专利号:WO-2022116382-A1 优先权日:2020-12-04 标题 :Human glucagon-like peptide-1 receptor activator and application thereof 发明人:LI YINXIONG; XIONG YUE; FANG JI 权利人:GUANGZHOU INST BIOMED & HEALTH 摘要:A human glucagon-like peptide-1 receptor (GLP-1R) activator, comprising a compound of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, and R6 are each independently selected from any one of H, C1-C4 alkyl, mercapto, phosphate, vinyl, or acetyl. The compound of formula I or the pharmaceutically acceptable salt thereof can improve glycolipid metabolism of the tissue cells of a whole body, enhance the oxidative degradation of lipid molecules, inhibit the expression of lipogenic genes, inhibit the activity of acetyl coenzyme A synthetases, reduce the synthesis of triglyceride, improve the synthesis and secretion of glucose-induced insulin, relieve insulin antagonism, relieve the compensatory amplification of pancreatic islets β cells, and improve the survival rate and function of a pancreatic cell in a type-II diabetes sample state.
专利号:CN-115353522-A 优先权日:2022-08-22 标 题:Regioselective Synthesis of Icaritin-Norcantharidin Conjugate and Its Antitumor Application
专利号:CN-120005740-A 优先权日:2023-11-14 标题:Recombinant microorganism for high-level synthesis of polyphenol compounds and application thereof
专利号:CN-115181112-A 优先权日:2022-08-19 标 题 :Synthesis of 6-bromocyclo-icaritin chromane 3, 4-diketone derivative and anti-tumor application thereof
专利号:CN-115353522-B 优先权日:2022-08-22 标 题 :Regioselective Synthesis of Icaritin-Norcantharidin Conjugate and Its Antitumor Application
专利号:WO-2025082260-A1 优先权日:2023-10-17 标题:Icaritin carbamate prodrug, and preparation method therefor and use thereof 发明人:JIANG QIKUN; ZHANG TIANHONG; LI FENGXIAO; WANG WEIPING; FAN JIAQI; Zhai Yixiu 权利人:UNIV SHENYANG PHARMACEUTICAL 摘要:Provided are a preparation method for and the use of an icaritin carbamate prodrug and a salt thereof, which belong to the pharmaceutical field. In particular, provided are an icaritin carbamate prodrug represented by formula 3-N or 7-N and a pharmaceutically acceptable salt thereof, and a preparation method therefor and the use thereof. Specifically, the icaritin carbamate prodrug is formed by subjecting a main metabolic site (3-site or 7-site hydroxyl) of a natural flavonoid compound icaritin to structural modification by means of a chemical synthesis method, and introducing a suitable group at the position. Amines used in such carbamates are aliphatic amines. The presence of the carbamate structure reduces the phase II metabolism of icaritin in SD rats. Compared with an icaritin bulk drug, the 3-N-01 prodrug has a significantly improved oral bioavailability, making same the optimal prodrug. In clinical medication, the prodrug is expected to be able to reduce the administration dosage and improve patient compliance, and is expected to offer an effective strategy for improving the oral bioavailability of phenolic drugs.
1: Liao J, Liu Y, Wu H, Zhao M, Tan Y, Li D, Long H, Dai Y, Yung S, Chan TM, Lu Q. The role of icaritin in regulating Foxp3/IL17a balance in systemic lupus erythematosus and its effects on the treatment of MRL/lpr mice. Clin Immunol. 2016 Jan;162:74-83. doi: 10.1016/j.clim.2015.11.006. Epub 2015 Nov 18. doi: 10.3892/or.2015.4335. Epub 2015 Oct 16. Chinese. doi: 10.18632/oncotarget.5578. doi: 10.1142/S0192415X15500627. Epub 2015 Sep 14. doi: 10.1111/1440-1681.12488. doi: 10.1016/j.ejmech.2015.06.006. Epub 2015 Jun 6. doi: 10.11817/j.issn.1672-7347.2015.05.010. Chinese. doi: 10.1016/j.biomaterials.2015.04.038. Epub 2015 May 15. Chinese. doi: 10.1093/carcin/bgv040. Epub 2015 Apr 23. 13: Wu T, Wang S, Wu J, Lin Z, Sui X, Xu X, Shimizu N, Chen B, Wang X. Icaritin induces lytic cytotoxicity in extranodal NK/T-cell lymphoma. J Exp Clin Cancer Res. 2015 Feb 15;34:17. doi: 10.1186/s13046-015-0133-x. 14: Zhu S, Wang Z, Li Z, Peng H, Luo Y, Deng M, Li R, Dai C, Xu Y, Liu S, Zhang G. Icaritin suppresses multiple myeloma, by inhibiting IL-6/JAK2/STAT3. Oncotarget. 2015 Apr 30;6(12):10460-72.
合成参考文献
参考文献:10.1002/term.1679 摘要:Xie XH, Wang XL, Zhang G, He YX, Leng Y, Tang TT, Pan X, Qin L. Biofabrication of a PLGA-TCP-based porous bioactive bone substitute with sustained release of icaritin. J Tissue Eng Regen Med. 2015 Aug;9(8):961–72. doi: 10.1002/term.1679. 摘要:Zhang S, Sun L, Huang Z. [Tissue distribution of glucuronidated icaritin metabolite in rats]. Wei Sheng Yan Jiu. 2015 Jul;44(4):692–4.