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-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:WO-2025128985-A1 优先权日:2023-12-14 标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-2022243244-A1 优先权日:2019-10-10 标 题 :Compositions and methods for in vivo synthesis of unnatural polypeptides 发明人:ROMESBERG FLOYD E; FISCHER EMIL C; HASHIMOTO KOJI; FELDMAN AARON W; DIEN VIVIAN T; ZHANG YORKE 权利人:SCRIPPS RESEARCH INST 摘要:Disclosed herein are compositions, methods, and kits for a cell incorporating unnatural amino acids into an unnatural polypeptide. Also disclosed herein are compositions, methods, and kits for increasing activity and yield of the unnatural polypeptide synthesized by the cell.
[参考文献]: Candace M Pfefferkorn, Et Al. 5-Fluoro-D,L-Tryptophan As A Dual Nmr And Fluorescent Probe Of α-Synuclein. Methods Mol Biol. 2012:895:197-209. [参考文献]: Jaap Broos, Et Al. In Vivo Synthesized Proteins With Monoexponential Fluorescence Decay Kinetics. J Am Chem Soc. 2004 Jan 14;126(1):22-3. [参考文献]: Kenji Hamase, Et Al. Sensitive High-Performance Liquid Chromatographic Assay For D-Amino-Acid Oxidase Activity In Mammalian Tissues Using A Fluorescent Non-Natural Substrate, 5-Fluoro-D-Tryptophan. J Chromatogr A. 2006 Feb 17;1106(1-2):159-64. [参考文献]: Madan Katragadda, Et Al. Hydrophobic Effect And Hydrogen Bonds Account For The Improved Activity Of A Complement Inhibitor, Compstatin. J Med Chem. 2006 Jul 27;49(15):4616-22. [参考文献]: N V Visser, Et Al. 5-Fluorotryptophan As Dual Probe For Ground-State Heterogeneity And Excited-State Dynamics In Apoflavodoxin. Febs Lett. 2009 Sep 3;583(17):2785-8.
合成参考文献
参考文献:10.1007/s00726-014-1766-3 摘要:Pantouris G, Serys M, Yuasa HJ, Ball HJ, Mowat CG. Human indoleamine 2,3-dioxygenase-2 has substrate specificity and inhibition characteristics distinct from those of indoleamine 2,3-dioxygenase-1. Amino Acids. 2014 Sep;46(9):2155–63. doi: 10.1007/s00726-014-1766-3. 参考文献:10.1007/s00294-005-0042-1 摘要:Schroda M. RNA silencing in Chlamydomonas: mechanisms and tools. Curr Genet. 2006 Feb;49(2):69–84. doi: 10.1007/s00294-005-0042-1.