小分子布鲁顿氏酪氨酸激酶抑制剂专利分析

Small Molecular Inhibitors Targeting Bruton's Tyrosine Kinase and Its Patent Analysis

布鲁顿氏酪氨酸激酶(BTK)是B细胞抗原受体信号转导通路中的关键激酶,目前已成为治疗血液恶性肿瘤和自身免疫失调疾病的热门靶标。针对肿瘤治疗与炎症控制而开发的小分子Btk抑制剂受到越来越多的关注。本文从Btk抑制剂的专利申请量趋势、技术目标国分布,主要技术发展脉络等方面,对Btk抑制剂的研发思路进行分析,梳理其各中心环系骨架之间的区别和联系,对多种结构的Btk抑制剂进行了详细介绍。

Bruton＇s Tyrosine Kinase （BTK） is a crucial terminal kinase, enzyme in the B- cell antigen receptor （BCR） signaling pathway, has emerged as an attractive target for therapeutic intervention in human malignancies and autoimmune disorders. Because of Btk＇s key roles in cancer and inflammation development, the development of small molecular inhibitors targeting Btk for treatment of cancer and inflammation have received more and more attention. The strategies for Btk inhibitors development was analyzed, the connections and differences between the key ring system of the skeleton were combined, and various structures of Btk＇s inhibitors were introduced.