专利号:US-6359144-B1 优先权日:1997-02-04 标 题 :Combinatorial libraries of bicyclic guanidine derivatives and compounds therein 发明人:OSTRESH JOHN M; MEYER JEAN-PHILIPPE; DOOLEY COLETTE T; BLONDELLE SYLVIE E; SCHONER CHRISTA C; HOUGHTEN RICHARD A 权利人:LION BIOSCIENCE AG 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of combinatorial libraries of bicyclic guanidine compounds. The present invention further provides the compounds made by the combinatorial synthesis and individually as well as methods of using the same.
专利号:US-4301065-A 优先权日:1977-05-25 标 题 :Novel polypeptides having thymic activity or an antagonistic activity and processes for their synthesis 发明人:BACH JEAN-FRANCOIS; DARDENNE MIREILLE; PLEAU JEAN-MARIE; HAMBURGER JEAN; BRICAS EVANGHELOS; MARTINEZ JEAN; BLANOT DIDIER; AUGER GENEVIEVE 权利人:ANVAR 摘要:The invention is concerned with novel polypeptides and processes for the synthesis thereof. It is concerned with compounds having the sequence X-Gln-Gly-Gly-Y in which Y represents -Ser-Asn and X represents Ser-, Lys-Ser-, Ala-Lys-Ser-, Glx-Ala-Lys-Ser-; Glx representing Pyro-Glu or Gln; and when X represents Glx-Ala-Lys-Ser-, Y may in addition represent -Ser; as well as their derivatives comprising one or two modified amino acids, with the exception of the unmodified compound PyroGlu-Ala-Lys-Ser-Gln-Gly-Ser-Asn. These polypeptides are useful as medicines.
专利号:WO-9811438-A1 优先权日:1996-09-13 标题 :Synthesis of quinazolinone libraries and derivatives thereof
参考标题:Diversity-Oriented Synthesis Of Macrocyclic Peptidomimetics 作者:Albert Isidro-Llobet,Tiffanie Murillo,Paula Bello,Agostino Cilibrizzi,James T. Hodgkinson,Warren R. J. D. Galloway,Andreas Bender,Martin Welch,David R. Spring |发布日期:2011.4.26 摘要:Structurally Diverse Libraries Of Novel Small Molecules Represent Important Sources Of Biologically Active Agents. In This Paper We Report The Development Of A Diversity-Oriented Synthesis Strategy For The Generation Of Diverse Small Molecules Based Around A Common Macrocyclic Peptidomimetic Framework, Containing Structural Motifs Present In Many Naturally Occurring Bioactive Compounds. Macrocyclic Peptidomimetics Are Largely Underrepresented In Current Small-Molecule Screening Collections Owing Primarily To Synthetic Intractability; Thus Novel Molecules Based Around These Structures Represent Targets Of Significant Interest, Both From A Biological And A Synthetic Perspective. In A Proof-Of-Concept Study, The Synthesis Of A Library Of 14 Such Compounds Was Achieved. Analysis Of Chemical Space Coverage Confirmed That The Compound Structures Indeed Occupy Underrepresented Areas Of Chemistry In Screening Collections. Crucial To The Success Of This Approach Was The Development Of Novel Methodologies For The Macrocyclic Ring Closure Of Chiral α-Azido Acids And For The Synthesis Of Diketopiperazines Using Solid-Supported N Methylmorpholine. Owing To Their Robust And Flexible Natures, It Is Envisaged That Both New Methodologies Will Prove To Be Valuable In A Wider Synthetic Context.
合成参考文献
参考文献:10.1038/s41563-025-02320-9 摘要:Lin Y, Li M, Luo Z, Meng Y, Zong Y, Ren H, Yu X, Tan X, Liu F, Wei T, Cheng Q. Tissue-specific mRNA delivery and prime editing with peptide-ionizable lipid nanoparticles. Nat Mater. 2026 Jan;25(1):133–45. doi: 10.1038/s41563-025-02320-9.