2-(2-Imidazolyl-(4)-aethylamino)-6-hydroxy-purin | 95324-34-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 2-(2-Imidazolyl-(4)-aethylamino)-6-hydroxy-purin
• 英文别名: 2-[2-(1(3)H-imidazol-4-yl)-ethylamino]-1,7(9)-dihydro-purin-6-one；2-[2-(1H-imidazol-5-yl)ethylamino]-1,7-dihydropurin-6-one
• CAS: 95324-34-8
• 化学式: C₁₀H₁₁N₇O
• 分子量: 245.244
• InChiKey: GJYZYUZMSDKICN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  111
• 氢给体数：
  4
• 氢受体数：
  3

文献信息

• Compositions and methods for detecting and modulating rna activity and gene expression
  申请人：ISIS PHARMACEUTICALS, INC.

  公开号：EP1418179A2

  公开（公告）日：2004-05-12

  Compositions and methods for modulating the activity of RNA and DNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. Reactive portions which act, alternatively, through phosphorodiester bond cleavage, through backbone sugar bond cleavage or through base modification are preferably employed. Groups which improve the pharmacodynamic and pharmacokinetic properties of the oligonucleotides are also useful in accordance with certain embodiments of this invention. Delivery of the reactive or non-reactive functionalities into the minor groove formed by the hybridization of the composition with the target RNA is also preferably accomplished. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided useful for elaboration of oligonucleotides and oligonucleotide analogs for such purposes.

  本文公开了调节 RNA 和 DNA 活性的组合物和方法。根据优选的实施方案，反义组合物由靶向部分和反应部分组成。反应部分最好通过磷酸二酯键裂解、骨架糖键裂解或碱基修饰起作用。根据本发明的某些实施方案，改善寡核苷酸药效学和药代动力学特性的基团也是有用的。最好还能将反应性或非反应性官能团输送到组合物与目标 RNA 杂交形成的次凹槽中。本发明还公开了治疗、诊断和研究方法。本发明还提供了合成核苷和核苷片段，可用于制备用于上述目的的寡核苷酸和寡核苷酸类似物。
• EP0604409A4
  申请人：——

  公开号：EP0604409A4

  公开（公告）日：1996-06-12
• COMPOSITIONS AND METHODS FOR DETECTING AND MODULATING RNA ACTIVITY AND GENE EXPRESSION
  申请人：ISIS PHARMACEUTICALS, INC.

  公开号：EP0604409A1

  公开（公告）日：1994-07-06
• OLIGONUCLEOTIDE ANALOGS FOR DETECTING AND MODULATING RNA ACTIVITY AND GENE EXPRESSION
  申请人：ISIS PHARMACEUTICALS, INC.

  公开号：EP0604409B1

  公开（公告）日：2004-07-14
• [EN] COMPOSITIONS AND METHODS FOR DETECTING AND MODULATING RNA ACTIVITY AND GENE EXPRESSION
  申请人：ISIS PHARMACEUTICALS, INC.

  公开号：WO1991010671A1

  公开（公告）日：1991-07-25

  (EN) Compositions and methods for modulating the activity of RNA and DNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. Reactive portions which act, alternatively, through phosphorodiester bond cleavage, through backbone sugar bond cleavage or through base modification are preferably employed. Groups which improve the pharmacodynamic and pharmacokinetic properties of the oligonucleotides are also useful in accordance with certain embodiments of this invention. Delivery of the reactive or non-reactive functionalities into the minor groove formed by the hybridization of the composition with the target RNA is also preferably accomplished. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided useful for elaboration of oligonucleotides and oligonucleotide analogs for such purposes.(FR) On décrit des compositions et des procédés servant à moduler l'activité ARN et ADN. Dans les modes de réalisation préférés, on prépare des compositions non codantes comprenant des parties cibles et des parties réactives. On utilise de préférence des parties réactives qui agissent par le clivage des liaisons phosphorodiesters, par le clivage des liaisons des sucres du squelette, ou par la modification des bases. Les groupes qui améliorent les caractéristiques pharmacolodynamiques et pharmacocinétiques des oligonucléotides sont également utiles dans certains modes de réalisation. On effectue également de préférence l'apport des fonctionnalités réactive et non réactive au sillon mineur formé par l'hybridation de la composition avec l'ARN cible. On décrit également des procédés thérapeutiques, diagnostiques et de recherche. On a prévu des nucléosides thérapeutiques, diagnostiques et de recherche. On a prévu des nucléosides synthétiques et des fragments nucléosides synthétiques utiles à l'élaboration des oligonucléotides et des analogues oligonucléotidiques.