专利号:US-2024082435-A1 优先权日:2021-02-26 标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents 发明人:PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS 权利人:TELIX INT INNOVATIONS PTY LTD 摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
专利号:US-2019177392-A1 优先权日:2014-09-23 标 题 :Synthesis of glp-1 peptides 发明人:PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS 权利人:NOVETIDE LTD 摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.
专利号:US-6316593-B1 优先权日:1996-02-09 标题:Synthesis of VIP analog 发明人:BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M 权利人:HOFFMANN LA ROCHE 摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.
专利号:WO-2024261319-A1 优先权日:2023-06-23 标题 :Methods of chemical synthesis of peptides 发明人:AL MUSAIMI OTHMAN; WILLIAMS DARYL ROBERT 权利人:IMPERIAL COLLEGE INNOVATIONS LTD 摘要:The present invention relates to methods for the synthesis of peptides and related compounds supported on a solid polymeric resin. The inventive method provides synthetic schemes that permit the coupling of two or more peptide fragments attached to the same polymeric support, in a fashion that allows access to previously unobtainable structures, and provides a more convenient and higher-yielding approach to known peptides, including those of commercial significance.
专利号:US-2024336649-A1 优先权日:2021-06-21 标 题 :Synthesis of covalent protein dimers that can inhibit myc-driven transcription 发明人:LOAS ANDREI; PENTELUTE BRADLEY L; POMPLUN SEBASTIAN; JBARA MUHAMMAD; SCHISSEL CARLY KATHERINE; RODRIQUEZ JACOB JOSHUA LEE; BUCHWALD STEPHEN LEFFLER; BOIJA ANN; KLEIN ISAAC; HAWKEN SUSANA WILSON; LI CHARLES HAN 权利人:MASSACHUSETTS INST TECHNOLOGY; WHITEHEAD INSTITUTE OF BIOMEDICAL RES 摘要:The disclosure relates to covalent protein dimers of MYC, MAX, and Omomyc; pharmaceutical compositions comprising the covalent protein dimers; methods of making the covalent protein dimers; and methods of treating disorders associated with MYC dysregulation (e.g., cancer) with the covalent protein dimers.
专利号:US-11518794-B2 优先权日:2016-08-19 标 题:Synthesis method for liraglutide with low racemate impurity 发明人:FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG 权利人:SHENZHEN JYMED TECH CO LTD 摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.
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合成参考文献
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