专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-8314251-B2 优先权日:2008-03-07 标 题 :Total synthesis of salinosporamide A and analogs thereof 发明人:LING TAOTAO; DANISHEFSKY SAMUEL 权利人:LING TAOTAO; DANISHEFSKY SAMUEL; NEREUS PHARMACEUTICALS INC 摘要:The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).
专利号:US-8067616-B2 优先权日:2006-04-06 标 题 :Total synthesis of salinosporamide A and analogs thereof 发明人:LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A 权利人:LING TAOTAO; MACHERLA VENKATA RAMI REDDY; POTTS BARBARA CHRISTINE; MANAM RAMA RAO; MCARTHUR KATHERINE A; NEREUS PHARMACEUTICALS INC 摘要:The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:WO-0063152-A1 优先权日:1999-02-22 标题:Acetylated and related analogues of chicoric acid as hiv integrase inhibitors 发明人:BURKE TERRENCE R; ZHAIWEI LIN; ZHAO HE; NEAMATI NOURI; POMMIER YVES 权利人:US HEALTH; BURKE TERRENCE R; ZHAIWEI LIN; ZHAO HE; NEAMATI NOURI; POMMIER YVES 摘要:Chicoric acid analogues and derivatives have activity against HIV-1 integrase. The structural features that are required for this activity are elucidated by assaying these analogues and derivatives against HIV-1 integrase. Furthermore, methods of synthesis of the enantiomers of chicoric acid itself, as well as its analogues and derivatives, are disclosed. Additionally, methods of use of chicoric acid analogues and derivatives to inhibit HIV-1 integrase are disclosed, as are compositions comprising chicoric acid analogues and derivatives.
专利号:US-2021284668-A1 优先权日:2018-06-19 标题:Gold (i)-phosphine 1,2,3-triazole derivatives with antibiotic properties 发明人:MISLIN GAËTAN; SCHALK ISABELLE; PLÉSIAT PATRICK; PAULEN AURÉLIE 权利人:CENTRE NAT RECH SCIENT; UNIV FRANCHE COMTE; CENTRE HOSPITALIER REGIONAL UNIV DE BESANCON; UNIV STRASBOURG 摘要:The present invention relates to gold (I)-phosphine 1,2,3-triazole compounds, and their use in a human or animal medicine. The present invention also relates to using such compounds for the prevention and/or treatment of an infection, i.e. inhibitors of growth of Gram-positive and/or Gram-negative bacteria. On another aspect the invention relates to the synthesis of the gold (I)-phosphine compounds of the invention and to their synthesis intermediates. The present invention finds applications in the medical, veterinary and/or chemical fields.
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