小核酸药物配体缀合递送技术专利分析

目的 为中国小核酸药物研发企业的研发战略规划和专利战略制定提供参考。方法 通过智慧芽专利数据库检索小核酸药物配体缀合技术相关专利，通过人工标引的方式筛选获得该领域的核心专利及外围专利。首先对相关专利整体进行申请趋势分析，其次对小核酸药物配体缀合3类技术的核心专利进行详细分析。结果与结论 从整体来看，小核酸药物配体缀合递送技术绝大多数核心专利均掌握在Ionis、Alnylam、Arrowhead、Arbutus等国际顶尖核酸药物研发企业手中，而中国企业的研究能力和专利布局强度较弱。小核酸药物配体缀合递送技术主要包括半乳糖衍生物缀合递送技术、脂质衍生物缀合递送技术、细胞穿透肽缀合递送技术。其中最具发展潜力的是半乳糖衍生物缀合递送技术。脂质衍生物缀合递送技术近年来相对于半乳糖衍生物缀合递送技术所受到的关注度相对较低，多数专利布局时间过早，大都处于失效状态。细胞穿透肽缀合递送技术近年来越来越受到重视。

Analysis of Patent Layout of Small Nucleic Acid Drug Ligand Conjugate Delivery Technology

OBJECTIVE To provide a reference for the R&D strategic planning and patent strategy formulation of small nucleic acid drug R&D companies in China. METHODS Searched patents related to small nucleic acid drug ligand conjugation technology through PatSnap patent database, and obtained core patents and peripheral patents in this field through manual indexing. Firstly, analyzed the overall application trend of related patents, and secondly analyzed the core patents of the three types of small nucleic acid drug ligand conjugation technologies in detail. RESULTS & CONCLUSION On the whole, most of the core patents of small nucleic acid drug ligand conjugate delivery technology are in the hands of top international nucleic acid drug R&D companies such as Ionis, Alnylam, Arrowhead, and Arbutus, while the research capabilities and patent layout strength of domestic companies are relatively weak. Separately, the small nucleic acid drug ligand conjugated delivery technology mainly includes galactose derivative conjugated delivery technology, lipid derivative conjugated delivery technology, and cell penetrating peptide conjugated delivery technology. The most promising direction is the delivery technology of galactose derivatives conjugated. Lipid derivative conjugated delivery technology has received relatively low attention in recent years compared to galactose derivative conjugated delivery technology. Most of the patents have been deployed too early and most of them are in a state of failure. The cell penetrating peptide conjugated delivery technology has attracted more and more attention in recent years.