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:US-2019177392-A1 优先权日:2014-09-23 标 题 :Synthesis of glp-1 peptides 发明人:PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS 权利人:NOVETIDE LTD 摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:WO-2024261319-A1 优先权日:2023-06-23 标题 :Methods of chemical synthesis of peptides 发明人:AL MUSAIMI OTHMAN; WILLIAMS DARYL ROBERT 权利人:IMPERIAL COLLEGE INNOVATIONS LTD 摘要:The present invention relates to methods for the synthesis of peptides and related compounds supported on a solid polymeric resin. The inventive method provides synthetic schemes that permit the coupling of two or more peptide fragments attached to the same polymeric support, in a fashion that allows access to previously unobtainable structures, and provides a more convenient and higher-yielding approach to known peptides, including those of commercial significance.
1: Bruen R, Curley S, Kajani S, Crean D, O'Reilly ME, Lucitt MB, Godson CG, McGillicuddy FC, Belton O. Liraglutide dictates macrophage phenotype in apolipoprotein E null mice during early atherosclerosis. Cardiovasc Diabetol. 2017 Nov 6;16(1):143. doi: 10.1186/s12933-017-0626-3. 2: Mann JFE, Ørsted DD, Brown-Frandsen K, Marso SP, Poulter NR, Rasmussen S, Tornøe K, Zinman B, Buse JB; LEADER Steering Committee and Investigators. Liraglutide and Renal Outcomes in Type 2 Diabetes. N Engl J Med. 2017 Aug 31;377(9):839-848. doi: 10.1056/NEJMoa1616011. doi: 10.1111/dom.12808. Epub 2016 Nov 21. Review. Liraglutide and Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2016 Jul 28;375(4):311-22. doi: 10.1056/NEJMoa1603827. Epub 2016 Jun 13. 6: Jacobsen LV, Flint A, Olsen AK, Ingwersen SH. Liraglutide in Type 2 Diabetes Mellitus: Clinical Pharmacokinetics and Pharmacodynamics. Clin Pharmacokinet. 2016 Jun;55(6):657-72. doi: 10.1007/s40262-015-0343-6. Review.
合成参考文献
参考文献:10.1016/s0140-6736(10)60225-5 摘要:Hallberg P, Schwan S, Melhus H. Liraglutide for weight loss in obese people. Lancet. 2010 Feb 13;375(9714):551; author reply 552–3. doi: 10.1016/s0140-6736(10)60225-5. 参考文献:10.1016/s0140-6736(10)60226-7 摘要:Thum T, Anker SD. Liraglutide for weight loss in obese people. Lancet. 2010 Feb 13;375(9714):551–2; author reply 552. doi: 10.1016/s0140-6736(10)60226-7. 参考文献:10.1007/s00210-011-0665-3 摘要:Ku HC, Chen WP, Su MJ. DPP4 deficiency preserves cardiac function via GLP-1 signaling in rats subjected to myocardial ischemia/reperfusion. Naunyn Schmiedebergs Arch Pharmacol. 2011 Aug;384(2):197–207. doi: 10.1007/s00210-011-0665-3. 参考文献:10.2165/11592040-000000000-00000 摘要:Cheung BM. Drug treatment for obesity in the post-sibutramine era. Drug Saf. 2011 Aug 01;34(8):641–50. doi: 10.2165/11592040-000000000-00000. 参考文献:10.1016/j.bbrc.2011.06.175 摘要:Nonogaki K, Suzuki M, Sanuki M, Wakameda M, Tamari T. The contribution of serotonin 5-HT2C and melanocortin-4 receptors to the satiety signaling of glucagon-like peptide 1 and liragultide, a glucagon-like peptide 1 receptor agonist, in mice. Biochemical and Biophysical Research Communications. 2011 Jul;411(2):445–8. doi: 10.1016/j.bbrc.2011.06.175.