Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of glycolysis, inhibitors of protein glycosylation, anti-virals, and down-regulators of insulin receptor and IGF-1 receptor for the treatment or prevention of inflammatory dermatological diseases or proliferative dermatological diseases.

Abstract: Disclosed are a therapeutic pharmaceutical agent for diseases associated with the decrease in the function of GNE protein, a food composition, and a food additive. The therapeutic pharmaceutical agent is characterized by comprising a compound capable of increasing the quantity of N-acetylneuraminic acid in cells. Examples of the compound to be contained in the therapeutic pharmaceutical agent include N-acetylneuraminic acid, an intermediate produced downstream from N-acetylmannosamine in an N-acetylneuraminic acid biosynthesis pathway, an N-acetylneuraminic acid derivative, an N-acetylmannosamine derivative, an N-acetylneuraminic acid-containing compound, an N-acetylneuraminic acid derivative-containing compound, an N-acetylmannosamine-containing compound, an N-acetylmannosamine derivative-containing compound, an inhibitor of a degrading enzyme for N-acetylneuraminic acid, an inhibitor of a degrading enzyme for N-acetylmannosamine, an inhibitor of a degrading enzyme for the intermediate, and others.

Abstract: An oligo-aminosaccharide compound formed by binding 3 to 6 saccharides, such as 2,6-diamino-2,6-dideoxy-?-(1?4)-D-glucopyranose oligomers, or a salt thereof, which has high affinity to a double-stranded nucleic acid.

Abstract: The invention relates to a crystalline form of 4-(?-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

Abstract: The present invention concerns a novel retinoic acid regulated gene whose expression product displays useful morphogenic/mitogenic properties. The present invention further concerns an isolated nucleic acid of SEQ ID NO:1 encoding a retinoic acid regulated expression product having an amino acid sequence of SEQ ID NO:2.

Abstract: A novel method is disclosed for simultaneous detection and quantification of two or more nucleic acid targets, without need for amplification. The method depends on spectral-temporal resolution of chemiluminescence emitted from independent hybridization-induced chemiluminescent signal (HICS) probes. The utility of this method has been demonstrated by use of resolvable N-linked acridinium and 2,7-dimethoxyacridinium ester labeled probes in a homogeneous assay for sensitive and simultaneous independent quantification of several bacterial and fungal target sequences. Compositions and kits for practicing the method of the present invention are also disclosed.

Abstract: Biomaterials that support cell attachment and growth are provided. In one aspect, biomaterials are provided comprising a first polymer matrix comprising reactive amino moieties and a second polymer matrix that interpenetrates with the first polymer matrix, where the second polymer matrix comprises a poly(alkylene oxide) comprising two or more alkylene oxide oligomers joined by gamma-thioether carbonyl linkages. In another aspect, biomaterials are provided comprising at least one biopolymer comprising amino groups, thiol groups, and bifunctional modifiers connecting at least some of the amino groups to at least some of the thiol groups; and at least one poly(alkylene oxide) cross-linked to at least two thiol groups of the biopolymer. The biomaterials may further comprise a pharmacologically active agent or cells. Methods of administering such biomaterials to a patient in need thereof are also provided.

Abstract: The instant invention provides compositions for the treatment of cancer. Specifically, the invention provides polypeptides and nucleic acid molecules comprising tumor-associated embryonic antigens, e.g., OFA-iLRP, and chemoattractant ligands, e.g., a proinflammatory chemokine such as MIP3?/CCL20 or ?-defensin mDF2?. The invention further provides cancer vaccines and methods for treating subjects having, or at risk of developing, cancer.

Abstract: Preparation and use of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.

Abstract: The invention provides isolated nucleic acids molecules, designated 33877, 47179, 26886, 46743, 27417, 32252, and 53320 nucleic acid molecules, which encode novel human transferase family members. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing 33877, 47179, 26886, 46743, 27417, 32252, or 53320 nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a 33877, 47179, 26886, 46743, 27417, 32252, or 53320 gene has been introduced or disrupted. The invention still further provides isolated 33877, 47179, 26886, 46743, 27417, 32252, or 53320 proteins, fusion proteins, antigenic peptides and anti-33877, 47179, 26886, 46743, 27417, 32252, or 53320 antibodies. Diagnostic methods utilizing compositions of the invention are also provided.

Abstract: The present invention provides branched water-soluble polymers that allow two or more water-soluble polymers to be conjugated to another species. The branched polymers provide access to therapeutic agents that are conjugated at a single site to two or more water-soluble polymers. The branched polymers are based upon branch points that are simple branched alkyl structures, reactive side-chain amino acids and small peptides of reactive side-chain amino acids, and saccharides. Also provided is a method for preparing mono-disperse poly(ethylene glycol) of a well-defined and determinable molecular weight, and a method for the rational end-functionalization of poly(ethylene glycol). Conjugates of the branched water-soluble polymers with diverse species, e.g., peptides, lipids, glycolipids and small molecules are also provided.

Abstract: The present invention relates to the use of glycan-binding polypeptides and glycans as a medicament, in particular for treating and/or preventing helminthic infections or an immune disease. Moreover, the present invention is directed to corresponding pharmaceutical compositions, food products and animal feed comprising isolated glycans and/or glycan-binding polypeptides. In addition, the present invention teaches methods for identifying anti-helminthic carbohydrate-binding polypeptides, for identifying helminthic glycan and gene targets involved in glycan-mediated toxicity, for identifying helminths susceptible to glycan-mediated toxicity, and for identifying anti-helminthic and anti-allergic substances.

Abstract: The invention relates to a gem-difluoride glycoconjugated compound with formula (I): where R represents II or a benzyl, acetyl, benzoyl alkyl group, R1 and R2 may be identical or different and represent H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyldiphenylsilyl protective group or an acetal group of the CR?R? type, where R? and R? may be identical or different and represent H or an alkyl, aryl, benzyl or thiophene group, R3 represents H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tertiobutyldiphenylsilyl protective group, R4 represents OR?, NGR?GR?, N3, or a phthalimide, where R? represents H or an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl or tertiobutyldiphenylsilyl protective group, GR? and GR? may be identical or different and represent II or an alkyl, benzyl, benzoyl, acetyl, alkyloxycarbonyl, allyloxycarbonyl or benzyloxycarbonyl group, R5 represents a free or protected hydroxyl group or a halogen, R6 represents H or an alkyl, acetyl, benz

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: The invention provides a new class of compounds exhibiting an inhibitory effect on neuraminidase (NA), hemagglutinin (HA) and structural M2 protein bearing viruses. These compounds are also useful as inhibitors of the replication factors of hepatitis virus type C (HVC). The invention also describes pharmaceutical compositions containing the compounds of the invention either alone or in combination admixed with a suitable and pharmaceutically acceptable carrier.

Abstract: Partially desulfated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives exhibit antiangiogenic activity and are devoid of anticoagulant activity.

Abstract: Derivatives of PSAs are synthesized, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.

Abstract: A pharmaceutical composition is provided that is useful for reducing sodium in the bloodstream of animals. In some embodiments, the pharmaceutical composition comprises a high-ion-affinity part and a substrate part. Additionally, methods of using the pharmaceutical composition and methods of treating diseases with the pharmaceutical composition are disclosed.

Abstract: Lactosamine derivatives and related methods suitable for the preparation, including large-scale production, of N-acetyllactosamine, lactosamine, numerous lactosamine salts and a number of lactosamine-containing oligosaccharides are provided.

Abstract: Disclosed is an external preparation containing nonsteroidal anti-inflammatory drugs (NSAIDs), which is suppressed in cytotoxicity induced by the NSAIDs. Also disclosed is a method for producing the external preparation. The present invention is based on the finding that skin disorders induced by nonsteroidal anti-inflammatory drugs (NSAIDs) can be suppressed when the NSAIDs form intermolecular compounds together with trehalose, which is an example of disaccharides. A disaccharide other than trehalose may be used therefor.

Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.

Abstract: A method of providing a prognosis of breast cancer is conducted by analyzing the expression of a group of genes. Gene expression profiles in a variety of medium such as microarrays are included as are kits that contain them.

Abstract: This invention pertains to the discovery that an amplification of the CYP24 gene or an increase in CYP24 activity is a marker for the presence of, progression of, or predisposition to, a cancer (e.g., breast cancer). Using this information, this invention provides methods of detecting a predisposition to cancer in an animal. The methods involve (i) providing a biological sample from an animal (e.g. a human patient); (ii) detecting the level of CYP24 within the biological sample; and (iii) comparing the level of CYP24 with a level of CYP24 in a control sample taken from a normal, cancer-free tissue where an increased level of CYP24 in the biological sample compared to the level of CYP24 in the control sample indicates the presence of said cancer in said animal.

Abstract: A peptide fragment of the netrin-4 protein and nucleic acids coding for the peptide are described. The peptide can inhibit endothelial cell proliferation and cell migration, as well as activate the proliferation and migration of pericytes and smooth muscle cells. Pharmaceutical formulations containing the peptide and/or the nucleic acids can be used to treat a variety of tumoral and non-tumoral pathologies.

Abstract: The present invention provide a compound represented by the following formula (1) wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention and a salt thereof can preferentially induce production of IL-4, which is one kind of cytokines that control action of immunocytes. Therefore, it is useful for the prophylaxis or treatment of autoimmune diseases, infectious diseases and the like, and prophylaxis or treatment of diseases caused by functional promotion of Th1 cells.

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 relates to a process for the preparation of unsaturated acylamidoalkylpolyhydroxy acid amides by reacting the reaction product of polyhydroxy acid lactone and aliphatic diamine with the anhydride of a monounsaturated carboxylic acid, to the unsaturated acylamidoalkylpolyhydroxy acid amides and also to a process for the preparation of polymers of unsaturated acylamidoalkylpolyhydroxy acid amides.

Abstract: The present invention is directed to, for example, an oligosaccharide having at an end thereof a 4-position halogenated galactose residue represented by formula (I): (wherein X represents a halogen atom, and R represents a monosaccharide, an oligosaccharide, or a carrier), a transferase inhibitor containing the oligosaccharide, and a method for inhibiting sugar chain elongation reaction in the presence of glycosyltransferase, the method including employing the inhibitor. The invention also provides a method for producing a 4-position halogenated galactose sugar nucleotide represented by formula (II): (wherein each of R1 to R3 represents a hydroxyl group, an acetyl group, a halogen atom, or a hydrogen atom; X represents a halogen atom; and M represents a hydrogen ion or a metal ion), wherein the method employs bacterium-derived galactokinase and bacterium-derived hexose-1-phosphate uridylyltransferase.

Abstract: Disclosed is a novel use of phytosphingosine. More particularly, disclosed are a composition for preventing or treating hyper-proliferative skin diseases comprising pachastrissamine as an active ingredient, a use of pachastrissamine or a pharmaceutically acceptable salt thereof for preparing a preventing/therapeutic agent of hyper-proliferative skin diseases, and a method for treating hyper-proliferative skin diseases administering an effective amount of pachastrissamine or a pharmaceutically acceptable salt thereof to a subject in need thereof. The pachastrissamine inhibits the degradation of FoxO3a protein and increases the expression of FoxO3a protein. Thus, the inventive pharmaceutical composition has a preventing of treating effect on hyper-proliferative diseases by inducing apoptosis of hyper-proliferative cells and inhibiting the cell cycle.

Abstract: Compounds and methods are provided for a single-step covalent attachment of a label to a molecule comprising forming a covalently attachable labeling reagent for alkylating the molecule. Then, combining the covalently attachable labeling reagent with a mixture containing the molecule, under conditions wherein the labeling reagent has reactivity with the molecule thereby forming a covalent bond.

Abstract: Provided are a method for producing a fraction containing more than 50% of CH represented by the general formula (1), which comprises at least the step of allowing a glucuronic acid donor, an N-acetylgalactosamine donor, a saccharide receptor, a chondroitin polymerase derived from the Escherichia coli K4 strain, and Mn2+ at a final concentration of 0.02 to 100 mM to coexist, and performing a reaction thereof under conditions of 20 to 40° C. and pH 6 to 8 for 0.5 minutes to 4 hours, and a method for producing a fraction containing more than 50% of CH represented by the general formula (2), which comprises at least the step of performing the reaction under same conditions for 10 hours or longer, which enable industrial scale production of a CH fraction of a controlled even number saccharide and odd number saccharide content ratio by a simple procedure at a low cost.

Abstract: Implantable biocompatible polymeric medical devices include a substrate with an acid or base-modified surface which is subsequently modified to include click reactive members.

Abstract: The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer.

Abstract: The present invention provides a phosphoramidate compound having the structure (I) wherein X comprises a monosaccharide group comprising the structure (II) or (III) or a pharmaceutically acceptable salt, ester or salt of such ester. The present invention also provides processes for the production of (I) and uses thereof.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: The present invention relates to a method for reductive amination of a water soluble carbohydrate. An aminated water soluble carbohydrate is a prerequisite in processes for further modification of cellulose. The synthesis of this molecule comprises, providing a water soluble carbohydrate, an amine and a reducing agent, which are reacted under acidic conditions, isolated to give an aminated water soluble carbohydrate with a yield larger than 60%. The invention also relates to an aminated hemicellulose molecule with a molecular weight of at least 1 kDa, especially xyloglucan.

Abstract: This invention relates to sustained release pharmaceutical compositions comprising O-desmethyl-venlafaxine, in particular to sustained pharmaceutical compositions comprising O-desmethyl-venlafaxine orotate and/or O-desmethyl-venlafaxine glucuronate.

Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.

Abstract: Compositions comprising matrix metalloproteinase 11 (MMP-11) or stromelysin-3 (ST-3) or the nucleic acid encoding the MMP-11 for use in vaccines for treating tumors and cancers, which overexpress MMP-11, are described. In particular embodiments, the compositions comprise a nucleic acid encoding a fusion polypeptide that includes the catalytically inactivated MMP-11 linked at the C-terminus to an immunoenhancing element wherein the codons encoding the MMP-11 and the immunoenhancing element have been optimized for enhanced expression of the fusion polypeptide in human cells. In other embodiments, the compositions comprise the catalytically inactivated MMP-11 linked at the C-terminus to an immunoenhancing element. The compositions can be used alone or in synergy with vaccines against other tumor associated antigens as well as with conventional therapies such as radiation therapy and chemotherapy.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: A hypoglycemic effect enhancer for enhancing the activity of an ?-glucosidase inhibitor, the enhancer comprising at least one kind of bacteria selected from the group consisting of bifidobacteria, lactic acid bacteria, saccharifying bacteria, and butyric acid bacteria.

Abstract: The present invention relates to compositions and methods of their production and use, including use in increasing de-N-acetyl sialic acid antigen of a mammalian cell and methods that exploit the increase in deNAc sialic acid antigen on such cells.

Abstract: Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.

Abstract: Methods are provided for designing a transition state inhibitor of orotate phosphoribosyltransferase (OPRT) and for inhibiting OPRT.

Abstract: Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.

Abstract: The present invention generally relates to the field of sialic acids, in particular to the field of sialic acid enriched food products and their uses. One embodiment of the present invention relates to a food product enriched with food-grade sialic acid producing bacteria and/or a fraction thereof containing sialic acid.

Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable salts thereof, and to formulations and uses of the compounds of formula (I) in the treatment of metabolic disorders.

Abstract: Processes for the synthesis of lipochitooligosaccharides were developed. A fully acylated oligoglucosamine precursor is prepared and reacted with a glucosamine monomer that has an amine protecting phthaloyl group. With removal of the phthaloyl group, a fatty acid may be added on the terminal glucosamine unit, forming a lipochitooligosaccharide. The processes can be adapted for use on a commercial scale.

Abstract: The invention provides adenosine analog compounds that act at P2Y receptors, e.g., the P2Y2 receptor, including pharmaceutical compositions; and uses thereof to treat or prevent diseases associated with that receptor, e.g., disorders relating to mucus secretion, such as cystic fibrosis, chronic obstructive pulmonary disorder (COPD), asthma, constipation, chronic idiopathic constipation, dry mouth (xerostomia), gum disease, and gastrointestinal problems caused by radiation and chemotherapy for cancer.

Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.