MQT-1426

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: MQT-1426
• 英文别名: D-Lys-N1-spermine；(2R)-2,6-diamino-N-[3-[4-(3-aminopropylamino)butylamino]propyl]hexanamide
• 化学式: C₁₆H₃₈N₆O
• 分子量: 330.517
• InChiKey: XTNRHIZWLNLONB-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  23
• 可旋转键数：
  17
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  131
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  精胺 在 盐酸 、 sodium carbonate 作用下， 以 四氢呋喃 、 甲醇 、 水 为溶剂， 反应 18.0h， 生成 MQT-1426
  参考文献：
  名称：

  Lysine–spermine conjugates: hydrophobic polyamine amides as potent lipopolysaccharide sequestrants

  摘要：

  Lipopolysaccharides (LPS), otherwise termed `endotoxins' are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of `Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammatory processes by targeting lipopolysaccharide do not exist at the present time. We have defined the pharmacophore necessary for small molecules to specifically bind and neutralize LPS and, using animal models of sepsis, have shown that the sequestration of circulatory LPS by small molecules is a therapeutically viable strategy. In this paper, the interactions of a focused library of lysine-spermine conjugates with lipopolysaccharide (LPS) have been characterized. Lysine-spermine conjugates with the epsilon-amino terminus of the lysinyl moiety derivatized with long-chain aliphatic hydrophobic substituents in acyl or alkyl linkage bind and neutralize bacterial lipopolysaccharides, and may be of use in the prevention or treatment of endotoxic shock states. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.01.038

文献信息

• BIOAVAILABLE POLYAMINES
  申请人：Aminex Therapeutics, Inc.

  公开号：EP3785706A1

  公开（公告）日：2021-03-03

  Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

  本文公开了阳离子质子化多胺药剂和阴离子有机羧酸盐的药剂盐，后者在质子化形式时具有疏水性，特别适合口服给药，这些盐在固体剂型中具有良好的生物利用度，可用于治疗癌症和药剂所针对的其他病症。
• Bioavailable polyamines
  申请人：AMINEX THERAPEUTICS INC.

  公开号：US10632145B2

  公开（公告）日：2020-04-28

  Disclosed herein are pharmaceutical salts of a cationic protonated polyamine pharmaceutical agent and an anionic organic carboxylate which is hydrophobic when in protonated form, particularly suited for oral administration, where these salts have good bioavailability in solid dosage forms and may be used in the treatment of cancer and other medical conditions for which the pharmaceutical agent is intended.

  本文公开了阳离子质子化多胺药剂和阴离子有机羧酸盐的药剂盐，后者在质子化形式时具有疏水性，特别适合口服给药，这些盐在固体剂型中具有良好的生物利用度，可用于治疗癌症和药剂所针对的其他病症。
• HYDROPHOBIC POLYAMINE ANALOGS AND METHODS FOR THEIR USE
  申请人：Aminex Therapeutics, Inc.

  公开号：EP1373185B1

  公开（公告）日：2017-03-01
• COMPOSITIONS AND METHODS FOR USE OF EFLORNITHINE AND DERIVATIVES AND ANALOGS THEREOF TO TREAT CANCERS, INCLUDING GLIOMAS
  申请人：Orbus Therapeutics, Inc.

  公开号：US20170273926A1

  公开（公告）日：2017-09-28

  Eflornithine is an agent that can be used to treat glioma, especially glioma of WHO Grade II or Grade III such as anaplastic glioma. Eflornithine can suppress or prevent mutations in glioma which can cause the glioma to progress to a higher grade. Compositions and methods can include eflornithine or a derivative or analog of eflornithine, together with other agents such as conventional anti-neoplastic agents for treatment of glioma, inhibitors of polyamine transport, polyamine analogs, or S-adenosylmethionine decarboxylase inhibitors.
• Combination Drug Substance of Polyamine Transport Inhibitor and DFMO
  申请人：Aminex Therapeutics, Inc.

  公开号：US20220096412A1

  公开（公告）日：2022-03-31

  Provided herein are combinations comprising difluoromethylornithine (DFMO), or an ionic form thereof, and a compound of the following structural formula: or a protonated form thereof, wherein values for the variables (e.g., a, b, c, d, e, n, R 1 , R 2 , X) are described herein. The combinations can provide combination drug therapy in a single pharmaceutical dosage form, and be used, for example, for the treatment of cancer.