专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-8846614-B2 优先权日:2011-08-25 标 题 :Process for the synthesis of 37-mer peptide pramlintide 发明人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL 权利人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL; USV LTD 摘要:A process for the production of pramlintide, a 37-mer peptide, is provided. The synthesis provides a high yield synthesis of the peptide in relatively pure form. Further purification can be achieved by preparative HPLC.
专利号:US-7435791-B2 优先权日:2001-07-19 标题:Process for rapid solution synthesis of peptides 发明人:EGGEN IVO FRANCI; TEN KORTENAAR PAULUS BERNARDUS; HAASNOOT CORNELIS ALBERT GRUSON 权利人:ORGANON NV 摘要:The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps (a)-(d):n (a) a coupling step, using an excess of an activated carboxylic component to acylate an amino component, (b) a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, (c) one or more aqueous extractions and optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step (b), referred to as step (b′), in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions. nn During the process of this invention the growing peptide need not be isolated until the final peptide sequence has been obtained. n This highly efficient process is useful for the production of oligo- and polypeptides of high purity.
专利号:WO-2017033128-A1 优先权日:2015-08-25 标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors 发明人:HOOK DAVID; KU JIE; ZHOU JIANGUANG 权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG 摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.
专利号:US-11738092-B2 优先权日:2019-12-04 标题:Methods and compositions for synthesis of therapeutic nanoparticles 发明人:WYENT EMILY A; BLUMENFELD CARL M; LAMM ROBERT J 权利人:DANTARI INC 摘要:Improved methods and reactants for the chemical synthesis of therapeutic nanoparticles are provided. The nanoparticles comprise a polymeric core, to which is attached one or more homing molecules and one or more therapeutic agents. Improvements in speed, yield and purity are attained using the methods disclosed herein.
专利号:US-2024209029-A1 优先权日:2021-04-21 标题:Adiponectin glycopeptides and compositions and methods of use thereof 发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN 权利人:UNIV HONG KONG 摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.