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部分国内小核酸化学修饰中核苷酸修饰专利

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所属报告：

siRNA药物行业深度报告：小核酸大时代靶向治疗新纪元-251014（23页）.pdf

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核苷酸修饰专利挑战较多，国内药企突破主要体现在新修饰单体。核苷酸结构主要通过对核糖上的 2'-OH 进行改造，以增强靶标结合亲和力并提高对核酸酶的稳定性。Alnylam 通过收购 Sirna Therapeutics 获得的 McSiggen Parents 涉及 siRNA 的正义链和反义链中 2’核糖修饰的类型和个数，包括2’-F、2’-O-甲基和 2’-脱氧修饰等。此外，通过改变糖环的构型可以进一步调控小核酸的热稳定性与配对能力。Alnylam 仅从 ESC 到 ESC+修饰，涉及的主要平台型修饰专利数量众多，涵盖了 WO2019105418A 、WO2018185241A、WO2018098328A、WO2012058210A、WO2013165816、AWO2013074974A 等在内的众多通式型修饰专利，保护范围互相交叉且彼此延伸，覆盖了无数种现行常规核苷单体各种可能的空间排布。在此背景下，引入新型修饰单体是国内药企的一个可行方向，无论是提升长期稳定性还是降低毒性，它们在小核酸中的应用都可能拓展技术创新与专利布局空间。新修饰单体方面，炫景生物提出关于反义链不同位点 TBDMS 修饰方案使用基本不减弱 Tm 值的核苷酸修饰策略；瑞博生物使用开环和无碱基修饰，两项专利都实现了降低 dsRNA 序列的脱靶效应，同时保持良好的药效活性的效果。另有公司在新核苷酸类似物上有所突破，例如舶望制药提出了一种新的双环脱碱基核酸类似物单体化合物，这种化合物可以并入到寡聚化合物的末端，增强对细胞核酸酶的抵抗力，还可以扩展到肝外组织，如眼科和中枢神经系统；大睿生物专利提出在正义链的 3’末端引入 STM1修饰，并且实现比 IB（已知的核苷酸类似物）更优的靶基因抑制效果。

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