DL-threo-1-phenyl-2-hexadecanoylamino-3-morpholino-1-propanol | 149022-18-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: DL-threo-1-phenyl-2-hexadecanoylamino-3-morpholino-1-propanol
• 英文别名: 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol；PPMP；1-phenyl-2-palimitoylamino-3-morpholino-1-propanol；1-phenyl-2-hexadecanoylamino-3-morpholino-1-propanol；DL-PPMP；N-[1-hydroxy-3-(morpholin-4-yl)-1-phenylpropan-2-yl]hexadecanamide；N-(1-hydroxy-3-morpholin-4-yl-1-phenylpropan-2-yl)hexadecanamide
• CAS: 149022-18-4
• 化学式: C₂₉H₅₀N₂O₃
• 分子量: 474.728
• InChiKey: OFBANDBMHLEMFA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.4
• 重原子数：
  34
• 可旋转键数：
  19
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] CONJUGATES OF THE B-SUBUNIT OF SHIGA TOXIN FOR ANTICANCER THERAPIES<br/>[FR] CONJUGUÉS DE LA SOUS-UNITÉ B DE TOXINE DE SHIGA POUR DES THÉRAPIES ANTICANCÉREUSES
  申请人：INST CURIE

  公开号：WO2014086952A1

  公开（公告）日：2014-06-12

  Conjugates or pharmaceutical compositions comprising conjugates of the B-subunit of Shiga toxin that are useful for cancer therapies are disclosed. More specifically, the pharmaceutical compositions comprise STxB conjugated to at least one antimitotic agent such as auristatin or pharmaceutically acceptable salts thereof through a bifunctional linker. Processes to make the conjugates, as well as methods to treat cancers are also disclosed.

  披露了用于癌症治疗的志贺毒素B亚单位偶联物或药物组合物。更具体地说，药物组合物包含通过双功能连接剂与至少一种抗有丝分裂剂如auristatin或药用可接受盐偶联的STxB。还披露了制造偶联物的方法以及治疗癌症的方法。
• Conjugates of the B-subunit of Shiga toxin for anticancer therapies
  申请人：Institut Curie

  公开号：EP2740493A1

  公开（公告）日：2014-06-11

  Conjugates or pharmaceutical compositions comprising conjugates of the B-subunit of Shiga toxin that are useful for cancer therapies are disclosed. More specifically, the pharmaceutical compositions comprise STxB conjugated to at least one antimitotic agent such as auristatin or pharmaceutically acceptable salts thereof through a bifunctional linker. Processes to make the conjugates, as well as methods to treat cancers are also disclosed.

  披露了用于癌症治疗的B亚单位志贺毒素偶联物或药物组合物。更具体地说，药物组合物包括通过双功能连接剂将STxB偶联至少一种抗有丝分裂剂，如auristatin或药用可接受盐。还披露了制造偶联物的方法以及治疗癌症的方法。
• SHIGA TOXIN B-SUBUNIT/CHEMOTHERAPEUTICS CONJUGATES
  申请人：Johannes Ludger

  公开号：US20110152252A1

  公开（公告）日：2011-06-23

  The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.

  本发明涉及使用志贺毒素B亚基部分作为治疗剂如抗癌剂的载体，例如，需要胞内摄取以发挥其抗癌效果的抗癌剂。尤其地，本发明提供了一种偶联物，该偶联物包括通过自焚间隔物与抗癌剂共价连接的志贺毒素部分，以及使用这种偶联物来增加抗癌药物的细胞摄取和/或对癌细胞的特异性的方法。还提供了涉及施用这种偶联物的治疗方法，以及用于执行这种治疗方法的药物组合物和试剂盒。
• Sphingosine Analogs, Compositions, and Methods Related Thereto
  申请人：Emory University

  公开号：US20140309275A1

  公开（公告）日：2014-10-16

  The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of or diagnosed with a malaria infection.

  该披露涉及化合物、药物组合物以及治疗或预防疾病的方法。在某些实施例中，该披露涉及治疗感染或癌症的方法，包括向需要的受试者施用本文披露的药物组合物。在典型实施例中，人们向患有疟疾感染风险、表现症状或被诊断患有疟疾感染的受试者施用含有鞘氨醇或鞘氨醇类似物的药物组合物。
• INHIBITORS OF THE SHIGA TOXINS TRAFFICKING THROUGH THE RETROGRADE PATHWAY
  申请人：Gillet Daniel

  公开号：US20110201601A1

  公开（公告）日：2011-08-18

  The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.

  本发明涉及使用一般式(I)和(II)化合物制备一种药物，用于预防和/或治疗由志贺毒素和相关毒素引起的疾病。