Abstract: The present invention relates to a novel nitrile glycoside of Formula I named NIAZIRIDIN and to analogues and derivatives thereof. The present invention also relates to a process for the isolation of a novel nitrile glycoside of Formula I below named NIAZIRIDIN and its derivatives and analogues by bioactivity-guided fractionation from the pods of Moringa oleifera. The present invention particularly relates to the bioenhancing activity of the novel nitrile glycoside of Formula I below named NIAZIRIDIN and its derivatives and analogues in enhancing bioactivity of commonly used antibiotics such as rifampicin, tetracycline and ampicillin against Gram (+) and (?) bacteria. The biomolecule also enhances the absorption of drugs, vitamins and nutrients through the gastro-intestinal membrane increasing their bio-availability. Therefore niaziridin can be used in combination therapy with drugs and nutrients resulting in reduced drug associated toxicity, reduced cost and duration of chemotherapy.

Abstract: The invention concerns novel troxerutin with high trihydroxy-ethyl-rutin content. Said troxerutin has at least 92 wt. % of 7,3?,4?-trihydroxyethyl rutin and a wettability expressed in minutes less than 10 minutes, when said wettability is measured in a test consisting in measuring the time taken by 3.5 g of said enriched troxerutin powder to leave the surface of a beaker containing 100 ml of water, at a stabilised temperature of 20° C., when said enriched troxerutin powder is poured at the surface of the water in said beaker, and a wettability less than 100 seconds when said wettability is measured in a test consisting in measuring the time taken by said enriched troxerutin to be wetted by the water contained in a receptacle, such as a beaker, when said enriched troxerutin has been deposited at the surface of the water, in the form of cores of 2 mm wide and 3 mm high weighing 63 ? 2 mg, at a stabilised temperature of 20° C. Said troxerutin has improved properties of wettability and solubility in water.

Abstract: By using xylobiose or xylooligosaccharide containing xylobiose as a main ingredient in place of lactulose, there is provided a blood ammonia lowering agent, a therapeutic agent of hyperammonemia or a therapeutic agent of hepatic encephalopathy that need be adminstered in smaller doses and which have no concern over side effects. Lactulose conventionally used as such drugs has to be administered in high doses and involves a safety problem when administered to patients with galactosemia or diabetes mellitus. The drug of the invention which contains xylobiose as a main ingredient solves these problems.

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: In order to provide the anti-retrovirus active compound with low anti-coagulant action and low cytotoxicity, compounds comprising glycoside or the salt thereof wherein lipid is linked to position 2 of sialic acid having all hydroxyl groups at positions 4, 7, 8 and 9 completely sulfated, or KDN (2-keto-3-deoxy-D-glycero-2-nononic acid) having all hydroxyl groups at positions 4, 5, 7, 8 and 9 completely sulfated are provided.

Abstract: The invention relates to a process for the production of peracylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents methyl, ethyl, propyl, isopropyl, tbutyl, phenyl, n means 2, 3 or 4, X means —COO— or —NH—and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of peracylated saccharides with 1-O-functionalized side chains on an enlarged scale.

Abstract: The present invention is a sunscreen composition that has at least one sunscreen agent and at least one glucoside emulsifier. The composition also has water. Preferably, the sunscreen composition also has at least one of the following additional components: emulsifier other than glucoside, emollient, skin-feel additive, moisturizing agent, film former/waterproofing agent, pH adjuster/chelating agent, preservative, or any combinations thereof. The composition is a stable oil-in-water emulsion.

Abstract: A glucoside containing isomaltol represented by formula (I): (wherein Sug represents a glucose residue or a sugar linkage composed of two or more glucose units) as an aglycon, a physiologically active substance containing the glucoside having human cytokine inducing ability increasing activity, a method for producing it, and food, medicine and feedstuff containing the substance.

Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group —C(O)—(CHR4)m—AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R3; R3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R2; and R4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed.

Abstract: The present invention describes isolated Fagopyritol A1, isolated Fagopyritol A3, and isolated Fagopyritol B3. Compositions which include two or more of Fagopyritol A1, Fagopyritol A2, Fagopyritol A3, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D-chiro-inositol, at least one of which is an isolated Fagopyritol A1, isolated Fagopyritol A3, or isolated Fagopyritol B3, are also disclosed. Methods for preparing substantially pure Fagopyritol A1, Fagopyritol A3, Fagopyritol B3, or mixtures thereof from buckwheat are also described. The fagopyritols can be used to prepare pharmaceutical compositions, the administration of which can be used to treat diabetes.

Abstract: The present invention provides a method for making glycoside compounds including the steps of: (a) lithiating an aromatic reactant having a leaving group using a lithium reagent in a first microreactor under non-cryogenic conditions to form a lithiated anion species, and (b) coupling the lithiated anion species with a carbonyl substituted reactant to form a glycoside.

Abstract: The present invention relates to a ternary glucosyl complex which is a bioprecursor of at least one retinoic active ingredient for percutaneous application, having formula (I), wherein E represents a linear hydrocarbon spacer group that is branched or cyclized and has an aliphatic or aromatic content capable of containing one or several heteroatoms of oxygen and carrying one or several carbonyl groups; A represents a radical of a molecule of said retinoic active ingredient linked to the spacer group by a carboxylate function and n=1 or 2.

Abstract: A novel C-glycoside of isopropylthiogalactoside (IPTG), isobutyl-C-galactoside (IBCG), is described. IBCG may be used as an IPTG substitute for increased induction of protein expression of plasmid-based genes for the production of recombinant proteins under the control of the lac promoter. IBCG offers the advantage over IPTG of being stable at ambient temperature.

Abstract: Novel carbohydrate-based compounds with an attached ring system that have antimicrobial or cytostatic activity. The compounds are administered to humans and animals for the treatment or amelioration of bacterial, fungal, viral or protozoal infections or tumors.

Abstract: The present invention provides pyrazole-O-glycoside derivatives represented by the following formulae, used as a diabetic medicine.

Abstract: A subject of the invention is the compounds of formula (I): R1═H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy, R2═H, Hal, R3═H, alkyl, Hal,  Rg and Rh: H, alkyl, aryl heterocycle, R5═H or O-alkyl, R6═alkyl or CH2—O-alkyl, R7═H or alkyl. The compounds of formula (I) have antibiotic properties.

Abstract: Compositions and pharmaceutical compositions are described which comprise: a component A comprising one or more flavonol glycosides, a component B comprising one or more tetrahydrofolic acid compounds, a component C comprising one or more calcium supplements, and a component D comprising one or more magnesium supplements. Methods of using such compositions and pharmaceutical compositions to treat and/or prevent osteoporosis and/or an inflammatory joint disease are also described.

Abstract: A novel class of antitumour compounds has been recognised based on the isolation from a new marine microbe, strain PO13-046, belonging to the genus Actinomadura sp.), of a compound designated IB-00208. The class of the formulae (I) or (II) where R1 can be hydrogen, acyl, alkyl, alkenyl, aryl, benzyl, alkali metal, and/or sugar, and R2 and R3 can be hydrogen, alkyl, or together R2 and R3 form an unsaturated bond. Such compounds demonstrate an interesting activity several cancel cell lines and against Gram-positive bacteria.

Abstract: The present invention provides compounds having the formula: wherein A is CH or N; B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H, halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and X and Y are independently selected from H, OH or halogen except that when one of X and Y is hydroxy or halogen, the other is hydrogen; and Z is OH or, when X is hydroxy, Z is selected from hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof; and compounds having the formula: wherein A, X, Y, Z and R are defined for compounds of formula (I) where first shown above; E is chosen from CO2H or a corresponding salt form, CO2R, CN, CONH2, CONHR or CONR2; and G is chosen from NH2, NHCOR, NHCONHR or NHCSNHR; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an este

Abstract: The present invention provides a starch that includes at least one glucose polymer having greater than 4% alpha 1-6 glycosidic linkages. The present invention further provides a starch hydrolyzate that includes at least one glucose oligomer having greater than 4% alpha 1-6 glycosidic linkages. The starch and starch hydrolyzate present invention have improved aqueous solution stability and are less likely to retrograde than are solutions of unbranched linear starches or starch hydrolyzates.

Abstract: The invention relates to a series of polyglycoside derivatives that have improved water-solubility by introducing into the molecule polyoxyalkylene groups like polyoxyethylene and polyoxypropylene. The compounds are very mild detergents and emulsifiers.

Abstract: A lactosyl glycoside or an N-acetyllactosaminyl glycoside useful as foods, functional food materials, medicines, and reagents is provided with high yield and inexpensively by using a transfer reaction represented by the following formula in the presence of an enzyme having an activity of cleaving a &bgr;1,4 glucosyl bond: LacA-X+Y→LacA-Y+X, wherein LacA represents lactose or N-acetyllactosaminide; X represents hydrogen (H), a saccharide, a glycoconjugate, or a phenolic compound; and Y represents a compound having an alcoholic hydroxyl group or a phenolic hydroxyl group.

Abstract: A versatile methodology to obtain efficient catalytic materials suitable for selective, liquid-phase oxidations of alcohols is described. Solid inorganic membranes were prepared by the sol-gel procedure by adding a solution of stable organic nitroxyl radicals at the onset of the polymerization of silicon alkoxide monomers. In this way, micro- and mesoporous materials can be obtained that axe effective and recyclable catalytic mediators for highly selective oxidations of a vast class of primary and secondary alcohols carried out with several primary oxidants. Delicate substrates such as carbohydrates and allylic alcohols can selectively be oxidized with these novel catalytic materials.

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: The use of bicyclic carbohydrates for the treatment of parasite infections is described. Different bicyclic carbohydrates have been tested in vitro against a number of protozoa. These compounds also have been screened against viruses, tumors, bacteria and fungi. Compound A1, a thiophenyl-containing bicyclic carbohydrate possessed significant activity against Trypanosoma brucei rhodiense, a parasite that causes the lethal sleeping sickness. Compound A2 and Compound A3, bicyclic carbohydrates with halogen containing aryl groups, possessed significant activity against Leishmania donovani, a parasite that causes leishmaniasis. Bicyclic carbohydrates in general, and Compound A1, Compound A2 and Compound A3 more specifically, could be possible treatments for the sleeping sickness and leishmaniasis in the future.

Abstract: A hydrogenated starch hydrolysate having the following saccharide contents (based on the solids content of the hydrogenated starch hydrolysate): A.<8 wt.-% of hydrogenated monosaccharides (DP=1); B.<41 wt.-% of hydrogenated disaccharides (DP=2); C.<15 wt.-% of hydrogenated trisaccharides (DP=3); D.<30 wt.-% of hydrogenated quat- to deca-oligosaccharides (DP=4 to 10); and E. from about 14 to about 38 wt.-% of hydrogenated undeca- or greater polysaccharides (DP≧11); and hard boiled candies which are produced from the hydrogenated starch hydrolysate.

Abstract: There have been obtained, by cultivation of Streptomyces sp. MK730-62F2 (deposit number of FERM BP-7218), antibiotic caprazamycins A to F having by the following general formula (I) wherein R is tridecyl group, 11-methyl-dodecyl group, and others. These caprazamycins have excellent antibacterial activities against various acid-fast bacteria and various bacteria as well as their drug-resistant strains.

Abstract: The invention relates to a novel compound oleanane triterpenoid oligoglycoside of formula 1 of the accompanying drawing (trivially called corniculatonin), the invention also relates to a process for the isolation of the novel compound from a mangrove plant Aegiceras corniculatum (Blanco) belonging to the family Myrsinaceae, it also discloses the antifungal properties of the said compound, the invention further relates to the use of the said compound as a food preservative, it further discloses a composition containing effective amount of the said compound for the treatment of fungi infections.

Abstract: Process for preparing a solubilization adjuvant, which comprises placing fusel oils in contact with one or more reducing sugars in the presence of an acid catalyst, at a temperature of between 50° C. and 130° C. and while removing the water from the reaction medium until a solution of alkyl glycosides is obtained, and separating the glycosides from this solution.

Abstract: A medicament containing at least one compound selected from the group consisting of compounds represented by General formula (1): wherein R101 represents an acyl residue of an unsaturated higher fatty acid, and R102 represents a hydrogen atom or an acyl residue of an unsaturated higher fatty acid, and pharmaceutically acceptable salts thereof, as an active ingredient.

Abstract: The invention relates to a series of polyglycoside derivatives that contain silicone functional groups introduced into the molecule by reaction with the hydroxyl groups present in the starting polyglycoside molecule. The compounds are prepared by reacting epoxy silicones with an alkyl polyglucoside under base catalysis.

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: Novel sulforhamnosylacylglycerol derivatives represented by General Formula (1): where R101 represents an acyl residue of a higher fatty acid and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid. The derivatives represented by General formula (1) are useful as, a DNA polymerase inhibitor and an anticancer agent.

Abstract: Substituted tetrahydropyran derivatives, processes for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical comprising them. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, R5 and X have the meaning mentioned in the description, a process for the preparation of the compounds of the formula I on a solid phase, and their use as pharmaceuticals.

Abstract: The invention relates to a method of crystallizing maltitol from a maltitol solution by supersaturating the solution in repsect of maltitol and crystallizing the maltitol from the solution. In the process of the invention, the maltitol-containing solution is brought to a supersaturated state, and the solution is subjected to evaporation, until a crystallization mass is obtained which has a crystal yield of 1 to 80% on maltitol, and a dry solids content of over 50%. After bringing the solution to a supersaturated state, the solution is preferably seeded by adding maltitol seed crystals. In one embodiment of the invention, additional feed liquid is added during the crystallization by evaporation.

Abstract: Novel salicyl alcohol derivatives having valuable cosmetically and pharmaceutically useful properties, such as prostaglandin synthesis inhibition, corresponding to the formula (I): R1—OCH2—Ph—O—Z—(R2)n  (I), a method for producing the same and their utilization in cosmetics and pharmacy.

Abstract: The present invention provides an oligosaccharide-supplying composition which contains 10 to 80% by weight of oligosaccharide, 0.3 to 10% by weight of a foaming component and 0.9 to 30% by weight of a neutralizing component and is in the form of foaming chewable tablets. The composition is highly useful in practice, has a uniform composition, excellent texture and high stability and can be easily taken.

Abstract: The present invention is directed toward a novel process for the preparation of pyranosides protected at the 1, 2, 4, and 6 or the 1, 3, 4, and 6 positions.

Abstract: Sulfofucosylacylglycerol derivatives represented by General Formula (1): where R101 represents an acyl residue of a higher fatty acid and R102 represents a hydrogen atom or an acyl residue of a higher fatty acid. The derivatives represented by General formula (1) are useful as a DNA polymerase inhibitor and an anticancer agent.

Abstract: A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated.

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: The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.

Abstract: A smaller molecule obtainable by allowing a sulfated fucan-digesting enzyme which digests a novel sulfated polysaccharide derived from an alga belonging to Laminariales to act on a sulfated fucan, and a method for producing the same.

Abstract: The invention relates to cosmetic and/or pharmaceutical preparations containing (a) water soluble &bgr;-(1,3) glucans that are substantially devoid of &bgr;-(1,6) links, and (b) deoxyribonucleic acids and their breakdown and degradation products.

Abstract: The present invention relates to a process for the production of hyaluronic acid (HA) derivatives. In particular, the process relates to multiple cross-linked hyaluronic acid derivatives, to navel cross-linked derivatives so obtained, and to products containing them and their uses in cosmetic, medical and pharmaceutical applications.

Abstract: An excipient comprising trehalose having a purity of 99.0% or more, a proportion of particles of 75 &mgr;m or more of 2 to 90 wt %, an average particle size of 10 to 250 &mgr;m, an apparent specific volume of 1.5 to 3.5 ml/g, and a whiteness of 90% or more.

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: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.

Abstract: Compound JK represented by the general formula (1): wherein R is H or —CH3; or a pharmaceutically acceptable salt thereof. Compound JK has an excellent antimicrobial activity even against resistant strains including MRSA and is useful as an anti-microbial agent.

Abstract: One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.