Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is an alkyl, alkeny or alkynyl group mono- or poly-substituted with —OH, —COOH or a combination of —OH and —COOH, and R9 contains an alkyl, alkeny or alkynyl group substituted with a heterocyclic ring, amino or sulfonyl. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.

Abstract: The present invention relates to biomaterials modified with non-proteinaceous catalysts for the dismutation of superoxide, and processes for making such materials. This modification may be by covalent conjugation, copolymerization, or admixture of the non-proteinaceous catalysts with the biomaterial. The resulting modified biomaterials exhibit a marked decrease in inflammatory response and subsequent degradation when placed in contact with vertebrate biological systems.

Abstract: Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein.

Abstract: The present invention relates to a process for the preparation of topiramate, intermediates in this process and a process for the preparation of these intermediates.

Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.

Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

Abstract: The present invention relates to the development of a hyaluronic acid and hyaluronic acid hybrid nanoparticle systems for the administration of active molecules, peptides, DNA and/or other hydrophilic or hydrophobic molecules, the composition of hyaluronic acid and hyaluronic acid hybrid nanoparticle systems, and the procedure for their development and use. These nanoparticles are made up of hyaluronic acid in salt form, preferentially the sodium salt of the polymers or hybridized with magnetic Fe particles. The nanoparticles are basically from natural polymers, biocompatibles and biodegradables. The nanoparticles allow the controlled release of the active molecules they transport and their orientation towards the target tissues. The present invention teaches a procedure to elaborate particles of hyaluronic acid with a diameter less than 180 nm., that incorporate an active ingredient, independent of its hydrophilic or hydrophobic nature. Procedures to produce the particles are described.

Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a particular glycomimetic linked to a particular BASA (Benzyl Amino Sulfonic Acid).

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: The invention provides methods and kits to detect liver cirrhosis in mammals. The diagnostic test is based on the profiling and identification of diagnostic carbohydrates present in a body fluid such as blood serum.

Abstract: A process for the oxidation of carbohydrate with UV light. The process comprises the steps of providing a carbohydrate, combining the carbohydrate with an oxidant and exposing the combined carbohydrate and oxidant to ultraviolet light. The process occurs at alkaline conditions.

Abstract: The invention relates to a process for the depolymerization of glycosaminoglycanes characterized by the use of electron beam radiation, optionally in the presence of an organic compound selected from the group consisting of ethers, alcohols, aldehydes, amides and formic acid. The invention also relates to the intermediate depolymerized heparin obtained by the process. The intermediate depolymerized heparin can be dissolved in a buffer solution and fractionated by gel permeation for obtaining the desired molecular weight.

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 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 human-derived novel chondroitin synthase, which is an enzyme for synthesizing a fundamental backbone of chondroitin and has both glucuronic acid transferase activity and N-acetylgalactosamine transferase activity.

Abstract: Provided herein are a coating or a device (e.g., absorbable stent) that includes a PEGylated hyaluronic acid and a PEGylated non-hyaluronic acid biocompatible polymer and the methods of use thereof.

Abstract: The present invention is to provide a low molecular weight hyaluronan by acting a hyaluronidase derived from a microorganism belonging to the genus Penicillium on a hyaluronan and a process for preparing the same, and an enzyme composition which can be suitably used for the preparation of the low molecular weight hyaluronan.

Abstract: The invention provides methods and kits to detect liver fibrosis or a change in the gradation of liver fibrosis in mammals. The diagnostic marker is based on the profiling and identification of diagnostic carbohydrates present in a body fluid such as blood serum.

Abstract: Galactosylceramide analogues represented by the following formula (1) or (2). (wherein X and Y each represent S or O, R1 and R2 each represent an alkyl group or an alkenyl group each having 9 to 35 carbon atoms. R3 represents an alkyl group or an alkenyl group each having 2 to 30 carbon atoms.) It is provided a ?-glucocerebrosidase activator which is easily available, and external skin preparations and a method of activating ?-glucocerebrosidase, in which improvement in formation of horny layer transmission barrier is expected by activating ?-glucocerebrosidase so that an improved effect in rough skin is also expected.

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: Water-based emulsifier wax gels are provided that include skin-identical sphingolipids The present invention also provides a process for the preparation of such gels, the use of such gels for the preparation of oil-in-water emulsions, and the resulting emulsions that contain the inventive gels.

Abstract: A new use of a suitable colloidal mixture of hyaluronic acids, of different molecular weights mixed together in a proper ratio in the treatment of the cutaneous diseases is described.

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: This invention provides compounds having excellent antitumor activity, which are represented by the following formulae in which R1, R2, R3, m, n and R4 have the significations as given in the specification.

Abstract: The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds and methods for preparing the compositions. The invention also provides novel boronate ester compounds. The invention further provides boronic acid anhydride compounds useful in the methods of the invention.

Abstract: The present invention provides compositions and methods for inhibiting cell migration, e.g., lymphocytes and inflammation. The invention also provides an improved process for preparing fluorinated N-acetylglucosamines.

Abstract: This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: The invention relates to a process for the depolymerization of glycosaminoglycanes characterized by the use of high-energy radiation in the presence of an organic compound selected from the group consisting of ethers, alcohols, aldehydes, amides and formic acid. The invention also relates to intermediate depolymerized heparin having a molecular weight of between 1,000 and 5,500, absorbance at 400 nm below 0.300 and ratio SO3?/COO?equal to or higher than in the starting heparin. The intermediate depolymerized heparin can be dissolved in a buffer solution and fractionated by gel permeation for obtaining the desired molecular weight.

Abstract: The present invention relates to a recombinant Bacillus host cell containing a recombinant vector including a nucleic acid segment having a coding region segment encoding enzymatically active hyaluronan synthase (HAS). The recombinant Bacillus host cell is utilized in a method for producing hyaluronic acid (HA).

Abstract: The invention relates to a method which comprises synthesizing bifunctional compounds then chiral compounds from the bifunctional compounds, also to synthesizing supports comprising these chiral compounds, and the use of these supports for preparing or separating enantiomers, or for asymmetric synthesis. The invention also relates to bifunctional compounds, their use as a source of functionalized polymers, and to the chiral compounds, also to the use of these chiral compounds in a chiral support in the form of a three-dimensional network or for separating or preparing enantiomers, principally for analytical or preparative chromatography, and in a support for the production of chiral molecules by asymmetric synthesis.

Abstract: The invention relates to the use of the disaccharide derivatives 3?-aminosucrose, sucrose-C6-acid and palatinose-C6?-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.

Abstract: The invention relates to the use of the disaccharide derivatives 3?-aminosucrose, sucrose-C6-acid and palatinose-C6?-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: Compounds and methods which are useful for the site-specific delivery and localization of drugs are provided. The compounds can be represented by the formula: A-L-D wherein A is an anchoring moiety; L is a linking group; and D is a drug.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: This invention relates generally to compounds and processes for synthesizing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid. The compounds of this invention are useful, inter-alia, for the inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies, including inflammatory and autoimmune diseases, such as bronchial asthma, rheumatoid arthritis, type I diabetes, multiple sclerosis, allograft rejection and psoriasis. This invention also relates to pharmacological compositions containing derivatives of 2-3-O-isopropylidene-?-L-xylo-2-hexulofuranosonic acid and the methods of treating such pathologies as listed above.

Abstract: The purification of the E.coli K5 polysaccharide by treatment with isopropyl alcohol and elimination of lipophilic substances is described. The purified product can be used to prepare, after N-deacetylation, new N,O-sulfated polysaccharides with high degree of sulfation.

Abstract: The present invention provides stable glycosaminoglycan (GSG) structures and methods of use of such GAG structures. These structures comprise a core of free GAG, a coating of crosslinked GAG surrounding the core, and a layer of a positively charged moiety surrounding the crosslinked GAG layer. These GAG structures provide improved stability, both in in vivo and external use. Furthermore, resurfacing of the structures provides improved cell adhesion and thus improved delivery of the GAG into living cells and tissues.

Abstract: Disclosed is a method of producing a polysaccharide-polypeptide conjugate by reacting a polysaccharide with a polypeptide which contains at least one free amino group, wherein a polysaccharide carrier comprising vicinal hydroxyl groups is oxidized under ring opening to create vicinal aldehyde groups and is reacted with one or more base-instable antigenic polypeptide(s) containing at least one free amino group, the polypeptide(s) being bound directly to the polysaccharide carrier via at least one azomethine bond.

Abstract: A carrier and a method for preparing it are provided for use in the delivery of therapeutic agents. A polysaccharide is reacted with an oxidizing agent to open sugar rings on the polysaccharide to form aldehyde groups. The aldehyde groups are reacted to form covalent oxime linkages with a second polysaccharide and each of the first and second polysaccharide is selected from the group consisting of hyaluronic acid, dextran, dextran sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, heparan, heparan sulfate and alginate.

Abstract: The present invention relates to a recombinant Bacillus host cell containing a recombinant vector including a nucleic acid segment having a coding region segment encoding enzymatically active hyaluronan synthase (HAS). The recombinant Bacillus host cell is utilized in a method for producing hyaluronic acid (HA).

Abstract: A process for producing hydrazinomonosaccharide derivatives and use of hydrazines in determining the structures of aldose and ketose monosaccharides located at the reducing ends of saccharides.

Abstract: A substituted polysaccharide comprising ?1-4 linkages having covalently bonded on the polysaccharide moiety thereof, at least one deposition enhancing group which undergoes a chemical change in water at a use temperature to increase the affinity of the substituted polysaccharide to a substrate, the substituted polysaccharide further comprising one or more independently selected silicone chains.

Abstract: The present invention relates to water-insoluble, crosslinked amide derivatives of hyaluronic acid and manufacturing method thereof, where the amide derivatives of hyaluronic acid are characterized by crosslinking, of polymer or oligomer having two or more amine groups, with hyaluronic acid or its hyaluronate salts through amidation reaction. The water-insoluble, crosslinked amide derivatives of hyaluronic acid according to the present invention may be diversely used for prevention of adhesion after surgical operation, correction of facial wrinkles, dermal augmentation, tissue engineering, osteoarthritic viscosupplement etc.

Abstract: Sebum production inhibitors containing as an active ingredient a compound of general formula (1) below having a glucuronic acid derivative and a glucosamine derivative in the structure or a pharmacologically acceptable salt thereof

Abstract: The present invention relates to a process for the preparation of oligosaccharides or oligosaccharide containing compounds, especially N-acetyl-chitooligosaccharides having a fucosylated monosaccharide. The invention also relates to novel oligosaccharides or oligosaccharide containing compounds, especially N-acetyl-chitooligosaccharides, which are fucosylated and optionally covalently bound to a carrier molecule.

Abstract: The purposes of this invention are preparation of the non-mucin type synthetic compounds-carrier conjugated compounds which are stable against enzymes, and which have the ability of specific reactivity to induce immune response for cancer and HIV. A compound of the general formula (1), wherein A represents OH or sialic acid and/or it's derivatives, and B represents OH or galactose and/or it's derivatives; T represents H or protecting groups of amine; M represents H or OH; X represents oxygen atom, —NH— or S(O)z (where z is 0, 1 or 2); Q is H or oxygen atom; V represents lower alkyl or H; W is straight or branched alkylene groups from 0 to 5; Z is straight or branched alkylene groups from 1 to 5; i, m, and t is 0 or 1; non-mucin type synthetic compounds or it's carrier conjugated compounds, which have above mentioned compounds as a core structure of antigen.

Abstract: For the prevention of the narrowing of the tubular walls of an animal after the tubular walls have been traumatized, the administration of a therapeutically effective non-toxic amount of a form of Hyaluronic Acid selected from Hyaluronic Acid, salts thereof and combinations thereof to the animal to prevent narrowing of the tubular walls.

Abstract: The present invention relates to novel synthetic polysaccharides with antithrombotic activity exhibiting at least one covalent bond with biotin or a biotin derivative and to a process employing avidin or streptavidin which makes it possible to neutralize these polysaccharides.