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公开(公告)号:US5777092A
公开(公告)日:1998-07-07
申请号:US795282
申请日:1997-02-04
IPC分类号: A61K47/48 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04 , A61K31/70
CPC分类号: A61K31/70 , A61K47/48192 , A61K47/48223 , C07D405/04 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00
摘要: Oligonucleotide-mimicking macromolecules that have improved nuclease resistance are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligonucleotides with three or four atom linking groups provide unique oligonucleotide-mimicking macromolecules that are useful in regulating RNA expression and in therapeutics. Methods of synthesis and use also are disclosed.
摘要翻译: 提供了具有改善的核酸酶抗性的寡核苷酸模拟大分子。 用三个或四个原子连接基团替代天然寡核苷酸中发现的正常磷酸二酯糖苷键,提供了可用于调节RNA表达和治疗学的独特的寡核苷酸模拟大分子。 也公开了合成和使用方法。
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公开(公告)号:US06900301B2
公开(公告)日:2005-05-31
申请号:US10153320
申请日:2002-05-22
IPC分类号: A61K47/48 , A61K49/00 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号: C07D405/04 , A61K47/59 , A61K49/0006 , C07D405/14 , C07F7/1804 , C07H19/073 , C07H21/02 , C07H21/04
摘要: Therapeutic oligonucleotide analogues which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligomers with four atom linking groups forms unique di- and poly-nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.
摘要翻译: 提供了具有改善的核酸酶抗性和改善的细胞摄取的治疗性寡核苷酸类似物。 在具有四个原子连接基团的天然低聚物中发现的正常磷酸二酯糖苷键之间的替换形成了用于调节RNA表达和治疗学的独特的二核苷酸和多核苷和核苷酸。 还公开了合成和使用方法。
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公开(公告)号:US5965721A
公开(公告)日:1999-10-12
申请号:US763354
申请日:1996-12-11
IPC分类号: A61K47/48 , A61K49/00 , C07D405/04 , C07D405/14 , C07F7/18 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00
CPC分类号: C07D405/04 , A61K47/48192 , A61K49/0006 , C07D405/14 , C07F7/1856 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H21/00 , C07H11/00
摘要: Therapeutic oligonucleotide analogues which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligomers with four atom linking groups forms unique di- and poly-nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.
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