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-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-4950418-A 优先权日:1986-10-09 标题 :Reagent for removing protective groups in peptide synthesis 发明人:YAJIMA HARUAKI; FUJII NOBUTAKA; GUTERRES GILBERTO M A; HONGUU TATSUHIKO 权利人:SHINETSU CHEMICAL CO 摘要:Reagent for removing protective groups employed in peptide synthesis comprises a combination of hard acid and soft base. The hard acid is trialkylsilyltrifluoromethanesulphonate R3SiO3SCF3 and the soft base is ether. The reagent provides high efficiency of deprotection and has a low tendency to cause side reaction.
专利号:EP-4271401-A1 优先权日:2021-01-04 标题:Synthesis of teduglutide
专利号:US-2015329593-A1 优先权日:2014-05-19 标题:Synthesis of Beta-Arrestin Effectors
专利号:US-5364840-A 优先权日:1989-12-05 标题:Synthetic calcitonin peptides 发明人:BASAVA CHANNA; HOSTETLER KARL Y 权利人:VICAL INC 摘要:Synthetic hypocalcemic peptides which are superior in biological properties to native calcitonins as clinically useful agents. The peptides comprise analogues of native calcitonins having amino acid additions at the N-terminal position which, either alone or together with substitutions, and deletions at other residues, act to improve potency, prolong duration of the hormonal effect, and increase oral or nasal bioavailability. Methods are provided for the synthesis of these peptides.