专利号:US-2024067694-A1 优先权日:2021-01-04 标 题:Synthesis of teduglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
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-11518794-B2 优先权日:2016-08-19 标 题:Synthesis method for liraglutide with low racemate impurity 发明人:FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG 权利人:SHENZHEN JYMED TECH CO LTD 摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.
专利号:US-10344069-B2 优先权日:2014-10-31 标 题:Process for the preparation of liraglutide 发明人:VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD 权利人:AURO PEPTIDES LTD; VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD 摘要:The present invention relates to a process for the preparation of Liraglutide, which comprises: a) synthesis of suitable fragments (protected) by solid phase peptide synthesis; b) coupling of the suitable fragments on solid support; c) concurrently cleaving the protected peptide from the solid support and de-protecting the peptide; d) purification of Liraglutide (crude) on reverse phase HPLC; e) isolating pure Liraglutide.
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.
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合成参考文献
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