专利号:CN-104284891-A 优先权日:2012-03-17 标 题:Conformational Restricted Total Synthesis of Macrocyclic Compounds
专利号:EP-2311786-A2 优先权日:2005-06-09 标题 :Methods for synthesis of encoded libraries
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-2024124517-A1 优先权日:2020-12-25 标题:Method for producing peptide compound containing n-substituted-amino acid residue 发明人:MORITA YUYA; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:An object of the present invention is to provide a method for efficiently producing a high-purity peptide compound with a high yield. It has been found that the object can be achieved by supporting a peptide on a solid phase synthesis resin prior to a first elongation reaction in a solid phase process.
专利号:CN-114085269-A 优先权日:2021-11-12 标 题:A kind of all-solid-phase synthesis method of Hoshinoamide A
专利号:CN-114085269-B 优先权日:2021-11-12 标题:A total solid-phase synthesis method of Hoshinoamide A
参考标题:First Total Synthesis Of Versicotide D And Analogs 作者:Laura Posada,Gloria Serra |发布日期:2019.11 摘要:The First Total Synthesis Of Cyclotetrapeptide Versicotide D Has Been Achieved In 21% Overall Yield Using Solid Phase Peptide Synthesis And Solution Cyclization. In Addition, In The Search For Candidates Of Antimalarial New Drugs, One Cyclic Tetrapeptide Analog Which Differs In The Sequence, And Four Cyclic Pentapeptide Containing N-Methyl Amino Acids, Were Prepared. The Obtained Compunds Were Evaluated
合成参考文献
参考文献:10.1038/s41564-021-01013-8 摘要:Li L, Koirala B, Hernandez Y, MacIntyre LW, Ternei MA, Russo R, Brady SF. Identification of structurally diverse menaquinone-binding antibiotics with in vivo activity against multidrug-resistant pathogens. Nature Microbiology. 2021 Dec 23;7(1):120–31. doi: 10.1038/s41564-021-01013-8.