专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
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:WO-2022156692-A1 优先权日:2021-01-22 标 题 :Cyclic peptide viral protease inhibitor, preparation method therefor, and application thereof in antiviral drugs 发明人:LI XINGZHOU; XU LEI; LI SONG; ZHONG WU; CAO RUIYUAN; XIAO JUNHAI; ZHOU XINBO; ZHENG ZHIBING; LI WEI; FAN SHIYONG; XIAO DIAN; WANG ZIHAO; XIE FEI 权利人:ACAD OF MILITARY MEDICAL SCIENCES 摘要:The present invention relates to the field of pharmaceutical chemicals, relates to a cyclic peptide compound as shown in formula M or a stereoisomer, a tautomer or a mixture of the compound, a pharmaceutically acceptable salt, a polymorph, a eutectic or a solvate of the compound, or a stable isotope derivative, a metabolite or a prodrug of the compound, and further relates to a method and an intermediate for synthesis of the cyclic peptide compound. The provided cyclic peptide compound has a strong inhibitory effect on 3CL protease of coronavirus and 3CL protease of picornaviridae, such as Enterovirus EV71 virus. By means of cell level activity testing, the provided cyclic peptide compound has a significant inhibitory effect on EV71 virus and coronavirus. Moreover, the cyclic peptide compound as shown in formula M can generate a virus inhibition effect on a cell level by inhibiting viral protease activity, and has a good application prospect in antiviral drugs.
专利号:US-4761404-A 优先权日:1985-07-01 标题:Phospholipid analogs useful as PAF synthesis inhibitors 发明人:BUGIANESI ROBERT L; PONPIPOM MITREE M; RUPPRECHT KATHLEEN M 权利人:MERCK & CO INC 摘要:There are disclosed phospholipid analogs which are useful as PAF synthesis inhibitors. These compounds inhibit PAF (platelet-activating factor) biosynthesis and are thereby useful in the treatment of various diseases or disorders mediated by the PAF such as, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, and adult respiratory distress syndrome.
1. Yao L, Li H, Tu K, Zhang L, Cheng Z, Zhu AX. Construction of NIR Light Controlled Micelles with Photothermal Conversion Property: Poly(poly(ethylene glycol)methyl ether methacrylate) (PPEGMA) as Hydrophilic Block and Ketocyanine Dye as NIR Photothermal Conversion Agent. Polymers (Basel). 2020 May 21;12(5):1181. doi: 10.3390/polym12051181.
合成参考文献
摘要:Harnying, W.; Berkessel, A., Science of Synthesis: Knowledge Updates, (2024) 1, 361.