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    Amino acid-containing compounds and derivatives labeled with halides and method of making
    1.
    发明申请
    Amino acid-containing compounds and derivatives labeled with halides and method of making 审中-公开
    含有氨基酸的化合物和用卤化物标记的衍生物及其制备方法

    公开(公告)号：US20060074231A1

    公开(公告)日：2006-04-06

    申请号：US10957220

    申请日：2004-10-04

    申请人： Tiberiu Siclovan ,  Faisal Syud ,  Bruce Johnson

    发明人： Tiberiu Siclovan ,  Faisal Syud ,  Bruce Johnson

    IPC分类号： C07K14/00 ,  C07D209/18 ,  C07H21/04 ,  C07C227/16

    CPC分类号： C07H21/04

    摘要： A method of labeling amino acid-containing compounds and derivatives thereof with a halide moiety comprises reacting a nucleophilic moiety on such compounds with a halogenated electrophilic compound. Radioactive halide-labeled amino acid-containing compounds can be targeted to diseased sites and provide a means to diagnose and/or treat the disease.

    摘要翻译： 用卤化物部分标记含氨基酸的化合物及其衍生物的方法包括使这些化合物上的亲核部分与卤代亲电子化合物反应。 放射性卤化物标记的含氨基酸的化合物可以靶向病变部位，并提供诊断和/或治疗疾病的手段。

    Labeled peptides for lectin-like oxidized low-density lipoprotein receptor (LOX-1)
    3.
    发明申请
    Labeled peptides for lectin-like oxidized low-density lipoprotein receptor (LOX-1) 审中-公开
    凝集素样氧化低密度脂蛋白受体（LOX-1）的标记肽

    公开(公告)号：US20050089470A1

    公开(公告)日：2005-04-28

    申请号：US10691532

    申请日：2003-10-24

    申请人： Bruce Johnson ,  Faisal Syud

    发明人： Bruce Johnson ,  Faisal Syud

    IPC分类号： A61K49/00 ,  C07B59/00 ,  A61K51/00 ,  C07F5/00

    CPC分类号： A61K49/0002 ,  C07B59/008

    摘要： The present invention relates to compounds labeled with imaging agents that also are capable of binding lectin-like oxidized low-density lipoprotein (LOX-1). The labeled compounds are useful for the diagnosis and monitoring of diseases in which inflammation plays a role, such as various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque and coronary artery disease, as well as rheumatoid arthritis.

    摘要翻译： 本发明涉及也能够结合凝集素样氧化低密度脂蛋白（LOX-1）的成像剂标记的化合物。 标记的化合物可用于诊断和监测炎症起作用的疾病，例如各种心血管疾病，包括但不限于动脉粥样硬化，易损斑块和冠状动脉疾病以及类风湿性关节炎。

    Pharmaceuticals for enhanced delivery to disease targets
    4.
    发明申请
    Pharmaceuticals for enhanced delivery to disease targets 审中-公开
    用于增强输送到疾病目标的药物

    公开(公告)号：US20050260131A1

    公开(公告)日：2005-11-24

    申请号：US10851359

    申请日：2004-05-20

    申请人： Mohan Amaratunga ,  Bahram Moasser ,  Faisal Syud ,  John Brogan ,  Daniel Kramer

    发明人： Mohan Amaratunga ,  Bahram Moasser ,  Faisal Syud ,  John Brogan ,  Daniel Kramer

    IPC分类号： C07H21/00 ,  C07K14/00 ,  A61K51/00 ,  A61K48/00 ,  A61K49/00 ,  C07K14/52 ,  C07K16/46

    CPC分类号： C07H21/00

    摘要： Pharmaceuticals for enhanced delivery to a disease target comprises a pair of compounds. The first compound comprises a first oligopeptide conjugated to a first moiety for coupling with a diagnostic or therapeutic active agent. The second compound comprises a second oligopeptide conjugated to a targeting species having a targeting moiety capable of binding to a target. The second oligopeptide has a sequence that is complementary to a sequence of the first oligopeptide. The first and second oligopeptides can be complementary PNA sequences. The pharmaceuticals are administered into a subject in methods for diagnosing or treating a disease condition, or assessing the effectiveness of a treatment of the disease condition.

    摘要翻译： 用于增强递送至疾病靶标的药物包含一对化合物。 第一化合物包含与第一部分缀合的第一寡肽，用于与诊断或治疗活性剂偶联。 第二化合物包含与具有能与靶标结合的靶向部分的靶向物质缀合的第二寡肽。 第二寡肽具有与第一寡肽的序列互补的序列。 第一和第二寡肽可以是互补的PNA序列。 药物在用于诊断或治疗疾病状况的方法或评估治疗疾病状况的有效性的方法中施用于受试者。

    Contrast agents for magnetic resonance imaging
    6.
    发明申请
    Contrast agents for magnetic resonance imaging 审中-公开
    磁共振成像对比剂

    公开(公告)号：US20050260137A1

    公开(公告)日：2005-11-24

    申请号：US10889618

    申请日：2004-07-12

    申请人： Havva Acar ,  Faisal Syud ,  Rachel Garaas ,  Peter Bonitatebus ,  Amit Kulkarni

    发明人： Havva Acar ,  Faisal Syud ,  Rachel Garaas ,  Peter Bonitatebus ,  Amit Kulkarni

    IPC分类号： A61K49/00 ,  A61K49/18

    CPC分类号： B82Y5/00 ,  A61K49/1839 ,  A61K49/186

    摘要： A contrast agent for magnetic resonance imaging having a plurality of nanoparticles. Each of the nanoparticles has: a signal generating core having a diameter of up to 10 nm; at least one organic layer of at least one of a polymer, a monomer, and a surfactant; and a water soluble outer shell of at least one of a polymer, a monomer, and a ligand. The organic layer is adsorbed upon and substantially surrounds and stabilizes the signal generating core. The water soluble outer shell solubilizes and provides biocompatibility for each of the nanoparticles. The contrast agents provide enhanced relaxivity, high signal-to-noise ratios, and targeting abilities. In addition, the contrast agents possess resistance to agglomeration, controlled particle size, blood clearance rate, and biodistribution. Methods of making such contrast agents and nanoparticles are also disclosed.

    摘要翻译： 一种用于具有多个纳米颗粒的磁共振成像的造影剂。 每个纳米颗粒具有：具有高达10nm的直径的信号产生芯; 聚合物，单体和表面活性剂中的至少一种的至少一种有机层; 以及聚合物，单体和配体中的至少一种的水溶性外壳。 有机层被吸附在基本上并且基本上包围和稳定信号产生芯。 水溶性外壳增溶并提供每种纳米颗粒的生物相容性。 造影剂提供增强的松弛度，高信噪比和靶向能力。 此外，造影剂具有抗凝集，受控粒度，血清清除率和生物分布。 还公开了制备这种造影剂和纳米颗粒的方法。

    Solid phase conjugation of complexing agents and targeting moieties
    7.
    发明申请
    Solid phase conjugation of complexing agents and targeting moieties 审中-公开
    络合剂和靶向部分的固相缀合

    公开(公告)号：US20060058218A1

    公开(公告)日：2006-03-16

    申请号：US10937323

    申请日：2004-09-10

    申请人： Faisal Syud ,  John Brogan ,  Daniel Kramer

    发明人： Faisal Syud ,  John Brogan ,  Daniel Kramer

    IPC分类号： A61K38/16 ,  C07K1/02

    CPC分类号： C07K1/13 ,  C07K1/1077

    摘要： There is provided a technique for conjugating one or more complexing agents with a targeting moiety, such as natural amino acids, unnatural amino acids, peptides, peptide nucleic acids, nucleotides, and analogs and derivatives thereof. The one or more complexing agents are conjugated at one or more free amino groups of the targeting moiety while the moiety is attached to a solid substrate.

    摘要翻译： 提供了一种用于将一种或多种络合剂与靶向部分（例如天然氨基酸，非天然氨基酸，肽，肽核酸，核苷酸及其类似物和衍生物）缀合的技术。 一种或多种络合剂在靶向部分的一个或多个游离氨基处缀合，而该部分连接到固体基质上。

    Compounds and methods for enhanced delivery to disease targets
    8.
    发明申请
    Compounds and methods for enhanced delivery to disease targets 审中-公开
    用于增强输送到疾病目标的化合物和方法

    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。