Abstract: The present invention relates to new and improved methods of synthesizing radiolabelling agents which can be used to label biomolecules for use as radiopharmaceuticals. It further relates to certain novel radiolabelling agents and their use in such methods. PET imaging methods and methods of diagnosis employing such radiolabelling agents form a further aspect of the invention.

Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.

Abstract: Provided are methods for the efficient stereoselective formation of glycosidic bonds, without recourse to prosthetic or directing groups.

Abstract: The present invention relates to pharmaceutical compositions comprising dapagliflozin and cyclodextrin, preferably (2-hydroxy)propyl-b-cyclodextrin or ?-cyclodextrin, preferably as inclusion complex. The invention further relates to a process for producing said pharmaceutical compositions. Finally, the invention relates to the use of cyclodextrin for producing dapagliflozin-containing dosage forms and to methods of purification of dapagliflozin.

Abstract: The invention relates to a method of inhibiting the insertion of one or more membrane proteins into a lipid bilayer. The invention also relates to a method of inserting a pre-determined number of membrane proteins into a lipid bilayer and lipid bilayers having a pre-determined number of membrane proteins inserted therein. The lipid bilayers of the invention are useful as sensor arrays, particularly for sequencing nucleic acids.

Abstract: Provided are methods of making compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides synthetic intermediates useful for preparing such compounds.

Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.

Abstract: Fire extinguishing compositions and methods of extinguishing a fire comprising compounds of formula (I) where Rf is a fluorocarbon group. The compounds and compositions described herein are useful as intermediates in the preparation of or as additives to AFFF (aqueous film forming foam) formulations used for the extinguishment of fuel and solvent fires.

Abstract: Use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases The invention relates to the use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases like osteoporosis. Preferred is the use of compounds of the formula I in which the radicals have the stated meanings.

Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: Solid forms of anhydrous (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol are disclosed, in addition to methods of their use in the treatment of various diseases and disorders.

Abstract: The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.

Abstract: Methods of synthesizing sodium glucose co-transporter 2 inhibitors, as well as compounds useful therein, are disclosed.

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: A method of preparing 2-deoxy-L-ribose represented by the following formula I is disclosed. The preparation method includes the steps of: treating L-arabinose with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-L-arabinopyranose; allowing the prepared 1-alkoxy-L-arabinopyranose to react with acyl chloride so as to prepare 1-alkoxy-2,3,4-triacyl-L-arabinopyranose; brominating the alkoxy group of the prepared 1-alkoxy-2,3,4-triacyl-L-arabinopyranose to prepare a 1-bromo-2,3,4-triacyl compound; allowing the prepared compound to react with zinc in the presence of ethyl acetate and an organic base so as to prepare glycal; treating the glycal with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose; treating the prepared 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose with a base to prepare 1-alkoxy-2-deoxy-L-ribopyranose; and hydrolyzing the prepared 1-alkoxy-2-deoxy-L-ribopyranose in the presence of an acid catalyst.

Abstract: Disclosed is a parasitic plant control agent which can control a parasitic plant effectively. Also disclosed is a parasitic plant control method. A parasitic plant can be controlled by inhibiting the metabolism of gentianose in the parasitic plant to inhibit the germination of the parasitic plant.

Abstract: The invention relates to transport mediator-bonded colloids comprising pharmaceutical substances or fluorescence markers, to a method for the production thereof, and to a pharmaceutical preparation comprising said compounds.

Abstract: Methods of improving the cardiovascular and/or metabolic health of patients, particularly those suffering from type 2 diabetes, are disclosed, as well as compounds and pharmaceutical compositions useful therein.

Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.

Abstract: The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

Abstract: The compounds of formula (I), wherein n is an integer from 0 to 4; R1 is a radical selected from the group consisting of H, CH3, CH2-CH3, C(CH3)3, COOH, CONH2 and C?CH; R2, R3, R4 and R5 are radicals independently selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkoxyl and (C1-C4)-alkyl; and R6 is a radical selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkoxyl, (C1-C4)-alkyl, R7, CH?CH—R7 and O—CH2—R7; wherein R7 is phenyl or phenyl mono- or independently di-substituted with F, Cl, Br, (C1-C3)-alkoxyl or (C1-C4)-alkyl, exhibit a similar chemotactic index to that of amygdalin (natural product whose chemotaxis profile is similar to that of peptide T) and, consequently, are useful for treating inflammatory and/or allergic dermatophathies, such as psoriasis, and are especially much less toxic than amygdalin.

Abstract: The present invention provides methods for preparing LPS antagonist lipodisaccharide B1287 and stereoisomers thereof, which compounds are useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock. Also provided are synthetic intermediates useful for implementing the inventive methods.

Abstract: The invention relates to substituted aromatic fluoroglycoside derivatives, and to the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to methods of lowering blood sugar and the treatment of type I and type II diabetes.

Abstract: A method of producing a radioactive-fluorine-labeled compound has a step of heating in a reaction vessel a mixture containing [18F] fluoride ions, a phase transfer catalyst, potassium ions, and water to evaporate water from the mixture (S10), and in the above step has a step of measuring a temperature of an outlet tube for discharging evaporated water during the heating of the reaction vessel (S12), and the evaporation process is finished at a timing determined based on the result of temperature measurement in the step (S12) of measuring the temperature (S16). Consequently, the amount of water present in the mixture can be controlled to an appropriate range and a stable yield can be achieved in the method of producing a radioactive-fluorine-labeled organic compound.

Abstract: 1-?-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-?-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.

Abstract: Sulfanyl-tetrahydropyran-based compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment of diseases and disorders such as diabetes and obesity are disclosed.

Abstract: It is an object of the present invention to provide a process for producing 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose in an industrially appropriate manner. The present invention provides a process for producing a 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose which comprises hydrogenating a compound represented by the formula (1) or formula (2) in the presence of a metal catalyst: wherein P1 and P2 independently represent a hydrogen atom or an acyl group, OP1 and OP2 may together form an acetal group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group; wherein X1 represents Br or I, P3 and P4 independently represent a hydrogen atom or an acyl group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group.

Abstract: The present invention discloses a process for the preparation of sucralose by the deacylation of trichlorosucrose-6-ethyl ester, wherein the deacylation reaction is performed in an alcohol solvent in the presence of organic base catalyst, so as to obtain sucralose.

Abstract: Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof The invention relates to substituted heterocyclic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation. The compounds are suitable for example as antidiabetics.

Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.

Abstract: The invention provides a method for the synthesis of an 18F-labelled product comprising deprotected of a protected 18F-labelled compound using a deprotection agent comprising a weak acid and wherein neutralisation and buffering of the deprotected product are carried out by the addition of a neutralisation agent. The deprotected product is buffered in a pH range suitable for subsequent autoclaving and formulation into an injectable radiopharmaceutical.

Abstract: Novel thiophene glycoside derivatives of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for their preparation are disclosed. The compounds are suitable, for example, as antidiabetics.

Abstract: Compounds having the formula (I): wherein A represents a group such as a cyclic group, R1 and R2 represent groups such as alkyl groups or hydroxymethyl groups, and n represents 1 or 2, or pharmacologically acceptable salts thereof or pharmacologically acceptable esters thereof have superior activity and stability, and are useful for the treatment and/or prevention of diabetes mellitus, or the like.

Abstract: This invention relates to a method for preparing a sucrose-6-ester.

Abstract: A process for the purification of sucralose in sucralose-containing feed streams is disclosed. The process includes multiple liquid-liquid extraction steps; optionally, a concentration step; multiple crystallization steps; optionally, a chromatography step; and various recycle steps.

Abstract: A process for the production of [18F]-TAFDG can produce [18F]-TAFDG in a high radiofluorination yield. A process for the production of an organic compound labeled with radioactive fluorine includes the steps of preparing a reaction solution containing [18F]fluoride ions, a phase transfer catalyst, potassium ions, 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-?-D-mannopyranose as a labeling precursor compound and a solvent, and giving a reaction condition to the reaction solution to obtain 1,3,4,6-tetra-O-acetyl-2-[18F]fluoro-2-deoxyglucose, in which the solvent contains water.

Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

Abstract: Fire extinguishing compositions and methods of extinguishing a fire comprising compounds of formula (I) where Rf is a fluorocarbon group.

Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.

Abstract: A process is described for acid mediated deacylation of acyl derivatives of chlorinated sucrose compounds comprising generating a predominantly organic phase condition in a process stream requiring deacylation treatment but allowing an optimum quantity of water content which is capable of participating in a hydrolysis reaction; this objective being achieved for the said process stream by following steps of (a) adding to it alcoholic solvent in an amount such that water content of final reaction mixture is between about 5% to 0.5%, (b) adding acid chloride to the same (c) adjusting the pH to 4 by adding acetate buffer in a methanolic solution and, (d) stirring the reaction until deacylation is complete. This process can be integrated in a process for production of a chlorinated compound, involving use of dimethylformamide during the process, to achieve deacylation without decomposition of dimethylformamide as well as the chlorinated sucrose product.

Abstract: The present invention discloses a process for the preparation of sucralose by the deacylation of trichlorosucrose-6-ethyl ester, wherein the deacylation reaction is performed in an alcohol solvent in the presence of organic base catalyst, so as to obtain sucralose.

Abstract: The present application discloses a method for crystallizing sucralose, which uses an alcohol solvent or a mixed solvent of alcohol and other solvent(s) in the crystallization of sucralose.

Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.

Abstract: One embodiment of the present invention is a process of making sucrose-6-ester from sucrose by transesterification in the presence of a solid super acid catalyst such as SO42?—TiO2/Al2O3 or SO42?—TiO2. The sucrose-6-acetate is then chlorinated to afford sucralose-6-acetate, using BTC or thionyl chloride. Sucralose-6-acetate is converted into TPSGA for the purpose of purification. TPSGA is de-esterified by sodium methoxide/methanol or sodium ethoxide/ethanol to give sucralose.

Abstract: Novel aromatic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted aromatic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and process for their preparation. The compounds are suitable for example as antidiabetics.

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: Novel thiophene glycoside derivatives of the formula I: in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for their preparation are disclosed. The compounds are suitable, for example, as antidiabetics.

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

Abstract: 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.