在Cu（I）催化剂存在下。所得到的标记的缀合物可用作诊断剂，例如作为放射性药物更具体地用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）或放射治疗。

4. 发明授权

US07972588B2 Radiolabelling methods 有权
标题翻译：放射性标记方法
公开(公告)号：US07972588B2
公开(公告)日：2011-07-05
申请号：US11721694
申请日：2005-12-09
申请人： Erik Arstad , Matthias Eberhard Glaser
发明人： Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/088 , A61K51/082 , A61K51/1051
摘要： The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N3 (II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
摘要翻译：本发明涉及放射性诊断和放射治疗剂，包括用放射性核素标记的生物活性载体。它还涉及标记载体的方法和试剂，例如肽，其包括式（I）化合物与式（II）化合物的反应：R * -L2-N3（II）或式（III）化合物）与式（IV）的化合物在Cu（I）催化剂的存在下反应。所得到的标记的缀合物可用作诊断剂，例如作为放射性药物更具体地用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）或放射治疗。

5. 发明授权

US08795631B2 Radiofluorination 有权
标题翻译：放射性氟化
公开(公告)号：US08795631B2
公开(公告)日：2014-08-05
申请号：US13119468
申请日：2009-10-20
申请人： Robert James Domett Nairne , Erik Arstad , Matthias Eberhard Glaser
发明人： Robert James Domett Nairne , Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07B59/001
摘要： The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.
摘要翻译：本发明涉及18F放射化学，特别涉及一种合成放射性氟化酰胺和胺的方法。本发明的方法在各种18F标记的正电子发射断层扫描（PET）示踪剂的放射合成中具有特别的应用。

6. 发明授权

US08071718B2 Selective radiolabeling of biomolecules 有权
标题翻译：生物分子的选择性放射标记
公开(公告)号：US08071718B2
公开(公告)日：2011-12-06
申请号：US11961108
申请日：2007-12-20
申请人： Omayra Liz Padilla De Jesus , Ernest William Kovacs , Matthias Eberhard Glaser , Erik Arstad , Faisal Ahmed Syud
发明人： Omayra Liz Padilla De Jesus , Ernest William Kovacs , Matthias Eberhard Glaser , Erik Arstad , Faisal Ahmed Syud
IPC分类号： A61K38/00 , A61K51/00
CPC分类号： A61K51/088 , A61K51/1051
摘要： Provided herein are methods for introducing fluorine atom onto a biomolecule comprising: (i) providing a linker comprising a thiol-reactive terminus and an azido/alkyne-reactive terminus; (ii) reacting the thiol-reactive terminus of the linker with a biomolecule comprising at least one thiol group or a reactive derivative thereof; and (iii) subsequently reacting the azido/alkyne-reactive terminus of the linker with a fluorine-substituted azide or alkyne respectively. Also provided are compositions and method of synthesis of bifunctional linkers and bioconjugates as well as radio-diagnostic agents comprising fluorine-labeled biomolecules.
摘要翻译：本文提供将氟原子引入到生物分子上的方法，包括：（i）提供包含硫醇反应性末端和叠氮基/炔反应性末端的连接体; （ii）使连接体的硫醇反应性末端与包含至少一个硫醇基或其活性衍生物的生物分子反应; 和（iii）随后使接头的叠氮基/炔反应性末端分别与氟取代的叠氮化物或炔反应。还提供了双官能接头和生物缀合物的组合物和合成方法以及包含氟标记的生物分子的放射诊断剂。

7. 发明申请

US20090087379A1 Radiofluorinated Compounds and their Preparation 失效
标题翻译：放射性氟化合物及其制备方法
公开(公告)号：US20090087379A1
公开(公告)日：2009-04-02
申请号：US12297347
申请日：2007-04-20
申请人： Erik Arstad , Matthias Eberhard Glaser
发明人： Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K51/04 , C07C335/02 , C07C331/16 , C07D205/04 , C07C215/02
CPC分类号： A61K51/087 , A61K51/088 , C07B59/008 , C07C215/08 , C07C215/14 , C07C271/28 , C07C331/28 , C07D205/04 , C07K1/13 , C07K14/47
摘要： The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
摘要翻译：本发明提供了含有伯氨基的生物分子如蛋白质和肽，特别是肽的[18 F] - 氟化方法。本发明还提供用于该方法的试剂，特别是用于制备的18F标记的假基团以及可用于制备[18 F] - 标记的假体基团的未标记的中间体。也可用作用作放射性药物的[18F]标记化合物，专门用于正电子发射断层扫描（PET）。

8. 发明授权

US08148575B2 Radiofluorinated compounds and their preparation 失效
标题翻译：放射性氟化合物及其制备方法
公开(公告)号：US08148575B2
公开(公告)日：2012-04-03
申请号：US12297347
申请日：2007-04-20
申请人： Erik Arstad , Matthias Eberhard Glaser
发明人： Erik Arstad , Matthias Eberhard Glaser
IPC分类号： C07C337/00
CPC分类号： A61K51/087 , A61K51/088 , C07B59/008 , C07C215/08 , C07C215/14 , C07C271/28 , C07C331/28 , C07D205/04 , C07K1/13 , C07K14/47
摘要： The present invention provides a process for [18F]-fluorination of biomolecules containing a primary amino group such as proteins and peptides and in particular of peptides. The invention further provides reagents for this process, in particular 18F-labelled prosthetic groups for use in the preparation as well as non-labelled intermediates useful in the preparation of the [18F]-labelled prosthetic groups. [18F]-labelled compounds useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET) are also provided.
摘要翻译：本发明提供了含有伯氨基的生物分子如蛋白质和肽，特别是肽的[18 F] - 氟化方法。本发明还提供用于该方法的试剂，特别是用于制备的18F标记的假基团以及可用于制备[18 F] - 标记的假体基团的未标记的中间体。也可用作用作放射性药物的[18F]标记化合物，专门用于正电子发射断层扫描（PET）。

9. 发明申请

US20110189089A1 RADIOFLUORINATION 有权
标题翻译：无线电辐射
公开(公告)号：US20110189089A1
公开(公告)日：2011-08-04
申请号：US13119468
申请日：2009-10-20
申请人： Robert James Domett Nairne , Erik Arstad , Matthias Eberhard Glaser
发明人： Robert James Domett Nairne , Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K51/04 , C07C209/42 , C07D471/04 , C07C231/02 , B01J19/00
CPC分类号： C07B59/001
摘要： The present invention relates to 18F radio-chemistry and in particular to a method for synthesising radiofluorinated amides and amines. The method of the invention has particular application in the radiosynthesis of a variety of 18F-labelled positron emission tomography (PET) tracers.
摘要翻译：本发明涉及18F放射化学，特别涉及一种合成放射性氟化酰胺和胺的方法。本发明的方法在各种18F标记的正电子发射断层扫描（PET）示踪剂的放射合成中具有特别的应用。

10. 发明申请

US20090311177A1 Radiolabelling Methods 有权
标题翻译：放射性标记方法
公开(公告)号：US20090311177A1
公开(公告)日：2009-12-17
申请号：US11721694
申请日：2005-12-09
申请人： Erik Arstad , Matthias Eberhard Glaser
发明人： Erik Arstad , Matthias Eberhard Glaser
IPC分类号： A61K51/08 , C07K1/13 , C07C247/02 , C07C19/08 , C07K2/00 , C07K5/08 , C07K7/64
CPC分类号： A61K51/088 , A61K51/082 , A61K51/1051
摘要： The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods and reagents labelling a vector such as a peptide comprising reaction of a compound of formula (I) with a compound of formula (II): R*-L2-N3 (II) or, a compound of formula (III) with a compound of formula (IV) in the presence of a Cu (I) catalyst. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.
摘要翻译：本发明涉及放射性诊断和放射治疗剂，包括用放射性核素标记的生物活性载体。它还涉及标记载体的方法和试剂，例如肽，其包括式（I）化合物与式（II）化合物的反应：R * -L2-N3（II）或式（III）化合物）与式（IV）的化合物在Cu（I）催化剂的存在下反应。所得到的标记的缀合物可用作诊断剂，例如作为放射性药物更具体地用于正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）或放射治疗。

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