专利号:CN-107056894-B 优先权日:2017-05-26 标 题:A kind of method for fragment method solid-phase synthesis of ganirelix acetate
专利号:US-5434138-A 优先权日:1990-08-04 标 题:Gonadoliberin antagonists 发明人:KOENIG WOLFGANG; SANDOW JUERGEN; KOLAR CENEK 权利人:HOECHST AG 摘要:Peptides of the formula in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R1), F is Leu, Trp or Phe, G is L-Ser(R1), H is Gly-NH2, D-Ala-NH2 or Azagly-NH2 and R1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.
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-107056894-A 优先权日:2017-05-26 标 题 :A kind of method for the solid-phase synthesis of ganirelix acetate by fragment method
参考标题:Design And Synthesis Of A Library Of Tertiary Amides: Evaluation As Mimetics Of The Melanocortins' Active Core 作者:Felikss Mutulis,Jana Kreicberga,Sviatlana Yahorava,Ilze Mutule,Larisa Borisova-Jan,Aleh Yahorau,Ruta Muceniece,Sandra Azena,Santa Veiksina,Ramona Petrovska |发布日期:2007.9.1 摘要:Acceptable Results. According To This Approach An Efficient Formation Of Schiff Bases Was Achieved In The Presence Of Ticl(4). Substances Were Isolated By Reversed Phase Chromatography; In Some Cases Isomers Were Additionally Separated By Chiral Chromatography On Chirobiotic T. When Tested On Human Recombinant Melanocortin Receptors All The Tertiary Amides Showed Some Binding Affinities; For The Highest Affinity