N-[2-(dimethylamino)ethyl]succinamic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: N-[2-(dimethylamino)ethyl]succinamic acid
• 英文别名: N-DIMETHYLAMINOETHYL SUCCINAMIC ACID；N-(2-dimethylaminoethyl)succinamic acid；4-[2-(Dimethylazaniumyl)ethylamino]-4-oxobutanoate
• 化学式: C₈H₁₆N₂O₃
• mdl: MFCD00463406
• 分子量: 188.227
• InChiKey: JCEDFENUDVHGNH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.3
• 重原子数：
  13
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  69.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  丁二酰氯 、 N,N-二甲基乙二胺 以 乙腈 为溶剂， 以84%的产率得到N-[2-(dimethylamino)ethyl]succinamic acid
  参考文献：
  名称：

  Biodegradable particulate vector for transporting molecules having

  摘要：

  准备一种可生物降解的颗粒载体，用于运输生物活性分子，包含一个包含生物活性分子的核心，一个共价键合到核心的第一层脂肪酸化合物和一个疏水键合到第一层的磷脂的第二层。核心的尺寸在10纳米到10微米之间，由交联多糖或寡糖基质形成，离子配体均匀地嫁接在其上。交联多糖可以是经环氧氯丙烷交联的葡聚糖、纤维素或淀粉。配体可以是从琥珀酸、磷酸、柠檬酸、甘氨酸、丙氨酸、谷氨酸和天冬氨酸中选择的酸性化合物，或者是胆碱、羟基胆碱、2-(二甲氨基)乙醇或2-(二甲氨基)乙胺等碱性化合物，通过酸性化合物固定在基质上。多糖或寡糖可以与角蛋白/胶原蛋白或弹性蛋白等蛋白共交联。可以通过将琥珀酸单氯化物在水溶液中与交联多糖或寡糖基质反应，嫁接琥珀酸到基质形成核心，研磨核心至尺寸在10纳米到10微米之间，干燥磨碎的核心，将脂肪酸化合物偶联到核心形成第一层，将磷脂疏水键合到第一层形成第二层来制备载体。琥珀酸单氯化物最好是通过将琥珀酸二氯化物与游离琥珀酸反应形成纯结晶的琥珀酸单氯化物而制备的。

  公开号：

  US05736371A1

文献信息

• Streptogramin derivatives, their preparation and compositions containing them
  申请人：Aventis Pharma S.A.

  公开号：US06569854B1

  公开（公告）日：2003-05-27

  Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond - - - represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they exist.

  通用公式（I）中的A组链霉素衍生物，其中： R1代表卤素原子或偶氮基或硫氰基， R2代表氢原子或甲基或乙基基， R3代表氢原子，或脂肪、环脂、芳香、芳基脂肪、杂环或杂环脂肪酯的残基，可能被取代， 连接- - - 代表单键（立体化学27R）或双键， 以及存在时的盐。
• Tetracyclic Anthraquinone Derivatives
  申请人：Tianjin Hemay Bio-Tech Co., Ltd

  公开号：US20150166595A1

  公开（公告）日：2015-06-18

  Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, n are defined as in the present application.

  公开了一种由式（I）表示的化合物及其药用可接受的盐，其中R1、R2、R3、R4、R5、W、n的定义如本申请中所述。
• Polarity-Tuning Derivatization-LC-MS Approach for Probing Global Carboxyl-Containing Metabolites in Colorectal Cancer
  作者：Xiqing Bian、Na Li、Binbin Tan、Baoqing Sun、Ming-Quan Guo、Guoxin Huang、Li Fu、W. L. Wendy Hsiao、Liang Liu、Jian-Lin Wu

  DOI：10.1021/acs.analchem.8b01873

  日期：2018.10.2

  Carboxyl-containing metabolites (CCMs) widely exist in living systems and are the essential components for life. Global characteristics of CCMs in biological samples are critical for the understanding of physiological processes and the discovery for the onset of relevant diseases. However, their determination represents a challenge due to enormous polarity differences, structural diversity, high structural similarity, and poor ionization efficiency in mass spectrometry. Herein, 5-(diisopropylamino)amylamine (DIAAA) derivatization coupled with liquid chromatography–mass spectrometry (LC-MS) was developed for mapping the CCMs. With this methodology, the sensitivity was significantly enhanced. More importantly, the hydrophobicity of polar CCMs, amino acids, TCA cycle intermediates, and short-chain fatty acids and the hydrophilicity of low-polar CCMs, long-chain fatty acids, and bile acids were significantly increased, resulting in a remarkable separation efficiency for which 68 CCMs can be simultaneously determined. Furthermore, the polarity-tuning effect was confirmed to be induced by the different impacts of aliphatic chains and nitrogen atom in DIAAA, the latter existing as a cation in the acidic mobile phase, using different derivatization reagents. Finally, this derivatization method was utilized to hunt for the potential biomarkers in colorectal cancer (CRC) patients and 52 CCMs, related with several key metabolic pathways, including amino acids metabolism, TCA cycle, fatty acid metabolism, pyruvate metabolism, and gut flora metabolism were identified. This innovative polarity-tuning derivatization-LC-MS approach was proved to be a valuable tool for probing global metabolome with high separation efficiency and sensitivity in various biological samples.

  含羧基代谢物（CCMs）广泛存在于生物系统中，是生命的基本组成部分。CCMs在生物样本中的全球特征对于理解生理过程和发现相关疾病的发生具有重要意义。然而，由于极性差异巨大、结构多样性、高结构相似性和在质谱中的离子化效率较低，它们的测定面临挑战。在此，我们开发了5-(二异丙基氨基)戊胺（DIAAA）衍生化结合液相色谱-质谱（LC-MS）的方法以绘制CCMs的分布。通过这种方法，灵敏度显著提高。更重要的是，极性CCMs、氨基酸、TCA循环中间体和短链脂肪酸的疏水性显著增强，而低极性CCMs、长链脂肪酸和胆汁酸的亲水性也显著增加，从而实现了卓越的分离效率，使得68种CCMs可以同时测定。此外，极性调节效应被证实是由于DIAAA中脂肪链和氮原子的不同影响所引起的，后者在酸性流动相中以阳离子的形式存在，使用不同的衍生化试剂。最后，该衍生化方法被用于寻找结直肠癌（CRC）患者的潜在生物标志物，识别出52种与多条关键代谢通路（包括氨基酸代谢、TCA循环、脂肪酸代谢、丙酮酸代谢和肠道菌群代谢）相关的CCMs。这种创新的极性调节衍生化-LC-MS方法被证明是探测各种生物样本全球代谢组的高分离效率和灵敏度的有价值工具。
• Tetracyclic anthraquinone derivatives
  申请人：TIANJIN HEMAY ONCOLOGY PHARMACEUTICAL CO., LTD.

  公开号：US10294260B2

  公开（公告）日：2019-05-21

  Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, W, n are defined as in the present application. Also disclosed is a method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound and a salt thereof according to the present application possess good anticancer and/or antitumor activity, and good water solubility and stability, as well as good tolerance in animal bodies. Also disclosed is a process for preparing a compound represented by formula (I) of the present application.

  公开了一种由式 (I) 代表的化合物及其药学上可接受的盐、 其中 R1、R2、R3、R4、R5、W、n 的定义与本申请相同。还公开了一种治疗癌症的方法，包括向有需要的受试者施用治疗有效量的式 (I) 所代表的化合物或其药学上可接受的盐。根据本申请的化合物及其盐具有良好的抗癌和/或抗肿瘤活性、良好的水溶性和稳定性，以及在动物体内良好的耐受性。本申请还公开了一种制备式（I）所代表的化合物的工艺。
• TETRACYCLIC ANTHRAQUINONE DERIVATIVES
  申请人：Tianjin Hemay Bio-Tech Co., Ltd.

  公开号：EP2824108B1

  公开（公告）日：2017-04-19