专利号:US-2023331778-A1 优先权日:2020-08-31 标 题 :An improved process for fmoc synthesis of etelcalcetide 发明人:LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN; CHAVRE PRAFUL SHAMRAO 权利人:USV PRIVATE LTD 摘要:The present invention relates to an improved process for the synthesis of Etelcalcetide and its analogs by solid phase synthesis of Fmoc protected amino acids in a sequential manner, followed by acetylation of terminal D-cys and cleavage of peptide from solid support. The crude heptapeptide thus obtained is reduced using Tris(2-carboxyethyl) phosphine hydrochloride, purified and oxidized with L-cysteine. The oxidized Etelcalcetide is purified and salt exchanged using a one-step reverse phase chromatography process. The purified Etelcalcetide hydrochloride is then precipitated using organic solvents, concentrated and lyophilized to purity of greater than 99.0%.
专利号:EP-0790982-B1 优先权日:1994-06-17 标 题 :Methods of synthesis of peptidyl argininals 发明人:WEBB THOMAS R; REINER JOHN E; TAMURA SUSAN Y; RIPKA WILLIAM C; DAGNINO RAYMOND JR; NUTT RUTH F 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein, which have formula (I), wherein R1 is selected from the group consisting of hydrogen, benzyloxycarbonyl, isonicotinyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 4-methoxybenzyloxycarbonyl, t-butoxycarbonyl, t-amyloxycarbonyl, isobornyloxycarbonyl, adamantyloxycarbonyl, 2-(4-biphenyl)-2-propyloxycarbonyl, 9-fluorenylmethoxycarbonyl and methylsulfonylethoxycarbonyl; R2 is selected from the group consisting of alkyl of 1 to about 12 carbon atoms and aralkyl of about 7 to about 15 carbon atoms, either of which is optionally substituted with hydroxy or -CO-Y, wherein Y is hydroxy, alkoxy of 1 to about 12 carbon atoms, aralkoxy of about 7 to about 15 carbon atoms, O-polymeric support or NH-polymeric support; R3 is selected from the group consisting of hydrogen, Fmoc, nitro, benzyloxycarbonyl, t-butoxycarbonyl and adamantyloxycarbonyl; and R4 is selected from the group consisting of hydrogen, alkyl of 1 to about 12 carbon atoms, aryl of about 6 to about 14 carbon atoms and aralkyl of about 7 to about 15 carbon atoms; and salts thereof.
专利号:US-5405949-A 优先权日:1993-03-29 标题 :Process for the synthesis of glycosaminoglycans with heparin or heparan structure modified in position 2 of the α-L-iduronic-2-O-sulfate acid 发明人:UNGARELLI FABRIZIO; PIANI SILVANO 权利人:ALFA WASSERMANN SPA 摘要:A process for the synthesis of glycosaminoglycans with heparin or heparan structure modified in position 2 of the α-L-iduronic-2-O-sulfate acid in which the sulfate group is, entirely or in part, substituted with a nucleophilic group, is described. The process is carried out by treating glycosaminoglycans having heparin or heparan structure with a nucleophilic reagent in alkaline solution.
专利号:US-5731413-A 优先权日:1994-06-17 标 题:Method of synthesis of peptidyl aldehydes 发明人:WEBB THOMAS ROY; REINER JOHN EUGENE; TAMURA SUSAN YOSHIKO; RIPKA WILLIAM CHARLES; DAGNINO JR RAYMOND; NUTT RUTH FOELSCHE 权利人:CORVAS INT INC 摘要:This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to novel! reagents useful therein.
专利号:US-11542283-B2 优先权日:2018-05-28 标题 :Synthesis of peptide borate ester compound and use thereof 发明人:QIN YANRU 权利人:JIANGSU CHIA TAI FENGHAI PHARMACEUTICAL CO LTD 摘要:Provided are a peptide borate ester compound or a pharmaceutically acceptable salt thereof, a preparation method therefor, and pharmaceutical use thereof. The peptide borate ester compound or pharmaceutically acceptable salt thereof has a structure as shown in Formula (I), and is useful in the preparation of proteasome inhibitors to treat solid tumors and hematoma.
专利号:US-11718864-B2 优先权日:2015-09-23 标 题 :Cells and method of cell culture 发明人:HILLER GREGORY WALTER; MITCHELL JEFFREY JOSEPH; MULUKUTLA BHANU CHANDRA; PEGMAN PAMELA MARY 权利人:PFIZER 摘要:The invention relates to a method of cell culture where the cells are modified to reduce the level of synthesis of growth and/or productivity inhibitors by the cell. The invention also relates to a method of cell culture for improving cell growth and productivity, in particular in fed-batch culture of mammalian cells at high cell density. The invention further relates to a method of producing cells with improved cell growth and/or productivity in cell culture and to cells obtained or obtainable by such methods.
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