专利号:US-9771377-B2 优先权日:2012-12-21 标 题 :Synthesis of FR901464 and analogs with antitumor activity 发明人:KOIDE KAZUNORI; OSMAN SAMI SAIF ELDIN ALI 权利人:UNIV OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION 摘要:The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
专利号:WO-9102739-A1 优先权日:1989-08-11 标题:Synthesis of glycosides having predetermined stereochemistry 发明人:DANISHEFSKY SAMUEL J 权利人:UNIV YALE 摘要:Methods of stereoselectively preparing a substituted 1,2-anhydrosugar wherein a substituted glycal is converted into a 1,2-anhydrosugar that is utilized to glycosylate a hydroxyl group containing glycal, are disclosed. Methods of preparing a saccharide multimer wherein a nucleophile is reacted with a substituted 1,2-anhydrosugar having a plurality of non-participating substituents, are disclosed. In addition, methods of preparing stereospecific halo-substituted saccharide multimers by haloglycosylation of a glycosyl donor substituted glycal and a glycosyl acceptor glycal derivative in the absence of water and in the presence of a halonium ion, are disclosed. Methods of preparing stereospecific particle-linked halo-substituted saccharide multimers, by haloglycosylation of a particle-linked nucleophilic hydroxyl group with a substituted glycal and a halonium ion, are also disclosed.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-8309599-B2 优先权日:2006-09-08 标题 :Synthesis of FR901464 and analogs with antitumor activity 发明人:KOIDE KAZUNORI; ALBERT BRIAN J; SIVARAMAKRISHNAN ANANTHAPADMANABHAN 权利人:KOIDE KAZUNORI; ALBERT BRIAN J; SIVARAMAKRISHNAN ANANTHAPADMANABHAN; UNIV PITTSBURGH 摘要:The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
专利号:US-2008096879-A1 优先权日:2006-09-08 标题:Synthesis of fr901464 and analogs with antitumor activity
专利号:US-7825267-B2 优先权日:2006-09-08 标 题 :Synthesis of FR901464 and analogs with antitumor activity