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-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
专利号:US-12441760-B2 优先权日:2013-08-29 标 题 :Amino diacids containing peptide modifiers 发明人:BARLOS KLEOMENIS; GATOS DIMITRIOS; BARLOS KOSTAS K; VASILEIOU ZOI 权利人:CHEMICAL & BIOPHARMACEUTICAL LABORATORIES OF PATRAS S A 摘要:The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.
专利号:BR-112014026077-B1 优先权日:2012-04-20 标 题 :METHOD OF SOLID PHASE SYNTHESIS OF A PROTECTED, PARTIALLY PROTECTED OR UNPROTECTED INSULIN B CHAIN OR AN INSULIN B CHAIN DERIVATIVE, AND METHOD FOR PREPARING AN INSULIN B CHAIN PEPTIDE
专利号:US-2014350219-A1 优先权日:2011-09-14 标题:Method for solid phase synthesis of liraglutide
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合成参考文献
参考文献:10.1007/s00125-002-0894-6 摘要:O'Harte FP, Gault VA, Parker JC, Harriott P, Mooney MH, Bailey CJ, Flatt PR. Improved stability, insulin-releasing activity and antidiabetic potential of two novel N-terminal analogues of gastric inhibitory polypeptide: N-acetyl-GIP and pGlu-GIP. Diabetologia. 2002 Sep;45(9):1281–91. doi: 10.1007/s00125-002-0894-6.