专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
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-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-9034630-B2 优先权日:2009-09-21 标题 :Modified gram-negative bacteria for use as vaccines 发明人:GORVEL JEAN-PIERRE; ARCE GORVEL VILMA; IRIARTE MAITE; MORIYON IGNACIO; CONDE-ALVAREZ RAQUEL 权利人:INST NAT SANTE RECH MED; CT NAT DE LA RECH SCIENTIFIQUE—CNRS; UNIV LA MEDITERRANEE—AIX MARSEILLE II; UNIV NAVARRA; UNIV AIX MARSEILLE 摘要:The invention relates to Gram-negative bacteria carrying an inactivated gene encoding a glycosyltransferase involved in the synthesis of the core of the LPS of said Gram-negative bacteria, wherein said inactivated gene results in the synthesis of a LPS having a modified core. These strains have an attenuated virulence but induce a humoral immunity sufficient for ensuring vaccination of the host.
专利号:EP-0548237-B1 优先权日:1990-09-10 标 题:Method for the production of an article from the Copolymer of Lactide and (e)-Caprolactone for medical applications 发明人:GRIJPMA DIRK WYBE; PENNINGS ALBERT JOHAN 权利人:UNIV GRONINGEN 摘要:The invention relates to a method for the production of an article from a copolymer of lactide and epsilon -caprolactone for medical applications, in which method the copolymer is obtained by a synthesis which is carried out as a bulk synthesis at a temperature of 80 to 160 DEG C. Articles according to the invention can be used in numerous fields, but are in particular advantageous if they are employed in biomedical fields. Examples are an implant for the repair of a meniscus or a blood vessel, stents or artificial skin. Stents are small spirals which are used to hold open (coronary) arteries which have silted up. Use in abdominal wall reconstruction is also possible.
专利号:US-2014256904-A1 优先权日:2011-08-15 标 题:Biotechnological synthesis process of omega-functionalized carbon acids and carbon acid esters from simple carbon sources 发明人:SCHAFFER STEFFEN; DECKER NICOLE; GIELEN JASMIN; HAEGER HARALD; HAAS THOMAS; POETTER MARKUS; HENNEMANN HANS-GEORG; WESSEL MIRJA; VOLLAND MICHAEL 权利人:SCHAFFER STEFFEN; DECKER NICOLE; GIELEN JASMIN; HAEGER HARALD; HAAS THOMAS; POETTER MARKUS; HENNEMANN HANS-GEORG; WESSEL MIRJA; VOLLAND MICHAEL; EVONIK DEGUSSA GMBH 摘要:The subject of the invention is a biotechnological process for the production of ω-functionalized carboxylic acids and of ω-functionalized carboxylate esters from simple carbon sources.
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合成参考文献
参考文献:10.1111/j.1365-2958.2011.07765.x 摘要:Hankins JV, Madsen JA, Giles DK, Childers BM, Klose KE, Brodbelt JS, Trent MS. Elucidation of a novel Vibrio cholerae lipid A secondary hydroxy‐acyltransferase and its role in innate immune recognition. Molecular Microbiology. 2011 Jul 18;81(5):1313–29. doi: 10.1111/j.1365-2958.2011.07765.x.