N-(4,5-Dihydroxy-6-hydroxymethyl-2-octyloxy-tetrahydro-pyran-3-yl)-acetamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(4,5-Dihydroxy-6-hydroxymethyl-2-octyloxy-tetrahydro-pyran-3-yl)-acetamide
• 英文别名: N-[4,5-dihydroxy-6-(hydroxymethyl)-2-octoxyoxan-3-yl]acetamide
• 化学式: C₁₆H₃₁NO₆
• 分子量: 333.42
• InChiKey: JXLKQDFJNOXCNT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  23
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  108
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• NOVEL TLR4 INHIBITORS FOR THE TREATMENT OF HUMAN INFECTIOUS AND INFLAMMATORY DISORDERS
  申请人：System of Higher Education University of Pittsburgh - of the Commonwealth

  公开号：US20130281395A1

  公开（公告）日：2013-10-24

  The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.

  本发明涉及通过给予新发现具有TLR4抑制活性的各种化合物来治疗感染性、炎症性和创伤后疾病的方法。除了治疗方法外，本发明还提供了包括所述化合物在内的药物组合物，以及适当的药物载体。由于TLR4是促炎性LPS信号级联中最上游的受体，本发明的治疗方法可以通过抑制或拮抗TLR4的作用来避免与其他细胞因子抑制剂相关的缺陷，这些细胞因子抑制剂作用于信号通路中较下游的位置，因此起到了不太特异（也许是非关键）的作用。
• N-ACETYGLUCOSAMINE DERIVATIVES AND USE THEREOF
  申请人：MIURA Kyoko

  公开号：US20080293673A1

  公开（公告）日：2008-11-27

  The present invention relates to An N-acetylglucosamine derivative represented by the following formula (1), and a hyaluronic acid production promoting agent containing the same and a skin external preparation containing the same: wherein R 1 is a hydrogen atom or an alkyl group having 2 to 18 carbon atoms; R 2 , R 3 , and R 4 are hydrogen atoms or acyl groups having 2 to 18 carbon atoms and may be all the same or different from others; the steric structure at position 1 may be α or β; provided that R 1 , R 2 , R 3 , and R 4 must not be all hydrogen atoms. It is intended to provide an easily available hyaluronic acid production promoting agent and a skin external preparation whereby the production of hyaluronic acid can be promoted in the skin and thus the skin can be maintained in a vital and moist state so that it is expected that the human skin can be prevented from age.

  本发明涉及以下式（1）所表示的N-乙酰葡萄糖氨衍生物，以及含有该衍生物的透明质酸生产促进剂和皮肤外用制剂：其中，R1是氢原子或具有2至18个碳原子的烷基；R2、R3和R4是氢原子或具有2至18个碳原子的酰基，可以全部相同或不同；位置1的立体结构可以是α或β；前提是R1、R2、R3和R4不能全部是氢原子。旨在提供一种易于获得的透明质酸生产促进剂和皮肤外用制剂，通过促进皮肤中透明质酸的产生，从而使皮肤保持活力和湿润状态，预防人体皮肤老化。
• TLR4 inhibitors for the treatment of human infectious and inflammatory disorders
  申请人：University of Pittsburgh—of the Commonwealth System of Higher Education

  公开号：US10300083B2

  公开（公告）日：2019-05-28

  The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.

  本发明涉及通过施用新发现的具有 TLR4 抑制活性的各种化合物来治疗感染性、炎症性和创伤后疾病的方法。除了治疗方法外，本发明还进一步提供了包含上述化合物的药物组合物以及合适的药物载体。由于 TLR4 是促炎性 LPS 信号转导级联中最上游的受体，本发明的治疗方法可抑制或拮抗 TLR4 的作用，从而避免与其他细胞因子抑制剂相关的陷阱，这些细胞因子抑制剂作用于更下游的通路，因此发挥的作用不那么特异（也许不那么关键）。
• Compositions and methods for treatment of inflammatory disorders
  申请人：THE JOHNS HOPKINS UNIVERSITY

  公开号：US10668092B2

  公开（公告）日：2020-06-02

  The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier.

  本发明涉及通过施用新发现的具有 TLR4 抑制活性的各种化合物来治疗感染性、炎症性和创伤后疾病的方法。除治疗方法外，本发明还进一步提供了药物组合物，其中包含上述化合物以及合适的药物载体。
• ANTAGONISTE SPÉCIFIQUE DE TLR4 DANS LE TRAITEMENT DU MYÉLOME MULTIPLE
  申请人：Etablissement Français du Sang

  公开号：EP3558323A1

  公开（公告）日：2019-10-30