Yuan Hong-Yu, Zhang Xiao-Lan, Zhang Xue-Hui, Meng Ling, Wei Ji-Fu
Nanjing Medical University, The First Affiliated Hospital, Research Division of Clinical Pharmacology , Nanjing , China.
Expert Opin Ther Pat. 2015;25(8):909-30. doi: 10.1517/13543776.2015.1044972. Epub 2015 Jun 12.
The etiology of rheumatoid arthritis (RA) is complex and diverse. Chronic inflammatory processes with joint dysfunction can cause permanent disability. Therefore, the development of new drugs and therapies for RA is very important.
This review analyzes the existing patents on anti-RA products in China to help pharmaceutical companies and individuals patent potential candidate drugs for RA treatment.
Three hundred and seventeen patents were analyzed, including 172 patents for Traditional Chinese Medicines (TCMs, 54.2%), 65 for synthetic compounds (20.5%), 55 for biological products (17.4%) and 25 patents for the drug preparation process (7.9%). Among the TCM patents, 73.8% were of various preparations for different Chinese medicines, 23.8% were of herbal extracts and 2.3% were of herbal extract derivatives. Synthetic compounds were involved in more than 30 targets, some small-molecule drugs that target signaling kinases such as p38 MAPK, Janus kinase may become important directions in the management of RA. Biological disease-modifying antirheumatic drugs (bDMARDs) are the most efficacious drugs for RA treatment. As the classic therapeutic target in RA, TNF-α has the largest number of bDMARD patents. In addition, it is expected that new targets such as high-mobility group protein B1, thioredoxin domain-containing protein 5 (TXNDC5) and B lymphocyte stimulator (BlyS) will play a significant role in RA as potential targets for new treatments. The largest number of all the published patent applications are claiming TCMs, which may provide substantial new information for anti-RA drug development. The largest number of all the published patent applications are claiming TCMs, which may provide huge information for anti-RA drug development.
类风湿性关节炎(RA)的病因复杂多样。伴有关节功能障碍的慢性炎症过程可导致永久性残疾。因此,开发用于治疗RA的新药和疗法非常重要。
本综述分析了中国抗RA产品的现有专利,以帮助制药公司和个人为治疗RA的潜在候选药物申请专利。
共分析了317项专利,其中中药专利172项(54.2%),合成化合物专利65项(20.5%),生物制品专利55项(17.4%),药物制备工艺专利25项(7.9%)。在中药专利中,73.8%是不同中药的各种制剂,23.8%是草药提取物,2.3%是草药提取物衍生物。合成化合物涉及30多个靶点,一些靶向信号激酶如p38丝裂原活化蛋白激酶、Janus激酶的小分子药物可能成为RA治疗的重要方向。生物病情改善抗风湿药物(bDMARDs)是治疗RA最有效的药物。作为RA的经典治疗靶点,肿瘤坏死因子-α(TNF-α)拥有最多的bDMARD专利。此外,预计高迁移率族蛋白B1、含硫氧还蛋白结构域蛋白5(TXNDC5)和B淋巴细胞刺激因子(BlyS)等新靶点将作为新治疗的潜在靶点在RA中发挥重要作用。所有已公布的专利申请中,声称是中药的数量最多,这可能为抗RA药物开发提供大量新信息。所有已公布的专利申请中,声称是中药的数量最多,这可能为抗RA药物开发提供大量信息。