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-4351762-A 优先权日:1981-03-10 标题:Rapid, quantitative peptide synthesis using mixed anhydrides 发明人:VERLANDER MICHAEL S; FULLER WILLIAM D; GOODMAN MURRAY 权利人:BIORESEARCH INC 摘要:In the synthesis of a polypeptide chain wherein an N alpha -urethane-protected amino acid mixed anhydride is coupled with an amino-unprotected second amino acid, the improvement comprising conducting said coupling at room temperature or above. This method provides rapid, essentially quantitative reactions without the necessity for reduced temperatures. The method is particularly useful in the solid-phase synthesis of peptides where shortened coupling cycles and improved yields of substantially pure products are obtained.
专利号:US-12441760-B2 优先权日:2013-08-29 标 题 :Amino diacids containing peptide modifiers 发明人:BARLOS KLEOMENIS; GATOS DIMITRIOS; BARLOS KOSTAS K; VASILEIOU ZOI 权利人:CHEMICAL & BIOPHARMACEUTICAL LABORATORIES OF PATRAS S A 摘要:The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.
专利号:US-6271345-B1 优先权日:1996-07-03 标 题 :Enzyme cleavable linker bound to solid phase for organic compound synthesis 发明人:WALDMANN HERBERT; SAUERBREI BERND; GRETHER UWE 权利人:BASF AG 摘要:An enzyme cleavable linker is prepared on which organic compounds are synthesized when the linker is bound to a solid phase. The linker contains a functional group on which a synthesized organic compound is bound when synthesis takes place, and a recognition site for a hydrolytic enzyme. Reacting the linker with the enzyme causes the linker to fragment at a site different from the recognition site to liberate the synthesized organic compound. The solid phase may be a crosslinked polyacrylamide containing an amino group for attaching the linker, and the linker is bound to the solid phase via a spacer. The spacer is attached to the solid phase by an ester, ether, amide or amine linkage, or a sulfide or phosphate linkage. In a specific reaction of forming a solid phase containing the linker, 2-acetoxy-5-hydroxymethylbenzoic acid is attached to an amino group-containing polymer via a spacer followed by conversion to a chloroformic ester.
专利号:US-6339160-B1 优先权日:1997-07-17 标题:Metalloproteinase inhibitors, their therapeutic use and process for the production of the starting compound in the synthesis thereof 发明人:POLITI VINCENZO; GAVUZZO ENRICO; GALLINA CARLO; STAZIO GIOVANNI DI; D ALESSIO SILVANA; SELLA ANTONIO; PIAZZA CINZIA; GIORDANO CESARE; GORINI BARBARA; PANINI GABRIELLA; PARADISI MARIO PAGLIALUNGA; CIRILLI MAURIZIO; POCHETTI GIORGIO; MAZZA FERNANDO 权利人:POLIFARMA SPA; CONSIGLIO NAZIONALE RICERCHE 摘要:Objects of the present invention are compounds of a peptido-mimetic character having the capacity of acting as inhibitors of metalloproteinases produced by venom of snake, and of other metalloproteinases of human origin which have been put in relation with various pathologies in man, including tumoral growth and metastatization, aterosclerosis, multiple sclerosis, Alzheimer's disease, osteoporosis, hypertension, rheumatoid arthritis and other inflammatory diseases. n Object of the present invention is also the procedure for the production of diethylester of (1)-phosphotryptophan, as an initial product necessary to synthesize all compounds mentioned above.
专利号:WO-2023040981-A1 优先权日:2021-09-20 标 题:Methods and compositions for weight management 发明人:HUA NG MENG; WANG RUIQI RACHEL; LIANG KUN; ZHENG ZIPENG; YANG JIE 权利人:AEGOGEN SUZHOU LTD 摘要:This present application relates to the use of small molecules for weight management, prevention of aging and the treatment of associated conditions and diseases. The present application also provides for the synthesis of some of the molecules and the administration of these molecules for drug discovery, nutrition and cosmeceutical purposes.
参考标题:Allenone-Mediated Racemization/epimerization-Free Peptide Bond Formation And Its Application In Peptide Synthesis 作者:Zhengning Wang,Xuewei Wang,Penghui Wang,Junfeng Zhao |发布日期:2021.7.14 摘要:Peptide Synthesis (Spps). The Robustness Of The Allenone-Mediated Peptide Bond Formation Was Showcased Incisively By The Synthesis Of Carfilzomib, Which Involved A Rare Racemization-/epimerization-Free N To C Peptide Elongation Strategy. Furthermore, The Successful Synthesis Of The Model Difficult Peptide Acp (65-74) On A Solid Support Suggested That This Method Was Compatible With Spps. This Method Combines
合成参考文献
参考文献:10.1038/s41538-019-0050-z 摘要:Shirako S, Kojima Y, Tomari N, Nakamura Y, Matsumura Y, Ikeda K, Inagaki N, Sato K. Pyroglutamyl leucine, a peptide in fermented foods, attenuates dysbiosis by increasing host antimicrobial peptide. npj Science of Food. 2019 Oct 07;3(1):18. doi: 10.1038/s41538-019-0050-z.