2'-O-(α-Methoxyethyl)-Guanosin | 56673-96-2

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷
• 英文名称: 2'-O-(α-Methoxyethyl)-Guanosin
• 英文别名: O^2'-(1-methoxy-ethyl)-guanosine；2-amino-9-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-(1-methoxyethoxy)oxolan-2-yl]-1H-purin-6-one
• CAS: 56673-96-2
• 化学式: C₁₃H₁₉N₅O₆
• 分子量: 341.324
• InChiKey: HGYFQNUWUWZCLU-NRJACJQQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  153
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• PROCESS FOR THE SYNTHESIS OF 2'-O-SUBSTITUTED PURINES
  申请人：Ravikumar Vasulinga

  公开号：US20080234475A1

  公开（公告）日：2008-09-25

  The present invention provides an improved process for the synthesis of 2′-O-substituted purine nucleosides. The process includes anhydro or thioanhydro ring opening of a selected 8,2′-cyclopurine nucleoside with a weak nucleophile in the presence of a Lewis acid ester, followed by reduction to afford the desired 2′-O-substituted purine nucleoside.

  本发明提供了一种改进的合成2'-O-取代嘌呤核苷的方法。该方法包括在路易斯酸酯的存在下，使用弱亲核试剂进行选择性的8,2'-环戊嘧啶核苷的无水或硫醇无水环开启，然后还原以得到所需的2'-O-取代嘌呤核苷。
• ENA NUCLEIC ACID DRUGS MODIFYING SPLICING IN mRNA PRECURSOR
  申请人：Matsuo, Masafumi

  公开号：EP1568769A1

  公开（公告）日：2005-08-31

  Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides.

  具有与肌营养不良蛋白 cDNA（基因库登录号 NM_004006.1）的核苷酸编号如 2571-2607、2578-2592、2571-2592、2573-2592、2578-2596、2578-2601 或 2575-2592 互补的核苷酸序列的寡核苷酸，以及包含此类寡核苷酸的肌营养不良症治疗剂。
• ENA Nucleic Acid Drugs Modifying Splicing in mRNA Precursor
  申请人：Matsuo, Masafumi

  公开号：EP2392660A2

  公开（公告）日：2011-12-07

  Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides.

  具有与肌营养不良蛋白 cDNA（基因库登录号 NM_004006.1）的核苷酸编号如 2571-2607、2578-2592、2571-2592、2573-2592、2578-2596、2578-2601 或 2575-2592 互补的核苷酸序列的寡核苷酸，以及包含此类寡核苷酸的肌营养不良症治疗剂。
• ENA nucleic acid drugs modifying splicing in mRNA precursor
  申请人：Matsuo, Masafumi

  公开号：EP2530153A1

  公开（公告）日：2012-12-05

  Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides.

  具有与肌营养不良蛋白 cDNA（基因库登录号 NM_004006.1）的核苷酸编号如 2571-2607、2578-2592、2571-2592、2573-2592、2578-2596、2578-2601 或 2575-2592 互补的核苷酸序列的寡核苷酸，以及包含此类寡核苷酸的肌营养不良症治疗剂。
• ANTISENSE OLIGONUCLEOTIDE CAPABLE OF ALTERING SPLICING OF DUX4 PRE-MRNA
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3998108A1

  公开（公告）日：2022-05-18

  The present invention aims at establishing a novel therapy for facioscapulohumeral muscular dystrophy. An oligonucleotide or a pharmaceutically acceptable salt thereof, wherein the oligonucleotide comprises an oligonucleotide of 15-30 bases consisting of a nucleotide sequence complementary to the region of nucleotide Nos. 502-556 or 578-612 of DUX4-fl mRNA consisting of the nucleotide sequence as shown in SEQ ID NO: 1; the 5' and/or 3' end of the oligonucleotide may be chemically modified; and the oligonucleotide is capable of switching the splice form of the DUX4 gene from DUX4-fl to DUX4-s. A pharmaceutical drug comprising the above oligonucleotide or a pharmaceutically acceptable salt thereof (e.g. therapeutic for facioscapulohumeral muscular dystrophy).

  本发明的目的是建立一种治疗面肱骨肌营养不良症的新型疗法。 一种寡核苷酸或其药学上可接受的盐，其中寡核苷酸包括由与 DUX4-fl mRNA 的核苷酸 Nos.寡核苷酸的 5'端和/或 3'端可进行化学修饰；并且寡核苷酸能够将 DUX4 基因的剪接形式从 DUX4-fl 转换为 DUX4-s。一种包含上述寡核苷酸或其药学上可接受的盐的药物（如治疗面肱骨肌营养不良症）。