5-methoxymethyluridine | 82448-44-0

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 5-methoxymethyluridine
• 英文别名: 1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(methoxymethyl)pyrimidine-2,4-dione
• CAS: 82448-44-0
• 化学式: C₁₁H₁₆N₂O₇
• 分子量: 288.257
• InChiKey: PDXQSLIBLQMPJS-FDDDBJFASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.3
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  129
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  5-methoxymethyluridine 生成 (2R,4R,5S,6S)-5-hydroxy-4-(hydroxymethyl)-11-(methoxymethyl)-3,7-dioxa-1,9-diazatricyclo[6.4.0.02,6]dodeca-8,11-dien-10-one
  参考文献：
  名称：

  CAKATA, SINDZI

  摘要：

  DOI：
• 作为产物：
  描述：

  5-methoxymethyl-1-(2',3',5'-tri-O-benzoyl-β-D-ribofuranosyl)pyrimidine-2,4(1H,3H)-dione 在 氨 作用下， 以 甲醇 为溶剂， 生成 5-methoxymethyluridine
  参考文献：
  名称：

  Synthesis of various 5-alkoxymethyluracil analogues and structure–cytotoxic activity relationship study

  摘要：

  A number of 5-alkoxymethyluracil analogues were synthesized to evaluate their cytotoxic activity. 5-Alkoxymethyluracil derivatives 1 were prepared via known nucleophilic substitution of 5-chloromethyluracil 5 and subsequently transformed to their corresponding nucleosides 2. All prepared compounds were submitted to cytotoxic activity testing against drug sensitive and drug resistant leukaemia cells and solid tumour derived cell lines. In addition, the cytotoxic activity of 5-alkoxymethyluracil analogues 1 and 2 was compared with the previously published 5-[alkoxy(4-nitrophenyl)methyl]uracil analogues 3 and 4. Extensive structure-cytotoxic activity relationship studies are reported. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.carres.2011.07.026

文献信息

• Anti-HCV nucleoside derivatives
  申请人：——

  公开号：US20030008841A1

  公开（公告）日：2003-01-09

  The present invention comprises novel and known purine and pyrimidine nucleoside derivatives which have been discovered to be active against hepatitis C virus (HCV). The use of these derivatives for the treatment of HCV infection is claimed as are the novel nucleoside derivatives disclosed herein.

  本发明涉及新颖和已知的嘌呤和嘧啶核苷衍生物，已发现这些衍生物对丙型肝炎病毒（HCV）具有活性。本发明声明利用这些衍生物治疗HCV感染，以及本文所披露的新颖核苷衍生物。
• POLYNUCLEOTIDES ENCODING COAGULATION FACTOR VIII
  申请人：ModernaTX, Inc.

  公开号：US20200268666A1

  公开（公告）日：2020-08-27

  The invention relates to mRNA therapy for the treatment of Hemophilia A. mRNAs for use in the invention, when administered in vivo, encode Factor VIII, isoforms thereof, functional fragments thereof, and fusion proteins comprising Factor VIII. mRNAs of the invention are preferably encapsulated in lipid nanoparticles (LNPs) to effect efficient delivery to cells and/or tissues in subjects, when administered thereto. mRNA therapies of the invention increase and/or restore deficient levels of Factor VIII expression and/or activity in subjects. mRNA therapies of the invention further decrease levels of toxic metabolites associated with deficient Factor VII I activity in subjects.

  该发明涉及用于治疗血友病A的mRNA疗法。该发明中使用的mRNA，在体内给予时，编码因子VIII，其异构体，其功能性片段，以及包含因子VIII的融合蛋白。该发明中的mRNA最好封装在脂质纳米粒子（LNPs）中，以实现有效地输送到受试者的细胞和/或组织中，当向其给予时。该发明中的mRNA疗法增加和/或恢复受试者中因子VIII表达和/或活性不足的水平。该发明中的mRNA疗法进一步降低与受试者中因子VIII活性不足相关的有毒代谢物的水平。
• [EN] MRNAS ENCODING IMMUNE MODULATING POLYPEPTIDES AND USES THEREOF<br/>[FR] ARNM CODANT DES POLYPEPTIDES DE MODULATION IMMUNITAIRE ET LEURS UTILISATIONS
  申请人：MODERNA TX INC

  公开号：WO2021076805A1

  公开（公告）日：2021-04-22

  The disclosure features lipid nanoparticle (LNP) compositions comprising immune modulating polypeptides and uses thereof. The LNP compositions of the present disclosure comprise mRNA therapeutics encoding immune modulating polypeptides, e.g., interleukin 2 (IL- 2) and/or granulocyte macrophage colony stimulating factor (GM-CSF). The LNP compositions of the present disclosure can stimulate T regulatory cells, e.g., increase the level and/or activity of T regulatory cells in vivo or ex vivo.

  披露了包含免疫调节多肽的脂质纳米粒子（LNP）组合物及其用途。本公开的LNP组合物包括编码免疫调节多肽的mRNA治疗药物，例如白细胞介素2（IL-2）和/或粒细胞巨噬细胞集落刺激因子（GM-CSF）。本公开的LNP组合物可以刺激T调节细胞，例如在体内或体外增加T调节细胞的水平和/或活性。
• [EN] CHEMICALLY MODIFIED MESSENGER RNA'S<br/>[FR] ARN MESSAGER CHIMIQUEMENT MODIFIÉ
  申请人：NOVARTIS AG

  公开号：WO2017153936A1

  公开（公告）日：2017-09-14

  This invention provides messenger RNA (mRNA) molecules comprising comprising an open reading frame that encodes a protein of interest, wherein said modified RNA comprises a modified nucleoside selected from the group consisting of: (I), (II), and (III), gene therapy vectors comprising same, methods of synthesizing same, and methods for gene replacement, gene therapy, gene transcription silencing, and the delivery of therapeutic proteins to tissue in vivo, comprising the molecules. The present invention also provides methods of reducing the immunogenicity of mRNA molecules.

  本发明提供了包含开放阅读框的信使RNA（mRNA）分子，该开放阅读框编码所需蛋白质的RNA被修改，所述修改的核苷酸选自以下组：（I），（II）和（III），包括同样的基因治疗载体，合成同样的方法，以及基因替换、基因治疗、基因转录沉默和递送治疗蛋白到体内组织的方法，包括这些分子。本发明还提供了减少mRNA分子免疫原性的方法。
• [EN] LIPID NANOPARTICLE COMPOSITIONS AND METHODS OF FORMULATING THE SAME<br/>[FR] COMPOSITIONS DE NANOPARTICULES LIPIDIQUES ET LEURS PROCÉDÉS DE FORMULATION
  申请人：MODERNATX INC

  公开号：WO2022178199A1

  公开（公告）日：2022-08-25

  Provided herein are methods of reducing adduct formation in lipid nanoparticle compositions comprising a polynucleotide, such as mRNA, and an ionizable lipid; also disclosed are lipid nanoparticle compositions having a reduced adduct content, and methods of detecting the adducts.

  本文提供了一种减少脂质纳米粒子组合物中加合物形成的方法，该组合物包括多核苷酸（如mRNA）和离子化脂质；本文还披露了具有减少加合物含量的脂质纳米粒子组合物，以及检测加合物的方法。