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-9919064-B2 优先权日:2012-08-10 标 题 :Compositions, methods, and systems for the synthesis and use of imaging agents 发明人:CESATI RICHARD R; RADEKE HEIKE S; PANDEY SURESH K; PUROHIT AJAY; ROBINSON SIMON P 权利人:LANTHEUS MEDICAL IMAGING INC 摘要:The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
专利号:US-2006167268-A1 优先权日:2002-04-09 标 题:Growth hormone secretagogues 发明人:EVERS BRITTA; GERD RUEHTER; MARTIN DE LA NAVA EVA M; TEBBE MARK J 权利人:ELI LILLY AND COMPANY PATENT D 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:US-2003082830-A1 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
专利号:US-5985844-A 优先权日:1992-03-26 标题:Homoerythromycin A derivatives modified at the 4'-and 8A-positions 发明人:HECK JAMES V; LEANZA WILLIAM J; RATCLIFFE RONALD W; SALZMANN THOMAS N; SHANKARAN KOTHANDARAMAN; SZYMONIFKA MICHAEL J; WILKENING ROBERT R 权利人:MERCK & CO INC 摘要:Compounds of the formula: where R is hydrogen, hydroxyl, alkyl or acyl, R' and R'' together are oxo, hydroxyimino or alkoxyimino, and R' and R'' independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
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
[参考文献]: Inês F Antunes, Et Al. Synthesis And Evaluation Of [18F]-Feanga As A Pet Tracer For Beta-Glucuronidase Activity. Bioconjug Chem. 2010 May 19;21(5):911-20.
合成参考文献
摘要:National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program., JAN1986