Abstract: Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.

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 invention relates to a complex consisted of a polysaccharide and an HBP, said polysaccharide being consisted from glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative. The invention also relates to a pharmaceutical composition comprising a complex according to the invention and to the use of a polysaccharide consisted of glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative, for the preparation of a pharmaceutical formulation of stable HBPs.

Abstract: The invention provides compositions containing a highly purified antiendotoxin compound and methods of preparing and using such compositions.

Abstract: Designed herein are multivalent heterobifunctional polymers for binding to a biological target exhibiting biological activity and to an effector template which can affect the biological activity of the biological target or detect the presence of the biological target. The polymers comprise a plurality of pre-arranged heterobifunctional ligands connected thereto, and each heterobifunctional ligand comprises a first functionality capable of binding to the biological target, and a second functionality capable of binding to the effector template. The heterobifunctional ligands are pre-arranged on the polymer so as to form a ternary complex between the polymer, the biological target and the effector template. The polymers, methods and compositions described herein provide an approach for the design and production of new therapeutic agents as well as agents useful in a variety of non-therapeutic applications.

Abstract: The disclosed is thiol-modified macromolecule derivatives having the general formula of (I) or (II), as well as the disulfide bond cross-linked materials and the thiol-reactive crosslinker cross-linked materials, wherein R1 and R2 are alkylene groups, substituted alkylene groups, aromatic groups or polyether groups and the like, respectively. R1 and R2 may have same or different chemical structure, and P is a residue of a macromolecule with side carboxyl group. The thiol-modified macromolecule derivative has a molecular weight of from 1000 to 5,000,000. The thiol-modified macromolecule derivative having the general formula of (I) or (II) of the present invention has a side chain with flexible chemical structure and adjustable properties, and has a number of advantages, such as mild reaction condition, high production yield, high degree of modifying, and the controllable modifying degree and so on.

Abstract: The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.

Abstract: Biologically compatible polymers carry an imide and can be used as an adhesive, a hydrogel or both. A second biologically compatible polymer reactive with the imidated polymer can be used therewith to seal openings.

Abstract: The present invention relates to compounds of the formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: An organic material including a hydrophilic polymer and an organic moiety having a hydroxyl substituted C6-C14 aromatic functional group, the organic moiety binding to an end or a side of the hydrophilic polymer.

Abstract: Provided is a complex obtained by reacting a polymer compound derivative obtained by modifying part of hydroxy groups or amino groups of a polymer compound having the hydroxy groups or amino groups with a compound represented by the following general formula (I) with one or more kinds of compounds represented by the following general formulae (II) to (V): (I) A-X—Si(Y)nR3-n (where A, X, Y, R, and n are as defined in claim 1) ; (II) M(OR1)nR24-n; (III) Al(OR1)pR23-p; (IV) Mg(OR1)gR22-q (where M, R1, R2, n, p, and q are as defined in claim 1); and (V) (where R3, R4, R5, and R6 are as defined in claim 1).

Abstract: Material characterized by that the material contains at least one biologically active di- or trisaccharide or higher oligosaccharide which is covalently bound via a spacer to cross-linked agarose.

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: An object of the present invention is to provide a novel trehalose compound that exhibits excellent immunostimulating activity and that can be supplied in a large quantity in an industrial scale, and a method for producing the trehalose compound, wherein the trehalose compound of the present invention exhibits excellent immunostimulating activity, and is represented by general formula (1) below: wherein R1, R2, R3 and R4 may be the same or different, and independently represent a C10-16 alkyl group. The trehalose compound of the present invention is produced by removing a protective group (R5) for a hydroxyl group from a trehalose compound represented by general formula (5) below: wherein R1, R2, R3 and R4 are the same as above. R5 is a protective group for a hydroxyl group.

Abstract: This invention provides cholesterol absorption inhibitors of Formula (I), and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

Abstract: A series of novel, melt- or mold-processable HA esters with varying aliphatic chain lengths are synthesized from silyl HA-quaternary (quat.) ammonium salt complex (preferably silyl HA-CTA, a silylated HA complex with cetyltrimethyl ammonium salt). Introduction of aliphatic acyl groups, preferably acid chlorides, to disrupt the strong HA intermolecular bonding, is done via acylation. Acylation takes place at the oxygen of the trimethylsilyloxy group —O—Si(CH3)3 in the silyl HA-CTA by removal of trimethylsilyl groups therefrom. Optionally, crosslinking may be performed during the shaping/molding of the HA esters into a structure/device, or thereafter, if at all. Native HA can then be regenerated/recovered by saponification hydrolysis, removing acyl groups, —CH3(CH2)10CO, and the cetyltrimethyl ammonium salt groups, -CTA, from HA ester. The structure/device of a preselected shape (e.g.

Abstract: A process for preparing hyaluronic acid primarily as a food supplement which is capable of absorption and assimilation by the human body includes desirable control of both the purity and molecular weight range of the resulting product. Chicken comb tissue is subjected to one of two disclosed processes for extracting, purifying, and controlling the molecular weight range of hyaluronic acid in solution, which is then dried and powdered to a form suitable for human consumption as a food supplement. The resulting hyaluronic acid product can also be used topically in creams or solutions for beneficial treatment of skin conditions, such as dry skin or wrinkling, for example.

Abstract: The present invention relates to percarboxylated polysaccharide selected from the group consisting of gellan, carboxymethylcellulose, pectic acid, pectin and hyaluronic acid derivatives; the process for their preparation and their use in the pharmaceutical, biomedical, surgical and healthcare fields.

Abstract: A glycopeptide of the formula S-L-X—P, wherein: S is selected from an optionally protected monosaccharide, an optionally protected polysaccharide, a polyalkylene oxide chain and a group of the formula II, wherein R1 and R3 are independently selected from H or Ac, R4 is Ac, and R2 is a group of formula IV, wherein R7 and R8 are each independently selected from an optionally protected monosaccharide and an optionally protected polysaccharide, A, B, C and D are each independently 1 or 2, and m is 1 to 5; -L- is a moiety of the formula III wherein R5 and R6 are independently selected from H and Me and n is 1 to 3; and P is a peptide chain containing at least one amino acid having on its side chain the atom X, wherein X is an oxygen, a sulphur atom or a —CH2— moiety.

Abstract: Described is chondroitin sulfate obtained from microbial sources, and related compositions and methods.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g. on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The invention relates to a method for manufacturing cellulose carbamate. In the method, an auxiliary agent and urea in solution form and possibly in solid form are absorbed into cellulose, and a reaction between cellulose and urea is carried out in a mixture containing cellulose, a liquid, the auxiliary agent, and urea The absorption of the auxiliary agent and urea into cellulose, and the reaction between the cellulose and the auxiliary agent at least partly are carried out in a working device. According to the invention, it is possible to manufacture cellulose carbamate without ammonia, organic solvents or other auxiliary agents, by using only a small quantity of water as a medium.

Abstract: A method and pharmaceutical composition for the enhancement of transfer of a therapeutic agent to a cell wherein the therapeutic agent is formulated in a buffer comprising a compound of Formula I: wherein: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of pentose monosaccharide groups, hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X2 and X3 is a saccharide group.

Abstract: This invention relates to galactosylceramide compounds.

Abstract: This invention provides cholesterol absorption inhibitors of Formula (I), and the pharmaceutically acceptable salts and esters thereof. The compounds arc useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

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: 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: The present invention provides biocompatible, biodegradable matrices formed from poly-?(1?4)glucopyranose and reactive hydrazide groups. The matrices can be used for various applications in the body, including drug delivery and cell therapy.

Abstract: The invention relates to a process for the depolymerization of glycosaminoglycanes characterized by the use of UVC radiation. The invention also relates to the intermediate depolymerized heparin obtained by the process. The intermediate depolymerized heparin can be dissolved in a buffer solution and fractionated by gel permeation for obtaining the desired molecular weight.

Abstract: A method for synthesizing uniformly sized hyaluronic acid (“HA”) particles that are substantially free from oil and surfactant contaminants. The method comprises crosslinking HA chains with 1-ethyl-3-(3-dimethlyaminopropyl) carbodiimide hydrochloride (“EDAC”) and adipic acid dihydrazide in a water/acetone mixture.

Abstract: The present invention relates to the modification of hyaluronic acid (HA) with aryl/alkyl succinic anhydrides (ASA) to produce aryl/alkyl succinic anhydride HA derivatives, to the derivatives as such, and to their applications and uses, particularly in the cosmetic and biomedical industries. The ASA-HA derivatives are expected to have interesting properties that can be used for advanced formulation (bind stronger to the skin compared to non-modified HA), possibly also in delivery systems for actives or drugs by encapsulation (nano/micro capsules) or formation of nano/micro spheres. Further, the low MW ASA-HA derivatives are expected to penetrate the skin more efficiently than non-modified HA of the same MW.

Abstract: Multiple strains and species of Campylobacter share a common glycan moiety which is present in a plurality of surface-exposed glycoproteins. This glycan has the formula: GalNAc-a1, 4-GalNAc-a1,4-[Glc-?1,3]GalNAc-a1,4-GalNAc-a1,4-GalNAc-a1,3-Bac, wherein Bac is 2, 4-diacetamido-2,4,6-trideoxy-D-glucopyranose. This glycan and immunologically active fragments of it have use as vaccines against campylobacter infection in humans and animals. As well, antibodies which specifically bind these compounds may be provided. Such antibodies and vaccines may be used to prevent or neutralize campylobacter infections in livestock thereby preventing this pathogen from entering the human food chain. The glycan may be linked to one or more amino acids to form a glycopeptide. As well, a method for determining the glycan structure of an intact glycoprotein consists of subjecting a sample to high resolution magic angle spinning nuclear magnetic resonance (HR-MAS-NMR) spectroscopy.

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: Glycolipid derivatives having the formula (I): wherein R1 indicates an aldopyranose residue, R2 indicates a hydrogen atom or hydroxyl group, A indicates —CH2—, —CH(OH)—CH2— or —CH?CHCH2—, Z indicates —O— or —CH2—, when Z is —O— and x is an integer of 4 to 16, y indicates an integer of 26 to 35, when Z is —O— and x indicates an integer of 17 to 25, y indicates an integer of 0 to 35, when Z is —CH2— and x indicates an integer of 4 to 15, y indicates an integer of 26 to 35, and when Z is —CH2— and x indicates an integer of 16 to 25, y indicates an integer of 0 to 35 and a drug containing the glycolipid derivative for treatment of autoimmune arthritis and other autoimmune disease, bronchial asthma and other allergic diseases or diseases in which NKT cells or stimulation of NKT cells is known to be participating in the deterioration of conditions.

Abstract: Preparation of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.

Abstract: The subject of the present invention is new substances which are derived from naturally occurring ceramides and sphingosine and also from synthetic compounds with principally the same structure in that they represent dimers, trimers, tetramers etc., hence i.e. oligomers of the initial substances.

Abstract: A process for the preparation of 2-hydroxymethyl-pyrrolidine-3,4-diols of the formulae: including the steps of: a) bioxidation of N-protected aminotetraols of the formula: b) deprotection of the corresponding 5-amino-5-deoxy-pentulose of the formula: and c) hydrogenation of the corresponding 5-amino-5-deoxy-pentulose of the formula:

Abstract: The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction rate of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction rate as that of the conventionally known gel.

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 a method of preparing affinity ligands, which method comprises to provide a cyclic scaffold comprising a thiol group, a carbonyl group and an amine group; to derivatize the amine group of said scaffold with an electrophile that carries either a functionality capable of affinity interaction or a functionality capable of a second interaction with a target molecule; and to open up the derivatized scaffold and add an amine that carries either a functionality capable of a second interaction or a functionality capable of affinity interaction with a target molecule. The method provides provide affinity ligands, which are capable of affinity interaction as well as a second kind of interaction.

Abstract: Hyaluronic acid oligosaccharides having a size selected from sizes of 4 to 60 saccharides, fractions containing the hyaluronic acid oligosaccharides and having particular physicochemical properties, and drugs containing the same. The hyaluronic acid oligosaccharides of the present invention are extremely useful, because they exert superior pharmaceutical effects as active ingredients of a heat shock protein expression promoter, cell death inhibitor, cell injury inhibitor and cell and tissue protecting agent (e.g., organ preservation agent, antiulcer agent, antihepatopathic agent, IL-10 production promoter or IL-8 production inhibitor) and exhibit high safety.

Abstract: The present invention relates to hyaluronic acid ester derivatives, whose carboxylic groups are partially esterified with hydroxy groups of propiophenone derivatives, to the hydrogel materials consisting of the said hyaluronic acid ester derivatives, to their preparation process by photocuring of the hyaluronic acid ester derivatives, and their use in the biomedical, sanitary and surgical fields, and in the medical field as controlled release systems for drugs.

Abstract: The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.

Abstract: A process for the synthesis of beta linked low molecular weight polymers of galactosamine and glucosamine has been developed. Through the use of high amounts of activating agents, efficient coupling of stable monomers is achieved. Using this process, chain extension is through the addition of single monomers, providing populations of single chain length polyhexosamines.

Abstract: A novel compound causing an oral cavity stimulus such as acridness, which is expressed by the following structural formula (I):

Abstract: Various azetidinone derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.

Abstract: The invention relates to Fmoc (9-fluorenyl-methoxycarbonyl)-based polymeric conjugates. These conjugates are useful for extending the in-vivo circulation of protein and peptide drugs.

Abstract: Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

Abstract: An optically active dihydroxyheptenoic acid ester having an aromatic group is separated from a solution containing a mixture of optical isomers of digydroxyheptenoic acid ester by liquid chromatography with a packing material constituted of a carrier and a polysaccharide derivative carried on the carrier. The polysaccharide derivative is a polysaccharide in which the hydrogen atoms constituting the hydroxyl and amino groups are partially or all replaced by one or more kinds of groups selected from among carbamoyl groups monosubstituted with aromatic groups having specific alkyl groups and benzoyl groups having specific alkyl groups. According to the invention, optically active dihydroxyheptenoic acid esters can be separated more distinctly.

Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts thereof, wherein R12 is an alkyl, alkeny or alkynyl group mono- or poly-substituted with —OH, —COOH or a combination of —OH and —COOH, and R9 contains an alkyl, alkeny or alkynyl group substituted with a heterocyclic ring, amino or sulfonyl. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.