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1. 发明申请

US20140275199A1 SUBSTITUTED 3-(BIPHENYL-3-YL)-4-HYDROXY-8-METHOXY-1-AZASPIRO[4.5]DEC-3-EN-2-ONE 有权
标题翻译：取代的3-（联苯-3-基）-4-羟基-8-甲氧基-1-氮杂[4.5] DEC-3-EN-2-ONE
公开(公告)号：US20140275199A1
公开(公告)日：2014-09-18
申请号：US14236279
申请日：2012-07-31
申请人： Ningshu Liu , Kai Thede , Ursula Mönning , Arne Scholz , Christoph-Stephan Hilger , Ulf Bömer , Reiner Fischer
发明人： Ningshu Liu , Kai Thede , Ursula Mönning , Arne Scholz , Christoph-Stephan Hilger , Ulf Bömer , Reiner Fischer
IPC分类号： C07D209/54 , A61K31/403
CPC分类号： C07D209/54 , A61K31/403
摘要： The invention relates to substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-ones, in particular for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of neoplastic disorders.
摘要翻译：本发明涉及取代的3-（联苯-3-基）-4-羟基-8-甲氧基-1-氮杂螺[4.5]癸-3-烯-2-酮，特别是用于治疗目的，用于药物组合物，它们在治疗中的用途，特别是用于预防和治疗肿瘤性疾病。

2. 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。

3. 发明申请

US20100129293A1 Near Infrared Imaging Agent 审中-公开
标题翻译：近红外成像剂
公开(公告)号：US20100129293A1
公开(公告)日：2010-05-27
申请号：US12693749
申请日：2010-01-26
申请人： Kai Licha , Bjórn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
发明人： Kai Licha , Bjórn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
IPC分类号： A61K49/00 , C07D403/02
CPC分类号： A61K49/0032 , A61K49/0017 , A61K49/0021 , A61K49/005 , C09B23/086 , C09B69/105
摘要： This invention relates to an in-vivo diagnostic method based on near infrared radiation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.
摘要翻译：本发明涉及一种基于近红外辐射（NIR辐射）的体内诊断方法，其使用水溶性染料及其生物分子加合物，其具有特定的光物理和药物化学性质，作为荧光和透照诊断的造影剂 NIR范围，新染料和含有这些染料的药物。

4. 发明申请

US20060165599A1 Near infrared imaging agent 失效
公开(公告)号：US20060165599A1
公开(公告)日：2006-07-27
申请号：US11387367
申请日：2006-03-22
申请人： Kai Licha , Bjorn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
发明人： Kai Licha , Bjorn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
IPC分类号： A61K49/00
CPC分类号： A61K49/0032 , A61K49/0017 , A61K49/0021 , A61K49/005 , C09B23/086 , C09B69/105
摘要： This invention relates to an in-vivo diagnostic method based on near infrared radiation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.

5. 发明授权

US06342201B1 Complex compounds for diagnosis of vascular diseases 失效
标题翻译：用于诊断血管疾病的复合物
公开(公告)号：US06342201B1
公开(公告)日：2002-01-29
申请号：US08765953
申请日：1997-07-17
申请人： Ludger Dinkelborg , Christoph Stephan Hilger , Wolfhard Semmler , Ulrich Speck , Peter Henklein
发明人： Ludger Dinkelborg , Christoph Stephan Hilger , Wolfhard Semmler , Ulrich Speck , Peter Henklein
IPC分类号： A61K5100
CPC分类号： C07K14/57536 , A61K51/088
摘要： The present invention concerns novel complexes for use in the diagnosis of vascular diseases, methods of manufacturing such complexes and diagnostic agents containing them. These complexes strongly enrich themselves in atherosclerotic plaques and are thus suitable for use in non-invasive procedures for diagnosing atherosclerosis.
摘要翻译：本发明涉及用于诊断血管疾病的新型配合物，制造这种复合物的方法和含有它们的诊断剂。这些复合物在动脉粥样硬化斑块中强烈丰富，因此适用于诊断动脉粥样硬化的非侵入性手术。

6. 发明授权

US06258340B1 In-vivo diagnostic method by near infrared radiation 有权
标题翻译：近红外辐射的体内诊断方法
公开(公告)号：US06258340B1
公开(公告)日：2001-07-10
申请号：US09518947
申请日：2000-03-06
申请人： Kai Licha , Björn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
发明人： Kai Licha , Björn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
IPC分类号： A61B1000
CPC分类号： A61K49/0032 , A61K49/0017 , A61K49/0021 , A61K49/005 , C09B23/086 , C09B69/105
摘要： This invention relates to a in-vivo diagnostic method based on near infrared ra ation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.
摘要翻译：本发明涉及一种使用水溶性染料及其生物分子加合物的近红外辐射（NIR辐射）的体内诊断方法，其具有特定的光物理和药物化学性质，作为用于荧光和透照诊断的造影剂 NIR范围，新染料和含有这些染料的药物。

7. 发明授权

US5961954A Chealators of type XN.sub.1 S.sub.1 X.sup.1 for radioactive isotopes, their metal complexes and their diagnostic and therapeutical uses 失效
标题翻译： XN1S1X1型的放射性同位素，它们的金属络合物及其诊断和治疗用途的耳尖
公开(公告)号：US5961954A
公开(公告)日：1999-10-05
申请号：US530326
申请日：1996-12-09
申请人： Christoph-Stephan Hilger , Ludger Dinkelborg , Wolfgang Kramp , Hans-Martin Schier
发明人： Christoph-Stephan Hilger , Ludger Dinkelborg , Wolfgang Kramp , Hans-Martin Schier
IPC分类号： A61K51/00 , A61K38/00 , A61K49/00 , A61K51/04 , A61K51/08 , C07C323/59 , C07C323/60 , C07F13/00 , C07K14/52 , C07K14/575 , C07C319/00 , C07D5/00
CPC分类号： C07K14/57536 , A61K51/0478 , A61K51/088 , C07C323/59 , C07C323/60 , C07F13/005 , A61K38/00
摘要： This invention relates to new bifunctional chelating agents with intermittent chalcogen atoms, pharmaceuticals containing these compounds, their use in radiodiagnostics and radiotherapy, and methods for the production of these compounds.The compound according to the invention has the general formula (I)M--Lwhere M represents a radionuclide and L a ligand of the general formula (II).It was found, surprisingly, that these new, bifunctional chelating agents with intermittent chalcogen atoms and their coupling products with compounds that accumulate specifically are excellently suited for producing radiopharmaceuticals for diagnostic and therapeutic purposes.
摘要翻译： PCT No.PCT / DE94 / 00372 Sec。 371日期1996年12月9日第 102（e）日期1996年12月9日PCT 1994年3月29日PCT公布。第WO94 / 22493号公报日期：1994年10月13日本发明涉及具有间歇性硫属原子的新型双功能螯合剂，含有这些化合物的药物，它们在放射诊断和放射疗法中的用途以及这些化合物的制备方法。根据本发明的化合物具有通式（I）M-L，其中M表示放射性核素，L表示通式（II）的配体。令人惊讶地发现，具有间歇性硫属原子的这些新的双功能螯合剂及其与特异性积累的化合物的偶联产物非常适合用于制备用于诊断和治疗目的的放射性药物。

8. 发明申请

US20140011853A1 SUBSTITUTED 3-(BIPHENYL-3-YL)-8,8-DIFLUORO-4-HYDROXY-1-AZASPIRO[4.5]DEC-3-EN-2-ONES FOR THERAPY 有权
标题翻译：取代的3-（联苯-3-基）-8,8-二氟-4-羟基-1-氮杂[4.5] DEC-3-EN-2-ONES治疗
公开(公告)号：US20140011853A1
公开(公告)日：2014-01-09
申请号：US13985940
申请日：2012-02-14
申请人： Ningshu Liu , Kai Thede , Ursula Mönning , Arne Scholz , Christoph-Stephan Hilger , Ulf Bömer , Reiner Fischer
发明人： Ningshu Liu , Kai Thede , Ursula Mönning , Arne Scholz , Christoph-Stephan Hilger , Ulf Bömer , Reiner Fischer
IPC分类号： A61K31/403 , A61K45/06 , C07D209/54
CPC分类号： A01N43/38 , A01N43/12 , A61K31/403 , A61K45/06 , C07D209/54
摘要： The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound.The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth.
摘要翻译：为了治疗目的，本发明涉及式（Ia）的取代的3-（联苯-3-基）-8,8-二氟-4-羟基-1-氮杂螺[4.5]癸-3-烯-2-酮，药物组合物及其在治疗中的用途，特别是用于预防和治疗肿瘤病症。本发明还涉及其中W，X，Y，Z，A，B，D和G具有上述含义的式（I）的新化合物，涉及多种制备方法和中间体，以及它们用作农药和/或除草剂和/或杀真菌剂。本发明还涉及选择性除草组合物，其包含首先是卤素取代的螺环酮醇，其次是作物植物相容性改善化合物。本发明还涉及通过将铵盐或鏻盐和任选的渗透剂加入到相应的组合物中来增强作物保护组合物的作用，包括特别是卤素取代的螺环酮醇，用于生产它们的方法和在农作物保护中作为农药和/或杀真菌剂的应用和/或用于防止不期望的植物生长。

9. 发明授权

US07655217B2 Near infrared imaging agent 失效
标题翻译：近红外成像剂
公开(公告)号：US07655217B2
公开(公告)日：2010-02-02
申请号：US11387367
申请日：2006-03-22
申请人： Kai Licha , Björn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
发明人： Kai Licha , Björn Riefke , Wolfhard Semmler , Ulrich Speck , Christoph-Stephan Hilger
IPC分类号： A61B10/00 , A61B5/00 , A61B8/00
CPC分类号： A61K49/0032 , A61K49/0017 , A61K49/0021 , A61K49/005 , C09B23/086 , C09B69/105
摘要： This invention relates to an in-vivo diagnostic method based on near infrared radiation (NIR radiation) that uses water-soluble dyes and their biomolecule adducts, each having specific photophysical and pharmaco-chemical properties, as a contrast medium for fluorescence and transillumination diagnostics in the NIR range, to new dyes and pharmaceuticals containing such dyes.
摘要翻译：本发明涉及一种基于近红外辐射（NIR辐射）的体内诊断方法，其使用水溶性染料及其生物分子加合物，其具有特定的光物理和药物化学性质，作为用于荧光和透照诊断的造影剂 NIR范围，新染料和含有这些染料的药物。

10. 发明授权

US06709693B1 Stents with a radioactive surface coating, processes for their production and their use for restenosis prophylaxis 失效
标题翻译：具有放射性表面涂层的支架，其生产过程及其用于再狭窄预防
公开(公告)号：US06709693B1
公开(公告)日：2004-03-23
申请号：US09627321
申请日：2000-07-27
申请人： Ludger Dinkelborg , Friedhelm Blume , Christoph-Stephan Hilger , Dieter Heldmann , Johannes Platzek , Ulrich Niedballa , Heribert Miklautz , Ulrich Speck , Stephan Duda , Gunnar Tepe , Bernhard Noll , Heidemarie Goerner
发明人： Ludger Dinkelborg , Friedhelm Blume , Christoph-Stephan Hilger , Dieter Heldmann , Johannes Platzek , Ulrich Niedballa , Heribert Miklautz , Ulrich Speck , Stephan Duda , Gunnar Tepe , Bernhard Noll , Heidemarie Goerner
IPC分类号： A61L2700
CPC分类号： A61K51/1282 , A61F2/82 , A61F2210/0095 , A61L31/082 , A61L31/14 , A61L31/16 , A61L31/18 , A61L2300/416 , A61L2300/44 , A61L2300/606 , A61N5/1002
摘要： The invention relates to radioactive stents, characterized in that the stent is coated on the surface with the radioactive isotope, as well as processes for their production.
摘要翻译：本发明涉及放射性支架，其特征在于，用放射性同位素将支架涂覆在表面上，以及其生产方法。

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