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-10793495-B2 优先权日:2015-08-14 标 题:Synthesis of polyaryl substituted aryl compounds 发明人:BOULOS RAMIZ; FEUTRILL JOHN 权利人:BOULOS & COOPER PHARMACEUTICALS PTY LTD 摘要:A method for the synthesis of a aryl compound of Formula (1).n nU T-W—R 1 ) n    (1)
专利号:WO-2017082924-A1 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 TERRENCE R JR; HYMEL DAVID 权利人:THE US SECRETARY DEPT 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. 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-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-10047122-B2 优先权日:2013-03-14 标 题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:QIAN WENJIAN; PARK JUNG EUN; LAI CHRISTOPHER C; KELLEY JAMES A; LEE KYUNG S; BURKE JR TERRENCE R 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The invention provides novel compounds that may serve as anticancer therapeutics. The compounds of the invention bind to polo-like kinases through the polo-box domain. In certain embodiments, the compounds of the invention are POM-protected peptide derivatives. The use of cationic bis-alkyl his residues in combination with a mono POM-protected phophoryl group results in a peptide possessing an overall neutral charge. The peptide derivatives of the invention have achieved both good efficacy and an enhanced bioavailability. The invention also provides methods of use, compositions, and kits thereof. Further, the invention provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-6235871-B1 优先权日:1997-12-03 标题:Synthesis of oligoarylamines, and uses and reagents related thereto 发明人:SINGER ROBERT A; SADIGHI JOSEPH P; BUCHWALD STEPHEN L; MACKEWITZ THOMAS 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The transition metal-catalyzed amination of aryl halides, in conjunction with an orthogonal protective group scheme, forms the basis of two routes to oligoaniline precursors. The oligoaniline precursors are soluble in a variety of common organic solvents, and are easily converted to the deprotected oligoanilines. The method allows the preparation of oligoanilines of even or odd chain lengths, and the incorporation of a variety of functional groups into the oligomers. Polyanilines of low polydispersity can also be prepared by this method.
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