Abstract: The present invention provides: a polysaccharide derivative containing a structure wherein hydrogen atoms in a hydroxyl group at the 2-position and the 3-position of a structure unit of polysaccharide are substituted with different substituents respectively represented by a specific general formula and a separating agent for optical isomers which contains such a polysaccharide derivative. The present invention can provide a novel polysaccharide derivative which has excellent optical isomer separating ability, making it suitable as a separating agent for optical isomers, and can provide a separating agent for optical isomers which contains the polysaccharide derivative.

Abstract: Crystalline solid forms of the anti-HCV compound (S)-isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphorylamino)propanoate (Compound I) are described Also provided are processes of making and methods of using the crystalline forms.

Abstract: A composition composed of an adhesive copolymer may be a reaction product of a first mixture and a monosaccharide monomer, in which the first mixture may be a reaction product of a diol monomer and a dicarboxylic monomer.

Abstract: The present invention discloses a matrix comprising a modified primary hydroxyl groups containing polysaccharide comprising repeating disaccharide units wherein in at least part of the disaccharide units the primary hydroxyl group is replaced by functional groups selected from halide groups or groups comprising sulfur or phosphorus atoms, like e.g. sulfate groups, sulfonate groups, phosphonate groups and phosphate groups.

Abstract: The present invention provides, among other things, phosphorylated and pyrophosphate derivatives of mono-, di- and oligosaccharides, as well as structural derivatives of these compounds. These compounds have a variety of uses including for pharmaceutical applications. Also provided are methods of use in the treatment of disease, including diseases related to oxygen delivery.

Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

Abstract: Methods to introduce highly phosphorylated mannopyranosyl oligosaccharide derivatives containing mannose-6-phosphate (M6P), or other oligosaccharides bearing other terminal hexoses, to carbonyl groups on oxidized glycans of glycoproteins while retaining their biological activity are described. The methods are useful for modifying glycoproteins, including those produced by recombinant protein expression systems, to increase uptake by cell surface receptor-mediated mechanisms, thus improving their therapeutic efficacy in a variety of applications.

Abstract: The present invention relates to the use of a specific family of glycerolipid compounds of formula (I) described in the detailed description or the manufacture of a medicament for the prevention or for the treatment of cancer metastasis.

Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: Film forming dental compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and a binder. The film forming dental compositions can include an amino sugar, a derivative of an amino sugar, or a pharmaceutically acceptable salt thereof, and can be useful in inhibiting biofilm formation in an oral cavity.

Abstract: There is provided the use of mannose-6-phosphate, or a salt, precursor or analogue thereof, for providing and/or maintaining a consistent skin colour, particularly to reducing redness of skin. There is also provided the use of mannose-6-phosphate, or a salt, precursor or analogue thereof, as a skin improvement agent for providing a cosmetic effect and mannose-6-phosphate, or a salt, precursor or analogue thereof, for use in treating normal or damaged skin, wherein damaged skin is skin that has been subject to epidermal and/or dermal damage.

Abstract: The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

Abstract: Hypersulfated disaccharides, preferably octasulfated sucrose, with utility in asthma or asthma related disorders are disclosed. The compounds may optionally be formulated with pharmaceutically acceptable excipients or delivery agents. The delivery agents are selected from the group consisting of natural or synthetic polymers, aerosols or other vehicles that facilitate the delivery or administration of the drug. The hypersulfated disaccharides are made from carbohydrate starting materials. Ion exchange or other suitable synthetic processes may be utilized to prepare the pharmaceuticals. The hypersulfated disaccharides are useful as anti-inflammatory agents.

Abstract: A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large- scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent; and removing the protection group. The coupling may include reacting a 3?-protected compound of formula: with a nucleotide derivative having a 5?-protection group, or reacting a 5?-protected compound of formula with a nucleotide derivative having a 3?-protection group.

Abstract: The present invention provides protonated compounds having antiviral and antimicrobial activity. The invention also provides antimicrobial compositions comprising protonated compounds of the invention. The protonated compounds of the invention provide efficacious antimicrobial activity against resistant strains of bacteria and opportunistic fungi. The invention also provides antiviral compositions comprising compounds of the invention. Viruses that may be treated by compositions of the invention include, but are not limited to, HIV, HSV, CMV, HBV, HCV and influenza virus.

Abstract: Microparticle compositions comprising metal ion-lipid complexes for drug delivery are described including methods of making the microparticle compositions and methods of treating certain conditions and disease states by administering the microparticle compositions. The metal ion-lipid complexes can be combined with various drugs or active agents for therapeutic administration. The microparticle compositions of the present invention have superior stability to other microparticle compositions resulting in a microparticle composition with longer shelf life and improved dispersability. The microparticle compositions of the present invention have a transition temperature (Tg) of at least 20° C. above the recommended storage temperature (Tst) for drug delivery.

Abstract: Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): —OX—Y (Ia) or —O—R1 (Ib) wherein X is C(O), S(O) or SO2; Y is NR1R2 or R3; R1 is C1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R2 is H or C1-6 alkyl; and R3 is C1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.

Abstract: The present invention provides improved methods for producing a solution containing high molecular weight isolated Streptococcus pneumoniae capsular polysaccharides having phosphodiester linkages between saccharide repeat units. In certain methods, CO2 is supplied to a fermentation culture of Streptococcus pneumoniae bacterial cells that produce capsular polysaccharide serotypes containing phosphodiester linkages between saccharide repeat units. Exemplary Streptococcus pneumoniae serotypes containing a phosphodiester linkage between saccharide repeat units include serotypes 6A, 6B, 19A, and 19F. Supplying CO2 to the fermentation culture includes adding bicarbonate ions to the fermentation culture, adding carbonate ions to the fermentation culture, adding mixtures of bicarbonate and carbonate ions to the fermentation culture, and overlaying the fermentation culture with CO2.

Abstract: Compounds of the formula: and compositions containing one or more such compounds, the compositions preferably being suitable for topical application to the skin.

Abstract: The present invention relates to percarboxylated polysaccharide selected from the group consisting of gellan, carboxymethylcellulose, pectic acid, pectin and hyaluronic acid derivatives; the process for their preparation and their use in the pharmaceutical, biomedical, surgical and healthcare fields.

Abstract: Provided are methods of designing a putative inhibitor of a human 5?-methylthioadenosine phosphorylase (MTAP). Also provided are methods of inhibiting a human MTAP.

Abstract: The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

Abstract: Phosphorylated protein (i.e., phosphoprotein) affinity resins and methods for making and using the same are provided. The subject resins include a substrate bonded to aspartate-based tetradentate ligand/metal ion complexes, where the tetradentate ligand/metal ion complexes have high specificity for phosphorylated amino acids. The subject resins find use in a variety of different applications, including phosphoprotein enrichment applications. Also provided are kits and systems that include the subject resins.

Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.

Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use.

Abstract: The invention concerns the use, in a composition for treating textile fiber articles in aqueous or moist medium, of an amphoteric polysaccharide, whereof the native skeleton is a polysaccharide consisting of a main chain comprising anhydrohexose units and branches comprising at least a neutral or anionic anhydropentose and/or anhydrohexose unit, the anhydrohexose and/or anhydropentose units being substituted of modified by groups bearing at least a (potentially) anionic load and/or at least a (potentially) cationic load, the degree of substitution or modification by the set of said groups bearing (potentially) anionic loads ranging between 0.01 and less than 3, with a ratio of the number of (potentially) anionic charges over the number of (potentially) cationic loads ranging between 99.5/0.

Abstract: Aminoalkyl glucosaminide phosphate (AGP) compounds that are adjuvants and immunoeffectors are described and claimed. The compounds have a 2-deoxy-2-amino glucose in glycosidic linkage with an aminoalkyl (aglycon) group. Compounds are phosphorylated at the 4 or 6 carbon on the glucosaminide ring and comprise three 3-alkanoyloxyalkanoyl residues. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

Abstract: Provided are compounds and compositions thereof that are useful for treating inflammation, particularly pulmonary inflammations including asthma and asthma-related pathologies such as allergy. Also provided are methods for using such compounds and compositions of the invention to treat patients suffering from, or predisposed to develop inflammation.

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 process for the isolation of a glycolipid enriched fraction from rice bran oil by subjecting crude rice bran oil to at least two steps of dewaxing/degumming, treating sludge obtained as a byproduct of the second said dewaxing/degumming to hexane extraction, and separating the glycolipid fraction. The glyolipid fraction so obtained can be further purified.

Abstract: Lipopolysaccharides and processes for producting the lipopolysaccharides are provided. The lipopolysaccharide has a lipid A portion, a core oligosaccharide portion, and an O-specific chain having a single repeating unit 06. A lipopolysaccharide may be produced by washing and drying and E. coli bacterial mass, subjecting the washed and dried bacterial mass to a phenol/water extraction, and treating the extract with RNases, DNases, and proteinase K.

Abstract: Phosphonites I of the formula 1 or 2 1

Abstract: The present invention discloses novel phosphoramidite reagents for use in oligonucleotide synthesis. The present invention further discloses novel methods for the conversion of terminal hydroxyl groups of oligonucleotides into phosphate monoesters. By employing novel reagents, as also disclosed herein, the methods are fully compatible with standard procedures for solid phase oligonucleotide synthesis and do not require additional processing steps. The inventive reagents to phosphorylate terminal hydroxyl groups of oligonucleotides are superior to the prior art in that they for the first time combine the desired attributes of being a solid compound for facile handling, comprising two &bgr;-eliminating protective groups removable as fast or faster than the standard cyanoethyl group, providing a DMT-group for easy monitoring of the coupling efficiency, and enabling a fast final deprotection of the phosphorylated oligonucleotide without any extra manipulation steps.

Abstract: Probes comprising an immobilised Phosphatidic Acid attached onto a solid support are described, for example, as shown in formula I and V: (a) the linker consists of aryl, heteroaryl, alkyl with possible heteroatoms and/or unsaturations, preferably chains of (CH2)n, with n=8-20, most preferably n=11; (b) the heteroatom X maybe O, S, or most preferably NH; (c) the functional group (FG) is a carbonyl from a carboxylate (thiolo)ester, or, most preferably an amide; (d) the R-substituent carries an aryl, alkyl group, or a combination, preferably R=CmH2m+1, m=8-20, m=16 optimal; (e) the ion M represents any cation, preferably Na+, NH4+; (f) unsaturations are allowed, such as in an arachidonyl side chain and (g) =solid support with attachment to functional group, where: R=aryl, alkyl group, or a combination, preferably R=CmH2m+1, m=8-20, m=16 is optimal.

Abstract: Novel lipid compounds and compositions comprising carbohydrate backbones are used to make supramolecular structures such as vesicles, liposomes (single lamellar, multilamellar, and giant), micelles, hexagonal phases, microemulsions and others. The novel compositions and supramolecular structures may be combined with active agents such as contrast agents and bioactive agents (e.g., therapeutic and diagnostic agents) in delivery methods.

Abstract: A nutritional composition which contains slightly negatively charged non-digestible polysaccharides having a molecular weight of 8 kD to 40,000 kD, characterized in that the rise in the viscosity of the composition caused by the polysaccharides is less than 20 mpa·s. This nutritional composition is used to reduce the uptake of high molecular weight substances, allergens and microorganisms through the intestinal wall, more particularly to reduce transport of high molecular weight substances, allergens and microorganisms through the intestinal wall, ore particularly to reduce transport of high molecular weight substances, allergens and microorganisms through the tight junctions in the intestines.

Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.

Abstract: Provided are methods of producing phosphitylated compounds, including 3′-O-phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of: (1) acid-base complexes derived from an amine base of Formula I 1

Abstract: The present invention provides an industrially excellent and novel process for producing methylcobalamin useful as medicines. Namely, it provides a process for producing methylcobalamin, which comprises the step of methylating cyanocobalamin or hydroxocobalamin in the presence of a reducing agent and a water-soluble methylating agent.

Abstract: The present invention discloses novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth. The invention further discloses pharmaceutical compositions comprising said molecules and their uses.

Abstract: A compound having the formula: 1

Abstract: Methods and Intermediates for the Preparation of Oligomers Containing Diastereomerically Enriched Phosphorothioate Linkages are Disclosed.

Abstract: Provided are compounds and compositions thereof that are useful for treating information, particularly pulmonary inflammations including asthma and asthma-related pathologies such as allergy. Also provided are methods for using such compounds and compositions of the invention to treat patients suffering from, or predisposed to develop inflammation.

Abstract: The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.

Abstract: A compound of formula (I) below, which exhibits excellent macrophage activity inhibitory action, is useful for the treatment or prophylaxis of inflammatory disorders, autoimmune diseases or septicemia. In a preferred embodiment, R1 and R3 each represents a C1-C20 alkanoyl group which may optionally be substituted with one or more substituent groups selected from substituent group A, R2 and R4 each represents a C1-C20 alkyl group which may optionally be substituted with one or more substituent groups selected from substituent group A, R5 is a hydrogen atom, a halogen atom, a hydroxy group, or a C1-C6 alkoxy group, and substituent group A is a halogen atom, a hydroxy group, an oxo group, a C1-C20 alkoxy group, or a C1-C20 alkanoyloxy group.

Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.

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 progress for the isolation of a glycolipid enriched fraction from rice bran oil by subjecting crude rice bran oil to at least two steps of dewaxing/degumming treating sludge obtained as a byproduct of the second said dewaxing/degumming to hexane extraction, and separating the glycolipid fraction. The glyolipid fraction so obtained can be further purified.

Abstract: Libraries are synthesized with oligomeric carbopeptoids and carbonucleotoids. Carbopeptoids are oligosaccharides having carbohydrate subunits linked to one another by amide bonds. Carbonucleotoids are oligosaccharides having carbohydrate subunits linked to one another by phosphodiester bonds. Carbopeptoid libraries may be fabricated using automated polypeptide synthesizers. Carbonucleotoid libraries may be fabricated using automated polynucleotide synthesizers.

Abstract: The present invention provides novel compounds that function as immunological adjuvants when co-administered with antigens, including, antigens used as vaccines for any disease or condition amenable to vaccination. The invention also provides adjuvant formulations comprising the novel compounds of the invention and methods for immunizing humans and non-human animals.