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-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-9938509-B2 优先权日:2010-12-08 标 题 :Biocatalysts and methods for the synthesis of armodafinil 发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN 权利人:CODEXIS INC 摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.
专利号:US-10087221-B2 优先权日:2013-03-21 标题 :Synthesis of hydantoin containing peptide products 发明人:HENKEL BERND 权利人:SANOFI AVENTIS DEUTSCHLAND 摘要:The present invention relates to a method of synthesizing a peptide product comprising at least one hydantoin group. The peptide product may be used as a reference material for the quality control of pharmaceutical peptides, particularly for the quality control of exendin peptides. Further, the invention relates to hydantoin building blocks, a method for manufacturing such building blocks and their use for the synthesis of peptide products.
专利号:US-7122628-B2 优先权日:2000-12-22 标 题:Process for the synthesis of a peptide having a Trp residue 发明人:JACKSON STEVEN ALLEN 权利人:IPSEN MFG IRELAND LTD 摘要:A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said protecting group is removed during cleavage of said peptide from the solid support.
专利号:US-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
[参考文献]: Hillas Pj, Et Al. A Mechanism For Hydroxylation By Tyrosine Hydroxylase Based On Partitioning Of Substituted Phenylalanines. Biochemistry. 1996;35(22):6969-6975. [参考文献]: Luck La, Et Al. Fluorescence And 19F Nmr Evidence That Phenylalanine, 3-L-Fluorophenylalanine And 4-L-Fluorophenylalanine Bind To The L-Leucine Specific Receptor Of Escherichia Coli. Protein Sci. 2000;9(12):2573-2576. [参考文献]: Jing Yuan, Et Al. Genetic Mapping Of Targets Mediating Differential Chemical Phenotypes In Plasmodium Falciparum. Nat Chem Biol. 2009 Oct;5(10):765-71. [参考文献]: P J Hillas, Et Al. A Mechanism For Hydroxylation By Tyrosine Hydroxylase Based On Partitioning Of Substituted Phenylalanines. Biochemistry. 1996 Jun 4;35(22):6969-75. [参考文献]: Phedias Diamandis, Et Al. Chemical Genetics Reveals A Complex Functional Ground State Of Neural Stem Cells. Nat Chem Biol. 2007 May;3(5):268-73.
合成参考文献
摘要:Nguyen, B. N.; Hii, K. K.; Szymański, W.; Janssen, D. B., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 643. 摘要:Bartsch, S.; Vogel, A., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 306. 摘要:Bartsch, S.; Vogel, A., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 302. 摘要:Parmeggiani, F.; Galman, J. L.; Montgomery, S. L.; Turner, N. J., Science of Synthesis, (2019) , 408. 摘要:Lloyd, C. M.; Dowell, K. F.; Brittain, W. D. G., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.