专利号:WO-9222662-A1 优先权日:1991-06-10 标 题:Methods for the synthesis of monofucosylated oligosaccharides terminating in di-n-acetyllactosaminyl structures 发明人:VENOT ANDRE P; KASHEM MOHAMMED A; SMITH RICHARD H 权利人:ALBERTA RES COUNCIL 摘要:Disclosed are methods for the preparation of monofucosylated and sialylated derivatives of the compound $g(b)Gal(1-4)$g(b)GlcNAc(1-3)$g(b)Gal(1-4)$g(b)GlcNAc-R. In particular, the methods of this invention provide for a multi-step synthesis wherein selective monofucosylation is accomplished on the 3-hydroxy group on only one of the GlcNAc units found in the $g(b)Gal(1-4)$g(b)GlcNAc(1-3)$g(b)Gal(1-4)$g(b)GlcNAc-R compound. In this step, monofucosylation is achieved by use of the $g(a)(1-3)fucosyltransferase.
专利号:US-9303051-B2 优先权日:2010-08-31 标 题 :Phosphonate ester derivatives and methods of synthesis thereof 发明人:WARE ROY W; ALMOND MERRICK R; LAMPERT BERNHARD M 权利人:CHIMERIX INC; CHIMERIX INC 摘要:The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.
专利号:US-5770407-A 优先权日:1996-12-10 标题:Process for preparing nucleotide inhibitors of glycosyltransferases 发明人:WONG CHI-HUEY; HAYASHI TAKASHI 权利人:SCRIPPS RESEARCH INST 摘要:Nucleotide linked 2-deoxy-2-fluoroglycosides are employed as potent competitive inhibitors of glycosyltransferases. More particularly, uridine-5'-diphospho-2-deoxy-2-fluoro-galactose (UDP-2F-Gal), guanidine-5'-diphospho-2-deoxy-2-fluoro-L-fucose (GDP-2F-Fuc), uridine-51-diphospho-2-deoxy-2-fluoro-D-glucose (UDP-2F-Glu), guanosine-5'-diphospho-2-deoxy-2-fluoro-D-mannose (GDP-2F-Man), cytosine-5'-monophospho-2-deoxy-2-fluoro-D-sialic acid, and cytosine-5'-monophospho-2-deoxy-2-KDO may be employed as inhibitors of β-1,4-galactosyltransferase, α-1,3-fucosyltransferase, glucosyltransferases, N-acetylglucosaminyltransferases, (α-mannosyltransferases, α-sialyltransferases, and KDO-transferases, respectively. Synthesis of nucleotide-linked-2-deoxy-2-fluoroglycosides is achieved using either chemoenzymatic or chemical methodologies.
专利号:US-5550155-A 优先权日:1991-06-10 标 题:Methods for the synthesis of monofucosylated oligosaccharides terminating in di-N-acetyllactosaminyl structures 发明人:KASHEM MOHAMMED A; VENOT ANDRE P; SMITH RICHARD 权利人:ALBERTA RES COUNCIL 摘要:Monofucosylated and monosialyated derivatives of the compound βGal(1-4)βGlcNAc(1-3)βGal(1-4)βGlcNAc-OR, where R is hydrogen, a saccharide, an oligosaccharide or an aglycon moiety have been found to be useful in modulating a cell-mediated immune inflammatory response in mammals.
专利号:US-5882901-A 优先权日:1991-06-10 标 题:Modified sialyl Lewisa compounds 发明人:VENOT ANDRE P; NIKRAD PANDURANG V; KASHEM MOHAMMED A 权利人:ALBERTA RES COUNCIL 摘要:The present invention is drawn to methods for the synthesis of Lewis a derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemo-enzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.
专利号:US-5939290-A 优先权日:1991-06-10 标题 :Modified sialyl Lewisx compounds 发明人:VENOT ANDRE P; NIKRAD PANDURANG V; KASHEM MOHAMMED A 权利人:ALBERTA RES COUNCIL 摘要:The present invention is drawn to methods for the synthesis of sialyl Lewis x derivatives modified at the C-2 and/or C-6 position of GlcNAc employing chemoenzymatic synthesis. The derivatives find use in the treatment and prevention of diseases.
[参考文献]: Earl R Kern, Et Al. Enhanced Inhibition Of Orthopoxvirus Replication In Vitro By Alkoxyalkyl Esters Of Cidofovir And Cyclic Cidofovir. Antimicrob Agents Chemother. 2002 Apr;46(4):991-5. [参考文献]: S C Perricone, Et Al. Synthesis And Diuretic Activity Of Alkyl- And Arylguanidine Analogs Of N,N'-Dicyclohexyl-4-Morpholinecarboxamidine In Rats And Dogs. J Med Chem. 1994 Oct 28;37(22):3693-700.
合成参考文献
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#07096