专利号:US-2020247841-A1 优先权日:2017-09-27 标 题 :Synthesis of icatibant 发明人:RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha 权利人:BIOCON LTD 摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.
专利号:US-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-11884714-B2 优先权日:2019-03-01 标 题:Cyclic peptide analogs of melanocortin and amanitin and methods of making such 发明人:PERRIN DAVID; TODOROVIC MIHAJLO; BÉNARD FRANÇOIS; ZHANG CHENGCHENG 权利人:UNIV BRITISH COLUMBIA; PROVINCIAL HEALTH SERVICES AUTHORITY 摘要:The invention described herein is based in part on the discovery of a protein/peptide crosslink, which introduces fluorescent properties, and which has been applied to synthesize analogues of melanocortin and amanitin as choice peptides to be explored in the context of isoindole peptides. Without limitation, it is expected that those trained in the art of peptide synthesis and stapling would appreciate the consequences of this invention such that other peptides of varied length can be similarly constrained by isoindole staples as featured herein.
专利号:AU-2018343242-A1 优先权日:2017-09-27 标 题 :Synthesis of Icatibant
专利号:EP-3688009-A1 优先权日:2017-09-27 标题:Synthesis of icatibant
[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):1793-1144. [参考文献]: Yang Li, Et Al. Non-Covalent Photo-Patterning Of Gelatin Matrices Using Caged Collagen Mimetic Peptides. Macromol Biosci. 2015 Jan;15(1):52-62.
合成参考文献
参考文献:10.1385/1-59259-783-1:349 摘要:Knight CG, Onley CM, Farndale RW. Peptide synthesis in the study of collagen-platelet interactions. Methods Mol Biol. 2004;273():349–64. doi: 10.1385/1-59259-783-1:349.