1-((1R,3R,4R,6S,7S)-7-羟基-1-(羟基甲基)-6-甲基-2,5-二噁双环[2.2.1]-3-庚基)-5-甲基嘧啶-2,4(1H,3H)-二酮 | 1197032-96-4

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 1-((1R,3R,4R,6S,7S)-7-羟基-1-(羟基甲基)-6-甲基-2,5-二噁双环[2.2.1]-3-庚基)-5-甲基嘧啶-2,4(1H,3H)-二酮
• 英文名称: 2'-o,4'-C-((1S)-Ethane-1,1-diyl)beta-D-ribose 5-methyl uridine
• 英文别名: 1-[(1R,3R,4R,6S,7S)-7-hydroxy-1-(hydroxymethyl)-6-methyl-2,5-dioxabicyclo[2.2.1]heptan-3-yl]-5-methylpyrimidine-2,4-dione
• CAS: 1197032-96-4
• 化学式: C₁₂H₁₆N₂O₆
• 分子量: 284.26
• InChiKey: LVNFLHPRWWSZDA-XCUBXJTOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  108
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] 5'-SUBSTITUTED BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM<br/>[FR] NUCLÉOSIDES BICYCLIQUES 5'-SUBSTITUÉS ET COMPOSÉS OLIGOMÈRES SYNTHÉTISÉS À PARTIR DESDITS NUCLÉOSIDES
  申请人：ISIS PHARMACEUTICALS INC

  公开号：WO2011115818A1

  公开（公告）日：2011-09-22

  Provided herein are novel 5'-(S)-CH3 substituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the furanose ring of each of the novel 5'-(S)-CH3 substituted bicyclic nucleosides includes a 2' to 4' bridging group. The 5'-(S)-CH3 substituted bicyclic nucleosides are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as for example increasing the binding affinity. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

  本文提供了新颖的5'-(S)-CH3取代的双环核苷，以及由其制备的寡聚化合物和使用这些寡聚化合物的方法。更具体地，每个新颖的5'-(S)- 取代的双环核苷的呋喃糖环包括一个2'到4'的桥联基团。预计这些5'-(S)- 取代的双环核苷将有助于增强它们所并入的寡聚化合物的一个或多个性质，例如增加结合亲和力。在某些实施例中，本文提供的寡聚化合物与靶RNA的部分杂交，导致靶RNA的正常功能丧失。
• 5'-SUBSTITUTED BICYCLIC NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM
  申请人：Migawa Michael T.

  公开号：US20130041144A1

  公开（公告）日：2013-02-14

  Provided herein are novel 5′-(S)—CH 3 substituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the furanose ring of each of the novel 5′-(S)—CH 3 substituted bicyclic nucleosides includes a 2′ to 4′ bridging group. The 5′-(S)—CH 3 substituted bicyclic nucleosides are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as for example increasing the binding affinity. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
• US9193752B2
  申请人：——

  公开号：US9193752B2

  公开（公告）日：2015-11-24
• [EN] BIS-MODIFIED BICYCLIC NUCLEIC ACID ANALOGS<br/>[FR] ANALOGUES D'ACIDE NUCLÉIQUE BICYCLIQUE BIS-MODIFIÉ
  申请人：ISIS PHARMACEUTICALS INC

  公开号：WO2010077578A1

  公开（公告）日：2010-07-08

  The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More particularly, the bis-modified bicyclic nucleosides have at least one substituent group at the 5'- methylene and on the bridge methylene and can be chiral. These bis-modified bicyclic nucleosides are expected to be useful for enhancing one or more property of oligomeric compounds including for example enhancing nuclease resistance.