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Nucleoside analogs and oligonucleotide derivatives comprising nucleotide analogs thereof

机译:核苷类似物和包含其核苷酸类似物的寡核苷酸衍生物

摘要

Nucleoside analogs (I) are new. Nucleoside analogs of formula (I) and their salts are new. [Image] A : bond, 1-4C alkylene, O(CH 2) m or NR 4(CH 2) n; m, n : 1-3; B : aromatic heterocyclyl or carbocyclyl both optionally substituted; R 1-R 4H, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, acyl, silyl, optionally protected phosphoric acid or PR 7R 8; or R 1-R 3amino protecting group; or R 3hydroxy protecting group; and R 7, R 8amino (optionally substituted by 1-5C alkyl), 1-5C alkoxy, 1-5C alkylthio, 1-6C cyanoalkoxy or optionally protected SH or OH. The protecting groups are for use in the synthesis of nucleic acids Independent claims are also included for: (1) nucleoside analogs of formula (II) and their salts; and (2) oligonucleotides and their salts comprising at least one nucleoside residue of formula (IA) or (IIA). [Image] R 5, R 6a group R 1 and R 2 respectively.
机译:核苷类似物(I)是新的。式(I)的核苷类似物及其盐是新的。 [图像] A:键,1-4C亚烷基,O(CH 2)m或NR 4(CH 2)n; m,n:1-3; B:任选被取代的芳族杂环基或碳环基; R 1 -R 4H,烷基,烯基,环烷基,芳基,芳烷基,酰基,甲硅烷基,任选地被保护的磷酸或PR 7R 8; R 1 -R 3氨基保护基;或R 3羟基保护基;或R 7,R 8氨基(任选地被1-5C烷基取代),1-5C烷氧基,1-5C烷硫基,1-6C氰基烷氧基或任选地被保护的SH或OH。该保护基用于核酸的合成。还包括以下独立权利要求:(1)式(II)的核苷类似物及其盐; (2)寡核苷酸及其盐,其包含至少一个式(IA)或(IIA)的核苷残基。 [图像] R 5,R 6a组分别为R 1和R 2。

著录项

  • 公开/公告号DK2354148T3

    专利类型

  • 公开/公告日2013-10-14

    原文格式PDF

  • 申请/专利权人 IMANISHI TAKESHI;

    申请/专利号DK20100011213T

  • 发明设计人 IMANISHI TAKESHI;

    申请日2003-02-13

  • 分类号C07H19/16;A61K31/712;A61P31/12;A61P35;C07H19/06;C07H19/10;C07H19/20;C07H21;

  • 国家 DK

  • 入库时间 2022-08-21 16:41:53

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