专利号:US-5139940-A 优先权日:1989-10-26 标题 :Activation compounds and methods of synthesis of activation compounds 发明人:ISAACS STEPHEN T; CIMINO GEORGE D; METCHETTE KENNETH C; TESSMAN JOHN W 权利人:ISAACS STEPHEN T; CIMINO GOERGE D; METCHETTE KENNETH C; TESSMAN JOHN W 摘要:The invention is directed to isopsoralen compound compositions that contain a variety of substitutions which yet permit their binding to nucleic acid polymers. Reaction conditions that activate these bound isopsoralens results in covalent crosslinking to the nucleic acid polymers. The resultant complex is inhibited from being a template for the template-directed enzymatic synthesis of a complementary nucleic acid polymer. Beside the isopsoralens compositions, the invention includes their synthesis, the nucleic acid complex production and detection, and the above inhibitory method of use of the isopsoralens.
专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:US-10005807-B2 优先权日:2013-04-12 标题 :Synthesis of sialylated/fucosylated human milk oligosaccharides 发明人:CHASSAGNE PIERRE; KHANZHIN NIKOLAY; HEDEROS MARKUS JONDELIUS; CHAMPION ELISE; MATWIEJUK MARTIN; DEKANY GYULA 权利人:GLYCOM AS 摘要:An achemo-enzymatic synthesis of oligosaccharides of formula 1 is presented wherein R is selected from —OH, —N 3 and —OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, —(CH 2) n —NH 2 and —(CH 2) n —N 3 wherein integer n is to 10, preferably 2 or 3, R is selected from sialyl moiety, —SO 3 H and —CH(R)—COOH wherein R is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that at least one of R 3 and R 4 is H, and A is a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.
专利号:WO-2014167537-A1 优先权日:2013-04-12 标题:Synthesis of sialylated/fucosylated oligosaccharides 发明人:KHANZHIN NIKOLAY; CHASSAGNE PIERRE; HEDEROS MARKUS; CHAMPION ELISE; MATWIEJUK MARTIN; DEKANY GYULA 权利人:GLYCOM AS 摘要:This invention relates to a chemo-enzymatic synthesis of oligosaccharidesof formula 1 wherein R is selected from -OH, -N 3 and -OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, -(CH 2 ) n -NH 2 and -(CH 2 ) n -N 3 wherein integer n is to 10, preferably 2 or 3, R 1 is selected from sialyl moiety, -SO 3 H and -CH(R 5 )-COOH wherein R 5 is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that one but only one of R 3 and R 4 is H, and A is selected from a bond and a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.
专利号:US-6303764-B1 优先权日:1998-09-24 标题:Synthesis of 4,7-dialkyl chromogenic glycosides of N-acetylneuraminic acids 发明人:SRIVASTAVA OM; SRIVASTAVA GEETA; DU MINGHUI; HINDSGAUL OLE; BUNDLE DAVID R; LIAV AVRAHAM 权利人:ZYMETX INC; HALIFEX FUND L P 摘要:The present invention provides an improved method of preparing a 4,7-di-O-alkyl chromogenic ketoside of N-acetylneuraminic acid (Neu5Ac) for use in detecting influenza virus types A and B. The ketosides are substrates that are selectively cleaved by a neuraminidase on influenza virus, but not be neuraminidases found on other viruses or on bacteria. The synthesis is efficient and provides large quantities of the ketoside for commercial development. The synthesis includes a step of alkylating the 4- and 7-hydroxyl groups of a protected alkyl ester alkyl ketoside derivative of Neu5Ac by a process that comprises contacting the derivative with a composition comprising an alkyl halide to form a 4,7-di-O-alkyl protected alkyl ester alkyl ketoside derivative of Neu5Ac. The synthesis alternatively includes protecting the 8- and 9-hydroxyl groups of an alkyl ester alkyl ketoside derivative of Neu5Ac by forming an 8,9-epoxide protected alkyl ester alkyl ketoside derivative of Neu5Ac.
专利号:US-2019078126-A1 优先权日:2017-09-08 标 题 :Polymerase-mediated, template-independent polynucleotide synthesis 发明人:BAIGA THOMAS; BURLEY MICHAEL ANDERSON; SMITH ALEXANDER 权利人:SIGMA ALDRICH CO LLC; MERCK PATENT GMBH 摘要:Methods for de novo synthesis of polynucleotides in which 3′-O-reversibly blocked nucleotides are attached to a solid support in the presence of an X family DNA polymerase and in the absence of a nucleic acid template.