Abstract: This invention provides compounds containing a 2-deoxy-2-amino-?-D-glucopyranose (glucosamine) glycosidically linked to a cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.

Abstract: Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.

Abstract: Disclosed are compounds having the formula wherein R2 is hydrogen, a monomeric glycoside or an oligomeric glycoside, R3 is hydrogen, a monomeric glycoside, an oligomeric glycoside, or a group having the formula R is a lower alkylene, R? is selected from the group consisting of moieties having the formula where X=0 or 1, Y=0 or 1, R1 is hydrogen or a pharmacologically active drug residue, R8 a pharmacologically active drug residue, R4, R5, and R6 are independently hydrogen, alkyl, aryl, aralkyl, and cycloalkyl or together form a nitrogen-containing ring, and R7 is hydroxyl or hydroxyalkyl.

Abstract: There are provided a novel microorganism Enterobacter sp. B20 strain which produces (E)-4-(2-isocyanovinyl)phenyl ?-rhamnopyranoside having a favorable effect of inhibiting melanogenesis and ?-L-rhamnopyranoside produced thereby. This novel microorganism is a gram-negative bacillus isolated from soil and shows motility owing to polar flagellum. The ?-L-rhamnopyranoside, which is produced by culturing the microorganism under aerobic conditions at a culture temperature of 10 to 37° C. and at a medium pH of about 5 to 9 usually for about 1 to 7 days, is useful as a highly safe and stable whitening agent.

Abstract: Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.

Abstract: This invention provides nucleic acid sequences and characterization of the gene cluster responsible for the biosynthesis of the enediyne C-1027 (produced by Streptomyces globisporus). Methods are provided for the biosynthesis of enediynes, enediyne analogs and other biological molecules. This invention also provides enediyne and enediyne analogs biosynthesized by manipulation of the C-1027 gene pathway.

Abstract: This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

Abstract: Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.

Abstract: A chemiluminescent system for detecting the presence of influenza virus in a biological fluid sample is provided. An influenza diagnostic kit is provided which includes (1) a sampling device for obtaining the biological fluid from a subject, (2) a chemiluminescent substrate material which, in the presence of influenza virus in the biological sample, will generate a chemiluminescent product that will produce detectable light, and (3) a means for detecting any generated light. A liquid sample containing the biological fluid, and preferably a diluent, are contacted with the an absorbent material containing the chemiluminescent substrate material. The substrate responds to neuraminidase activity intrinsic to influenza A and influenza B virus particles, such that when the substrate is in contact with influenza virus, the substrate is cleaved to yield a chemiluminescent product that then decomposes to produce light which can then be detected.

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 invention described herein relates to: the use of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in the manufacture of a composition for the treatment of rumen acidosis; a method of treatment of rumen acidosis which comprises administration of an effective amount of an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase to a ruminant; a formulation suitable for the treatment of rumen acidosis in an animal which comprises an effective inhibitor of a bacterial ?-amylase and/or ?-glucosidase in admixture with a suitable excipient, diluent or carrier selected with regard to the intended route of administration and standard pharmaceutical/veterinary/farming practice; screening methods useful in the identification of a suitable inhibitor of a bacterial ?-amylase and/or ?-glucosidase for the treatment of acidosis in a ruminant; a process for improving ruminant milk quality and/or quantity which comprises treatment of a ruminant with an effective amount of an inhibitor of bacte

Abstract: A composition containing an alk(en)yl oligoglycoside betaine esterquat corresponding to formula I: R1O(G)nOCOCR2R3NR4R5R6??(I) wherein R1 is an alk(en)yl group having from about 4 to about 22 carbon atoms, G is a sugar unit containing 5 or 6 carbon atoms and n is a number from 1 to about 10, R2 is H or a CH3 group, R3 is H or a linear and/or branched alk(en)yl group having from 1 to about 6 carbon atoms, R4, R5 and R6, independently of one another, represent a linear and/or branched alk(en)yl group having from 1 to about 24 carbon atoms or a linear and/or branched hydroxyalk(en)yl group having from 1 to about 24 carbon atoms.

Abstract: A sensor for the detection of tetrameric multivalent neuraminidase within a sample is disclosed, where a positive detection indicates the presence of a target virus within the sample. Also disclosed is a trifunctional composition of matter including a trifunctional linker moiety with groups bonded thereto including (a) an alkyl chain adapted for attachment to a substrate, (b) a fluorescent moiety capable of generating a fluorescent signal, and (c) a recognition moiety having a spacer group of a defined length thereon, the recognition moiety capable of binding with tetrameric multivalent neuraminidase.

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: Functional polyvalent oligomer for applications in medicine and biotechnology are disclosed. These oligomers have the formula (1) wherein R is H, CH3, C2H5, R1, is H, NH2, OH, COOH, X is N-Acetyl Glucosamine, mannose, galactose and sialic acid, fructose, ribulose, erythrolose, xylulose, psicose, sorbose, tagatose, glucopyranose, fructofuranose, deoxyribose, galactosamine, sucrose, lactose, isomaltose, maltose, cellobiose, cellulose and amylose, Y is H, COOH, OH or NH2, and n is from 3 to 50. The present invention also relates to synthesis of such oligomeric ligands. The method of synthesis of the present invention for oligomerization can be—applied to other ligands such as sialic acid, mannose and galactose and can -be used for the prevention of infections.

Abstract: A method of forming a glycosidic bond utilizing an activated thioglycoside is disclosed. The thioglycoside is activated by an N,N-dialkylsulfinamide and trifluoromethanesulfonic anhydride. The method allows the facile synthesis of disaccharides, oligosacchraides, and polysaccharides in solution or on a polymer support.

Abstract: The invention relates to a series of polyglycoside derivatives that contain water-soluble groups introduced into the molecule by reaction with the hydroxyl groups present in the starting polyglycoside molecule. The preferred products have more than one water-soluble group per molecule and are made with mild reagents to avoid discoloration and mal odor. The most preferred products have between 2 and 3 functional groups per molecule. The compounds are amino functional and betaine functional alkyl polyglucoside.

Abstract: Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. In particular, the compounds are based on the 1,6 linkage of a sugar residue and a cyclitol.

Abstract: The present invention relates to a novel method of chemically preparing functionalized derivatives of ?-(1,3)-glucans, enabling obtaining oligosaccharides which are free or which comprise specific groups such as, for example, sulphate, phosphate, methyl, in pre-defined positions. This method includes a reaction between a glycosyl donor of formula (Ia) or (Ib) and a glycosyl acceptor of formula (II), defined in the claims. Application: Preparation of biologically active compounds which can be used in the agricultural, cosmetic or pharmaceutical fields.

Abstract: Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. Preferred compounds of the invention are based on the substituted cyclitols, such as the chiro-inositol derivative pinitol (3-O-methyl-chiro-inositol).

Abstract: Methods for making the functionalized glycoconjugates include (a) contacting a cell with a first monosaccharide, and (b) incubating the cell under conditions whereby the cell (i) internalizes the first monosaccharide, (ii) biochemically processes the first monosaccharide into a second saccharide, (iii) conjugates the saccharide to a carrier to form a glycoconjugate, and (iv) extracellularly expresses the glycoconjugate to form an extracellular glycoconjugate comprising a selectively reactive functional group. Methods for forming products at a cell further comprise contacting the functional group of the extracellularly expressed glycoconjugate with an agent which selectively reacts with the functional group to form a product. Subject compositions include cyto-compatible monosaccharides comprising a nitrogen or ether linked functional group selectively reactive at a cell surface and compositions and cells comprising such saccharides.

Abstract: Compositions and methods are provided for use in the treatment of cancer.

Abstract: Bifunctional antibiotics that target both bacterial RNA and resistance-causing enzymes are disclosed. The A-site of bacterial 16S rRNA serves as the target site for most aminoglycoside antibiotics. Resistance to this class of antibiotics is frequently developed by microbial enzymatic acetylation, phosphorylation or ribosylation of aminoglycosides, modifications that weaken their interactions with the target RNA. Using surface plasmon resonance (SPR), the binding affinity and stoichiometry of various amino-glycosides have been investigated and it was found that neamine, the key pharmacophore of the deoxystreptamine class of amino-glycosides, binds to the A-site in a two to one stoichiometry with a Kd of 10 ?M for each binding site. A library of neamine dimers was prepared and their affinities to 16S rRNA A-site were determined by SPR, with Kd=40 nM for the best dimer (an ˜103-fold increase in affinity). Antibiotic activities of the dimers were determined for several bacterial strains by the Kirby-Bauer method.

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: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.

Abstract: Methods and compositions for treating or ameliorating diseases and other conditions, such as infectious diseases, autoimmune diseases and allergies are provided. The methods employ cyclic AGPs for selectively stimulating immune responses in animals and plants.

Abstract: The invention provides micelles, pharmaceutical formulations comprising micells, solutions comprising micells, methods for preparing micells, methods for delivering micells to patients, and methods for treating sepsis, endotoxemia, septic shock and systemic inflamatory response syndrome in patients by adiministering micelles. The micelles comprises compounds of Forumala (A): wherein the substituents are as defined herein.

Abstract: Compositions and methods are provided for use in the treatment of cancer.

Abstract: Compositions comprising inositolphosphoglycans (IPGs) and ribose are disclosed, and their use in the prevention or treatment of ischaemic-reperfusion injury. This treatment increases the energy generating systems of cells by employing the mitochondrial oxidative restoration system. The use of the compositions in preserving organs for transplantation is also disclosed.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: The present invention provides a method for immobilizing a polysaccharide (PS) to a solid surface, said polysaccharide having a keto-carboxy group (—C(?O)—COOH) or a ketal or hemiketal group corresponding thereto, e.g. derived from KDO (2-keto-3-deoxy-D-manno-octonic acid)), the method comprising the steps of: (a) forming a covalent bond between the carboxy group of the polysaccharide and a reporter molecule (RM), thereby forming a polysaccharide-reporter molecule conjugate (PS-RM), said reporter molecule comprising a recognition/substrate site (e.g. biotin or an anthraquinone); and (b) immobilizing the polysaccharide-report molecule conjugate by forming a specific bond (e.g. by photocoupling or formation of an affinity pair) between the recognition/substrate site of said reporter molecule and a reception/reagent site of the solid surface. The present invention also provides a solid surface thus obtainable and the use of such solid surfaces for diagnostic purposes, e.g.

Abstract: The geometric isomers of olefins and olefinic compounds are separated by means of liquid chromatography using a stationary phase comprising an organosilane with a pendant aliphatic functional group such as C18 and a mobile phase which includes an additive comprising alkanes and alkenes.

Abstract: Purpurin-carbohydrate conjugates and their method of preparation and use for treatment of cancer cells. The conjugates have the general formula: wherein R6 and R7 taken together are ?NR11 or are independently —OR11, where at least one R11 is preferably a mono or polysaccharide moiety and R1-R8 are various groups formed from carbon and hydrogen and optionally oxygen and nitrogen where R3 and R4 may together from a covalent bond.

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.

Abstract: A fullerene derivative represented by the formula (I): [wherein, A is a residue of monosaccharides or disaccharides, and Alk is a lower alkylene group, the group represented by the formula (X): is a fullerene residual skeleton, and n is an integral number of 1 or 2] or its salt produces a formulation usable for PDT which has more hydrophilicity and lipophilicity, is expected to have selectivity to tumor cells by cell recognition, shows no toxicity to the cells in a dark place and has a cytocidal effect by light irradiation.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: The invention relates to the field of pharmacology. More particularly, the invention relates to the treatment of prostate conditions, such as BPH. The invention provides new therapeutic compositions and methods for treating BPH, as well as chronic prostatitis, prostadynia, and irritative bladder conditions, other than interstitial cystitis. The compositions and methods according to the invention, which may be administered orally, efficaciously and safely treat the designated conditions by causing regression of established lesions and reduction of bladder irritation. In particular, the compositions and methods of the invention treat BPH by reducing the size of the prostate gland and decreasing the associated obstructive symptoms.

Abstract: Methods are provided for detecting the binding of a first member to a second member of a ligand pair, comprising the steps of (a) combining a set of first tagged members with a biological sample which may contain one or more second members, under conditions, and for a time sufficient to permit binding of a first member to a second member, wherein said tag is correlative with a particular first member and detectable by non-fluorescent spectrometry, or potentiometry, (b) separating bound first and second members from unbound members, (c) cleaving the tag from the tagged first member, and (d) detecting the tag by non-fluorescent spectrometry, or potentiometry, and therefrom detecting the binding of the first member to the second member.

Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

Abstract: The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.

Abstract: Methods and compositions for treating or ameliorating diseases and other conditions, such as infectious diseases, autoimmune diseases and allergies are provided. The methods employ mono- and disaccharide-based compounds for selectively stimulating immune responses in animals and plants.

Abstract: The present invention provides compounds and methods of synthesizing furanose and aminofuranose compounds of Formula I which are useful fro treating rheumatoid arthritis, immunomodulatory diseases and disorders, inflammation, and diseases and disorders characterized by exhibiting tissue proliferation.

Abstract: Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. Preferred compounds of the invention are based on the substituted cyclitols, and in particular cyclitols linked to a sugar moiety where the molecule is substituted with a negatively charged group such as phosphate.

Abstract: The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I 1

Abstract: The present invention provides bacterial immunogenic agents for administration to humans and non-human animals to stimulate an immune response. Also provided are methods for vaccination of mammalian species, especially human patients, with variants of the E. coli FimH protein, said variants being derived from different strains of E. coli, and to production of antibodies that protect the vaccine recipient against infection by pathogenic bacterial species. In another aspect the invention provides antibodies against such proteins and protein complexes that may be used as diagnostics and/or as protective/treatment agents for pathogenic bacterial species. A plasmid-based method of producing polypeptides, especially fused polypeptides, such as the complex of a bacterial chaperone and a bacterial adhesin, is also disclosed.

Abstract: An improved process for the purification of crude aqueous solutions of acarbose by passing such solutions through a strong acid cation-exchange resin, saturating such resin and recovering as an eluate a substantially pure acarbose solution. Purities of more than 98%, and preferably about 99% or higher, are thus obtained.

Abstract: The present invention is to obtain novel anti-inflammatory agents having decreased antibacterial activity and increased anti-inflammatory action, and is psedoerythromycin derivatives represented by the following general formula [I], wherein R1 and R2 are same or different and each represents H, alkyl, alkynyl, acyl or sulfonyl, in which these groups may optionally have substituents, and Me indicates methyl.

Abstract: A glycosphingolipid having a sugar chain containing &agr;-glucosamine and &bgr;-glucosamine is disclosed. Such glycosphingolipid is advantageous in that possibly being manufactured in a facile and inexpensive manner, and that exhibiting moisturizing effect and immuno-enhancing activity.

Abstract: Compounds having a mimetic or antagonistic property of an inositol phosphoglycan, and the uses of these compounds are disclosed, together with the use, e.g. to treat a condition ameliorated by administration of an IPG second messenger or an IPG antagonist thereof. Preferred compounds of the invention are based on the substituted cyclitols, and in particular, the compounds are based on the 1,6 linkage of two or more sugar residues to a cyclitol.