公开(公告)号：US20070140974A1

公开(公告)日：2007-06-21

申请号：US11304028

申请日：2005-12-15

申请人： Andrew Torres ,  Faisal Syud ,  Nichole Wood ,  Amit Kulkarni ,  Mark Baillie ,  Bahram Moasser ,  Brian Bales ,  Anton Beletskii ,  Peter Bonitatebus

发明人： Andrew Torres ,  Faisal Syud ,  Nichole Wood ,  Amit Kulkarni ,  Mark Baillie ,  Bahram Moasser ,  Brian Bales ,  Anton Beletskii ,  Peter Bonitatebus

IPC分类号： A61K49/10

CPC分类号： A61K49/1848 ,  A61K47/59 ,  A61K47/62 ,  A61K47/6923 ,  A61K47/6929 ,  A61K49/1857 ,  A61K49/1866 ,  B82Y5/00 ,  B82Y25/00 ,  G01N33/552 ,  G01R33/5601 ,  H01F1/0054

摘要： In some embodiments, the present invention is directed to novel targeted contrast agents for magnetic resonance imaging (MRI). The present invention is also directed to methods of making such targeted MRI contrast agents, and to methods of using such MRI contrast agents. Typically, such targeted MRI contrast agents provide enhanced relaxivity, improved signal-to-noise, targeting ability, and resistance to agglomeration. Methods of making such MRI contrast agents typically afford better control over particle size, and methods of using such MRI contrast agents typically afford enhanced blood clearance rates and biodistribution.

摘要翻译： 在一些实施方案中，本发明涉及用于磁共振成像（MRI）的新型靶向造影剂。 本发明还涉及制备这种靶向MRI造影剂的方法，以及使用这种MRI造影剂的方法。 通常，这种靶向MRI造影剂提供增强的舒张度，改善的信噪比，靶向能力和抵抗聚集。 制造这种MRI造影剂的方法通常能够更好地控制粒径，并且使用这种MRI造影剂的方法通常提供增强的血液清除率和生物分布。

公开(公告)号：US20070009428A1

公开(公告)日：2007-01-11

申请号：US11175668

申请日：2005-07-06

申请人： Faisal Syud ,  Nichole Wood ,  Andrew Torres ,  Mark Baillie ,  Dinko Trotter ,  Cristina Hehir ,  Ming Zhao ,  Daniel Kramer

发明人： Faisal Syud ,  Nichole Wood ,  Andrew Torres ,  Mark Baillie ,  Dinko Trotter ,  Cristina Hehir ,  Ming Zhao ,  Daniel Kramer

IPC分类号： A61K51/00

CPC分类号： A61K51/04 ,  A61K47/6899 ,  B82Y5/00

摘要： A set of compounds that includes an active-agent labeled species and a pretargeting conjugate is disclosed. The active agent-labeled species includes a ligand coupled to an active agent. The pretargeting conjugate includes a protein conjugated to a targeting species having a targeting moiety capable of binding to an in-vivo target or a biomarker produced by or associated with the target. The protein is substantially free of a cofactor. Also disclosed are methods of administering the pretargeting species and the active-agent labeled species to a subject for diagnosing or treating a disease condition, or assessing the effectiveness of a treatment of the disease condition.

摘要翻译： 公开了一组包含活性剂标记的物质和预靶向缀合物的化合物。 活性剂标记的物质包括与活性剂偶联的配体。 预靶向缀合物包括与靶向物质缀合的蛋白质，其具有能够结合体内靶标的靶向部分或由靶产生或与靶标相关的生物标志物。 蛋白质基本上不含辅因子。 还公开了将预靶向物种和活性剂标记物种施用于受试者以诊断或治疗疾病状况或评估治疗疾病状况的有效性的方法。

公开(公告)号：US20070009427A1

公开(公告)日：2007-01-11

申请号：US11175595

申请日：2005-07-06

申请人： Faisal Syud ,  Nichole Wood ,  Andrew Torres ,  Mark Baillie ,  Dinko Eduardo Trotter ,  Cristina Hehir ,  Ming Zhao ,  Daniel Kramer

发明人： Faisal Syud ,  Nichole Wood ,  Andrew Torres ,  Mark Baillie ,  Dinko Eduardo Trotter ,  Cristina Hehir ,  Ming Zhao ,  Daniel Kramer

IPC分类号： A61K51/00

CPC分类号： B82Y5/00 ,  A61K47/6899 ,  A61K51/04

摘要： A set of compounds that includes an active-agent labeled species and a pretargeting conjugate is disclosed. The active agent-labeled species includes a ligand coupled to an active agent. The pretargeting conjugate includes a protein conjugated to a targeting species having a targeting moiety capable of binding to an in-vivo target or a biomarker produced by or associated with the target. The protein and the ligand are covalently attached. Also disclosed are methods of administering the pretargeting species and the active-agent labeled species to a subject for diagnosing or treating a disease condition, or assessing the effectiveness of a treatment of the disease condition.

摘要翻译： 公开了一组包含活性剂标记的物质和预靶向缀合物的化合物。 活性剂标记的物质包括与活性剂偶联的配体。 预靶向缀合物包括与靶向物质缀合的蛋白质，其具有能够结合体内靶标的靶向部分或由靶产生或与靶标相关的生物标志物。 蛋白质和配体共价连接。 还公开了将预靶向物种和活性剂标记物种施用于受试者以诊断或治疗疾病状况或评估治疗疾病状况的有效性的方法。

公开(公告)号：US20070009435A1

公开(公告)日：2007-01-11

申请号：US11175596

申请日：2005-07-06

申请人： Faisal Syud ,  Nichole Wood ,  Daniel Kramer ,  Mark Baillie ,  Dinko Eduardo Trotter ,  Anup Sood ,  Ming Zhao

发明人： Faisal Syud ,  Nichole Wood ,  Daniel Kramer ,  Mark Baillie ,  Dinko Eduardo Trotter ,  Anup Sood ,  Ming Zhao

IPC分类号： A61K51/00 ,  A61K48/00 ,  C07H21/02 ,  C07F9/6533

CPC分类号： C07F9/65586 ,  A61K49/0002 ,  A61K51/0491 ,  A61K51/0495 ,  C07F9/65616

摘要： A set of compounds that includes an active agent-labeled species and a pretargeting conjugate is disclosed. The active agent-labeled species includes a first oligomeric nucleotide or mimic thereof conjugated to a linker having a first moiety coupled with a diagnostic active agent. The pretargeting conjugate includes a second oligomeric nucleotide or mimic thereof conjugated to a targeting species having a targeting moiety capable of binding to a target or a marker produced by or associated with the target. The second oligomeric nucleotide or mimic thereof has a sequence that is at least partially complementary to a sequence of the first oligomeric nucleotide or mimic thereof. Also disclosed are methods of administering the pretargeting conjugate and active agent-labeled species to a subject for diagnosing a disease condition or assessing the effectiveness of a treatment of the disease condition.

摘要翻译： 公开了一组包含活性剂标记的物质和预靶向缀合物的化合物。 活性剂标记的物质包括与具有与诊断活性剂偶联的第一部分的接头缀合的第一寡聚核苷酸或其模拟物。 预靶向缀合物包括与靶向物质缀合的第二寡聚核苷酸或其模拟物，所述靶向物质具有能够结合靶标的靶向部分或由靶产生或与靶标相关的标记。 第二寡聚核苷酸或其模拟物具有与第一寡核苷酸序列至少部分互补的序列或其模拟物。 还公开了将预靶向缀合物和活性剂标记物质施用于受试者以诊断疾病状况或评估治疗疾病状况的有效性的方法。