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-2015182634-A1 优先权日:2012-12-28 标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action 发明人:COYNE CODY P; BEAR RYAN; JONES TONI 权利人:COYNE CODY P; BEAR RYAN; JONES TONI 摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.
专利号:EP-0443532-B1 优先权日:1990-02-20 标题:Temporary minimal protection synthesis of LH-RH analogs 发明人:NESTOR JOHN J JR; MCCLURE NATALIE L 权利人:SYNTEX INC 摘要:A solid phase synthesis of LH-RH analogs in which the amino acids serine and histidine, if present, are side chain protected during the synthesis with groups labile to selected alpha -amino or deprotecting agents.
专利号:US-8314209-B2 优先权日:2007-12-12 标 题 :Lipid-assisted synthesis of polymer compounds and methods for their use 发明人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO 权利人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO; UNIV CALIFORNIA 摘要:The invention herein disclosed provides for methods for the synthesis of polymers from monomers. In particular the method provides for the synthesis of polynucleotides from mononucleotides in the absence of catalytic enzymes. The method comprises providing an aqueous solution having a plurality of phospholipid molecules and monomer molecules; subjecting the aqueous solution to fluctuating temperature conditions; subjecting the aqueous solution to fluctuating cycles of drying and hydrating conditions; subjecting the aqueous solution to fluctuating [H + ] conditions; the fluctuating conditions thereby allowing formation of a chemical bond between at least two monomers to create a polymer. The invention is of particular use in the fields of molecular biology, structural biology, cell biology, molecular switches, molecular circuits, and molecular computational devices, and the manufacture thereof.
专利号:US-11858901-B2 优先权日:2019-10-30 标 题:3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6 trifluoromethyl benzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, process for its preparation, and its use in the synthesis of elagolix 发明人:BALLETTE ROBERTO; JIMÉNEZ ALONSO OSCAR; GARCÃ?A GARCÃ?A ELENA; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A new intermediate is useful in the synthesis of elagolix. A process for obtaining the intermediate includes reacting a precursor with iodine monochloride in the presence of an organic solvent. A process for preparing elagolix makes use of the intermediate. The intermediate can be 3-((R)-2-(amino-2-phenylethyl)-1-(2-fluoro-6-trifluoromethylbenzyl)-5-iodo-6-methyl-1H-pyrimidine-2,4-dione or a salt thereof, such as a hydrochloride.
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