Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: The invention relates to the modification of hyaluronic acid by means of a protonized DTPA bis anhydride in a non-basic polar aprotic solvent in absence of any external base to form crosslinked products. The reaction runs via the formation of a complex and the acylating agent is the hyaluronan co-cation itself, i.e. protonized DTPA bis anhydride. The final crosslinked derivative (linker) comprises three carboxylic groups and three tertiary amines which are capable of complexing various metals effectively. The final DTPA crosslinked hyaluronic acid may also be hydrophobized by means of mono, bis or tris functional alkylating agents.

Abstract: Provided are thieno[3,4-d]pyrimidin-7-yl and furo[3,4-d]pyrimidin-7-yl ribosides, riboside phosphates and prodrugs thereof as well as intermediates and methods of preparation. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.

Abstract: Provided are imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract: Pro-drugs of all non-steroidal anti-inflammatories with free acid function derivatized with an ester group, which have the general structural formula given below (I) where A is: aspirin, diflunisal, benorylate, ibufenac, diclofenac, indomethacin, sulindac, ketorolac, ibuprofen, naproxen, ketoprofen, fenoprofen, flurbiprofen, mefenamic acid, meclof enamic acid, flufenamic acid, niflumic acid, and where in the ester group R can be a sugar (amongst which aldose, or ketose pentose, or esose selected from a group of D- and L-enantioiuers of ribose, glucose, galactose, mannose, arabinose, xilose, allose, altrose, gulose, idose and talose and substituted derivatives thereof, such as glucosamine, galactosamine, N-acetyl glucosamine, N-acetyl galactosamine, N-acetyl ribosamine), a disaccharide, a trisaccharide or an oligosaccharide.

Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract: Described is use of a netrin selected among netrin-4, mutated netrin-4, netrin-1, netrin G1 or netrin-3, or one of their fragments or a nucleotide sequence encoding one of the netrins or one of the fragments, or an anti-idiotypic antibody of one of the netrins or of one of the fragments, or of a Fab fragment of the anti-idiotypic antibodies, for preparing a medicine for preventing or treating tumoral or non-tumoral pathologies.

Abstract: The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.

Abstract: The present invention relates to a method of identifying a candidate therapeutic agent. The method comprises contacting a G-Protein Coupled Receptor (GPCR) with a compound of General Formula (I), or a pharmaceutically acceptable salt thereof determining whether the compound inhibits or effects signal transduction activity of the GPCR, wherein a compound that inhibits or effects the activity of the GPCR is a candidate therapeutic agent.

Abstract: An object of the present invention is to provide an inexpensive and simple extraction method for a sialic acid-containing compound from a raw material which is easily available and has no risk of contamination with pathogens affecting animals (raw material which has high safety) without requiring the use of a reagent harmful to the human body and environment. The present invention is also aimed at providing an extraction method for a sialic acid-containing compound, the method comprising: crudely extracting a soluble component from a plant body (in particular, seeds of cereal and/or seeds of bean) or a processed product of the plant body with water, an alcohol, or an aqueous alcohol; and separating and recovering the sialic acid-containing compound from the resultant crude extract solution by dialysis, salt precipitation, or column chromatography.

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 particular glycomimetics alone or linked to a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).

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: A compound comprising a metal chelate linked to a hexose carrier for use as a metallopharmaceutical diagnostic or therapeutic agent is provided. The compound is suitable for imaging by single-photon emission computed tomography, computer assisted tomography, magnetic resonance spectroscopy, magnetic resonance imaging, positron emission tomography, fluorescence imaging or x-ray.

Abstract: Described herein are compounds such as macromolecules that have been modified in order to facilitate crosslinking by introduction of at least one hydrazide-reactive group and/or aminooxy-reactive group, and methods of making and using thereof for scar-free wound healing, for delivering bioactive agents or living cells, for preventing adhesion after a surgical procedure or for bone and cartilage repair. The macromolecule can be an oligonucleotide, a necleic acid, a polypeptide, a lipid, a glycoprotein, a glycolipid, a polysaccharide, a protein or a synthetic polymer, preferably a glycosaminoglycan like hyaluronan.

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: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.

Abstract: Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action.

Abstract: The present invention provides a metal chelator and methods that facilitate binding, detecting, monitoring and quantitating of zinc ions in a sample. The metal chelating moiety of the zinc-binding compound is an analog of the well-known calcium chelator, BAPTA (1,2-bis(2-aminophenoxy)ethane-N,N,N?,N?-tetraacetic acid), wherein the chelating moiety has been modified from a tetraacetic acid moiety to a tri- di- or monoacetic moiety. This change in acetic acid groups on the metal chelating moiety results in the selective bindings of zinc ions in the presence of calcium ions, both of which are present in biological fluids and intracellular cytosolic fluid and organelles.

Abstract: A stable and high-purity protected pseudouridine in crystal form is provided represented by the following structural formula: wherein M represents a trityl group or a derivative thereof, which is a useful material for producing an RNA oligomer or a similar substance. A method for producing the crystalline protected pseudouridine is also provided, which method includes crystallizing a protected pseudouridine from a solution containing the protected pseudouridine, by use of an ester solvent and/or an alcoholic solvent. The method, which does not need a silica gel column treatment, can be performed in a simple manner, does not impose a load on the environment, and realizes low-cost production of a target crystalline protected pseudouridine.

Abstract: Method for preparing the disaccharide [?-D-Gldp(1?3)]-?-L-Rhap-YR wherein Y is selected from —O— and —S— and R is selected from the group consisting of: C1-C6 alkyl, C1-C6 alkenyl, aryl, allyl, —CO-alkyl (C1-C6), —CO-alkenyl (C1-C6), —CO-aryl comprising the step of using a mutant of a wild type glycoside hydrolase.

Abstract: This invention relates to processes for production of alkylamino glucosaminide phosphate compounds, and of disaccharide compounds, including various novel intermediates and intermediate processes. In one aspect, glycosyl halides are produced by reaction of an O-silyl glycoside with a dihalomethyl alkyl ether.

Abstract: Disclosed is a mixture of: a bone/cartilage formation promoting agent containing sulfated galactosaminoglycan having greater than or equal to 0.6 numbers of ester sulfate groups on average per constituent monosaccharide or a salt thereof as an active ingredient; a factor having a bone/cartilage formation promoting action; or a bone filler (BMP, TGF-?, FGF, IGF, insulin, PDGF, HGF, midkine, pleiotrophin, collagen, gelatin, proteoglycan, fibronectin, osteocalcin, osteopontin, osteonectin, bone sialoprotein, hydroxyapatite, dicalcium phosphate anhydride, dicalcium phosphate dehydrate, ?-tricalcium phosphate, amorphous calcium phosphate, octacalcium phosphate, ?-tricalcium phosphate, PLLA, PLGA, titanium, decalcified bone, autogeneous bone, or the like).

Abstract: This invention relates to certain Aloesin derivatives with natural amino acids, peptides, and amino sugars (formula I).

Abstract: The present invention relates to folates, compositions and uses thereof; In particular, this invention describes a crystalline or amorphous compound which is a substituted or unsubstituted folate or a reduced folate, or the natural or unnatural isomers thereof, of at least one organic base, as well as compositions and uses thereof. The compounds of the invention show a long lasting stability as well as a peculiarly high water-solubility.

Abstract: One aspect of the present invention relates to solution-phase approaches to GPI synthesis. Another aspect of the present invention relates to key building blocks, and syntheses thereof, useful for GPI assembly. Yet another aspect of the invention relates to an automated method for the synthesis of GPIs and fragments thereof.

Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, in which each compound is adapted to occupy the binding site of human IDO, which comprises a large hydrophobic pocket A and a second, proximal hydrophobic pocket B, the compound comprising at least one of the following elements: (i) a large hydrophobic fragment to substantially fill pocket A in the binding site of human IDO; (ii) an atom that can coordinate to the heme iron of human IDO, (iii) a positively charged group that can form a salt-bridge with the heme 7-propionate of the human IDO; (iv) a negatively charged group that can form a salt-bridge with Arg231 of the human IDO; (v) a hydrophobic group that can form van der Waals interactions with pocket B; and (vi) one or more substituents that can hydrogen bond to Ser167 and to Gly262, and as IDO inhibitors and their therapeutic use, eg in the treatment of cancer.

Abstract: The present invention relates to amino acids, complexes, and compounds comprising deuterium and tritium isotopes preferably alpha deuterated amino acids, polypeptides, antibodies, derivatives and saccharide-amino acid complexes and conjugates. In some embodiments, the invention relates to methods of using compounds comprising deuterium for imaging biochemical concentrations and distributions in mammalian tissues using nuclear magnetic resonance spectroscopy. In some embodiments, the invention relates to the used of said amino acids derivatives and complexes in boron neutron capture therapy. In some embodiments, the present invention relates to the preparation of amino acids, polypeptides, antibodies, derivatives and saccharide complexes/conjugates comprising heavy hydrogen isotopes. In some embodiments, the invention relates to racemizing amino acids starting from compositions of any optical purity.

Abstract: The present invention provides compositions and methods for the treatment of atherosclerosis and other related diseases. In some embodiments, a method comprises providing a composition and forming a coating of the composition on at least a portion of the interior and/or exterior surface of a tissue lumen or other body surface. The composition may remain associated with the tissue lumen or other body surface even in the presence of a strong flow of a fluid (e.g., blood flow in a blood vessel). The composition may associate with the tissue lumen via a plurality of covalent bonds. In some cases, the compositions may comprise at least one additive, for example, a therapeutically active agent or an imaging agent.

Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars, and isomers and salts thereof (formula I).

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: The invention relates to the use of ?-glycolipids as immunomodulators. More particularly, the invention relates to the use of ?-glycolipids, preferably, ?-lactosyl-ceramide, ?-glucosylceramide, ?-galactosyl-ceramide, ceramid and ?-lactosyl-ceramide, as well as any mixture or combination thereof for the treatment of immune related disorders. The present invention further relates to a process for the modulation of the Th1/Th2 cell balance toward anti-inflammatory cytokine producing cells, in a subject suffering from an immune related disorder. Therapeutic compositions and method for the preparation of these compositions are also provided.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 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 derivative compounds having one or more benzo nitrogens.

Abstract: This invention provides compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a physiologically acceptable monomer, dimer, oligomer, or polymer, wherein X is a glycosaminoglycan; and n is a number from 1 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond.

Abstract: A process for producing a polysaccharide sponge comprises the steps of (A) freezing a photoreactive polysaccharide solution, and (B) irradiating the frozen photoreactive polysaccharide solution with light to crosslink the photoreactive polysaccharide, thereby obtaining the polysaccharide sponge. The process includes simplified steps requiring no removal of solvent, and has such an advantage that impurities are easily removed therefrom.

Abstract: The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Abstract: It is an object of the present invention to provide an extraction method for a sialic acid-containing compound from a natural raw material, which has no risk of contamination with pathogens affecting animals, can achieve mass production, and does not require the use of an organic solvent harmful to the environment and human body. Provided is an extraction method for a water-soluble sialic acid-containing compound, the method comprising: crudely extracting a water-soluble component with water, polyol, or water containing either an acid or an alkali or polyol from a plant body or a processed product of the plant body, in particular, seeds of cereal or seeds of bean; and separating and recovering the water-soluble sialic acid-containing compound from the resultant crude extract solution with a column packed with a serotonin affinity support.

Abstract: The present invention provides novel Quercetin derivatives of formula (I) and pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1 is hydrogen, benzyl or substituted benzyl; R2 is hydrogen, benzyl or substituted benzyl, linear or branched (C1-C6) alkyl, substituted alkyl, aryl, substituted aryl, heterocycle and substituted heterocycle, useful for treatment of various disorders including cancer, multi-drug resistant cancers, viral infections etc. The invention also provides a process for the preparation of compounds of formula (I) and pharmaceutical compositions comprising the same.

Abstract: Glucopyranosyl-substituted benzyl-benzonitrile 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: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.

Abstract: Methods are described for the preparation of combinatorial libraries of potentially biologically active disaccharide compounds. These compounds are variously functionalized, with a view to varying lipid solubility size, function an other properties, with the particular aim of discovering novel drug or drug-like compounds, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of disaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of pharmaceutically useful groups and isosteres.

Abstract: This invention relates to certain chirally-correct mitoprotectant phosphorylated heterocyclic agents [formula (I)], which are useful for the treatment of dermatological disorders that include challenged skin from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial dysfunction; age spots; acne, loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness; skin depigmentation, and combinations thereof;

Abstract: Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): —OX—Y (Ia) or —O—R1 (Ib) wherein X is C(O), S(O) or SO2; Y is NR1R2 or R3; R1 is C1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R2 is H or C1-6 alkyl; and R3 is C1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.

Abstract: The glmS riboswitch is a target for antibiotics and other small molecule therapies. Compounds can be used to stimulate, active, inhibit and/or inactivate the glmS riboswitch. The atomic structures of the glmS riboswitch can be used to design new compounds to stimulate, active, inhibit and/or inactivate riboswitches.

Abstract: Disclosed herein is a method for extracting a biosubstance from a root of a hair, including the step of using as the hair a hair that has pulling force of at least a predetermined reference value to pull out the hair.

Abstract: The invention relates to novel hybrid compounds containing at least one polysaccharide entity (PS), such as guar, in which at least one hydroxyl function is substituted by at least one A polyoxyalkylene entity (PEG). The swivel Ro between the entity PS and the entity A is obtained by click chemistry and has the following formula (II.1) or (II.2), in which Z is a carbon or nitrogen atom. These hybrid compounds can be used as emulsifiers, particularly in cosmetics.

Abstract: The present invention generally provides compositions methods and composition relating to the diagnosis and/or treatment of cancers having a cell surface de-N-acetylated sialic acid antigen, e.g., an at least partially de-N-acetylated ganglioside and/or a de-N-acetylated sialic acid-modified cell surface protein.

Abstract: The present invention relates to pentose and pentose derivatives that are effective at increasing glucose transport in a non-insulin dependent manner, and to uses thereof for a) treating and/or preventing hyperglycemia; b) treating and/or preventing the complications of hyperglycemia; c) treating diabetes; d) increasing the rate of cellular glucose transport; e) increasing the rate of cellular glucose uptake; f) improving the ability of a subject to metabolize glucose; g) treating daily blood glucose fluctuations; h) reducing blood sugar levels; i) reducing the dosage of anti-diabetic medication needed for treatment of diabetes. The present invention further provides novel pentose derivatives having beneficial properties in terms of pharmacokinetics, to pharmaceutical compositions comprising these novel compounds and uses thereof.

Abstract: This invention provides a method of treating a subject suffering from an obstructive respiratory disease, including the step of administering to a subject a compound comprising a lipid or phospholipid moiety bound to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof, in an amount effective to treat the subject suffering from an obstructive respiratory disease.

Abstract: Glucopyranosyl-substituted benzonitrile derivatives 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.