专利号:WO-2023030277-A1 优先权日:2021-08-30 标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD 摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-7714063-B2 优先权日:2007-11-15 标 题 :Solid support for Fmoc-solid phase synthesis of peptides 发明人:SRIVASTAVA KRIPA SHANKER; DAVIS MATTHEW RYAN 权利人:MALLINCKRODT INC 摘要:The present invention provides compositions and processes for the solid phase synthesis of polypeptides. In particular, the present invention provides solid supports and processes for preparing solid supports for the synthesis of polypeptides.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-5212288-A 优先权日:1990-02-20 标 题:Temporary minimal protection synthesis of serine-containing polypeptides 发明人:NESTOR JR JOHN J; MCCLURE NATALIE L; ARZENO HUMBERTO 权利人:SYNTEX INC 摘要:In a process for the solid phase synthesis of a polypeptide containing at least one serine residue, the improvement comprising temporarily protecting the side chain of the serine residue with a protecting group which is removed immediately following the addition of the serine to the peptide chain.
参考文献:10.1542/peds.2005-0538 摘要:Hirsch HJ, Gillis D, Strich D, Chertin B, Farkas A, Lindenberg T, Gelber H, Spitz IM. The histrelin implant: a novel treatment for central precocious puberty. Pediatrics. 2005 Dec;116(6):e798–802. doi: 10.1542/peds.2005-0538.