专利号:WO-2023012709-A1 优先权日:2021-08-05 标 题 :An improved process for fmoc synthesis of semaglutide 发明人:LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN 权利人:USV PRIVATE LTD 摘要:The present invention relates to an improved process for the synthesis of glucagon-like-peptide-1 (GLP-1) and its analogs by using combination of solid and solution phase synthesis of Fmoc protected amino acids in a sequential manner, optionally incorporating Boc protected dipeptide for unnatural amino acid in the Sequence of GLP-1, cleaving GLP-1 sequence from the resin followed by purification; attaching side-chain to the desired amino acid in the solution phase to synthesize desired GLP-1 analog, purifying it to Semaglutide. Temperature gradient is applied during initial coupling of amino acids to facilitate completion of difficult coupling reactions.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:WO-2025128985-A1 优先权日:2023-12-14 标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.
1: Ye L, Tang P, Wan H, Zhong X, Chen X, Liu C, Huang R. A Comprehensive Review on the Cardioprotective and Nephroprotective Effects of Semaglutide, and Its Therapeutic Efficacy and Mechanisms in Cardiorenal Syndrome. Drug Des Devel Ther. 2026 Mar 24;20:581491. doi: 10.2147/DDDT.S581491. 2: Lu M. Angiogenesis and inflammation in the retinopathy risk of insulin and semaglutide - a review. Int J Retina Vitreous. 2026 Mar 18. doi: 10.1186/s40942-026-00811-8. Epub ahead of print. 7(3):102614. doi: 10.1016/j.xcrm.2026.102614. 4: Gupta S, Makkar BM, Kesavadev J, Kumar A. Semaglutide Hype or Hope: Evidence- based Review in Diabesity. J Assoc Physicians India. 2026 Mar;74(3):103-107. doi: 10.59556/japi.74.1439. 74(2E):e8-e20. doi: 10.59556/japi.74.1375.
合成参考文献
摘要: 参考文献:10.1186/s12933-017-0499-5 摘要:Xu J, Rajaratnam R. Cardiovascular safety of non-insulin pharmacotherapy for type 2 diabetes. Cardiovascular Diabetology. 2017 Feb 02;16(1):18. doi: 10.1186/s12933-017-0499-5. 参考文献:10.1007/s40618-018-0893-1 摘要:Giugliano D, Maiorino MI, Bellastella G, Esposito K. Dissonance among treatment algorithms for hyperglycemia in type 2 diabetes: an egalitarian dialog. Journal of Endocrinological Investigation. 2018 Apr 27;42(2):237–42. doi: 10.1007/s40618-018-0893-1. 参考文献:10.1007/s13300-018-0428-y 摘要:Witkowski M, Wilkinson L, Webb N, Weids A, Glah D, Vrazic H. A Systematic Literature Review and Network Meta-Analysis Comparing Once-Weekly Semaglutide with Other GLP-1 Receptor Agonists in Patients with Type 2 Diabetes Previously Receiving Basal Insulin. Diabetes Therapy. 2018 Apr 30;9(3):1233–51. doi: 10.1007/s13300-018-0428-y. 参考文献:10.1177/2168479017750129 摘要:Baldrick P. Juvenile Animal Testing: Assessing Need and Use in the Drug Product Label. Ther Innov Regul Sci. 2018 Sep;52(5):641–8. doi: 10.1177/2168479017750129.