专利号:WO-2023030278-A1 优先权日:2021-08-30 标题:Full-liquid-phase synthesis method for reelin drug 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN SANTAI PHARMACEUTICAL CO LTD 摘要:Provided is a full-liquid-phase synthesis method for a reelin drug, belonging to the technical field of medicine synthesis. A liquid-phase method is used to synthesize 'Trp-Ser-Tyr' fragments, 'R5-Leu' fragments, 'PYR-His' fragments, and 'Arg-Pro-Gly-NH2' respectively, wherein R=D-Trp, Gly or D-2-NAL; and a reelin drug is synthesized in a '3+2+2+3' fragment condensation manner. The method has the characteristics of low reaction costs, non use of toxic reagents, a high product yield, and high purity, and is environmentally friendly, and is thus suitable for large-scale production.
专利号:US-2025109170-A1 优先权日:2021-12-01 标 题 :Method for manufacturing ganirelix 发明人:KIM JAE IL; HWANG KOOK SANG; LEE JU YOUNG; KIM DONG MIN; JO EUN JIN; LEE SEUL GI 权利人:ANYGEN CO LTD 摘要:In a method for manufacturing ganirelix, a peptide intermediate A represented by Chemical Formula 19 is obtained, a peptide intermediate B represented by Chemical Formula 21 is obtained, and ganirelix represented by Chemical Formula 13 is obtained through a convergent synthesis of the peptide intermediate A and the peptide intermediate B. Ganirelix can be obtained in high purity and high yield, and the commercial mass-production process therefor is feasible, and also, an economical advantage, that is, the reduction in the production costs compared to conventional technologies, is provided. Furthermore, it is possible to obtain a large quantity of Ganirelix more safely than conventional technologies.
专利号:US-12098218-B2 优先权日:2015-12-17 标题 :Process for the manufacture of degarelix and its intermediates 发明人:RICCI ANTONIO; ZANON JACOPO; CABRI WALTER; GURYANOV IVAN; ORLANDIN ANDREA; BIONDI BARBARA; FORMAGGIO FERNANDO; VISENTINI DARIO 权利人:FRESENIUS KABI IPSUM S R L 摘要:The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
专利号:CN-114181285-A 优先权日:2021-12-31 标题 :A kind of method of solid-liquid synthesis of nafarelin
专利号:CN-103351428-A 优先权日:2013-08-05 标 题 :Synthesis of degarelix by a solid-phase fragmentation method
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1063.
合成参考文献
参考文献:10.1111/cbdd.12307 摘要:Qiu S, Chen F, Liu Y, Lai L. Discovery of novel secretory phospholipase A2 inhibitors using virtual screen. Chem Biol Drug Des. 2014 Aug;84(2):216–22. doi: 10.1111/cbdd.12307.