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31. 发明申请

US20130066055A1 NEW BINDER-DRUG CONJUGATES (ADCS) AND USE THEREOF 审中-公开
标题翻译：新的联合药物联合会（ADCS）及其使用
公开(公告)号：US20130066055A1
公开(公告)日：2013-03-14
申请号：US13451950
申请日：2012-04-20
申请人： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte Christine Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörissen , Sandra Borkowski
发明人： Hans-Georg Lerchen , Lars Linden , Sherif El Sheikh , Jörg Willuda , Charlotte Christine Kopitz , Joachim Schuhmacher , Simone Greven , Christoph Mahlert , Beatrix Stelte-Ludwig , Sven Golfier , Rudolf Beier , Iring Heisler , Axel Harrenga , Karl-Heinz Thierauch , Sandra Bruder , Heike Petrul , Hannah Jörissen , Sandra Borkowski
IPC分类号： C07K17/02
CPC分类号： A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/422 , A61K31/4245 , A61K31/5355 , A61K31/536 , A61K31/537 , A61K31/5377 , A61K39/3955 , A61K45/06 , A61K47/542 , A61K47/6803 , A61K47/6851 , A61K47/6859 , A61K47/6869 , A61K47/6889 , C07K5/0205 , C07K5/0207 , C07K5/06 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K7/02 , C07K7/06 , C07K16/18 , C07K16/28 , C07K16/2812 , C07K16/2863 , C07K16/30 , C07K2317/21 , C07K2317/24 , C07K2317/565 , C07K2317/76
摘要： The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
摘要翻译：本申请涉及针对目标C4.4a的N，N-二烷基硫酸钠的新粘合剂 - 药物共轭物（ADC），这些ADC的活性代谢物，制备这些ADC的方法，使用这些ADC 治疗和/或预防疾病，以及使用这些ADC用于制备用于治疗和/或预防疾病的药物，更特别是过度增殖和/或血管生成疾病，例如癌症疾病。这样的治疗可以作为单一疗法来实施，或者与其它药物组合或进一步的治疗措施。

32. 发明授权

US08367065B2 Targeted polymeric prodrugs containing multifunctional linkers 失效
标题翻译：含有多功能接头的靶向聚合物前药
公开(公告)号：US08367065B2
公开(公告)日：2013-02-05
申请号：US12402839
申请日：2009-03-12
申请人： Hong Zhao , Prasanna Reddy , Maria Belen Rubio
发明人： Hong Zhao , Prasanna Reddy , Maria Belen Rubio
IPC分类号： A61K47/48 , A61K31/4015 , A61K31/4025 , A61K31/444 , A61K31/44 , A61K31/7088 , A61K39/395 , C07H21/02 , C07K16/00 , C07K17/02 , C07D207/40 , C07D403/12
CPC分类号： C07K7/08 , A61K47/551 , A61K47/60 , A61K47/64 , C07D207/416 , C07D207/448 , C07D213/71 , C07D487/04 , C07K5/0821 , C07K7/06
摘要： The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.
摘要翻译：本发明提供了含有多功能接头的单链抗体定向聚合前药。还公开了制备聚合物递送系统的方法和使用其的治疗哺乳动物的方法。

33. 发明申请

US20130004522A1 PHOTOTRIGGERED NANOPARTICLES FOR CELL AND TISSUE TARGETING 审中-公开
标题翻译：用于细胞和组织靶向的光吸收纳米颗粒
公开(公告)号：US20130004522A1
公开(公告)日：2013-01-03
申请号：US13499543
申请日：2010-09-30
申请人： Tal Dvir , Daniel S. Kohane , Matthew Ryan Banghart , Robert S. Langer
发明人： Tal Dvir , Daniel S. Kohane , Matthew Ryan Banghart , Robert S. Langer
IPC分类号： A61K38/08 , C07K17/02 , A61K39/395
CPC分类号： A61K9/0009 , A61K9/5138 , A61K9/5146 , A61K9/5153 , A61K41/0042 , A61K47/6921 , A61K47/6935 , A61N5/0601 , A61N5/062
摘要： The present invention relates, in part, to a novel and simple particulate system that targets and binds any tissue selectively upon light illumination. The particulate system can be used for targeted delivery of substances to predefined cells or tissues in an individual.
摘要翻译：本发明部分涉及一种新颖且简单的颗粒系统，其在光照射下靶向和结合任何组织。颗粒系统可用于将物质定向递送到个体中预定的细胞或组织。

34. 发明申请

US20120329998A1 LUMINESCENT GOLD NANOPARTICLE FUNCTIONALIZED BY N-(4-AMINOBUTYL)-N-ETHYLISOLUMINOL, PREPARATION AND APPLICATION THEREOF 有权
标题翻译：由N-（4-氨基丁基）-N-乙基磺酰胺官能化的发光金纳米颗粒，其制备和应用
公开(公告)号：US20120329998A1
公开(公告)日：2012-12-27
申请号：US13582434
申请日：2010-07-08
申请人： Hua Cui , Dayong Tian
发明人： Hua Cui , Dayong Tian
IPC分类号： C07F1/12 , C07H23/00 , C07K17/02 , C07K19/00 , B82Y40/00 , B82Y30/00
CPC分类号： G01N33/54346 , G01N21/76 , G01N33/553 , G01N33/582
摘要： Provided is luminescent gold nanomaterial functionalized by N-(4-aminobutyl)-N-ethylisoluminol, methods of preparation and application thereof. The functionalized gold nanoparticle nanomaterial are formed by N-(4-aminobutyl)-N-ethylisoluminol bonding to the surface of the gold nanomaterial. The functionalized gold nanomaterial are prepared by directly reducing chloroauric acid with N-(4-aminobutyl)-N-ethylisoluminol, wherein N-(4-aminobutyl)-N-ethylisoluminol acts as reducer and stabilizer simultaneously. The preparation method is simple, fast and no need of special conditions. The preparation methods can be performed in a wide temperature range, for example, 15-35° C. The size and pattern of the functionalized gold nanomaterial can be specified by choosing the ratio of chloroauric acid to N-(4-aminobutyl)-N-ethylisoluminol. The obtained functionalized nano gold particles exhibit excellent chemiluminescence properties. Said functionalized gold nanomaterial can be combined with biomolecules to form biomolecular probe, which can be used for immunoassay, nucleic acid analysis, molecular imaging, sensor, etc., and has a broad application prospect in the field of clinical analysis biomedicine, food safety, and environment monitoring.
摘要翻译：提供由N-（4-氨基丁基）-N-乙基异豆酚醇功能化的发光金纳米材料，其制备和应用方法。官能化的金纳米颗粒纳米材料由N-（4-氨基丁基）-N-乙基异豆胺醇键合到金纳米材料的表面。功能化的金纳米材料通过用N-（4-氨基丁基）-N-乙基异豆酚直接还原氯金酸制备，其中N-（4-氨基丁基）-N-乙基异豆胺醇同时作为还原剂和稳定剂。制备方法简单，快速，无需特殊条件。制备方法可以在宽温度范围内进行，例如15-35℃。官能化金纳米材料的尺寸和图案可以通过选择氯金酸与N-（4-氨基丁基）-N - 乙基异豆酚。所获得的官能化纳米金颗粒表现出优异的化学发光性能。所述功能化金纳米材料可与生物分子结合形成生物分子探针，可用于免疫测定，核酸分析，分子成像，传感器等，在临床分析生物医药，食品安全，和环境监测。

35. 发明申请

US20120282178A1 Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules 有权
标题翻译：改进的蛋白质，肽和其他分子的F-18标记的方法和组合物
公开(公告)号：US20120282178A1
公开(公告)日：2012-11-08
申请号：US13474260
申请日：2012-05-17
申请人： William J. McBride , Christopher A. D'Souza , David M. Goldenberg
发明人： William J. McBride , Christopher A. D'Souza , David M. Goldenberg
IPC分类号： C07K17/02 , C07D255/02 , A61K51/10
CPC分类号： C07K19/00 , A61K47/6897 , A61K51/0406 , A61K51/0491 , A61K51/08 , A61K51/082 , A61K51/083 , A61K51/088 , A61K51/109 , B82Y5/00
摘要： The present application discloses compositions and methods of synthesis and use of 68Ga, 18F or 19F labeled molecules of use in PET or MRI imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a chelating moiety, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 68Ga, 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. In more preferred embodiments, a chelating moiety or targetable construct may be conjugated to a targeting molecule, such as an antibody or antibody fragment.
摘要翻译：本申请公开了在PET或MRI成像中合成和使用68Ga，18F或19F标记分子的组合物和方法。优选地，18F或19F通过与IIIA族金属形成络合物并将该复合物与可以直接或间接连接到靶向分子的螯合部分结合而与靶向分子缀合。在其它实施方案中，68Ga，18F或19F标记的部分可以包含与靶向疾病相关抗原的双特异性抗体组合使用的可靶向构建体。在更优选的实施方案中，螯合部分或可靶向构建体可以与靶向分子缀合，例如抗体或抗体片段。

36. 发明申请

US20120276001A1 BIFUNCTIONAL POLYAZAMACROCYCLIC CHELATING AGENTS 有权
标题翻译：双官能聚氨酯螯合剂
公开(公告)号：US20120276001A1
公开(公告)日：2012-11-01
申请号：US13476794
申请日：2012-05-21
申请人： Zoltan Kovacs , Garry E. Kiefer , Corinne Bensimon , A. Dean Sherry , Gyula Tircso , Cara Ferreira
发明人： Zoltan Kovacs , Garry E. Kiefer , Corinne Bensimon , A. Dean Sherry , Gyula Tircso , Cara Ferreira
IPC分类号： C07D471/04 , C07K17/02 , A61P35/00 , A61K51/10 , A61K51/08 , C07F5/00 , A61K51/04
CPC分类号： C07D273/00 , A61K9/0019 , A61K51/0482 , A61K51/1093 , C07D257/02 , C07D471/08
摘要： A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111In or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.
摘要翻译：式（I）的双官能多氮杂环螯合剂：其中：变量A，L，Q，Q 1，X，Y，Z，Z 1，m，n和r如本申请的说明书所定义。还描述了上述螯合剂与金属离子离子的络合物，例如90Y，111In或177Lu的离子; 共价连接到生物载体上的复合物的共轭物; 和含有该缀合物的药物组合物。还描述了涉及给药药物组合物的哺乳动物的治疗性治疗方法。

37. 发明申请

US20120258071A1 Compositions and Methods of Use for MGD-CSF in Disease Treatment 有权
标题翻译： MGD-CSF在疾病治疗中的组成和使用方法
公开(公告)号：US20120258071A1
公开(公告)日：2012-10-11
申请号：US13446254
申请日：2012-04-13
申请人： Dirk Behrens , Elizabeth Bosch , Stephen K. Doberstein , Robert Forgan Halenbeck , Kevin Hestir , Min Mei Huang , Ernestine Lee , Haishan Lin , Thomas Linnemann , Shannon Marshall , Justin G. P. Wong , Ge Wu , Aileen Zhou , Cindy Leo , Lewis T. Williams
发明人： Dirk Behrens , Elizabeth Bosch , Stephen K. Doberstein , Robert Forgan Halenbeck , Kevin Hestir , Min Mei Huang , Ernestine Lee , Haishan Lin , Thomas Linnemann , Shannon Marshall , Justin G. P. Wong , Ge Wu , Aileen Zhou , Cindy Leo , Lewis T. Williams
IPC分类号： A61K38/19 , C07K17/02 , A61P35/00 , A61P37/00 , A61P31/00 , C07K17/00 , C07K19/00
CPC分类号： C07K16/243 , A61K38/00 , C07K14/53
摘要： Disclosed is a newly identified secreted molecule, identified herein as “monocyte, granulocyte, and dendritic cell colony stimulating factor” (MGD-CSF), the polypeptide sequence, and polynucleotides encoding the polypeptide sequence. Also provided is a procedure for producing the polypeptide by recombinant techniques employing, for example, vectors and host cells. Additionally, procedures are described to modify the disclosed novel molecules of the invention to prepare fusion molecules. Also disclosed are methods for using the polypeptides and active fragments thereof for treatment of a variety of diseases, including, for example, cancer, autoimmune and inflammatory diseases, infectious diseases, and recurrent pregnancy loss.
摘要翻译：公开了一种新鉴定的分泌型分子，本文鉴定为单核细胞，粒细胞和树突细胞集落刺激因子（MGD-CSF），多肽序列和编码多肽序列的多核苷酸。还提供了通过使用例如载体和宿主细胞的重组技术产生多肽的方法。另外，描述了修饰所公开的本发明新颖分子以制备融合分子的方法。还公开了将多肽及其活性片段用于治疗各种疾病（包括例如癌症，自身免疫性和炎性疾病，感染性疾病和复发性妊娠损失）的方法。

38. 发明授权

US08268962B2 Molecules for targeting compounds to various selected organs or tissues 有权
标题翻译：用于将化合物靶向各种选择的器官或组织的分子
公开(公告)号：US08268962B2
公开(公告)日：2012-09-18
申请号：US12685369
申请日：2010-01-11
申请人： Johannes Antonius Heemskerk , Judith Christina Theodora Van Deutekom , Petra Van Kuik-Romeijn , Gerard Johannes Platenburg
发明人： Johannes Antonius Heemskerk , Judith Christina Theodora Van Deutekom , Petra Van Kuik-Romeijn , Gerard Johannes Platenburg
IPC分类号： C07K17/02
CPC分类号： A61K49/0056 , A61K47/62 , A61K49/0032 , A61K49/0047
摘要： The invention provides conjugates, comprising an organ, tissue or tumor cell homing molecule linked to a moiety. Such a moiety can be, for example, an oligonucleotide, small interfering RNA, gene, virus, protein, pharmaceutical or detectable agent. In addition the invention provides methods to diagnose or treat a pathology of the muscle or heart, by administrating to a subject having or suspected of having a pathology a molecule or conjugate that homes to, binds to and is taken up by the muscle cells or heart cells.
摘要翻译：本发明提供了缀合物，其包含与部分连接的器官，组织或肿瘤细胞归巢分子。这样的部分可以是例如寡核苷酸，小干扰RNA，基因，病毒，蛋白质，药物或可检测的试剂。此外，本发明提供了诊断或治疗肌肉或心脏的病理学的方法，通过施用于具有或怀疑具有病理学的受试者的家族，结合和被肌肉细胞或心脏摄取的分子或结合物细胞。

39. 发明申请

US20120219495A1 NOVEL TETRAAZA MACROCYCLIC COMPOUND, PREPARATION METHOD THEREOF AND USE THEREOF 有权
标题翻译：新型四氯化碳大环化合物，其制备方法及其用途
公开(公告)号：US20120219495A1
公开(公告)日：2012-08-30
申请号：US13395346
申请日：2010-09-09
申请人： Jeong Soo Yoo , Darpan Pandya
发明人： Jeong Soo Yoo , Darpan Pandya
IPC分类号： A61K51/10 , C07F1/08 , C07F3/06 , C07F5/00 , C07K17/02 , A61K51/08 , A61K39/395 , A61K49/00 , A61P35/00 , A61P31/04 , A61P37/08 , A61P31/10 , A61P31/12 , A61P33/00 , A61P37/00 , A61P25/28 , A61P9/00 , A61P25/00 , C07D487/08
CPC分类号： C07D487/08 , A61K51/0482 , A61K51/082 , A61K51/088 , A61K51/1051 , C07D257/02 , C07D257/10
摘要： Provided are a cross-bridged tetraaza macrocyclic compound of a novel structure that can be used, for example, as a contrast agent for diagnostic imaging or a radiopharmaceutical and a method for preparing the same.The disclosed tetraaza macrocyclic compound is able to form a stable metal complex at a lower temperature and allows easy conjugation with a bioactive substance or a chemically active substance, when compared to the existing cross-bridged tetraaza macrocyclic compounds.
摘要翻译：提供了可用于例如用于诊断成像的造影剂或放射性药物的新结构的交叉桥联四氮杂大环化合物及其制备方法。所公开的四氮杂大环化合物能够在较低温度下形成稳定的金属络合物，并且与现有的交叉桥联四氮杂环化合物相比，可以容易地与生物活性物质或化学活性物质缀合。

40. 发明申请

US20120213699A1 SINGLE CHAIN FRAGMENT OF MONOCLONAL ANTIBODY 9B9 AND USES THEREOF 审中-公开
标题翻译：单链抗体9B9的单链片段及其用途
公开(公告)号：US20120213699A1
公开(公告)日：2012-08-23
申请号：US13463523
申请日：2012-05-03
申请人： Irina Balyasnikova , Sergei Danilov
发明人： Irina Balyasnikova , Sergei Danilov
IPC分类号： A61K39/395 , C07K17/00 , C07K17/02 , C12N15/13 , A61K51/10 , A61K35/00 , C07K16/46 , A61P9/00 , A61P9/12 , A61P9/04 , A61P9/10 , A61P13/12 , A61P29/00 , A61P31/00 , A61P1/00 , A61P19/02 , A61P37/08 , C12N9/96 , C12N15/63 , C12N1/21 , C12P21/02 , C12N5/10 , C07K16/40
CPC分类号： C07K16/40 , C07K2317/622 , C07K2319/00
摘要： Anti-ACE single chain fragment antibodies are disclosed. The present invention relates to using these antibodies, and polymers thereof, in methods for detecting, diagnosing, prognosing, preventing, or treating diseases associated with ACE expressing tissue.
摘要翻译：公开了抗ACE单链片段抗体。本发明涉及在检测，诊断，预后，预防或治疗与表达ACE的组织相关的疾病的方法中使用这些抗体及其聚合物。

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