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21. 发明申请

WO2012113733A1 NANOPARTIKEL ALS MRT-KONTRASTMITTEL ZUR DIAGNOSTIK DES HEPATOZELLULÄREN KARZINOMS 审中-公开
标题翻译：纳米粒子作为MRI造影剂用于诊断肝细胞癌
公开(公告)号：WO2012113733A1
公开(公告)日：2012-08-30
申请号：PCT/EP2012/052811
申请日：2012-02-17
申请人： JOHANN WOLFGANG GOETHE-UNIVERSITÄT, FRANKFURT AM MAIN , KREUTER, Jörg , ULBRICH, Karsten , LANGER, Klaus , KNOBLOCH, Thomas , PIIPER, Albrecht , KÖBERLE, Verena , KORKUSUZ, Hüdayi , VOGEL, Thomas J.
发明人： KREUTER, Jörg , ULBRICH, Karsten , LANGER, Klaus , KNOBLOCH, Thomas , PIIPER, Albrecht , KÖBERLE, Verena , KORKUSUZ, Hüdayi , VOGEL, Thomas J.
IPC分类号： A61K47/48 , A61K49/06 , A61K49/18
CPC分类号： A61K49/1881
摘要： Die vorliegende Erfindung betrifft Nanopartikel, umfassend einer Gadoliniumverbindung und/oder inkorporiertes Perfluorooctylbromid, zur Verwendung als Kontrastmittel in einer Magnetresonanztomographie (MRT) gestützten Diagnose von Lebererkrankungen, insbesondere von Hepatozellulärem Karzinom (HCC). Die erfindungsgemäßen PLGA und HSA Nanopartikel wurden mit einer Gadoliniumverbindung (Gd-DTPA) beladen und konnten erfolgreich zur verbesserten Kontrastierung in der MRT von HCC eingesetzt werden. Weiterhin beschreibt die Erfindung neuartige Kontrastmittel beinhaltend die erfindungsgemäßen Nanopartikel, insbesondere zur Verwendung in der Diagnose, Überwachung und/oder Früherkennung von HCC. Weiterhin wird ein Verfahren zur Diagnose, Überwachung und/oder Früherkennung von HCC bereitgestellt.
摘要翻译：本发明涉及一种包括钆化合物和/或非法人全氟溴辛烷，用作在磁共振成像（MRI）肝脏疾病的辅助诊断，特别是肝细胞癌（HCC）的造影剂的纳米颗粒。所述PLGA和本发明的HSA纳米颗粒负载用钆（Gd-DTPA）和用于HCC的MRI改进的对比度可以成功地使用。此外，本发明涉及新的造影剂，其包括描述了本发明的纳米颗粒，特别是用于诊断，监测和/或早检测HCC的用途。此外，提供了用于诊断，监测和/或早检测HCC的方法。

22. 发明申请

WO2011071970A2 NANOPARTICLE CARRIER SYSTEMS BASED ON POLY(DL-LACTIC-CO-GLYCOLIC ACID) (PLGA) FOR PHOTODYNAMIC THERAPY (PDT) 审中-公开
标题翻译：基于聚合（DL-LACTIC-CO-GLYCOLIC ACID）（PLGA）用于光化学治疗（PDT）的纳米载体系统
公开(公告)号：WO2011071970A2
公开(公告)日：2011-06-16
申请号：PCT/US2010/059367
申请日：2010-12-08
申请人： BIOLITEC, INC. , LANGER, Klaus , KNOBLOCH, Thomas , RÖDER, Beate , PREUSS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , von BRIESEN, Hagen , LÖW, Karin , WAGNER, Sylvia
发明人： LANGER, Klaus , KNOBLOCH, Thomas , RÖDER, Beate , PREUSS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , von BRIESEN, Hagen , LÖW, Karin , WAGNER, Sylvia
IPC分类号： A61K47/30 , A61K33/20 , A61K9/127 , A61P35/00 , A61P27/02 , A61P29/00
CPC分类号： A61K9/5153 , A61K33/20 , A61K41/0071
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticutate formulations for clinical use in photodynamic therapy comprising a hydrophobic photosensitizer, poly(lactic-co-glycolic) acid and stabilizing agents are provided. These nanoparticulate pharmaceutical formulations provide therapeutically effective amounts of photosensitizer for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers, whose efficacy and safety are enhanced by such nanoparticulate formulations. It also leaches the method of preparing PLGA-based nanoparticles under sterile conditions. In one of the preferred embodiments of the present invention PLGA-based nanoparticles have a mean particle size less than 500nm and the photosensitizer is temoporfϊn, 5,10,15,20-tetrakis(3-hydroxyphenyl)-chlorin ( m THPC). In another embodiment, the photosensitizer 2,3-dihydroxy-5,10,15,20-tetrakis(3- hydroxyphenyl)-chlorin ( m THPD-OH) is formulated as a nanoparticle for parenteral administration. Yet, in another embodiment preferred photosensitizer is 5,10,15,20-tetrakis(3- hydroxyphenyl)-porphyrin ( m THPP). The formulations can be used for treating hyperptasic and neoplasia conditions, inflammatory problems, and more specifically to target tumor cells.
摘要翻译：提供了在储存中稳定的组合物以及用于临床用于光动力疗法的基于药物的纳米颗粒制剂的方法，其包括疏水性光敏剂，聚（乳酸 - 共 - 乙醇酸）酸和稳定剂。这些纳米颗粒药物制剂提供治疗有效量的用于肠胃外给药的光敏剂。特别地，四吡咯衍生物可以用作光敏剂，其功效和安全性通过这种纳米颗粒制剂增强。它还浸出了在无菌条件下制备基于PLGA的纳米颗粒的方法。在本发明的一个优选实施方案中，基于PLGA的纳米颗粒具有小于500nm的平均粒度，并且光敏剂是temoporf TM，5,10,15,20-四（3-羟基苯基） - 氯化物（mTHPC）。在另一个实施方案中，将光敏剂2,3-二羟基-5,10,15,20-四（3-羟基苯基） - 青霉素（mTHPD-OH）配制成用于肠胃外给药的纳米颗粒。然而，在另一个实施方案中，优选的光敏剂是5,10,15,20-四（3-羟基苯基） - 卟啉（mTHPP）。该制剂可用于治疗高血压和瘤形成症状，炎症问题，更具体地用于靶向肿瘤细胞。

23. 发明申请

WO2011071968A3 NANOPARTICLE CARRIER SYSTEMS BASED ON HUMAN SERUM ALBUMIN FOR PHOTODYNAMIC THERAPY 审中-公开
公开(公告)号：WO2011071968A3
公开(公告)日：2011-06-16
申请号：PCT/US2010/059364
申请日：2010-12-08
申请人： BIOLITEC, INC. , LANGER, Klaus , WACKER, Matthias , RÖDER, Beate , PRUESS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , VON BRIESEN, Hagen , WAGNER, Sylvia
发明人： LANGER, Klaus , WACKER, Matthias , RÖDER, Beate , PRUESS, Annegret , ALBRECHT, Volker , GRÄFE, Susanna , WIEHE, Arno , VON BRIESEN, Hagen , WAGNER, Sylvia
IPC分类号： A61K38/38 , A61K38/18 , A61K31/54 , A61K31/40 , A61K49/00 , A61P35/00
摘要： Compositions, which are stable in storage, and a method of production of pharmaceutical based nanoparticulate formulations for photodynamic therapy comprising a hydrophobic photosensitizer, human serum albumin (HSA) and stabilizing agent are provided. These nanoparticulate formulations provide therapeutically effective amounts of photosensitizer (PS) for parenteral administration. In particular, tetrapyrrole derivatives can be used as photosensitizers whose efficacy and safety are enhanced by such nanoparticulate formulations. A method of preparing the HSA-based nanoparϋcles under sterile conditions is also provided. In one of the preferred embodiments of the present invention temoporfin, a hydrophobic PS, is formulated as a nanoparticle for parenteral administration. The formulations are useful for treating hyperplasic and neoplasic conditions, inflammatory problems, and more specifically to target tumor cells.

24. 发明申请

WO2009010263A2 KREISPROZESS ZUR HERSTELLUNG VON BARIUMSULFAT UND LITHIUMMETALLPHOSPHATVERBINDUNGEN 审中-公开
标题翻译： CIRCLE用于生产硫酸钡和磷酸锂金属化合物
公开(公告)号：WO2009010263A2
公开(公告)日：2009-01-22
申请号：PCT/EP2008/005738
申请日：2008-07-14
申请人： SÜD-CHEMIE AG , VOGLER, Christian , LANGER, Klaus , POLLNER, Andreas , NUSPL, Gerhard
发明人： VOGLER, Christian , LANGER, Klaus , POLLNER, Andreas , NUSPL, Gerhard
IPC分类号： C01F11/46 , C01B25/45
CPC分类号： C01F11/462 , C01B25/45 , C01P2004/52 , C01P2004/62 , C01P2006/80 , Y10T428/2982
摘要： Die vorliegende Erfindung betrifft einen Kreisprozess zur Herstellung von Bariumsulfat und Lithiumeisenphosphat umfassend das (i) Bereitstellen einer wässrigen, lithium- und sulfationenhaltigen Lösung und (ii) Zugeben von festem Bariumhydroxid bei einer Temperatur von mehr als 50°C und (iii) wobei die Zugabe des Bariumhydroxids über einen Zeitraum von weniger als 15 Minuten erfolgt. Weiter betrifft die vorliegende Erfindüng Bariumsulfat erhältlich durch das erfindungsgemäße Verfahren.
摘要翻译：本发明涉及一种循环过程用于生产硫酸钡和磷酸铁锂，其包括（i）提供一种含水的锂和硫酸含离子溶液，和（ii）将固体氢氧化钡在高于50℃和（iii）增加的温度的氢氧化钡发生在一段少于15分钟。此外，本Erfindüng钡关注通过本发明方法获得。

25. 发明授权

US4801579A Novel cystine compounds, their preparation and use 失效
标题翻译：新型胱氨酸化合物，其制备和用途
公开(公告)号：US4801579A
公开(公告)日：1989-01-31
申请号：US115796
申请日：1987-11-02
申请人： Naderer Rainer , Buxbaum Lothar , Langer Klaus
发明人： Naderer Rainer , Buxbaum Lothar , Langer Klaus
IPC分类号： C07K5/08 , C07K1/02 , C07K5/06 , C07K5/065 , C07K5/083 , A61K37/00 , C07C103/00
CPC分类号： C07K5/0806 , C07K5/06026 , C07K5/06078 , Y10S930/26
摘要： Novel cystine compounds of the general formula I are proposed wherein the independently of one another each represent a, preferably natural, L-amino acid, in particular glycine, alanine, proline, threonine, serine, valine, arginine, lysine or ornithine; the R.sub.1 independently of one another each stand for an acyl group of an organic acid with 2 to 5 carbon atoms, preferably for acetyl-, propionyl-, succinyl- or hydroxysuccinyl- or for a, preferably natural, L-amino acid which via its carboxylic group is linked amide-like to the amino group of the amino acid AS, the amino acids indicated as preferred for AS also being preferred for the amino acids of R.sub.1, or the two R.sub.1 together form the acyl group of an organic dicarboxylic acid, preferably the succinic or malic group; and the R.sub.2 independently of one another each are an alkoxy group with 1 to 4 carbon atoms, preferably methoxy or ethoxy, the hydroxy group, where in case of the meaning of R.sub.2 =OH the carboxylic group(s) are each present as such or as an inorganic or organic salt, preferably with NaOH or KOH, organic bases or basic amino acids such as L-lysine, L-ornithine, L-arginine or L-histidine, or the radical of a further amino acid bound via an amide group, the carbocylic group(s) of the amino acid optionally also having the form of an inorganic or organic salt; further processes for their preparation as well as nutrient compositions formed therewith.
摘要翻译：提出了通式I的新型胱氨酸化合物，其中AS彼此独立地代表，优选天然的L-氨基酸，特别是甘氨酸，丙氨酸，脯氨酸，苏氨酸，丝氨酸，缬氨酸，精氨酸，赖氨酸或鸟氨酸; R1彼此独立地代表具有2至5个碳原子的有机酸的酰基，优选乙酰基，丙酰基 - ，琥珀酰基 - 或羟基琥珀酰基 - 或优选天然的L-氨基酸，其通过其羧基与氨基酸AS的氨基连接，对于AS优选的氨基酸优选为R1的氨基酸，或者两个R 1一起形成有机二羧酸的酰基，优选琥珀酸或苹果酸基团; 并且R 2彼此独立地为具有1至4个碳原子的烷氧基，优选甲氧基或乙氧基，羟基，其中在R2 = OH的情况下，羧基基团各自独立地存在，或作为无机或有机盐，优选使用NaOH或KOH，有机碱或碱性氨基酸如L-赖氨酸，L-鸟氨酸，L-精氨酸或L-组氨酸，或通过酰胺基结合的另外的氨基酸的基团，氨基酸的碳基基团任选地还具有无机或有机盐的形式; 进一步的制备方法以及与其形成的营养组合物。

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