Abstract: A chlorinating agent such as a chloroiminium species is used to remove or neutralize tertiary acetamide present as a contaminant in a tertiary formamide solvent. Tertiary formamide solvent purified or treated in this manner can be used as a reaction vehicle for the chlorination of sucrose-6-acylates, thereby improving the yields of the desired sucralose-6-acylate (an intermediate in the production of sucralose).

Abstract: The present application describes compounds of Formula I and Formula IA and as disclosed herein, that are useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: Novel utilization of sucralose which is a high intense sweetener. Compositions containing sucralose including: sweetening compositions having excellent sweetness qualities based on the characteristics of sucralose; foods with a masked unpleasant smell and unpleasant taste; performance food compositions (viscous food compositions, gel food compositions, emulsified food compositions); foods with improved flavors; preservatives and foods with improved quality of taste; and flavor compositions with improved flavors. Novel utilization of sucralose as a sweetener improver, a masking agent for unpleasant smell/unpleasant taste, a flavor improver, a function improver (viscosity, gelling properties, emulsification properties), a taste characteristic improver, and a flavor improver/enhancer.

Abstract: The present invention provides a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil, comprising fucoidan or a fucoidan-containing material; a method for inhibiting side effects of drug therapy for colorectal cancer using 5-fluorouracil, which comprises administering fucoidan or a fucoidan-containing material to a colorectal cancer patient; and use of fucoidan or a fucoidan-containing material for the production of a side effect inhibitor of drug therapy for colorectal cancer using 5-fluorouracil.

Abstract: A microfluidic reactor has a reaction chamber which is configured as an annular channel. It is provided that segments have been formed in the annular channel such that a sequence of inlets and outlets (allows an alternation between the process fluids (A and B) to take place. Furthermore, particles which circulate in the annular channel and can be used, for example, for the adsorption and desorption of ions may be provided in the annular channel. In this way, the ions concerned can, for example, be extracted from the process fluid (A) and transferred into the process fluid (B). In a method, the reactor can be used for example for the purpose of obtaining 18F? ions from water enriched therewith and feeding them to a solvent such as acetonitrile. In the further course of the method, the 18F? ions can be used for producing a radiopharmaceutical (for example FDG).

Abstract: Disclosed is a medium-molecular weight fucoidan which can be used in treating and/or preventing proliferative diseases, in particular, cancer. Specifically disclosed are a medium-molecular weight fucoidan, a method for producing the same, a medicinal composition containing the same, and use of the medium-molecular weight fucoidan in producing a drug for treating and/or preventing preventing proliferative diseases, in particular, cancer. The aforesaid medium-molecular weight fucoidan has an average molecular weight of about 6,000 to about 2,000,000, preferably an average molecular weight of about 40,000 to about 330,000, more preferably an average molecular weight of about 40,000 to about 244,000, and still more preferably an average molecular weight of about 80,000 to about 200,000.

Abstract: Provided are a sulfated C-glycoside which is a novel compound serving as a precursor of chafuroside and chafuroside analogs; a method for efficiently producing the sulfated C-glycoside; and a method for efficiently producing chafuroside and chafuroside analogs using said sulfated C-glycoside. A sulfated C-glycoside represented by general formula (A1) or (B1) [wherein R1, R2 and R3 independently represent each a hydrogen atom or an OH group] is obtained by extracting tea leaves or tea tannins with water, a lower alcohol solvent having 1 to 3 carbon atoms or a liquid mixture comprising the same. Alternatively, the sulfated C-glycoside is produced by reacting a flavone C-glycoside such as isovitexin or vitexin with a sulfate group-introducing agent to thereby sulfate the flavone C-glycoside. By heating the sulfated C-glycoside thus obtained, chafuroside and chafuroside analogs are efficiently produced.

Abstract: Granular sucralose-containing particles are produced by the methods of the invention, which involve coating sucralose from solution to form granules with this coated sucralose on an outer region thereof. The granules may incorporate agglomerated sucralose particles, with the solution-coated sucralose adding mass and generally resulting in a granule having a relatively smoothed and rounded. The granules have good flow properties, are low dusting, and resist caking. Methods of making the granules involve spraying an aqueous sucralose solution onto a fluidized bed of sucralose particles, followed by drying to form the granules.

Abstract: The present invention relates to pharmaceutical compositions containing fucoidan for stimulating and activating osteogenesis. The compositions according to the present invention contain fucoidan as an active ingredient to increase the activities of alkaline phosphatase and the production of osteocalcin, and to increase the production of bone morphogenetic protein (BMP-2).

Abstract: The present invention provides: a method for synthesizing a halogen-substituted saccharide from a leaving group-substituted saccharide in a short-time and continuously; a reaction composition; and a device for synthesis of same, i.e., the method being for synthesizing a halogen-substituted saccharide from a leaving group-substituted saccharide by a halogen-substituted saccharide synthesis reaction using a subcritical fluid or a supercritical fluid as the reaction solvent; the reaction composition of the same being an aqueous solution of halogen-substituted saccharide; and the device for synthesis being a device for producing the same, the method being for producing a halogen-substituted saccharide with a subcritical fluid or a supercritical fluid at a temperature of 100 to 400° C. and a pressure of 0.

Abstract: Low molecular weight sulphated L-fucose polysaccharide fraction having a molecular weight ranging from 11 to 30 kDa when measured with TEST A, a sulphate content ranging from 10 and 50% w/w relative to the total weight of the fraction, a fucosis content ranging from 30 and 70% w/w relative to the total weight of the fraction, and a polydispersity index ranging from 1 and 2, wherein the fraction is obtainable by free radical depolymerisation of a crude fucan of vegetal origin; process for manufacturing same; pharmaceutical composition and medicament containing same and their use for inhibiting neovascularisation.

Abstract: The present invention relates to low molecular weight sulfated galactans, obtained from algae, particularly genus Botryocladia, preferably species Botryocladia occidentallis, which have no effect on the factor XII activation of the clotting cascade, having antithrombotic heparinoid activity. The present invention also refers to a pharmaceutical composition comprising said sulfated galactans and the use thereof, as heparin substitute, in the treatment or prophylaxis of arterial or venous thrombosis in humans and animals. Furthermore, the present invention provides a method of extraction of the said sulfated galactans.

Abstract: Aspects of the invention include methods for enhancing blood coagulation in a subject. In practicing methods according to certain embodiments, an amount of a non-anticoagulant sulfated polysaccharide (NASP) is administered to a subject to enhance blood coagulation in the subject. Also provided are methods for preparing a NASP composition having blood coagulation enhancing activity. Compositions and kits for practicing methods of the invention are also described.

Abstract: Various pentosan polysulfate (PPS) formulations useful for treatment of osteoarthritis, interstitial cystitis, and other conditions of mammals are provided. These formulations showed improved resistance to degradation and discoloration and improved stability at physiological pH, even after sterilization. Capillary electrophoresis analysis of these formulations indicates that various formulations remain stable under conditions that caused degradation of PPS in prior art PPS formulations.

Abstract: A novel crystal form of 1-(?-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.

Abstract: The present invention discloses a sulfated derivative of polysaccharide extracted from gastrodia elata BL., the preparation method thereof and the use thereof in preparing antineoplastic medicaments, wherein, the gastrodia elata polysaccharide has the following structure: wherein, x and y are each an integer, and x+y=16, “n” is and integer, and the mean molecular weight of the polysaccharide from gastrodia elata is estimated as 2.8×105, the specific rotation of the polysaccharide is +95° in a 0.5 mg/mL aqueous solution thereof; the sulfated position is mainly at 6-hydroxy of the gastrodia elata polysaccharide, with mean molecular weight of 6.5×104 and a specific rotation of +150.0° in a 0.5 mg/mL aqueous solution thereof.

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: Glucopyranosyl-substituted benzene derivatives of general formula I where the groups R1 to R6 as well as R7a, R7b, R7c are defined herein and the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Abstract: Aspects of the invention include methods for enhancing blood coagulation in a subject. In practicing methods according to certain embodiments, an amount of a non-anticoagulant sulfated polysaccharide (NASP) is administered to a subject to enhance blood coagulation in the subject. Also provided are methods for preparing a NASP composition having blood coagulation enhancing activity. Compositions and kits for practicing methods of the invention are also described.

Abstract: This invention relates to compounds represented by formula (I): wherein the variables are defined as herein above, which are useful for treating diseases and conditions mediated by the sodium D-glucose co-transporter (SGLT), e.g. diabetes. The invention also provides methods of treating such diseases and conditions, and compositions etc. for their treatment.

Abstract: A method for isolating sulphated glycosaminoglycans washes a mechanically cleaned tissue, exposes tissue in a solution of 0.1M phosphate pH 5.8-6.0 buffer heated to a temperature of 65° C. for 30 minutes, overcooks the tissue in activated 0.1-0.4% papain at 65° C. for 6-24 hours, cools the papain digest to 4° C., removes fats and undigested tissue residues, selectively isolates the sulphated glycosaminoglycans for 4-10 hours on a solid carrier, obtained from bone tissue collagen with particle sizes ranging from 0-01 to 0.35 cm3, washes the carrier with 0.05-0.1 N-hydrochloric acid, degreases and eluates the carrier with a solution of 0.6-0.15 N-mineral salt in 0.8 N-acetic acid or in 0-01-0-025 N-alkali liquor, precipitates the sulphated glycosaminoglycans with ethanol, centrifuges with 1500 r.p.m. for 15 minutes at a temperature of 4° C., washes the precipitate with ethanol or acetone, and dries and sterilizes the precipitate.

Abstract: Methods and apparatus for facilitating the synthesis of compounds in a nonflow-through device are presented. Application of the nonflow-through methods and microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the introduction of a pressurized gas through a tangential slit into a vortex reactor of the nonflow-through device, while one or more liquids are delivered to the reaction chamber through the same or different inlet ports. The introduction of the pressurized gas produces a cyclonic motion of the mixture within the reactor. Such a mechanism may be used to facilitate the evaporation of various liquids within the reactor at lower temperatures, thus reducing the production of unwanted byproducts that are associated with the use of high temperatures. In addition, thorough mixing of various liquids may be effected rapidly while allowing chemical reactions to take place efficiently within the vortex reactor.

Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Abstract: A method for the preparation of a sucrose-6-ester is disclosed. In a first step of the method, sucrose in a polar aprotic solvent is reacted with an organotin-based acylation promoter. The water of reaction is removed at a temperature that does not exceed about 80° C. In one aspect, the water is removed by distillation of part of the polar aprotic solvent at reduced pressure. In a second step, a carboxylic acid anhydride is added. In one aspect, the resulting reaction mixture is maintained at a temperature of 10° C. or less for a period of time sufficient to produce a sucrose-6-ester. The sucrose-6-ester can be converted to sucralose.

Abstract: A process for the production of sucrose-6-ester is disclosed. The process includes, in order, the steps of: (a) providing a first reaction mixture including sucrose, a reaction vehicle, and an organotin-based acylation promoter; (b) removing water from the first reaction mixture to afford a second reaction mixture that is substantially free from water; and (c) adding a carboxylic acid anhydride to the second reaction mixture to afford a third reaction mixture, thereby producing a sucrose-6-ester; wherein: during step (b), the removing of water includes distillation of water with the reaction vehicle using an apparatus supplying a heat flux of from 500 to 25,000 BTU/hrft2 (1577 to 78865 W/m2) selected from the group consisting of wiped film evaporators, agitated thin film evaporators, falling film evaporators and rising film evaporators.

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: The present invention provides for the use of iota- and/or kappa-carrageenan for the manufacture of an antiviral pharmaceutical composition for the prophylaxis or treatment of a pathological condition or disease caused by or associated with an infection by a respiratory virus selected from the group consisting of orthomyxovirus, paramyxovirus, adenovirus and coronavirus. The present invention further provides for the use of fucoidan, in particular of high molecular weight fucoidan, for the manufacture of an antiviral pharmaceutical composition for the prophylaxis or treatment of a pathological condition or disease caused by or associated with an infection by a respiratory virus selected from the group consisting of orthomyxovirus and paramyxovirus.

Abstract: This invention relates to a compound of generic formula (I): (I) as well as a pharmaceutically acceptable salt thereof a tautomer, optical isomer or a mixture of optical isomers in any proportion, in particular a mixture of enantiomers, and particularly a racemate mixture, in particular for use thereof as a drug, notably in the treatment of diabetes.

Abstract: The invention discloses a method for improving the yield of sucralose, including reacting sucrose to produce sucrose-6-acetate in the existence of an azo reagent as a catalyst and acetic acid as an acylating agent in a proper solvent; then reacting sucrose-6-acetate with a proper chlorinating agent to produce sucralose-6-acetate in a non-proton polar solvent with TCA as a catalyst; and at last, alcoholyzing sucralose-6-acetate in KOH/methanol to obtain sucralose.

Abstract: Tetrasubstituted glucopyranosylated benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Abstract: Glucopyranosyl-substituted difluorobenzyl-benzene derivatives of general formula (I) as defined according to claim 1, including the tautomers, the stereoisomers thereof, the mixtures thereof and the salts thereof. The compounds according to the invention are suitable for the treatment of metabolic disorders.

Abstract: We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.

Abstract: The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of primary or secondary organofluoro compound by reacting fluorine salt containing radioactive isotope fluorine-18 with primary or secondary alkyl halide or primary or secondary alkyl sulfonate in the presence of alcohol of Chemical Formula 1 as a solvent to obtain high yield of organofluoro compound. Synthesis reaction according to the present invention may be carried out under mild condition to give high yield of the organofluoro compounds and the reaction time is decreased, and thereby is suitable for the mass production of the organofluoro compounds.

Abstract: Disclosed is a hetero-bifunctional ligand for use in inducing internalization of a target receptor. The hetero-bifunctional ligand includes a target receptor-binding agent that specifically binds the target receptor linked to an internalizing receptor-binding agent that specifically binds to an internalizing receptor, where the two binding agents are non-identical. Also disclosed is a method of inducing the internalization of a target receptor on a cell. The method includes contacting a cell with a hetero-bifunctional ligand, where binding of the hetero-bifunctional ligand induces internalization of a target receptor of the cell. Also disclosed a method of treating a disease or condition associated with a target receptor using the disclosed hetero-bifunctional ligand and pharmaceutical compositions including a hetero-bifunctional ligand.

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: 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: The present invention is directed to fructose-based radiopharmaceuticals, pharmaceutical compositions comprising same, precursors and methods for preparing same, and methods of using same for diagnostic imaging of cancer cells and non-imaging tracer studies.

Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.

Abstract: The invention relates to methods for processing [18F]-fluoride target water using a solid-support bound Cryptand of formula (I) and to apparatus for performing such methods. The resultant [18F]-fluoride is useful for preparation of radiopharmaceuticals by nucleophilic fluorination, specifically for use in Positron Emission Tomography (PET).

Abstract: The present application provides compositions comprising hyaluronic acid having low levels of functional group modification, mixtures formed by controlled reaction of such lightly modified hyaluronic acid with suitable difunctional or multi-functional crosslinkers, and hydrogel precursor compositions and the resulting hydrogels. The compositions are lightly cross-linked and possess low pro-inflammatory properties when injected in vivo, and can be used as, for example, medical devices, biomedical adhesives and sealants, and for localized delivery of bioactive agents, among other uses.

Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

Abstract: A toothpaste composition comprising a surfactant, an abrasive, a humectant, triglyceride oil, a carboxylated polysaccharide, and a sulphated or sulphonated polysaccharide and the use of a sulphated or sulphonated polysaccharide, in particular a carrageenan, to improve the in-use foam quality of a toothpaste.

Abstract: A chromatographic process of DMF removal from an aqueous composition is described comprising its loading on a column of hydrophobic fixed bed adsorbent and eluting out DMF with an aqueous alkaline buffer. This method is useful to remove DMF as a process of general application wherever simultaneous removal and isolation of DMF is desired from an organic molecule which is not an organic solvent, is soluble in DMF. This method can be used for simultaneous removal of DMF from reaction mixtures and isolation of Trichlorogalactose (TGS) or TGS-6-acetate in a process of production of TGS.

Abstract: The present invention relates to a biomaterial for cell or tissue culture, based on a polymeric carrier, which contains at least one crosslinkable hydrophilic polymer. The polymer is functionalized with groups that are selected from maleimide, vinylsulfonic, acrylate, alkyl halide, azirine, pyridyl, thionitrobenzene acid groups, or arylating groups. The invention relates further to a method of production of said biomaterial, and the use of particular functionalizing groups for the production of a biomaterial for the cultivation of tissue and/or cells. The biomaterial can have biofactors that exert a particular action on cells.

Abstract: The present invention relates to a process to prepare sucralose.

Abstract: The invention generally relates to systems and methods for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using a bifunctional compound that inhibits both fatty acid metabolism and glycolysis. Thus, the invention links a fatty acid metabolism inhibitor to a glycolysis inhibitor. More particularly, the invention provides novel bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a glucose derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of 2-deoxy-D-glucose.

Abstract: A process for the selective binding of an aggregating abnormal form of a protein in the presence of the nonaggregating normal form of the protein, including contacting under selective binding conditions a material containing both the abnormal and normal forms with a binding agent which is a polyionic material having a binding avidity for the aggregating form of the protein as present in the sample.

Abstract: The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.

Abstract: Granular sucralose-containing particles are produced by the methods of the invention, which involve coating sucralose from solution to form granules with this coated sucralose on an outer region thereof. The granules may incorporate agglomerated sucralose particles, with the solution-coated sucralose adding mass and generally resulting in a granule having a relatively smoothed and rounded. The granules have good flow properties, are low dusting, and resist caking. Methods of making the granules involve spraying an aqueous sucralose solution onto a fluidized bed of sucralose particles, followed by drying to form the granules.

Abstract: The present invention relates to compounds of the following general formula (I) their process of preparation and their use in the treatment or the prophylaxis of tuberculosis.