N-succinimidyl 5-iodo-3-pyridinecarboxylate | 131865-61-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: N-succinimidyl 5-iodo-3-pyridinecarboxylate
• 英文别名: N-Succinimidyl-5-iodo-3-pyridinecarboxylic acid；(2,5-dioxopyrrolidin-1-yl) 5-iodopyridine-3-carboxylate
• CAS: 131865-61-7
• 化学式: C₁₀H₇IN₂O₄
• 分子量: 346.081
• InChiKey: PZINFSHCXYXHOY-UHFFFAOYSA-N

物化性质

• 沸点：
  454.1±55.0 °C(Predicted)
• 密度：
  2.03±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  76.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-amino-6,7-dimethoxy-2-(piperazin-1-yl)quinoline 、 N-succinimidyl 5-iodo-3-pyridinecarboxylate 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以35%的产率得到4-amino-6,7-dimethoxy-2-[4-(5-iodonicotinoyl)piperazinyl]quinoline
  参考文献：
  名称：

  Radioiodinated ?1-adrenergic receptor ligands

  摘要：

  本文描述了三种放射性碘化α1-肾上腺素能受体配体[125I]5a-c的合成和初步表征。这些示踪剂是L-760,478,1b的类似物，而L-760,478,1b本身是哌唑嗪1a的类似物。最高亲和力的示踪剂[125I]5a对α1受体亚型的亲和力比哌唑嗪高六倍。这些配体可用于α1受体亚型的自动放射研究。版权所有 © 2001 John Wiley & Sons, Ltd.

  DOI：

  10.1002/jlcr.433

文献信息

• SPECIFIC BINDING PROTEINS AND USES THEREOF
  申请人：Old Lloyd J.

  公开号：US20110076232A1

  公开（公告）日：2011-03-31

  The present invention relates to specific binding members, particularly antibodies and fragments thereof, which bind to amplified epidermal growth factor receptor (EGFR) and to the de2-7 EGFR truncation of the EGFR. In particular, the epitope recognized by the specific binding members, particularly antibodies and fragments thereof, is enhanced or evident upon aberrant post-translational modification. These specific binding members are useful in the diagnosis and treatment of cancer. The binding members of the present invention may also be used in therapy in combination with chemotherapeutics or anti-cancer agents and/or with other antibodies or fragments thereof.

  本发明涉及特定结合成员，尤其是与扩增的上皮生长因子受体（EGFR）和EGFR的de2-7 EGFR截短形式结合的抗体及其片段。特别是，当发生异常的翻译后修饰时，特定结合成员，尤其是抗体及其片段所识别的表位会被增强或显现。这些特定结合成员在癌症的诊断和治疗中非常有用。本发明的结合成员还可以与化疗药物或抗癌剂以及/或其他抗体或其片段联合使用于治疗中。
• METHODS OF PREPARING TRIAZOLE-CONTAINING RADIOIODINATED COMPOUNDS
  申请人：Valliant John

  公开号：US20140065070A1

  公开（公告）日：2014-03-06

  The present application relates to methods of preparing radiohalogenated compounds, to compounds useful in such methods and to radiohalogenated compounds useful for imaging and/or therapy. In particular, the present application relates to methods of preparing radiohalogenated compounds of Formula I, to compounds useful in such methods and to radiohalogenated compounds of Formula I:

  本申请涉及制备放射性卤代化合物的方法，以及在这些方法中有用的化合物和用于成像和/或治疗的放射性卤代化合物。具体而言，本申请涉及制备Formula I的放射性卤代化合物的方法，以及在这些方法中有用的化合物和Formula I的放射性卤代化合物。
• Specific binding proteins and uses thereof
  申请人：Old Lloyd J.

  公开号：US20090220510A1

  公开（公告）日：2009-09-03

  The invention relates to specific binding members, particularly antibodies and active fragments thereof, which recognize an aberrant post-translationally modified, particularly an aberrant glycosylated form of the EGFR. The binding members, particularly antibodies and fragments thereof, of the invention do not bind to EGFR on normal cells in the absence of amplification of the wild-type gene and are capable of binding the de2-7 EGFR at an epitope which is distinct from the junctional peptide. Antibodies of this type are exemplified by the novel antibody 806 whose VH and VL sequences are illustrated as SEQ ID NOs: 2 and 4 and chimeric antibodies thereof as exemplified by ch806.

  该发明涉及特定结合成员，特别是抗体及其活性片段，这些成员能够识别异常的翻译后修饰，特别是EGFR的异常糖基化形式。该发明的结合成员，特别是抗体及其片段，在野生型基因扩增的情况下不与正常细胞上的EGFR结合，并且能够与一个与连接肽不同的表位上的de2-7 EGFR结合。这种类型的抗体以新型抗体806为例，其VH和VL序列示例为SEQ ID NOs：2和4，以及以ch806为例的嵌合抗体。
• PSMA-BINDING AGENTS AND USES THEREOF
  申请人：Pomper Martin

  公开号：US20110142760A1

  公开（公告）日：2011-06-16

  Prostate-specific membrane antigen (PSMA) binding compounds having radioisotope substituents are described, as well as chemical precursors thereof. Compounds include pyridine containing compounds, compounds having phenylhydrazine structures, and acylated lysine compounds. The compounds allow ready incorporation of radionuclides for single photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging, for example, prostate cancer cells and angiogenesis.

  本文描述了具有放射性同位素替代基的前列腺特异性膜抗原（PSMA）结合化合物，以及它们的化学前体。这些化合物包括含有吡啶结构的化合物、含有苯肼结构的化合物和酰化赖氨酸化合物。这些化合物允许容易地纳入放射性核素，用于单光子发射计算机断层扫描（SPECT）和正电子发射断层扫描（PET）成像，例如前列腺癌细胞和血管生成。
• Multifunctional stealth nanoparticles for biomedical use
  申请人：Centre National de la Recherche Scientifique

  公开号：EP2210616A1

  公开（公告）日：2010-07-28

  The present invention relates to the field of drug delivery nanosystems. More precisely, the present invention concerns a copolymer with advantageous properties for the outer coating of various nanoparticles. Said copolymer comprises at least three types of monomers with stealthy, coupling and therapeutic properties respectively, as well as an optional fourth type of monomers with targeting properties. The present invention also relates to core-shell or hollow shell nanoparticles coated by an external layer of the copolymer according to the invention. Several types of core-shell nanoparticles are envisaged. The invention also concerns methods for preparing said nanoparticles, as well as pharmaceutical compositions or medicaments comprising them.

  本发明涉及给药纳米系统领域。更确切地说，本发明涉及一种具有优势特性的共聚物，可用于各种纳米粒子的外涂层。所述共聚物包括至少三种分别具有隐形、耦合和治疗特性的单体，以及可选的第四种具有靶向特性的单体。本发明还涉及由本发明共聚物外层包覆的核壳或空壳纳米粒子。本发明设想了多种类型的核壳纳米粒子。本发明还涉及制备上述纳米粒子的方法，以及包含这些纳米粒子的药物组合物或药物。