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.
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