Abstract: Aspects of the invention relate to novel synthetic compounds having binding affinity with galectin proteins.

Abstract: Inhibitors of sodium glucose cotransporter 1 (SGLT1), compositions comprising them, and methods of their use to treat diseases and disorders such as diabetes are disclosed. Particular compounds are of the formula: the various substituents of which are defined herein.

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: 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 present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.

Abstract: Hydrophilic N-linked pharmaceutical compositions, methods of their preparation and use in neuraxial drug delivery comprising a glycosyl CNS acting prodrug compound covalently N-linked with a saccharide through an amide or an amine bond and a formulary consisting of an additive, a stabilizer, a carrier, a binder, a buffer, an excipient, an emollient, a disintegrant, a lubricating agent, an antimicrobial agent or a preservative, with the proviso that the saccharide moiety is not a cyclodextrin or a glucuronide.

Abstract: Dental compositions are provided comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein n is an integer from about 2 to about 5.

Abstract: Sialic acid derivatives of the formula (I) in which the symbols have the definitions stated in the description are suitable as medicaments, more particularly for diseases whose course is influenced by Siglec ligands.

Abstract: Provided are water and alcohol extracts of Rhizoma arisaematis, compounds isolated from Rhizoma arisaematis (such as 3-O-(9,12-octadecadienoyl)-glyceryl-?-D-galactopyranoside, N-(?-D-ribofuranos-1-yl)-phenylalanine, and adenosine), pharmaceutical compositions comprising the aforementioned ingredients, as well as uses thereof for promoting wound healing. In one embodiment, the pharmaceutical composition is a topical formulation, such as a cream, ointment, foam, lotion, plaster, gel, and emulsion.

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: The present invention relates to a topical composition for use on skin containing theanine derivatives as active components and, more particularly, to a topical composition for use on skin having anti-aging, skin wrinkle repair, skin barrier enhancement, skin immunity enhancement, skin moisturizing, and atopy alleviation effects by containing theanine derivatives as active components.

Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material. Furthermore, the present invention relates to the use of the sorbent according to the invention for the purification of organic molecules, in particular pharmaceutically active compounds, preferably in chromatographic application.

Abstract: Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: or a pharmaceutically acceptable salt thereof, wherein L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, Y1, Y2, Y3, Y4, R1, R2, R3, R4, R5, R6, are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Abstract: The present invention provides a compound comprising a helminth-derived glycan and/or glycoconjugate thereof (e.g., a compound comprising a Lewisx antigen (e.g., LNFPIII), a non-Lewisx antigen (e.g., LNnT, LDN, and LDN derivatives), or a mixture of Lewisx and non-Lewisx antigens (e.g., SEA)), useful as a therapeutic compound for treating or preventing diseases associated with fat accumulation in the liver. The compounds of the invention are useful for treating or preventing the development of a fatty liver disease in a subject that has the disease or is at risk of developing the disease, and inhibiting lipogenesis in hepatocytes. The invention also provides methods of regulating the Erk-c-fos/AP-1-FXR? signalling pathway by administering a compound comprising a helminth-derived glycan and/or glycoconjugate thereof to a subject with a fatty liver disease, or contacting a hepatocyte with a compound comprising a helminth-derived glycan and/or glycoconjugate thereof.

Abstract: The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.

Abstract: A 1,2-dideoxy-1,2-diamino oligosaccharide or polysaccharide in its free base, salt or metal-complex form as shown in General Formula 1 and derivative thereof is described. R1, R2 and R3 are each independently selected from the group consisting of H and a carbohydrate moiety, with the proviso that at least one of the groups R1, R2 or R3 is a carbohydrate moiety; R4 is selected from the group consisting of: H, optionally substituted C1-20-alkyl, optionally substituted heteroalkyl, optionally substituted C2-20-alkenyl, optionally substituted C2-20-alkynyl, optionally substituted C3-10-cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl.

Abstract: Novel methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) or glycosylamine under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product containing an aziridinyl ring. Optional subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product. Coupling of a peptide thioacid and glycosylamine yields a glycosylated peptide.

Abstract: Acadesine derivatives as a drug, as well as the derivatives for the treatment of cancer and in particular for the treatment of chronic myeloid leukemia are described. Also, product containing the derivatives and at least one second active ingredient as a combination product for simultaneous, separate or sequential administration, in the treatment of cancer, as well as a pharmaceutical composition containing the derivatives and a pharmaceutically acceptable carrier are described. Finally, a method for inhibiting the in vitro cell proliferation including the placement of an in vitro cell in contact with the derivatives and methods for synthesis of said derivatives and methods for synthesis of the derivatives are described.

Abstract: Disclosed are derivatives of (tetrahydropyranyl)methyl acrylamide and polymers derived therefrom, as well as methods of making such compounds and polymers. Adhesives, coatings, and plastics which include such polymers are also described.

Abstract: Provided is an organic nanotube having a hydrophobized inner surface, formed by molecules including an asymmetric bipolar lipid molecule represented by the following General Formula (1) and a derivative thereof represented by the following General Formula (2), wherein the organic nanotube has a hydrophilized outer surface and a hydrophobized inner surface of a hollow cylinder and is formed by binary self-assembly, the organic nanotube encapsulates a hydrophobic guest in the hollow cylinder, has a function of refolding a denatured protein, and has a function of sustainably-releasing a hydrophobic drug according to the change in hydrophobicity of the inner surface of the tube or external stimulus, In Formulas (1) and (2), wherein the same symbols have the same meanings, G is a 1-glucopyranosyl group or 2-glucopyranosyl group, and n is an integer of 12 to 22.

Abstract: Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets.

Abstract: Dental compositions are provided comprising a compound of Formula I or a pharmaceutically acceptable salt thereof: wherein n is an integer from about 2 to about 5.

Abstract: A library of glycosylated chlorambucil analogs which are useful as anti-tumor and/or anti-metastatic agents is disclosed. The glycosylated chlorambucil analogs have the general formula wherein represents a reducing sugar moiety.

Abstract: The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.

Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same.

Abstract: A process for the simultaneous substitution and crosslinking of a polysaccharide via its hydroxyl functional groups, in an aqueous phase, which includes the following steps: a polysaccharide is placed in an aqueous medium, it is brought into the presence of at least one precursor of a substituent, it is brought into the presence of a crosslinking agent, the substituted and crosslinked polysaccharide is obtained and isolated, wherein process is carried out in the presence of a basic or acidic catalyst, the concentration of which is between 3.16×10?7 and 0.32 mol/L, and at a temperature of less than 60° C. In one embodiment, the polysaccharide is in the form of a gel or hydrogel which is used in particular as augmentation biomaterial.

Abstract: The present invention relates to process for reducing the endotoxin content of a sample of fermentation broth containing polysialic acid and endotoxin comprising the sequential steps: (i) adding to the sample a base having a pKa of at least 12 to form a basic solution having a pH of at least 12, incubating the solution for a pre-determined time at a pre-determined temperature; and (ii) recovery of PSA, suitably by (iii) passing the sample through an anion-exchange column whereby polysialic acid is absorbed on the ion exchange resin; (iv) washing the column with one washing buffer, whereby polysialic acid remains absorbed on the ion exchange resin; and (v) eluting the polysialic acid from the column using an elution buffer to provide a product solution of polysialic acid having reduced endotoxin content.

Abstract: The invention relates to a method for producing 1,4-benzothiepin-1,1-dioxide derivatives substituted with benzyl groups.

Abstract: The present invention relates to a theanine derivative, a preparation method thereof, and a use thereof for anti-acne treatment, having a selective inhibitory effect on Propionibacterium acnes in the skin.

Abstract: The present invention provides cationic lipids, methods for preparing the same, and delivery systems comprising the same. The present invention can provide cationic lipids which enhance the efficiency of intracellular or in vivo delivery of multiple-anionic target compounds such as drugs, anticancer agents, nucleic acids, etc., have no intracellular toxicity, but show increased stability, methods for preparing the same, and delivery systems comprising the same.

Abstract: The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.

Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.

Abstract: The present invention provides methods of producing compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides neoglycoside digitoxin analogs that include compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.

Abstract: Compositions comprising compounds having an aldohexose moiety, a highly fluorinated moiety, and a nitrogen-containing functional group linking the moieties together are disclosed. The aldohexose-based fluoroadditives are effective in reducing the surface tension of water and are useful in various surfactant applications. Also disclosed are processes for making aldohexose-based fluoroadditives.

Abstract: The invention relates to methods of use for compounds in treating, reducing the incidence, reducing the severity or pathogenesis of an intestinal disease or condition in a subject, including, inter alia, inflammatory bowel disease, Crohn's disease, ulcerative colitis, or a combination thereof.

Abstract: The present invention discloses a set of glycosylated warfarin analogs which are useful as anti-tumor or anti-metastatic agents and as reagents for studying sugar uptake in cells.

Abstract: Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V and methods of their use, wherein, Ring 1 comprises an aryl or heteroaryl ring having 4 to 8 carbon atoms, among which atoms are counted “X” and “Y”; each of X and Y is optional; X, when present is either —C(R1)2— or —C(R)2—; Y, when present, is either —CH2— or —CH2—CH2—; z, R5 and R5? are optional, and when present z, R5 and R5? together form a lower alkyl or a substituted lower alkyl moiety; N is part of either an amine or an amide linkage; E is a saccharide which forms a linkage with N through a single bond from a carbon or oxygen atom thereof; R1 and R4 are selected form the group consisting of hydrogen, hydroxyl, halogen, halo-lower alkyl, alkoxyl, alkoxyl-lower alkyl, halo-alkoxy, thioamido, amidosulfonyl, alkoxylcarbonyl, carboxamide, aminocarbonyl, and alkylamino-carbonyl; R2 and R3 are hydroxyl; R5 and R6, when present, are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carbonyl

Abstract: Implantable matrices and methods are provided. The matrices are configured to fit at or near a target tissue site, the matrices comprise biodegradable materials and ligands bound to the matrices and are configured to bind receptors and allow influx of cells into the implantable matrices, wherein the ratio of ligands to receptors is from about 1.5 to about 0.5.

Abstract: The present invention provides for monophosphorylated lipid A derivatives and carbohydrate derivatives that are useful as agents in the treatment of diseases and conditions, including cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I-IV. In addition, methods for the treatment of cancers are provided.

Abstract: Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets.

Abstract: A library of glycosylated chlorambucil analogs which are useful as anti-tumor and/or anti-metastatic agents is disclosed. The glycosylated chlorambucil analogs have the general formula wherein represents a reducing sugar moiety.

Abstract: Flavonoid glycosides, such as isoquercitrin, are shown to stimulate the formation of neuritis and neuronal synapses in neurons and neuronal progenitor (stem) cells.

Abstract: Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity.

Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives with improved properties, method for producing the same, drugs containing said compounds and use thereof.

Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with fluorine, method for producing the same, drugs containing said compounds and use thereof.

Abstract: The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.

Abstract: A monosaccharide compound of formula I as shown in the specification. Processes for the preparation of the compound of formula I and methods of screening for antibacterial or antibiotic compounds involving the compound of formula I.

Abstract: The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same.

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.