专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-8742028-B2 优先权日:2009-05-06 标 题:Solid support for Fmoc-solid phase synthesis of peptide acids 发明人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R 权利人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R; MALLINCKRODT LLC 摘要:The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.
专利号:US-5124478-A 优先权日:1987-12-22 标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
专利号:US-8796454-B2 优先权日:2012-05-04 标 题 :Synthesis of [2.2.2]-diazabicyclic ring systems 发明人:SCHEERER JONATHAN R 权利人:COLLEGE WILLIAM & MARY 摘要:Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.
专利号:US-5679773-A 优先权日:1995-01-17 标题 :Reagants and methods for immobilized polymer synthesis and display 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:Compounds and methods for solid phase synthesis of organic molecules including peptides, oligonucleotides, benzodiazepines, beta -turn mimetics, and prostaglandins. The present invention provides new reagents in the form of linking groups and resins and substrates having attached linking groups which are useful in solid phase synthesis of high density arrays of organic molecules. The invention also provides methods which increase yields of various organic synthesis strategies.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
[参考文献]: Graciliana Lopes, Et Al. Can Phlorotannins Purified Extracts Constitute A Novel Pharmacological Alternative For Microbial Infections With Associated Inflammatory Conditions. Plos One. 2012;7(2):E31145. [参考文献]: Jong H Kim, Et Al. Antifungal Activity Of Redox-Active Benzaldehydes That Target Cellular Antioxidation. Ann Clin Microbiol Antimicrob. 2011 May 31:10:23. [参考文献]: Justin Maresh, Et Al. Rational Design Of Inhibitors Of Vira-Virg Two-Component Signal Transduction. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3281-6. [参考文献]: Lidia Montero, Et Al. Anti-Proliferative Activity And Chemical Characterization By Comprehensive Two-Dimensional Liquid Chromatography Coupled To Mass Spectrometry Of Phlorotannins From The Brown Macroalga Sargassum Muticum Collected On North-Atlantic Coasts. J Chromatogr A. 2016 Jan 8:1428:115-25. [参考文献]: Ulrik Boas, Et Al. The Ortho Backbone Amide Linker (O-Bal) Is An Easily Prepared And Highly Acid-Labile Handle For Solid-Phase Synthesis. J Comb Chem. 2002 May-Jun;4(3):223-8.
合成参考文献
摘要:Minbiole, K. P. C., Science of Synthesis, (2009) 46, 166. 摘要:Hlina, J. A., Science of Synthesis Knowledge Updates, (2021) 1, 132. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 59. 摘要:Schnürch, M.; Hämmerle, J.; Stanetty, P., Science of Synthesis Knowledge Updates, (2010) 1, 157. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 330.