(5-Acetamido-3,4-diacetyloxy-6-methoxyoxan-2-yl)methyl acetate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (5-Acetamido-3,4-diacetyloxy-6-methoxyoxan-2-yl)methyl acetate
• 化学式: C₁₅H₂₃NO₉
• mdl: MFCD01118823
• 分子量: 361.34
• InChiKey: BKJUFVXNIJMMKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  25
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  127
• 氢给体数：
  1
• 氢受体数：
  9

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。
• NUCLEIC ACID, COMPOSITION AND CONJUGATE CONTAINING SAME, AND PREPARATION METHOD AND USE
  申请人：Suzhou Ribo Life Science Co., Ltd.

  公开号：EP3719125A1

  公开（公告）日：2020-10-07

  Provided are a siRNA for inhibiting the expression of hepatitis B virus gene, and a pharmaceutical composition and conjugate containing the siRNA. Each nucleotide in the siRNA is independently a modified nucleotide. The siRNA comprises a sense strand and an antisense strand. The sense strand of the siRNA comprises a nucleotide sequence 1 having the same length and no more than three nucleotides different from the nucleotide sequence shown in SEQ ID NO: 155, and the antisense strand of the siRNA comprises a nucleotide sequence 2 having the same length and no more than three nucleotides different from the nucleotide sequence shown in SEQ ID NO: 156.

  本文提供了一种用于抑制乙型肝炎病毒基因表达的 siRNA，以及含有该 siRNA 的药物组合物和共轭物。 siRNA 中的每个核苷酸都是独立的修饰核苷酸。 siRNA 包括有义链和反义链。 siRNA 的有义链包括与 SEQ ID NO: 155 所示核苷酸序列具有相同长度且相差不超过三个核苷酸的核苷酸序列 1，而 siRNA 的无义链包括与 SEQ ID NO: 156 所示核苷酸序列具有相同长度且相差不超过三个核苷酸的核苷酸序列 2。
• NUCLEIC ACID, COMPOSITION AND CONJUGATE CONTAINING NUCLEIC ACID, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Suzhou Ribo Life Science Co., Ltd.

  公开号：EP3719126A1

  公开（公告）日：2020-10-07

  Provided are a siRNA for inhibiting the expression of an angiopoietin-like protein 3 (ANGPTL3) gene, and a pharmaceutical composition and a conjugate comprising the siRNA; wherein each nucleotide in the siRNA is independently a modified or unmodified nucleotide, and the siRNA comprises a sense strand and an antisense strand; the sense strand comprises a nucleotide sequence A, the nucleotide sequence A having the same length as the nucleotide sequence as represented by SEQ ID NO:1 with no more than 3 nucleotide differences; the antisense strand comprises a nucleotide sequence B, the nucleotide sequence B having the same length as the nucleotide sequence as represented by SEQ ID NO:2 with no more than 3 nucleotide differences.

  提供了一种用于抑制血管生成素样蛋白3(ANGPTL3)基因表达的siRNA，以及包含该siRNA的药物组合物和共轭物；其中，siRNA中的每个核苷酸独立地为修饰或未修饰的核苷酸，且siRNA包括有义链和反义链；有义链包括核苷酸序列A，该核苷酸序列A与SEQ ID NO.1所代表的核苷酸序列具有相同的长度，且核苷酸差异不超过3个；反义链包括核苷酸序列B，该核苷酸序列B与SEQ ID NO:1所代表的核苷酸序列具有相同的长度，且核苷酸差异不超过3个；反义链包括核苷酸序列C，该核苷酸序列C与SEQ ID NO:1所代表的核苷酸序列具有相同的长度，且核苷酸差异不超过3个：1 所代表的核苷酸序列具有相同的长度，但核苷酸差异不超过 3 个；反义链包括核苷酸序列 B，核苷酸序列 B 与 SEQ ID NO:2 所代表的核苷酸序列具有相同的长度，但核苷酸差异不超过 3 个。
• METHOD FOR SYNTHESIS OF REACTIVE CONJUGATE CLUSTERS
  申请人：Ionis Pharmaceuticals, Inc.

  公开号：EP3811977A1

  公开（公告）日：2021-04-28

  Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods. The reactive conjugate cluster has the formula: (L-A-N(H)C(=O)-E-)m-Bga wherein: L is a ligand; A is C2 to C10 alkyl optionally interrupted with one or more groups selected from -O-, -N(H)- and C(=O); E is a single bond or C1 to C10 alkyl optionally interrupted with one or more groups selected from -O-, -N(H)-and C(=O); Bga is a reactive branching group; m is from 2 to 6 - and C(=O); m is from 2 to about 6;

  本文提供了用于合成活性共轭簇的改进方法以及用于此类方法的中间体。特别是，本文提供的改进方法通过减少所需合成步骤的数量，提高了活性共轭簇的合成效率。使用改进方法制备的活性共轭簇不包括使用现有方法形成的任何反式酰化杂质。与现有方法相比，改进方法还能提高总体产量和成本效益。 活性共轭团簇的化学式为 (L-A-N(H)C(=O)-E-)m-Bga 其中 L 是配体； A 是选自-O-、-N(H)-和 C(=O)的一个或多个基团任选间断的 C2 至 C10 烷基； E 是单键或 C1 至 C10 烷基，可选择被一个或多个选自-O-、-N（H）- 和 C（=O）的基团打断 选自-O-、-N(H)-和 C(=O)的一个或多个基团； Bga 是活性分支基团； m 为 2 至 6 - 和 C（＝O）；m 为 2 至约 6；
• 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）。