专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-5367072-A 优先权日:1990-12-14 标 题 :Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS R 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-4311645-A 优先权日:1980-03-24 标 题 :Synthesis of SRS-active compounds 发明人:ROSENBERGER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:A chemical synthesis of an SRS-A active compound from the reaction product of 1-halo-2-octyne and the ether of 2-penten-4-yn-1-ol including intermediates in the synthesis, some of which being antagonists of SRS-A useful for treating allergic reactions.
专利号:US-10905769-B2 优先权日:2015-11-13 标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-4800166-A 优先权日:1985-04-19 标题:Method and apparatus for monitoring the automated synthesis of peptides 发明人:HORN MARCUS J; RECCHIA JOANNE 权利人:APPLIED PROTEIN TECHNOLOGIES 摘要:A method for monitoring a solid-phase peptide synthesis for free amino ends of unreacted peptide chains, the monitoring occurring at the end of each addition of a blocked amino acid to the peptide chains which are anchored to the solid phase. The method includes reacting the solid phase with a monitoring agent that forms a covalent bond with unblocked amino groups. The solid phase is then washed to remove the unreacted monitoring agent. A cleaving reagent is then used to selectively remove the covalently bound monitoring reagent from the ends of the unblocked peptide chains, while leaving the blocked chains intact. The amount of monitoring agent thus removed is then quantitatively measured to determine what proportion of the initial peptide chains failed to react with the blocked amino acid. Preferred monitoring agents for use in this process include trityl (triphenylmethyl) -based groups, and particularly preferred agents are trityl, monomethoxytrityl, dimethoxytrityl, and trimethoxytrityl chlorides.
专利号:US-4432906-A 优先权日:1981-09-14 标 题 :Inhibitors of SRS-synthesis 发明人:COHEN NOAL; WEBER GIUSEPPE 权利人:HOFFMANN LA ROCHE 摘要:Methyl derivatives of arachidonic acid and intermediates thereto have been synthesized. These derivatives are inhibitors of SRS-A synthesis and are useful for treating and preventing allergic reactions.
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合成参考文献
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