专利号:WO-2024181781-A1 优先权日:2023-02-27 标 题:Substrate for synthesis of biological polymers having anti-aggregation function and biological polymer synthesis method using same 发明人:JANG MYOUNG HOON; CHOI JAE SUN 权利人:SP2 TX INC 摘要:The present invention relates to a substrate for the synthesis of biological polymers having an anti-aggregation function, and a biological polymer synthesis method using the substrate. The substrate according to an aspect may have anti-aggregation functionality to enable high-yield and high-purity processes in the synthesis of biological polymers.
专利号:WO-2023039068-A1 优先权日:2021-09-08 标题:Compositions and methods for synthesis of peptide nucleic acid intermediates 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:NEUBASE THERAPEUTICS INC 摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
专利号:WO-2024165450-A1 优先权日:2023-02-09 标题:Method of chemical synthesis of single-chain antibody fragments and products thereby obtained 发明人:FIGINI MARIANGELA; LUISON ELENA 权利人:GLYTECH INC; FIGINI MARIANGELA 摘要:A new method is disclosed for the protein full-chemical synthesis of single-chain antibody fragments (scFv); the obtained products are structurally close and functionally equivalent to their biological counterpart, being however, advantageously free of impurities and more reproducible in properties. The method includes the general steps of: (a) separately synthetizing sub-sequences (peptide fragments) (b) sequentially assembling the sub-sequences obtained in step (a) in the order as they appear in the target scFv amino acid sequence, and (c) performing oxidative folding of the assembled whole peptide molecule obtained in step (b) and dialyzing the resulting product in a buffer.
专利号:US-11414375-B2 优先权日:2016-07-29 标题:Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide 发明人:ZHAO JUNFENG; HU LONG; XU SILIN; ZHAO ZHENGUANG 权利人:UNIV JIANGXI NORMAL 摘要:Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.
专利号:US-2025282813-A1 优先权日:2021-04-09 标 题 :Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates 发明人:OKADA YOHEI; SUZUKI HIDEAKI; LUTHER ANATOL 权利人:BACHEM HOLDING AG 摘要:A novel pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates are provided. The pseudo solid phase protecting group is represented by formula II wherein: * indicates the point of attachment to an oxygen atom of a hydroxyl moiety of the nucleoside, the nucleotide, the oligonucleotide, or of the conjugate of a nucleoside, a nucleotide or an oligonucleotide to be protected; c is 0 or 1; a is an integer of 1 to 12; R3 is H; R5 is O—R6 or H, where R6 is a C8-C40 aliphatic hydrocarbon group; each of R4 is independently O—R6, where R6 is at each occurrence independently a C8-C40 aliphatic hydrocarbon group; b is 1 to 3; with the proviso that if b is 1, at least one of R3 and R5 is not H; and with the further proviso that the sum of all carbon atoms contained in the R3, R4, and R5 moieties present is larger than 23 and smaller than 200.
专利号:US-2025090698-A1 优先权日:2018-11-27 标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases 发明人:CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.
[参考文献]: Daniel J Rubin, Et Al. Structural, Nanomechanical, And Computational Characterization Of D,L-Cyclic Peptide Assemblies. Acs Nano. 2015 Mar 24;9(3):3360-8. [参考文献]: Fazel Shabanpoor, Et Al. Bi-Specific Splice-Switching Pmo Oligonucleotides Conjugated Via A Single Peptide Active In A Mouse Model Of Duchenne Muscular Dystrophy. Nucleic Acids Res. 2015 Jan;43(1):29-39. [参考文献]: Joshua D Carter, Et Al. Coupling Strategies For The Synthesis Of Peptide-Oligonucleotide Conjugates For Patterned Synthetic Biomineralization. J Nucleic Acids. 2011:2011:926595. [参考文献]: Liz O'Donovan, Et Al. Parallel Synthesis Of Cell-Penetrating Peptide Conjugates Of Pmo Toward Exon Skipping Enhancement In Duchenne Muscular Dystrophy. Nucleic Acid Ther. 2015 Feb;25(1):1-10. [参考文献]: Ting-Jung Chen, Et Al. Targeted Herceptin-Dextran Iron Oxide Nanoparticles For Noninvasive Imaging Of Her2/neu Receptors Using Mri. J Biol Inorg Chem. 2009 Feb;14(2):253-60.
合成参考文献
摘要:Drabowicz, J.; Kiełbasiński, P.; Łyżwa, P.; Mikołajczyk, M.; Zając, A., Science of Synthesis, (2009) 42, 737. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 264. 摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2019) 1, 415. 摘要:Goetzke#, F. W.; Modicom#, F.; Fletcher, S. P., Science of Synthesis, (2022) , 344. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).