disodium;3,5-diiodo-1-methyl-4-oxopyridine-2,6-dicarboxylate

• 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: disodium;3,5-diiodo-1-methyl-4-oxopyridine-2,6-dicarboxylate
• 化学式: C8H3I2NNa2O5
• 分子量: 492.9
• InChiKey: GMQNYSMZUWAAIN-UHFFFAOYSA-L

计算性质

• 辛醇/水分配系数(LogP)：
  -7.67
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  101
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• Process for buffering concentrated aqueous slurries
  申请人：EASTMAN KODAK COMPANY

  公开号：EP0720046A2

  公开（公告）日：1996-07-03

  A process for buffering concentrated aqueous slurries comprising the steps of:    providing a particulate solid substance comprising a weak acid functional group, having effective pKa1 > 1 and less than 1% by weight aqueous solubility at pH = pKa1;    providing an aqueous solution consisting essentially of water or a mixture of water with water-miscible solvent, at pH less than the greater of 7 and pKa1 + 2;    providing a buffering salt of a weak acid, where the weak acid associated with this buffering salt has pKa2 and wherepKa1 - 2 ≦ pKa1'; and    combining said aqueous solution, said particulate solid substance, and said buffering salt to form a slurry;    wherein said process is essentially devoid of any step comprising the addition of any weak acid, other than that arising from reaction between said buffering salt and said particulate solid substance, having greater than 2% by weight aqueous solubility at pH = pKa1 is disclosed. An aqueous-based slurry comprising:    a particulate solid substance comprising a weak acid functional group having effective pKa1 > 1 and less than 1% by weight aqueous solubility at pH = pKa1;    an aqueous continuous phase at pH < pKa1 + 3;    a buffering salt of a weak acid, where the weak acid associated with this buffering salt has pKa1' and wherepKa1 - 2 ≦ pKa1'; and    where the incremental molar ionic strength in the continuous phase of said slurry resulting from said buffering salt is less than 0.04 mol/L is disclosed. A process for dispersing a particulate solid substance in a continuos aqueous phase comprising the steps of:    providing a comminution reactor;    providing a particulate solid substance comprising a weak acid functional group, having effective pKa1 > 1 and less than 1% by weight aqueous solubility at pH = pKa1;    providing an aqueous solution consisting essentially of water or a mixture of water with water-miscible solvent, at pH less than the greater of 7 and pKa1 + 2;    providing a buffering salt of a weak acid, where the weak acid associated with this buffering salt has pKa1' and wherepKa1 - 2 ≦ pKa1';    providing milling media;    combining said particulate solid substance, said aqueous solution, said buffering salt, and said milling media in said comminution reactor to produce a multiphase mixture; and    milling said mixture to produce a reduced particle size slurry of said particulate solid substance is disclosed.

  一种缓冲浓缩水浆的工艺，包括以下步骤 提供一种含有弱酸官能团的颗粒状固体物质，其有效 pKa1 > 1，且在 pH = pKa1 时的水溶性小于 1%（按重量计）； 提供一种主要由水或水与水混溶溶剂的混合物组成的水溶液，pH 值小于 7 和 pKa1 + 2 中的较大值； 提供弱酸缓冲盐，其中与该缓冲盐相关的弱酸具有 pKa2 且 pKa1 - 2 ≦ pKa1'；以及 将所述水溶液、所述颗粒状固体物质和所述缓冲盐混合形成浆液； 其中所述工艺基本上不包括添加任何弱酸的步骤，但所述缓冲盐和所述颗粒状固体物质之间的反应所产生的弱酸除外，本发明公开了在 pH = pKa1 时水溶性大于 2% （按重量计）的弱酸。 一种水基浆料，包括 含有弱酸官能团的颗粒状固体物质，其有效 pKa1 > 1，在 pH = pKa1 时的水溶性小于 1%（重量比）； 在 pH < pKa1 + 3 时的连续水相； 弱酸的缓冲盐，其中与该缓冲盐相关的弱酸具有 pKa1'，且 pKa1 - 2 ≦ pKa1'；以及由所述缓冲盐产生的所述浆液连续相中的摩尔离子强度增量小于 0.04 mol/L。 一种在连续水相中分散颗粒固体物质的工艺，包括以下步骤 提供一个粉碎反应器； 提供一种包含弱酸官能团的颗粒状固体物质，其有效 pKa1 > 1，在 pH = pKa1 时的水溶性小于 1%（按重量计）； 提供一种主要由水或水与水混溶溶剂的混合物组成的水溶液，pH 值小于 7 和 pKa1 + 2 中的较大值； 提供弱酸缓冲盐，其中与该缓冲盐相关的弱酸具有 pKa1'，且 pKa1 - 2 ≦ pKa1'； 提供研磨介质； 在所述粉碎反应器中将所述颗粒固体物质、所述水溶液、所述缓冲盐和所述研磨介质混合，以产生多相混合物；以及 公开了研磨所述混合物以产生所述颗粒状固体物质的粒径减小浆料的方法。
• Pharmaceutical combination comprising adenosine A1 receptor antagonists and radiocontrast media
  申请人：Solvay Pharmaceuticals GmbH

  公开号：EP1870093A1

  公开（公告）日：2007-12-26

  The present invention relates to pharmaceutical combinations comprising a therapeutically effective amount of at least one selective adenosine A1 antagonist combined with at least one radiocontrast media. The invention also relates to the use of said combinations in the manufacture of a medicament for the treatment of radiocontrast media induced nephropathy. Furthermore, the invention is relating to a kit comprising a single dosage form of said combination of at least one adenosine A1 antagonist and at least one radiocontrast media.

  本发明涉及由治疗有效量的至少一种选择性腺苷 A1 拮抗剂与至少一种放射性造影剂组合而成的药物组合物。本发明还涉及使用所述组合物制造治疗放射性造影剂诱发的肾病的药物。此外，本发明还涉及一种试剂盒，该试剂盒包含上述至少一种腺苷 A1 拮抗剂和至少一种放射造影剂组合的单一剂型。
• CERASOME DELIVERY SYSTEM FOR USE IN TARGETED ACTIVATION OF CD44 MOLECULE, PREPARATION METHOD THEREFOR AND USE
  申请人：Beijing Inno Medicine Co., Ltd.

  公开号：EP3610859A1

  公开（公告）日：2020-02-19

  A cerasome delivery system for use in the targeted activation of a CD44 molecule, a preparation method and use thereof: a surface of a cerasome is partially modified by a targeting ligand, the targeting ligand being a ligand which may specifically bind to an activated CD44 molecule. The cerasome delivery system may be used for the diagnosis, prevention and treatment of vulnerable plaque or diseases associated with vulnerable plaque.

  一种用于靶向激活 CD44 分子的 cerasome 递送系统、其制备方法和用途：cerasome 的表面部分被靶向配体修饰，靶向配体是一种可与激活的 CD44 分子特异性结合的配体。该cerasome递送系统可用于易损斑块或与易损斑块相关疾病的诊断、预防和治疗。
• LIPOSOMAL NANOCARRIER DELIVERY SYSTEM FOR TARGETING ACTIVE CD44 MOLECULE, PREPARATION METHOD THEREFOR, AND USES THEREOF
  申请人：Beijing Inno Medicine Co., Ltd.

  公开号：EP3744317A1

  公开（公告）日：2020-12-02

  A liposomal nanocarrier delivery system for targeting an active CD44 molecule, preparation method therefor, and uses thereof. The surface of the liposome is partially modified by a targeting ligand, wherein the targeting ligand is a ligand that can be specifically combined with the active CD44 molecule. The liposomal nanocarrier delivery system can be used for diagnosing, preventing, and treating vulnerable plaque or diseases related to vulnerable plaque.

  一种用于靶向活性 CD44 分子的脂质体纳米载体递送系统、其制备方法及其用途。脂质体的表面部分被靶向配体修饰，其中靶向配体是可与活性 CD44 分子特异性结合的配体。该脂质体纳米载体递送系统可用于诊断、预防和治疗易损斑块或与易损斑块相关的疾病。
• Methods and compositions for treating conditions associated with an abnormal inflammatory responses
  申请人：First Wave Bio, Inc.

  公开号：US10292951B2

  公开（公告）日：2019-05-21

  This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

  本公开的化学实体（例如，具有线粒体解偶联剂活性的化合物或其药学上可接受的盐和/或水合物和/或共晶体；例如，化合物，如烟酰胺或其药学上可接受的盐和/或水合物和/或共晶体；例如、化合物，如尼可刹米类似物，或其药学上可接受的盐和/或水合物和/或共晶体），这些化合物可用于治疗受试者（如人类）中以异常炎症反应（如炎症性肠病）为特征的病理学的一种或多种症状。本公开内容还包括组合物以及使用和制造组合物的其他方法。