Abstract: A novel compound, 2?/3?-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2? and 3? regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2?-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2?/3?-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2?/3?-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2?/3?-O-acetyl-ADP-ribose are also provided.

Abstract: Provided are a method of producing a porous chitosan scaffold, the method including: providing an aqueous acidic solution having chitosan and a solvent which does not dissolve the chitosan; and freeze-drying the aqueous acidic solution, wherein the solvent is selected from the group consisting of a C3-C8 aliphatic alcohol having one hydroxy group, ethylene glycol monoethylether, ethylene glycol monobutylether, dioxane, tetrahydrofuran, dimethylcarbonate, acetone and acetonitrile, and a chitosan scaffold produced using the method.

Abstract: The present invention provides a method for preparing a hybrid gene. The method includes a step of amplifying a P450 gene fragment contained in a sample using primers designed on the basis of regions of a plurality of P450 in which amino acid sequences are highly conserved and a step of preparing the hybrid gene using the amplified fragments and a known P450 gene. The method includes no culturing step or a step of normalizing extracted DNAs and is useful in isolating a P450 gene from various microbial resources. The present invention further provides a fused cytochrome P450 monooxygenase containing a peptide which is linked to the C-terminus of a P450 protein with a linker portion disposed therebetween and which has the same function as that of a reductase domain contained in a cytochrome P450 monooxygenase originating from Rhodococcus sp. strain NCIMB 9784.

Abstract: A nucleic acid amplification method, includes: performing nucleic acid amplification using a microchip that comprises: a specimen introduction section; a reaction section; and a channel that connects the reaction section and the specimen introduction section, wherein the method further comprises preventing a reaction solution from evaporating during the amplification reaction, and a microchip, includes: a specimen introduction section; a reaction section; and a channel that connects the reaction section and the specimen introduction section, wherein the microchip executes a method for preventing a specimen containing a nucleic acid from evaporating.

Abstract: The present invention concerns an improved method for the isolation of nucleic acids such as DNA and RNA from bacterial, plant, animal or human cells as well as from cell cultures and virus cultures.

Abstract: The present invention relates to a method of producing methyl esters of a hyaluronic acid, said method comprising the steps of: (a) providing a suspension comprising the acid form of the hyaluronic acid in methanol; (b) adding an organic solution of trimethylsilyldiazomethane to the suspension and mixing, whereby methyl esters of hyaluronic acid are produced; and (c) recovering the hyaluronic acid methyl esters.

Abstract: A method for sulfonating compounds having one or more free hydroxyl functional groups and/or one or more optionally substituted primary or secondary functional groups, including treating the compounds with a complex of SO3-DMF in the presence of an acid capture agent.

Abstract: The present invention provides novel methods and reagents for detecting the binding of protein targets to nucleic acid ligands. Using Universal Protein Stains (UPS), proteins bound by nucleic acid ligands may be labeled with a detectable moiety. The methods and reagents are particularly useful for the detection of protein targets bound to multiplexed arrays of nucleic acid ligands. The present invention also provides novel methods for the multiplexed evaluation of photocrosslinking nucleic acid ligands. The methods allow one simultaneously to: (1) evaluate the performance (dynamic range) of a plurality of photocrosslinking nucleic acid ligands; and (2) assess the specificity of each photocrosslinking nucleic acid ligand for its cognate target protein. Photocrosslinking nucleic acid ligands with the most desirable properties can then be selected for use in diagnostic and prognostic medical assays.

Abstract: Novel calcium-independent phospholipases A2; genes encoding the same; an antibody against them; an inherent promoter or a regulator gene which comprises a base sequence occurring in intron and inducing site-specific expression in response to an external stimulus; a method of expressing a target protein in response to an external stimulus; and an organism having this gene transferred thereinto. Novel calcium-independent phospholipases A2 having an amino acid sequence represented by SEQ ID NO: 1, 3 or 5 or an amino acid sequence derived from such an amino acid sequence by the substitution, deletion or addition of one or more amino acids; a gene having a base sequence occurring in an intron and being capable of initiating RNA transcription due to an external stimulus such as a stimulus with kainic acid or an electrical stimulus; a method of regulating expression by using the gene; and an organism having the gene transferred thereinto.

Abstract: A microplate having a substrate with a hydrophobic surface and a plurality of hydrophilic reaction spots on the hydrophobic surface. Each of the plurality of reaction spots having an amphiphilic polymer and a polynucleotide conjugated to the amphiphilic polymer.

Abstract: Glucosamine phosphate having a purity of at least about 99 wt. %, and a maximum halide content of about 0.01 wt. %. Preferably, the glucosamine phosphate is stabilized by coating it with at least one pharmaceutically acceptable polymer comprising a water-soluble, water-immiscible and/or water-swellable homopolymer and/or copolymer. Suitable polymers include carboxypolymethylene hompolymers and copolymers; polyethylene glycol homopolymers and copolymers; polypropylene glycol homopolymers and copolymers; ethylcellulose; povidone homopolymers and copolymers; polyacrylic acid homopolymers and copolymers; polyacrylamide homopolymers and copolymers; polysaccharides; and mixtures of two or more of the foregoing polymers. The resultant coated glucosamine phosphate composition will be stable at ambient temperatures and upon exposure to the atmosphere.

Abstract: Glucosamine sulfate having a purity of at least about 99 wt. %, and a maximum halide content of about 0.01 wt. %. Preferably, the glucosamine sulfate is stabilized by coating it with at least one pharmaceutically acceptable polymer comprising a water-soluble, water-immiscible and/or water-swellable homopolymer and/or copolymer. Suitable polymers include carboxypolymethylene homopolymers and copolymers; polyethylene glycol homopolymers and copolymers; polypropylene glycol homopolymers and copolymers; ethylcellulose; povidone homopolymers and copolymers; polyacrylic acid homopolymers and copolymers; polyacrylamide homopolymers and copolymers; polysaccharides; and mixtures of two or more of the foregoing polymers. The resultant coated glucosamine sulfate composition will be stable at ambient temperatures and upon exposure to the atmosphere.

Abstract: The present invention relates to a process for the production of cross-linked hyaluronic acid (HA) derivatives, in particular multiple, e.g. double cross-linked hyaluronic acid derivatives. The invention also provides novel cross-linked HA derivatives, products containing them and their uses in medical and pharmaceutical and cosmetic applications.

Abstract: The present invention provides a process for producing a N4-acyl-5?-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.

Abstract: The present invention is a method for manufacturing a phosphorylcholine group-containing polysaccharide wherein the aldehyde derivative-containing compound obtained by the oxidative ring-opening reaction of glycerophosphorylcholine is added to a polysaccharide containing amino groups as well as a new polysaccharide having phosphorylcholine groups obtained from this manufacturing method. The object of the present invention is to provide a phosphorylcholine group-containing polysaccharide that is superior in biocompatibility and moisture retention, and is useful as a polymer material for medical use, as well as a simple method of manufacturing it. The polysaccharide of the present invention is utilized, for example, in artificial organs, biomembranes, coating agents for medical tools, drug delivery, and in cosmetics.

Abstract: A method for the preparation of water-soluble chitosan with high purity and biological activity includes steps of: reacting chitosan oligo sugar acid salt, covalently bonded to an organic or inorganic acid, with trialkylamine in phosphate buffered saline followed by addition of an organic solvent to remove acid salt at C-2 position; adding the thus obtained reaction mixture to an inorganic acid to remove trialkylamine salt at C-6 position; and passing the thus obtained free amine chitosan through an activated carbon/ion exchange resin. The free amine chitosan is water-soluble and has a high bioavailability for application to the medicine and food industries.

Abstract: The invention relates to a method which is used to efficiently mark proteins with the help of a micromixer, in addition to a device which enables said inventive method to be carried out in an economical manner and with additional auxiliary agents.

Abstract: The present invention relates to a method for producing a chitosancontaining salt having the function of lowering blood pressure. The method comprises the steps of: (a) dissolving an acid-soluble chitosan in organic acid, or dissolving a water-soluble chitosan derivative in water, to prepare a chitosan solution; (b) spraying the chitosan solution on salt particles to bind the chitosan to the salt particles; and (c) drying the chitosan-bound salt particles. According to the present invention, the chitosan or its derivative is bound to the salt particles by spraying or mixing such that the chitosan-containing salt can be produced without performing a recrystallizing step. Thus, the production cost of the chitosan-containing salt can be significantly decreased.

Abstract: The present invention is directed to a nucleic acid comprising a sequence encoding a modified glutenin polypeptide, wherein the sequences encoding one or more cysteine residues responsible for intermolecular crosslinking via disulfide bridges were deleted or substituted by sequences encoding other amino acids without amending the reading frame of the coding sequence.

Abstract: An asparagine-linked ?2,3-oligosaccharide having undeca- to hepta-saccharides, an asparagine-linked ?2,6-oligosaccharide having undeca- to hepta-saccharides and containing fluorine and an asparagine-linked oligosaccharide derivative containing at least one fucose in N-acetylglucosamine on the nonreducing terminal side of an asparagine-linked oligosaccharide wherein the asparagine has amino group protected with a lipophilic protective group, and a process for producing these compounds.

Abstract: The present invention is directed to homogeneous phase enzyme-catalyzed processes for producing modified chitosan polymers or oligomers. An enzyme is reacted with a phenolic substrate in the presence of a chitosan polymer or oligomer to produce a modified chitosan polymer or oligomer. The invention also includes modified chitosan polymers or oligomers produced by the novel processes, in particular modified chitosan polymers or oligomers having useful functional properties, such as base solubility and/or high viscosity.

Abstract: This invention relates to processes for production of alkylamino glucosaminide phosphate compounds, and of disaccharide compounds, including various novel intermediates and intermediate processes. In one aspect, glycosyl halides are produced by reaction of an O-silyl glycoside with a dihalomethyl alkyl ether.

Abstract: The present invention provides novel intermediates, which preferably include 3-substituted, alkyl 2,2-difluoro-3-hydroxy-3-(2,2-dialkyldioxolan-4-yl)-propionate derivatives, and 3,5-disubstituted-2-deoxy-2,2-difluoro-1-oxo-D-ribose derivatives. The present invention also provides processes for producing such intermediates and processes for producing gemcitabine therewith.

Abstract: A process for the preparation of ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid. Said process comprises: a) the reaction of a triazole of the formula ?with a protected ribofuranose of the formula b) the removal of the Pg groups and, optionally, the conversion into a carboxyamide group of the R2 group of the compound obtained of the formula ?DD/mac—01.07.02.

Abstract: A process for the preparation of L-ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid.

Abstract: The invention relates to starch derivatives of formula (I), in which: X represents a bromine or iodine atom; R? represents a straight-chain or branched alkyl group, aryl group or aralkyl group, and; R—CO— represents an oxidized substituted or unsubstituted starch radical that is oxidized on the reducing terminal group to form a carboxylic acid. Starch derivatives of formula (I) can selectively couple to active substances containing SH groups and have a prolonged half-life period in the human body.

Abstract: A 3-branched asparagine-linked oligosaccharide derivative of the formula (1) wherein the nitrogen of amino group of asparagine is modified with a lipophilic protective group, biotin group or FITC group; a 3-branched asparagine-linked oligosaccharide derivative which contains at least one fucose in N-acetylglucosamine on the nonreducing terminal side of the asparagine-linked oligosaccharide of the derivative; asparagine-linked oligosaccharides and oligosaccharides thereof wherein Q is a lipophilic protective group, biotin group or FITC group.

Abstract: A process for purifying and preparing highly pure acarbose from acarbose-containing fermentation broth. The acarbose is purified through steps of alcohol precipitation, a strongly acidic cation exchanger chromatography and an immobolized enzyme affinity chromatography. Acarbose is generally applied in treating diabetes.

Abstract: The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of ?-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the ?-enriched anomer of gemcitabine hydrochloride of formula (IIb) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).

Abstract: The present invention provides a method for preparation of 2?-deoxy-2?,2?-difluoro-?-cytidine or pharmaceutically acceptable salt thereof, comprising starting from 1,6-anhydro-?-D-glucose as raw material, oxidizing, and fluorinating to obtain 2-deoxy-2,2-difluoro-D-ribofuranose as intermediate. The 2?-deoxy-2?,2?-difluoro-?-cytidine was finally prepared from the intermediate of 2-deoxy-2,2-difluoro-D-ribofuranose. The method is simple in operation and has a high yield. The method can effectively be used in large-scale production.

Abstract: A gelatinizer having gel-forming capability in both organic solvents and water, is provided. The hydrogelatinizer is represented by: (where, A is a sugar residue, and R is an alkyl group).

Abstract: The present invention herein provides a chitosan-containing polysaccharide and a method for the preparation thereof as well as a medicine and a food containing the polysaccharide. The chitosan-containing polysaccharide is prepared by a method comprising the steps of heat-treating a fungus in a concentrated aqueous caustic alkali solution; subjecting the resulting solution to a solid-liquid separation treatment; dissolving the resulting solid contents in an aqueous organic acid solution; adding, to the resulting solution, an alcohol or a caustic alkali to thus form precipitates; washing the resulting precipitates; and then drying them. This chitosan-containing polysaccharide is a compound in which homopolymers of glucosamine are linked with glucan through covalent bonds; it has a molar ratio of glucosamine and glucose constituting the polysaccharide ranging from 1:5 to 5:1; it has a molecular weight of about 150,000; and it does not contain any ?(1?3) bonds, but comprises ?(1?4) bonds and ?(1?6) bonds.

Abstract: A process is described for preparing a substrate for the transglycosylase enzymes of bacterial cell wall biosynthesis. The chemical synthesis makes available a sustainable and substantially pure source of supply of lipid II, including analogs thereof, that may be used in the identification of new therapeutic agents capable of disrupting steps in bacterial cell wall biosynthesis.

Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (?)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.

Abstract: Therapeutic 5-aminosalicylic acid derivative compositions having general formula (I), wherein R is a 1-deoxy sugar residue or a poly(ethylene glycol) chain-containing residue, are provided. The compositions enable topical delivery of 5-aminosalicylic acid to the gastrointestinal tract following oral administration in pharmaceutical preparations.

Abstract: A high molecular weight polysaccharide intracellular adhesin (SAE) antigen having the general structure of poly-1,6,?-2-amidoglucopyranoside, which is variable substituted with N-acetyl and O-succinyl substituents is described. Also, a method is given for isolating this antigen from Staphylococcus aureus. The SAE can be used in a vaccine, either alone, conjugated to an immunogenic protein, and/or with an immunogenic adjuvant.

Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.

Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.

Abstract: The present invention describes a new class of cross-linked derivatives of partially N-deacetylated hyaluronic acid or derivatives thereof, comprising at least one repeating unit of formula (I) hereinafter depicted and a process for the preparation of said cross-linked derivatives, comprising a multicomponent condensation reaction involving the carboxy groups and the amino groups originating from a partial N-deacetylation of hyaluronic acid or derivatives, together with an aldeyde and an isocyanide. The derivatives thus obtained can be used, alone or in association with biologically and/or pharmacologically active substances, for the preparation of pharmaceutical compositions, biomaterials, surgical and healthcare articles, slow release systems and for the coating of biomedical objects.

Abstract: Water-soluble chitosan having a low concentration of endotoxin is disclosed. Products containing the water-soluble chitosan are also disclosed. Methods of making and using water-soluble chitosan having a low concentration of endotoxin are further disclosed.

Abstract: The invention relates to the use of morpholino-nucleosides of formula: in which R1 represents a nucleic base and R2 represents a group corresponding to one of the following formulae: —(CH2)n—NH2 —(CH2)n—SH —(CH2)n—COOH —(CH2)n—OH —(CH2)n—NH—R3 —(CH2)n—SR3 —(CH2)n—CO—R3 —(CH2)n—OR3 in which n is an interger ranging from 1 to 12 and R3 is a group derived from a label, from a protein, from an enzyme, from a fatty acid or from a peptide, as chain terminators in a process of DNA or RNA sequencing by the Sanger method, or for the labelling of DNA or RNA fragments.

Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.

Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5?)-tetraphosphate, and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5?)-tetraphosphate (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. wherein: X is Na, NH4 or H, provided that all X groups are not H.

Abstract: By the reaction of chitosan with iminothiolactones such as 2-iminothiolane, thiol groups can be covalently immobilized on the polymer. The resulting chitosan derivatives exhibit thiol groups which are capable of forming inter- and intramolecular disulfide bonds. Because of this crosslinking process the viscosity of polymer solutions is strongly improved. Moreover, the cationic character of the polymer is strongly improved.

Abstract: The invention describes new hyaluronan derivatives where the hydroxyl groups are esterified or carbamoylated in amounts ranging from 0.01% to 100% and the carboxyl groups are either totally or partially esterified with alcohols or are in the form of salt.

Abstract: Glucosamine suitable for human or animal consumption is disclosed. The glucosamine is derived from microbial biomass containing chitin. Suitable starting materials include substantially uniform microbial fungal sources, such as fungal sources derived from Aspergillus sp., Penicillium sp., Mucor sp. and combinations thereof. Methods of producing glucosamine by acid hydrolysis of fermented fungal biomass are also disclosed.

Abstract: A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase, a nucleoside is prepared from the 1-phosphorylated saccharide derivative obtained and a base with improved stereoselectivity and a higher yield. This process is an anomer-selective process for preparing a 1-phosphorylated saccharide derivative and a nucleoside.

Abstract: The present invention relates to a purification method of hydroxypropylmethyl cellulose phthalate, more particularly to a method of preparing high-purity hydroxypropylmethyl cellulose phthalate through a simple crushing process which comprises: increasing fluidity of reaction product mixture by adding fluidization solvent as a post-treatment process; and spraying it into water through a spray nozzle. As a result, formation of fine granular hydroxypropylmethyl cellulose phthalate particles prevents inter-particle coagulation during the a post-treatment process, and phthalic anhydride reactant, free phthalic acid and remaining acetic acid solvent can be removed effectively.

Abstract: An orally administered soft gelatin formulation preparation of low molecular weight Hyaluronic Acid (HA) for use as a nutritional supplement to provide the primary benefit of internally causing the softening of the human skin.

Abstract: The present invention provides a new class of compounds presenting a high compatibility with tissues and organic fluids. Such new compounds are polysaccharides essentially formed of units of uronic acid and/or hexosamine, containing nitro groups —ONO2 covalently bonded to the saccharide structure. Preferably, the polysaccharides according to the invention are prevalently formed of disaccharide repeating units formed of uronic acid and hexosamine. These compounds, in psychological conditions, selectively release NO, allowing a reduction in the amount of NO needed to achieve a determined therapeutical effect. This result has been achieved by functionalizing polysaccharides essentially formed of units of uronic acid and/or hexosamine, with subsituents containing a ONO2 ? group.