专利号:US-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-9260371-B2 优先权日:2004-11-01 标题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN RUTH; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; SLETTEN ELLEN MAY 权利人:UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-9422232-B2 优先权日:2009-07-09 标题:Reductive release probes containing a chemoselectively cleavable α-azidoether linker and methods of use thereof 发明人:FRANZINI RAPHAEL M; KOOL ERIC TODD 权利人:FRANZINI RAPHAEL M; KOOL ERIC TODD; UNIV LELAND STANFORD JUNIOR 摘要:Probes comprising one or more selectively cleavable α-azidoether moieties are provided; and linkers comprising the one or more selectively cleavable α-azidoether moieties. The α-azidoether moiety will undergo a Staudinger reaction with a suitable reducing agent, resulting in cleavage. The probes find use in a variety of detection assays, e.g. specific polynucleotide binding assays, polypeptide binding assays, etc. The cleavable linkers are suitable for synthetic reactions, e.g. to prepare probes of the invention; in the synthesis of cleavable peptide conjugates; and the like.
专利号:US-5616698-A 优先权日:1994-01-10 标题:Polymer-supported solution synthesis of oligosaccharides 发明人:KREPINSKY JIRI J; DOUGLAS STEPHEN P; WHITFIELD DENNIS M 权利人:UNIV TORONTO 摘要:The present invention provides improved syntheses of oligosacchairdes. In accordance with preferred embodiments, anomeric specificity in such syntheses can be attained using polymer-supported liquid synthetic design with certain novel diether linkers. The present invention also provides novel strategies for capping imcompletely glycosylated hydroxyls.
专利号:US-6417396-B1 优先权日:1997-09-24 标 题 :Quenching reagents for solution phase synthesis 发明人:NIKAM SHAM 权利人:WARNER LAMBERT CO 摘要:A method for enhancing the purity of a desired compound comprising:Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents;Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: andStep (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.
专利号:US-9603951-B2 优先权日:2010-02-08 标题 :Methods and apparatus for synthesizing imaging agents, and intermediates thereof 发明人:LAZEWATSKY JOEL; DEVINE MARYBETH 权利人:LANTHEUS MEDICAL IMAGING INC 摘要:The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 18 F). Various embodiments of the invention may be useful as sensors, diagnostic tools, and the like. In some cases, methods for evaluating perfusion, including myocardial perfusion, are provided. Synthetic methods of the invention have also been incorporated into an automated synthesis unit to prepare and purify imaging agents that comprise a radioisotope. In some embodiments, the present invention provides a novel methods and systems comprising imaging agent 1, including methods of imaging in a subject comprising administering a composition comprising imaging agent 1 to a subject by injection, infusion, or any other known method, and imaging the area of the subject wherein the event of interest is located.
[参考文献]: Stefania Colarusso, Et Al. Evolution, Synthesis And Sar Of Tripeptide Alpha-Ketoacid Inhibitors Of The Hepatitis C Virus Ns3/ns4A Serine Protease. Bioorg Med Chem Lett. 2002 Feb 25;12(4):705-8.
合成参考文献
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