Abstract: The present application is generally directed to microfluidic devices and methods for the achievement and assessment of chemical and radiochemical purity of (microfluidic) radio-synthesis products. More particularly, the current application relates to systems for purification and analysis of radiochemical products yielded by microfluidic synthesis devices.

Abstract: Methods of treating glioblastoma and pancreatic cancer are provided by the administration of a therapeutically effective amount of a iodo-hexose compound to a subject in need thereof. The subject disclosure includes methods of treating glioblastoma and pancreatic cancer comprising the administration of a therapeutically effective amount of a 2-deoxy-2-iodo-D-hexose compound including 2-deoxy-2-iodo-D-mannose, 2-deoxy-2-iodo-D-glucose, 2-deoxy-2-iodo-D-galactose, and/or 2-deoxy-2-iodo-D-talose to a subject in need thereof.

Abstract: The present invention provides nitrogen-containing fused cyclic derivatives represented by the following general formula or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula one of R1 and R4 represents a group represented by the following general formula (S) (in which R5 and R6 represent H, OH, a halogen atom, etc.; Q represents an alkylene group etc.; and ring A represents an aryl group etc.), and the other represents H, OH, an amino group, etc.; R2 and R3 represent H, OH, an amino group, a halogen atom, and an optionally substituted alkyl group, etc.; A1 represents O, S, etc.

Abstract: Methods and apparatus for facilitating the synthesis of compounds in a batch device are presented. Application of the batch type microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the selective introduction of multiple reagents via an enhanced rotary flow distribution valve through a single inlet port of the synthetic device. The sequential introduction of multiple reagents through a single inlet port allows an optimal delivery of highly concentrated reagents into the reactor and facilitates the synthesis of the desired products with a minimal loss of materials during transfers, which is critical to the synthesis of radiolabeled biomarkers.

Abstract: The invention relates to a dose of 2.5 mg of the pentasaccharide methyl O-(2,3,4-tri-O-methyl-6-O-sulfo-?-D-glucopyranosyl)-(1?4)-O-(2,3-di-O-methyl-?-D-glucopyranosyl uronic acid)-(1?4)-O-(2,3,6-tri-O-sulfo-?-D-glucopyranosyl)-(1?4)-O-(2,3-di-O-methyl-?-L-idopyranosyl uronic acid)-(1?4)-2,3,6-tri-O-sulfo-?-D-glucopyranoside or a pharmaceutically acceptable salt thereof for use in therapy, in particular for the treatment of venous thromboembolic events in patients with deep venous thrombosis.

Abstract: A process for the preparation of Pentosan polysulfate sodium comprising a step of purifying depolymerized crude Pentosan polysulfate sodium by filtration through NF membrane system.

Abstract: A method for the manufacture of an agarose separation gel: The method is characterized in comprising the steps of: i) providing a solution of agar, and ii) one, two or more substeps (ii.A, ii.B, ii.C etc) which each comprises desulphating thereby transforming agar to agarose having a degree of substitution of sulphate groups that is at most 75% of the degree of substitution of sulphate groups in native agar, iii) gelling the dissolved agar prior to step (ii) and/or securing so that the desulphated agar is in g form at least after one or more of the substeps of step (ii), and imperatively after step (ii). An agarose separation gel that exhibits a. a plurality of methoxy groups each of which are at the same position as in native agar and with a degree of substitution in the range of 1-100% of the degree of substitution of native agar, and b. sulphate groups with a degree of substitution which is <75% of the degree of substitution for sulphate groups in native agar.

Abstract: The invention is directed to compounds of the formula (I) described herein, a pharmaceutically acceptable salt thereof, or a prodrug thereof, and pharmaceutical compositions and methods of treatment.

Abstract: The present invention relates to a method for improving stability of non fluoridated sugar derivatives, and in particular glucose derivatives such as 1,3,4,6-tetra-O-acetyl-2-O-trifluoromethanesulfonyl-?-D-mannopyranose which are used as precursors for production of radiofluoridated sugar derivatives for use in in vivo imaging procedures such as positron emission tomography (PET). The method comprises storing the non fluoridated sugar derivative in an organic solvent. The resultant formulations of the non fluoridated sugar derivative and cassettes for automated synthesis apparatus comprising the same are also claimed.

Abstract: Radiolabeled tracers for sodium/glucose cotransporters (SGLTs), their synthesis, and their use are provided. The tracers are methyl or ethyl pyranosides having an equatorial hydroxyl group at carbon-2 and a C1 preferred conformation, radio-labeled with 18F, 123I, or 124I, or free hexoses radiolabeled with 18F, 123I, or 124I. Also provided are in vivo and in vitro techniques for using these and other tracers as analytical and diagnostic tools to study glucose transport, in health and disease, and to evaluate therapeutic interventions.

Abstract: The invention concerns a C-glycoside compound of formula (I); wherein: n is equal to 1 or 2; Y represents H or halogen; X is an alkyl chain bearing at least one amino, amide, acid, ester, carbonyl, alcohol, aryl function or a carbonyl, ester amide, amino, alcohol group; the R's, identical or different, represent a OH or OR? group where R? is an alkyl, benzyl, benzoyl, acetyl, pivaloyl, trialkylsilyl, tertiobutyldiphenylsilyl group or one or more sugars; R1 represents OR?, NR?R??, N3, or a phthalamide with R? and R??, identical or different, represent H or an alkyl, aryl, benzyl, benzoyl, acetyl, alkoxycarbonyl, allyloxycarbonyl, benzyloxycarbonyl group; R2 represents H or halogen or a OH, OR, NR?R?? or N3 group, as well as derivatives thereof in physiologically or pharmaceutically acceptable base, mineral or organic acid-addition salt, hydrate or solvate form.

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

Abstract: Chemical compounds, being the alkyl sulfate of sulfated saccharides, particularly, dextrin, dextran, and cyclodextrin, and pharmaceutical compositions containing these compounds. The compounds of the invention provide antiviral activity, particularly in the treatment and prevention of sexually-transmitted diseases. Methods of treating viral infection and preventing viral transmission include administration include administration of the compounds of the invention orally, topically, subcutaneously, by muscular injection, by intraperitoneal injection and by intravenous injection.

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 compound of the formula I A method is also provided for treating diabetes and related diseases employing the above compound alone or in combination with another therapeutic agent.

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

Abstract: Dithiocarbonate-containing macromer that contain biodegradable or water-soluble segments, and polymers derived from the reaction of these dithiocarbonate-containing macromers, are disclosed. The polymers derived from these dithiocarbonate-containing macromers with biodegradable or water-soluble segments are useful in medical and pharmaceutical applications.

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: 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: A process of azeotropic removal of dimethylformamide, abbreviated as DMF, from a process stream containing DMF requiring its removal, is described wherein the said Process Stream being obtained in a process for preparation of 4,1?,6? trichlorogalactosucrose, abbreviated as TGS, or TGS-6-ester including TGS-6-acetate or TGS-6-benzoate, comprising steps of (a) evaporation of the said process stream under reduced pressure to a concentrate to effect removal of a part of DMF azeotropically, (b) diluting the concentrate obtained at the end of step (a.) of this claim with water, preferably to about 5 to 10 times the volume of the said concentrate, and (c) repeating the cycles of evaporation under reduced pressure and dilution with water for more number of times until content of DMF in the concentrated mass is reduced to 0.5% or less of the concentrate.

Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: Methods and devices for a fully automated synthesis of radioactive compounds for imaging, such as by positron emission tomography (PET), in a fast, efficient and compact manner are disclosed. In particular, the various embodiments of the present invention provide an automated, stand-alone, hands-free operation of the entire radiosynthesis cycle on a microfluidic device with unrestricted gas flow through the reactor, starting with target water and yielding purified PET radiotracer within a period of time shorter than conventional chemistry systems. Accordingly, one aspect of the present invention is related to a microfluidic chip for radiosynthesis of a radiolabeled compound, comprising a reaction chamber, one or more flow channels connected to the reaction chamber, one or more vents connected to said reaction chamber, and one or more integrated valves to effect flow control in and out of said reaction chamber.

Abstract: Iduronic acid (IdoUA)-free heparan sulfate (HS)-like compounds are provided. Also provided are methods of synthesizing IdoUA-free HS-like compounds. The methods can include providing at least one O-sulfotransferase (OST) enzyme and a reaction mixture comprising 3?-phosphoadenosine 5?-phosphosulfate (PAPS); and incubating a polysaccharide substrate with the at least one OST and the reaction mixture, whereby the HS-like compounds are synthesized. Also disclosed are methods of synthesizing a library of HS-like compounds and methods of determining the mechanism of activity of HS-like compounds.

Abstract: The present invention provides a process capable of industrially producing 5-deoxy-L-arabinose, important as a raw material for the production of sapropterin useful as a therapeutic agent for atypical hyperphenylalaninemia, satisfactorily efficiently even with a simple production apparatus. Provided is the process for producing 5-deoxy-L-arabinose characterized by including: reacting L-rhamnose with a C11-16 straight chain alkyl mercaptan compound in the presence of an acid catalyst to prepare L-rhamnose dialkylmercaptal; subjecting then the obtained compound to an oxidation reaction to prepare a sulfonyl derivative; and subjecting then the sulfonyl derivative to a carbon-reduction reaction to prepare 5-deoxy-L-arabinose.

Abstract: A process for the production of [18F]fluoro-2-deoxyglucose can produce [18F]fluoro-2-deoxyglucose in a high and stable yield of synthesis. A process for the production of a compound labeled with radioactive fluorine includes the preparing a reaction solution by adding, under a hermetic condition, TATM and an inert organic solvent to a mixture containing [18F]fluoride ions, a phase transfer catalyst and potassium ions, giving a reaction condition to the reaction solution under a hermetic condition to obtain [18F]-TAFDG, and subjecting the obtained [18F]fluoro-2-deoxyglucose to a deprotection process and, optionally, to a purification process to obtain [18F]fluoro-2-deoxyglucose.

Abstract: The invention is directed to compounds of the formula (I) described herein, a pharmaceutically acceptable salt thereof, or a prodrug thereof, and pharmaceutical compositions and methods of treatment.

Abstract: New microfluidic devices, useful for carrying out chemical reactions, are provided. The devices are adapted for on-chip solvent exchange, chemical processes requiring multiple chemical reactions, and rapid concentration of reagents.

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: Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

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 invention relates to novel amphoteric polysaccharide compounds containing sulfonate function(s) corresponding to the formula (I) in which P represents a polysaccharide chain; X, Y and Z each represent a linear or branched, saturated or unsaturated, optionally hydroxylated C1-C12 divalent hydrocarbon-based group optionally comprising at least one ether and/or amine function in the hydrocarbon-based chain, or a group —Si(R)2—[O—Si(R)2]q-A-; r is 0 or 1; An represents an anionic group chosen from formula (II) CAT represents a quaternary ammonium group or a cationic polymer chain obtained by grafting and polymerization of ethylenic monomers bearing a quaternary ammonium function, Sulfo represents a sulfonic or sulfonate group; and n, m and p are such that the total degree of substitution of the polysaccharide does not exceed 2. The invention also relates to compositions comprising them and to their use in cosmetics.

Abstract: Processes for isolation and purification of enantiomerically enriched compositions comprising tramadol and topiramate, and also for the subsequent isolation of 1S,2S-tramadol hydrochloride, are disclosed herein.

Abstract: In one embodiment of the invention a method to prepare sucralose-6-acylate through chlorinating sucrose-6-acylater by BTC in the process of sucralose preparation is disclosed. In this embodiment a Vilsmeier reagent is firstly prepared below 0° C. by dissolving BTC in DMF or in component solvent, containing DMF, toluene, dichloroethane, chloroform and carbon tetrachloride. Consequently, sucrose-6-ester was chlorinated by Vilsmeier reagent. BTC can also be dissolved in one or several organic solvent such as toluene, dichloroethane, chloroform and carbon tetrachloride, and added to a DMF solution of sucrose-6-acylate for chlorination. Sucralose was prepared through de-esterifying the obtained sucralosed 6-ester using sodium methoxide/methanol or sodium ethoxide/ethanol.

Abstract: Novel antenna polymers characterized by a polymeric background of a biodegradable water soluble polymer and chromophores chemically bonded to the polymeric background have been found to be useful as photocatalysts in aqueous media. On completion of the desired photochemical reaction, the residual medium can safely be discharged to the natural environment as the catalyst residues undergo biodegradation to form environmentally harmless products.

Abstract: The present invention relates to the synthesis of a haemocompatible polymer, consisting of a polyurethane bound covalently to sulphated hyaluronic acid. These sulfated derivatives have anticoagulative, non-thrombogenic, antiviral and anti-inflammatory properties. They also have the ability to inhibit platelet adhesion, aggregation and activation. The invention is particularly advantageous in resisting the enzyme hyaluronidase, therefore ensuring anti-coagulant activities for longer periods of time when compared to similar compounds. This biocompatible polymer material is well suited for surgical or other medicinal uses.

Abstract: Positron emitting compounds and methods of their production are provided. The compounds have the formula: (F)m G (R)n wherein each R is a group comprising at least one carbon, nitrogen, phosphorus or sulfur atom and G is joined to R through said carbon, nitrogen, phosphorus or sulfur atom; G is silicon or boron; m is 2 to 5 and n is 1 to 3 with m+n=3 to 6 when G is silicon; m is 1 to 3 and n is 1 to 3 with m+n=3 to 4 when G is boron; and wherein the compound further comprises one or more counterions when the above formula is charged; and wherein at least one F is 18 F.

Abstract: A glycopolymer composition is provided comprising glycopolymer molecules having a polymer backbone; a first pendent unit comprising a linking group connected to said polymer backbone and a saccharide moiety connected to said linking group, optionally a second pendent unit; a phenyl ring at a first end of the polymer backbone; and a cyanoxyl group at the second end of the polymer backbone, useful as intermediates for making bioactive glycopolymers which bind to bioactive molecules, viruses, cells and substrates for protein separation, cell culture, ad drug delivery systems, as well as in targeting for treatment of wound healing and other pathological conditions.

Abstract: The methods of the present invention prepare carrageenan products from processed seaweed material having a solids content of less than 25% by weight solids, using shear stress treatment. The carrageenan products comprise at least about 60% by weight of carrageenan and at least about 2% by weight of acid insoluble material. The carrageenan products of the present invention are useful as components in food products, such as, dairy products, meats, and dessert gels as well as non-food products, such as, toothpaste formulations, cosmetics, paints, films and delivery capsules.

Abstract: The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with ?-cyclodextrin in an aqueous complexation medium comprising ?-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with ?-cyclodextrin and its inclusion complexes.

Abstract: The invention relates to a series of polyglycoside derivatives that contain water-soluble sulfosuccinate groups introduced into the molecule by reaction with the hydroxyl groups present in the starting polyglycoside molecule, with the chloro material. 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.

Abstract: Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: The invention concerns the use, in a composition for treating textile fiber articles in aqueous or moist medium, of an amphoteric polysaccharide, whereof the native skeleton is a polysaccharide consisting of a main chain comprising anhydrohexose units and branches comprising at least a neutral or anionic anhydropentose and/or anhydrohexose unit, the anhydrohexose and/or anhydropentose units being substituted of modified by groups bearing at least a (potentially) anionic load and/or at least a (potentially) cationic load, the degree of substitution or modification by the set of said groups bearing (potentially) anionic loads ranging between 0.01 and less than 3, with a ratio of the number of (potentially) anionic charges over the number of (potentially) cationic loads ranging between 99.5/0.

Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids, which include a portion or analogue thereof) linked to a carbohydrate or glycomimetic.

Abstract: In a reaction system having at least two liquid-liquid interfaces between an organic phase of raw material containing a compound(s) to be separated and an aqueous phase of an aqueous solution of inclusion-complexing agent and between that aqueous phase and an organic phase(s) of extraction solvent(s), the compound(s) to be separated is entrapped into the aqueous phase through formation of an inclusion complex(es) of the inclusion-complexing agent with the compound(s), while the compound(s) is entrapped into the organic phase(s) of extraction solvent(s) through dissociation of said inclusion complex(es). The foregoing operation is performed using, for example, a squarish U-shaped tube or an H-shaped tube with bottom plates. Preferred examples of inclusion-complexing agent include highly water-soluble branched cyclodextrins.

Abstract: The present invention provides for a method for treatment and prevention of Type II Diabetes Mellitus and its complications comprising the step of administering to a patient a therapeutically-effective amount of Rhamnan Sulphate, its functional analogs, or its physiologically acceptable salts, in therapeutic proportions. Anticoagulation activity in the blood plasma of a patient is not appreciably increased.

Abstract: The present invention relates to an inclusion complex of Rifampicin and cyclodextrin (CD) that can be used as an anti-tubercular drug. The present invention also relates to a process for synthesizing inclusion complexes of the anti-tubercular drug, Rifampicin, with ?-CD (?-cyclodextrin) and HP-?-CD (2-hydroxy propyl cyclodextrin) and characterization of these inclusion complexes.

Abstract: A composition for sweetening ingestable solids or liquids. The composition is compressed and comprises less than about 7.5 weight-% sucralose and one or more diluents. The composition is compressed at a pressure of greater than 2 pounds per square inch. A method of forming the composition and a system for delivering the composition are also provided.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

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.