首页> 外国专利> Isolerte eller syntetiske oligonukleotidanaloger eller salt eller ester derav som inkluderer 5-aza-cytosin, farmasøytisk sammensetning derav, alle for anvendelse i fremstilling av et medikament, farmasøytisk kombinasjon derav, alle for anvendelse i terapi, samt et sett derav

Isolerte eller syntetiske oligonukleotidanaloger eller salt eller ester derav som inkluderer 5-aza-cytosin, farmasøytisk sammensetning derav, alle for anvendelse i fremstilling av et medikament, farmasøytisk kombinasjon derav, alle for anvendelse i terapi, samt et sett derav

机译：分离的或合成的寡核苷酸类似物或其盐或酯，包括5-氮杂胞嘧啶，其药物组合物，全部用于制造药物，其药物组合，全部用于治疗，及其一套

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摘要

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-de-oxyguanosine 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.

机译：提供了在寡核苷酸序列中掺入5-氮杂-胞嘧啶的寡核苷酸类似物，例如以5-氮杂-2'-脱氧胞苷（地他滨）或5-氮杂胞苷的形式。特别地，提供富含地西他滨-脱氧鸟苷胰岛（DpG和GpD）的寡核苷酸类似物，以靶向人基因组中的CpG胰岛，尤其是在对异常高甲基化敏感的基因的启动子区域中。此类类似物可用于调节DNA甲基化，例如有效抑制C-5位胞嘧啶的甲基化。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亚磷酰胺结构单元，用于合成，配制和施用这些化合物或组合物以治疗诸如癌症和血液疾病的病症的方法。

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公开/公告号NO344764B1

专利类型
公开/公告日2020-04-20

原文格式PDF
申请/专利权人 ASTEX PHARMACEUTICALS INC;
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申请/专利号NO20080002050
发明设计人 PHIASIVONGSA PASIT;REDKAR SANJEEV;
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申请日2008-04-29
分类号A61K31/282;A61K9;A61K31/337;A61K31/4406;A61K31/7084;A61K33/24;A61K45/06;C07H19/20;C07H21;C12N15/11;
国家 NO
入库时间 2022-08-21 11:16:52

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