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凝血因子Ⅹa抑制剂专利技术分析

赵冬梅, 房长进, 邱志霞

赵冬梅, 房长进, 邱志霞. 凝血因子Ⅹa抑制剂专利技术分析[J]. 中国药科大学学报, 2019, 50(3): 364-373. DOI: 10.11665/j.issn.1000-5048.20190314
引用本文: 赵冬梅, 房长进, 邱志霞. 凝血因子Ⅹa抑制剂专利技术分析[J]. 中国药科大学学报, 2019, 50(3): 364-373. DOI: 10.11665/j.issn.1000-5048.20190314
ZHAO Dongmei, FANG Changjin, QIU Zhixia. Patent analysis for coagulation factor Xa inhibitors[J]. Journal of China Pharmaceutical University, 2019, 50(3): 364-373. DOI: 10.11665/j.issn.1000-5048.20190314
Citation: ZHAO Dongmei, FANG Changjin, QIU Zhixia. Patent analysis for coagulation factor Xa inhibitors[J]. Journal of China Pharmaceutical University, 2019, 50(3): 364-373. DOI: 10.11665/j.issn.1000-5048.20190314

凝血因子Ⅹa抑制剂专利技术分析

基金项目: 国家自然科学基金资助项目(No.81503149) #赵冬梅,房长进对本论文的贡献相同

Patent analysis for coagulation factor Xa inhibitors

  • 摘要: 抗凝血药物被广泛用于血栓栓塞性疾病的预防和治疗。近年来,凝血因子Ⅹa抑制剂成为新型抗凝血药物的研发热点,但目前上市的抗凝药物仍存在长期使用会增加出血风险等不良反应。本文通过文献检索,对凝血因子Ⅹa抑制剂相关专利申请状况进行了分析,以百时美施贵宝公司和广东东阳光药业有限公司作为该领域重点企业代表,对其专利申请发展路线进行梳理,总结凝血因子Ⅹa抑制剂化合物的改造位点和研发方向,以期能够为国内研发机构和相关企业对凝血因子Ⅹa的新药研发、专利保护以及知识产权布局提供有益的参考和建议。
    Abstract: Anticoagulant drugs are widely used in the prevention and treatment of thromboembolic diseases. In recent years, coagulation factor Xa inhibitors have become a hot spot for the development of new anticoagulant drugs. However, the anticoagulant drugs currently used still have side-effects such as increased bleeding risk. This paper analyzes the patent applications of coagulation factor Xa inhibitors, and summarizes the development route of patent application of Bristol-Myers Squibb Company and Guangdong Dongyang Pharmaceutical Co. , Ltd. as representatives of key enterprises, in order to provide some useful references and recommendations for the development, patent protection countermeasure and intellectual property strategy of coagulation factor Xa for domestic pharmaceutical enterprises.
  • [1] Xu C.CADD studies on FXa inhibitors and benzothiazole derivatives(计算机辅助药物设计对FXa抑制剂和苯并噻唑衍生物的研究)[D].Shanghai:Shanghai Institute of Technology,2016.
    [2] Chen H,Wang YG,Meng L,et al.Research progress on coagulation factor Xa inhibitors[J].Pharm Clin Res(药学与临床研究),2013,21(6):655-659.
    [3] Xu HR.Design,Synthesis and Biological activity studies of novel factor Xa inhibitors(新型凝血因子Xa抑制剂的设计、合成及生物活性研究)[D].Jinan:Shandong University,2017.
    [4] Feng RM,Lyu H,Qi GF.Discussion on drug design and inventive step of patent[J].Shandong Chem Ind(山东化工),2017,46(21):129-130.
    [5] Xu K,Zhang HB,Zhou JP,et al.Recent advances in the development of factor Xa[J].Chin J New Drugs(中国新药杂志),2012,21(20):2380-2387.
    [6] Chen X,Zhang HB,Huang WL,et al.Acvances in the research of factor Xa inhibitors[J].J China Pharm Univ(中国药科大学学报),2010,41(2):104-111.
    [7] Young RJ.The successful quest for oral factor Xa inhibitors;learnings for all of medicinal chemistry[J]?Bioorg Med Chem Lett,2011,21(21):6228-6235.
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出版历程
  • 刊出日期:  2019-06-24

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