Hexaethylene glycol monophosphate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Hexaethylene glycol monophosphate
• 英文别名: 2-[2-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethyl dihydrogen phosphate
• 化学式: C₁₂H₂₇O₁₀P
• 分子量: 362.31
• InChiKey: PTMCGHPIYOSATH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3
• 重原子数：
  23
• 可旋转键数：
  18
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  133
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• MMP-TARGETED THERAPEUTIC AND/OR DIAGNOSTIC NANOCARRIERS
  申请人：Mallinckrodt Inc.

  公开号：US20130183236A1

  公开（公告）日：2013-07-18

  The present invention provides targeted delivery compositions and methods of using the compositions for treating and diagnosing a disease state in a subject.

  本发明提供了针对性递送组合物以及使用这些组合物治疗和诊断受试者疾病状态的方法。
• Oligonucleotide analogues incorporating 5-aza-cytosine therein
  申请人：Phiasivongsa Pasit

  公开号：US20070072796A1

  公开（公告）日：2007-03-29

  Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2′-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.

  提供了含有5-aza-胞嘧啶的寡核苷酸类似物，例如以5-aza-2'-脱氧胞嘧啶（地西他滨）或5-aza-胞嘧啶的形式出现在寡核苷酸序列中。特别地，提供了含有地西他滨-脱氧鸟嘌呤岛（DpG和GpD）的寡核苷酸类似物，以针对人类基因组中的CpG岛，特别是易于发生异常高甲基化的基因启动子区域。这样的类似物可用于调节DNA甲基化，例如有效抑制C-5位置的胞嘧啶的甲基化。提供了合成这些寡核苷酸类似物和调节核酸甲基化的方法。还提供了用于合成寡核苷酸类似物的磷酰胺酰胺建筑块，以及用于合成、制剂和给药这些化合物或组合物以治疗癌症和血液疾病等疾病的方法。
• Short oligonucleotides for the inhibition of VEGF expression
  申请人：Hoechst Marion Roussel Deutschland GmbH

  公开号：EP0979869A1

  公开（公告）日：2000-02-16

  The present invention relates to a short oligonucleotide or a derivative thereof which has a sequence that corresponds to a particular part of a nucleic acid sequence which encodes VEGF (vascular endothelial growth factor) and which has a length of maximum 15 nucleotides, the invention further relates to a method of making the oligonucleotide and the use thereof. A short oligonucleotide or a derivative thereof, which has a length of 10 to 15 nucleotides and which corresponds to a part of a VEGF encoding sequence, wherein the part of the VEGF encoding sequence to which the oligonucleotide corresponds to has one of the sequences SEQ ID NO. 1, SEQ ID NO. 2, SEQ ID NO. 3, SEQ ID NO. 4, SEQ ID NO. 5 or SEQ ID NO. 6 or a part thereof, wherein SEQ ID NO. 1 is   5'- CCCGGCCCCGGTCGGGCCTCCG - 3', SEQ ID NO. 2 is   5'- CGGGCCTCCGAAACC -3' , SEQ ID NO. 3 is   5'- GCTCTACCTCCACCATGCCAA -3', SEQ ID NO. 4 is   5'- GTGGTCCCAGGCTGCACCCATGGC -3', SEQ ID NO. 5 is   5'- CATCTTCAAGCCATCC -3', and SEQ ID NO. 6 is   5'- TGCGGGGGCTGCTGC -3'.

  本发明涉及一种短寡核苷酸或其衍生物，其序列对应于核酸序列的特定部分，该核酸序列编码VEGF（血管内皮生长因子），其长度不超过15个核苷酸，本发明还涉及一种制造该寡核苷酸的方法及其用途。 一种短寡核苷酸或其衍生物，其长度为 10 至 15 个核苷酸，与 VEGF 编码序列的一部分相对应，其中寡核苷酸所对应的 VEGF 编码序列的一部分具有 SEQ ID NO.1、SEQ ID NO.2、SEQ ID NO.3、SEQ ID NO.4、SEQ ID NO.5 或 SEQ ID NO.6 序列之一或其一部分、 其中 SEQ ID NO. 1 是 5'- CCCGGCCCCGGTCGGGCCTCCG - 3'、 SEQ ID NO. 2 是 5'- CGGGCCTCCGAAACC -3' 、 SEQ ID NO. 3 是 5'- GCTCTACCTCCACCATGCCAA -3'、 SEQ ID NO. 4 是 5'- GTGGTCCCAGGCTGCACCCATGGC -3'、 SEQ ID NO. 5 是 5'- CATCTTCAAGCCATCC -3', 和 SEQ ID NO. 6 是 5'- TGCGGGGGCTGCTGC -3'。
• Antisense oligonucleotides for the inhibition of VEGF expression
  申请人：Hoechst Marion Roussel Deutschland GmbH

  公开号：EP0978561A1

  公开（公告）日：2000-02-09

  The present invention relates to an oligonucleotide or a derivative thereof which has a sequence that corresponds to a part of a nucleic acid which encodes VEGF (vascular endothelial growth factor) and which has the ability to inhibit tumor growth in animal tumor models, the invention further relates to the preparation of such oligonucleotide and the use thereof. An oligonucleotide or a derivative thereof which has the sequence SEQ ID NO. 4 or a part thereof, wherein SEQ ID NO. 4 is 3'-GTACCTACAGATAGTCGCGTCGATGACGGTAGG-5, with the first proviso, that not all internucleoside bridges in the oligonucleotide are phosphodiester internucleoside bridges and not all phosphodiester internucleoside bridges are replaced by phosphorothioate internucleoside bridges and/or the second proviso, that the oligonucleotide contains no modified nucleosides selected from C5-propynyl uridine, C5-propynyl cytidine, C5-hexynyl uridine, C5-hexynyl cytidine, 6-aza uridine and 6-aza cytidine.

  本发明涉及一种寡核苷酸或其衍生物，其序列与编码血管内皮生长因子（VEGF）的核酸的一部分相对应，并且具有抑制动物肿瘤模型中肿瘤生长的能力，本发明进一步涉及这种寡核苷酸的制备及其用途。 一种寡核苷酸或其衍生物，其序列为 SEQ ID NO. SEQ ID NO. 4 是 3'-GTACCTACAGATAGTCGCGTCGATGACGGTAGG-5、 与 第一个但书，即寡核苷酸中并非所有的核苷酸间桥都是磷酸二酯核苷酸间桥，也并非所有的磷酸二酯核苷酸间桥都被硫代磷酸酯核苷酸间桥取代，和/或第二个但书、寡核苷酸不含有选自 C5-丙炔基尿苷、C5-丙炔基胞苷、C5-己炔基尿苷、C5-己炔基胞苷、6-氮杂尿苷和 6-氮杂胞苷的修饰核苷。
• Multimetric oligonucleotide compounds
  申请人：Translate Bio MA, Inc.

  公开号：US10093924B2

  公开（公告）日：2018-10-09

  The disclosure provides multimeric oligonucleotide compounds, comprising two or more target-specific oligonucleotides (e.g., antisense oligonucleotides (ASOs)), each being resistant to cleavage, and linked together by a cleavable linker. In particular, two or more linked target-specific oligonucleotides, each to a different target, allows concomitant inhibition of multiple genes' expression levels, while exhibiting favorable pharmacokinetic and pharmacodynamic properties. Methods of making and uses of the described compounds are also provided.

  本公开提供了多聚物寡核苷酸化合物，包括两个或多个靶向特异性寡核苷酸（如反义寡核苷酸（ASO）），每个寡核苷酸都具有抗裂解性，并通过可裂解连接体连接在一起。特别是两个或更多链接的靶标特异性寡核苷酸，每个都针对不同的靶标，可以同时抑制多个基因的表达水平，同时表现出良好的药代动力学和药效学特性。还提供了所述化合物的制造方法和用途。