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:WO-0006525-A9 优先权日:1998-07-25 标题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
专利号:WO-0006525-A2 优先权日:1998-07-25 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
专利号:US-2009227575-A1 优先权日:2008-03-04 标 题 :7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS 发明人:VENKATESAN ARANAPAKAM MUDUMBAI; CHEN ZECHENG; DOS SANTOS OSVALDO; BROOIJMANS NATASJA; GOPALSAMY ARIAMALA 权利人:WYETH CORP 摘要:A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I n n n n n n n n n n wherein Ar, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and n are as defined in the specification, and methods for making same.
专利号:US-6448443-B1 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
专利号:US-5521179-A 优先权日:1991-04-18 标题 :Heterocyclic amides 发明人:BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.