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1. 发明申请

US20080207523A1 COMPOUNDS AS APTAMER-DIMERS AND THEIR USES IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译：化合物作为APTAMER-DIMERS及其在诊断和治疗中的用途
公开(公告)号：US20080207523A1
公开(公告)日：2008-08-28
申请号：US11851789
申请日：2007-09-07
申请人： Matthias Friebe , Andrew Stephens , Ananth Srinivasan , Maren Hecht
发明人： Matthias Friebe , Andrew Stephens , Ananth Srinivasan , Maren Hecht
IPC分类号： A61K38/08 , C07K7/06 , A61P35/00 , C07K1/00
CPC分类号： C07K14/001 , A61K38/00 , A61K47/65 , A61K51/088 , C07K7/02
摘要： The object of the present invention is solved by compositions of peptide linkers and their use for synthesis and annealing of aptamer oligonucleotides in form of dimers. The present invention in particularly provides said compositions for the use as a diagnostic and/or therapeutic agent.In another preferred embodiment the present invention relates to a kit for preparing a radiopharmaceutical preparation, said kit comprising a vial comprising a quantity of the compound according to the invention.A further preferred embodiment of the present invention relates to methods of producing said compounds, comprising synthesis of said compound in an automated peptide synthesizer.In another preferred embodiment the present invention concerns the use of said compounds according to the present invention for the manufacture of a medicament, preferably for diagnosis or therapy of proliferative diseases.In a further preferred embodiment the present invention concerns methods for treating or diagnosing patients administering or utilizing the compounds according to the present invention.
摘要翻译：本发明的目的是通过肽接头的组合物及其用于以二聚体的形式合成和退火适体寡核苷酸的用途来解决的。本发明特别提供了用作诊断和/或治疗剂的所述组合物。在另一个优选的实施方案中，本发明涉及一种用于制备放射性药物制剂的试剂盒，所述试剂盒包含一定量的包含本发明化合物的小瓶。本发明的另一优选实施方案涉及生产所述化合物的方法，包括在自动肽合成仪中合成所述化合物。在另一个优选的实施方案中，本发明涉及根据本发明的所述化合物在制备药物中的用途，优选用于诊断或治疗增殖性疾病。在另一优选实施方案中，本发明涉及用于治疗或诊断施用或使用本发明化合物的患者的方法。

2. 发明申请

US20090068103A1 APTAMERS LABELED WITH 68GA 审中-公开
标题翻译：标配68GA的APTAMERS
公开(公告)号：US20090068103A1
公开(公告)日：2009-03-12
申请号：US11851807
申请日：2007-09-07
申请人： Ludger Dinkelborg , Matthias Friebe , Maren Hecht , Lutz Lehmann , Bernhard Noll
发明人： Ludger Dinkelborg , Matthias Friebe , Maren Hecht , Lutz Lehmann , Bernhard Noll
IPC分类号： A61K51/08 , C07K7/06 , C07D257/00 , C07H21/02 , C07H21/04 , A61K51/04 , A61K38/14 , A61K31/711 , C07F19/00
CPC分类号： C12N15/115 , A61K51/0491 , C12N2310/16 , C12N2310/3517
摘要： This invention relates to novel nucleotide-based compounds, methods of making radiolabeled compounds and use of such compounds for diagnostic imaging. Provided are compounds according to Formula (I) A-B-L-C, wherein A stands for an aptamer, B is absent or stands for a bridging structure, L is a linker, and C is a metal ion chelator. All substituents are defined in detail in the description. Preferred embodiments of said compounds bind to Tenascin-C.
摘要翻译：本发明涉及新的基于核苷酸的化合物，制备放射性标记的化合物的方法和用于诊断成像的这些化合物的用途。提供根据式（I）的化合物A-B-L-C，其中A代表适体，B不存在或代表桥连结构，L是连接体，C是金属离子螯合剂。所有取代基在说明书中详细定义。所述化合物的优选实施方案结合腱生蛋白-C。

3. 发明申请

US20110137063A1 COMPOUNDS AND PROCESSES FOR PRODUCTION OF RADIOPHARMACEUTICALS 审中-公开
标题翻译：化合物和生产无机物的方法
公开(公告)号：US20110137063A1
公开(公告)日：2011-06-09
申请号：US13002123
申请日：2009-06-24
申请人： Ananth Srinivasan , Mathias Berndt , Keith Graham , Matthias Friebe , Heribert Schmitt-Willich
发明人： Ananth Srinivasan , Mathias Berndt , Keith Graham , Matthias Friebe , Heribert Schmitt-Willich
IPC分类号： C07C309/77 , C07C309/80 , C07C309/86 , C07C309/68 , C07C309/76 , C07C209/74 , C07C227/18 , C07C209/84 , C07C227/40
CPC分类号： C07B59/00 , C07B2200/05 , C07C309/65 , C07C309/73
摘要： The present invention relates to novel perfluorinated precursors for the production of F-18 labeled radiotracers for Positron Emission Tomography (PET) and processes for radiolabeling and purification using these precursors. The invention also comprises radiopharmaceutical kits using these precursors and processes.
摘要翻译：本发明涉及用于生产用于正电子发射断层扫描（PET）的F-18标记放射性示踪剂的新型全氟化前体和使用这些前体的放射性标记和纯化的方法。本发明还包括使用这些前体和方法的放射性药物试剂盒。

4. 发明申请

US20130209363A1 METHOD FOR PRODUCTION OF F-18 LABELED AMYLOID BETA LIGANDS 审中-公开
公开(公告)号：US20130209363A1
公开(公告)日：2013-08-15
申请号：US13702007
申请日：2011-05-30
申请人： Mathias Berndt , Matthias Friebe , Fabrice Samson , Rainer Braun , Gunnar Garke , Marianne PATT , Andreas Schildan , Christoph Smuda
发明人： Mathias Berndt , Matthias Friebe , Fabrice Samson , Rainer Braun , Gunnar Garke , Marianne PATT , Andreas Schildan , Christoph Smuda
IPC分类号： A61K51/04
CPC分类号： A61K51/04 , A61K51/0455 , A61K51/121 , C07B59/00 , C07B2200/05 , C07C213/08 , C07C217/80
摘要： This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.

5. 发明授权

US08491906B2 Selective targeting of tumor vasculature using antibody molecules 有权
标题翻译：使用抗体分子选择性靶向肿瘤脉管系统
公开(公告)号：US08491906B2
公开(公告)日：2013-07-23
申请号：US10507178
申请日：2003-03-11
申请人： Laura Borsi , Barbara Carnemolla , Enrica Balza , Patrizia Castellani , Luciano Zardi , Matthias Friebe , Christoph-Stephan Hilger
发明人： Laura Borsi , Barbara Carnemolla , Enrica Balza , Patrizia Castellani , Luciano Zardi , Matthias Friebe , Christoph-Stephan Hilger
IPC分类号： A61K39/395 , C07K16/30
CPC分类号： A61K51/1018 , C07K16/18 , C07K2317/21 , C07K2317/52 , C07K2317/565 , C07K2317/622 , C07K2319/00
摘要： The present invention relates to selectively targeting tumoral vasculature in vivo using a human recombinant scFv, L19, to the angiogenesis marker ED-B domain of fibronectin. In preferred embodiments, a complete human IgG1 is employed having the variable regions of L19. In other preferred embodiments is employed a mini-immunoglobulin generated by fusing the scFv L19 to the constant CH4 domain of a secretory IgE isoform that naturally contains a cysteine in its COOH terminal and which forms a covalently linked dimer. Different in vivo behavior of the antibody formats is exploitable for different diagnostic and/or therapeutic purposes, depending on clinical needs and disease. The antibody molecules may be labelled as described.
摘要翻译：本发明涉及使用人重组scFv L19向体内血管生成标记ED-B结构域选择性靶向肿瘤脉管系统。在优选的实施方案中，使用具有L19可变区的完整人IgG1。在其它优选实施方案中，使用通过将scFv L19融合到其COOH末端中天然含有半胱氨酸且形成共价连接的二聚体的分泌型IgE同种型的恒定CH4结构域产生的微型免疫球蛋白。根据临床需要和疾病，抗体形式的不同体内行为可用于不同的诊断和/或治疗目的。抗体分子可以如所述标记。

6. 发明申请

US20110064673A1 New L-Glutamic acid and L-Glutamine derivative (III), use thereof and method for obtaining them 审中-公开
标题翻译：新的L-谷氨酸和L-谷氨酰胺衍生物（III），其用途及其获得方法
公开(公告)号：US20110064673A1
公开(公告)日：2011-03-17
申请号：US12992956
申请日：2009-05-14
申请人： Ludger Dinkelborg , Heribert Schmitt-Willich , Keith Graham , Norman Koglin , Mathias Berndt , Matthias Friebe , Andre Muller
发明人： Ludger Dinkelborg , Heribert Schmitt-Willich , Keith Graham , Norman Koglin , Mathias Berndt , Matthias Friebe , Andre Muller
IPC分类号： A61K49/10 , C07C229/24 , A61K31/198 , A61P35/00 , A61P35/02 , C07C229/36
CPC分类号： C07C227/16 , A61K49/10 , C07B59/001 , C07B2200/05 , C07C229/24 , C07C229/36 , C07C237/06 , C07C2601/04
摘要： The present invention relates to fluorinated glutamic acid (glutamate) and glutamine derivatives wherein the fluorine atom is 19F. The glutamic acid (glutamate) and glutamine derivatives are compound(s) of general Formula I, which encompasses all possible diastereoisomers and/or enantiomere derivatives or mixtures thereof.
摘要翻译：本发明涉及氟代谷氨酸（谷氨酸）和谷氨酰胺衍生物，其中氟原子是19F。谷氨酸（谷氨酸）和谷氨酰胺衍生物是通式I的化合物，其包括所有可能的非对映异构体和/或对映体衍生物或其混合物。

7. 发明申请

US20100217011A1 [F-18]-LABELED L-GLUTAMIC ACID, [F-18]-LABELED L-GLUTAMINE, DERIVATIVES THEREOF AND USE THEREOF AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译： [F-18] -L-氨基酸，[F-18] -L-谷氨酰胺，其衍生物及其用途及其制备方法
公开(公告)号：US20100217011A1
公开(公告)日：2010-08-26
申请号：US12513112
申请日：2007-10-30
申请人： Ludger Dinkelborg , Matthias Friebe , Nikolaevna Raisa Krasikowa , Yuri Belokon , Fedorovna Olga Kuznetsova , Keith Graham , Lutz Lehmann , Mathias Berndt
发明人： Ludger Dinkelborg , Matthias Friebe , Nikolaevna Raisa Krasikowa , Yuri Belokon , Fedorovna Olga Kuznetsova , Keith Graham , Lutz Lehmann , Mathias Berndt
IPC分类号： C07F15/04 , C07D207/24 , C07D207/16 , C07C229/24 , C07C227/16
CPC分类号： A61K51/0402 , C07B59/001 , C07B2200/05 , C07C227/16 , C07C229/24 , C07C251/24 , C07C271/22 , C07C309/66 , C07C309/73 , C07D207/16 , C07D207/26 , C07D207/28 , C07F15/045
摘要： The compounds and the synthesis of [F-18]-labeled L-glutamic acid, [F-18]-labeled L-glutamate, their derivatives as set forth in formula (I) and their uses are described.
摘要翻译：描述了[F-18]标记的L-谷氨酸[F-18] - 标记的L-谷氨酸酯，式（I）所示的衍生物及其用途的化合物和合成。

8. 发明授权

US09017645B2 Homoglutamic acid derivatives 有权
标题翻译：谷氨酸衍生物
公开(公告)号：US09017645B2
公开(公告)日：2015-04-28
申请号：US13509062
申请日：2010-11-08
申请人： Heribert Schmitt-Willich , Niels Böhnke , Norman Koglin , Andre Müller , Mathias Berndt , Matthias Friebe , Lutz Lehmann
发明人： Heribert Schmitt-Willich , Niels Böhnke , Norman Koglin , Andre Müller , Mathias Berndt , Matthias Friebe , Lutz Lehmann
IPC分类号： A61B5/055 , C07C271/22 , A61K49/10 , A61K51/04 , C07B59/00 , C07C229/24 , C07C229/30 , C07C255/58
CPC分类号： C07C271/22 , A61K49/10 , A61K51/04 , A61K51/0402 , C07B59/001 , C07B2200/05 , C07C229/24 , C07C229/30 , C07C255/58
摘要： This invention relates to homoglutamic acid derivatives suitable for labeling or already labeled with 18F or 19F, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.
摘要翻译：本发明涉及适用于标记或已经用18F或19F标记的高谷氨酸衍生物，制备此类化合物的方法，包含这些化合物的组合物，包含这些化合物或组合物的试剂盒以及用于诊断成像的这些化合物，组合物或试剂盒的用途。

9. 发明申请

US20140243532A1 NOVEL PRECURSORS OF GLUTAMATE DERIVATIVES 有权
标题翻译：谷氨酸衍生物的新前辈
公开(公告)号：US20140243532A1
公开(公告)日：2014-08-28
申请号：US14115127
申请日：2012-04-30
申请人： Christina Hultsch , Michael Harre , Filip Novak , Mathias Berndt , Matthias Friebe , Heribert Schmitt-Willich , Dae Yoon Chi , Byoung Se Lee , Sang Don Park
发明人： Christina Hultsch , Michael Harre , Filip Novak , Mathias Berndt , Matthias Friebe , Heribert Schmitt-Willich , Dae Yoon Chi , Byoung Se Lee , Sang Don Park
IPC分类号： C07C309/77 , C07C229/36 , C07D215/36 , C07C303/28
CPC分类号： C07C309/77 , C07B59/001 , C07B2200/05 , C07C227/16 , C07C227/18 , C07C229/24 , C07C229/36 , C07C303/28 , C07C309/73 , C07C309/74 , C07D215/36
摘要： This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.
摘要翻译：本发明涉及适用于18F放射性标记谷氨酸衍生物的新型前体，制备此类化合物的方法及其中间体，包含此类化合物的组合物，包含此类化合物的组合物或组合物以及用于18 F放射性标记谷氨酸衍生物的方法，其中所获得的18 F放射性标记的谷氨酸衍生物为适用于正电子发射断层扫描（PET）的增殖性疾病的诊断成像，例如哺乳动物肿瘤。

10. 发明申请

US20110243846A1 BENZOTHIAZOLE AMIDES FOR DETECTION OF AMYLOID BETA 审中-公开
标题翻译：用于检测AMYLOID BETA的苯并咪唑类
公开(公告)号：US20110243846A1
公开(公告)日：2011-10-06
申请号：US13139116
申请日：2009-11-28
申请人： Jorma Hassfeld , Ulrike Roehn , Matthias Friebe , Lutz Lehmann , Tobias Heinrich , Sabine Krause , Damian Brockschnieder , Thomas Dyrks , Andrea Thiele , Ulf Boemer , Ursula Moenning , Markus Berger , Stephan Siegel
发明人： Jorma Hassfeld , Ulrike Roehn , Matthias Friebe , Lutz Lehmann , Tobias Heinrich , Sabine Krause , Damian Brockschnieder , Thomas Dyrks , Andrea Thiele , Ulf Boemer , Ursula Moenning , Markus Berger , Stephan Siegel
IPC分类号： A61K51/04 , C07D277/82 , C07F7/22 , C07F5/02 , C07D417/12 , A61P43/00
CPC分类号： C07D277/82 , C07D417/12
摘要： This invention relates to compounds (benzothiazoles) suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.
摘要翻译：本发明涉及适用于标记或已经由18F标记的化合物（苯并噻唑），制备这种化合物的方法，包含这些化合物的组合物，包含这些化合物或组合物的试剂盒以及用于诊断成像的这些化合物，组合物或试剂盒的用途。

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