Abstract: Processes for the synthesis of the Factor Xa anticoagulent Fondaparinux, and related compounds are described. Also described are protected pentasaccharide intermediates as well as efficient and scalable processes for the industrial scale production of Fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions.

Abstract: Heparin-like compounds inhibit collagen-induced platelet aggregation in flowing whole blood. The compounds share properties displayed by native mast-cell derived heparin proteoglycans (HEP-PG) and/or heparin glycosaminoglycan (HEP-GAG) molecules. The compounds are useful in prevention and treatment of severe vascular disorders including arterial thrombosis.

Abstract: A method for targeted delivery of therapeutic compounds from hydrogels is presented. The method involves administering to a cell a hydrogel in which a therapeutic compound is noncovalently bound to heparin.

Abstract: The invention relates to methods and products associated with analyzing and monitoring heterogeneous populations of sulfated polysaccharides. In particular therapeutic heparin products including low molecular weight heparin products and methods of analyzing and monitoring these products are described.

Abstract: A photocrosslinked polysaccharide pseudo-sponge exhibiting a low swelling property and a high degradation ability in vivo while retaining a suitable strength. The polysaccharide pseudo-sponge is produced by a crosslinking reaction of a photoreactive polysaccharide obtained by introducing a photoreactive group into a polysaccharide, and exhibits a low swelling property and a blue dextran-low dyeaffinity.

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: The present invention describes sulodexide or at least one of its components for use in the reduction of circulating matrix metalloproteinase (MMPs), in particular MMP-9. Sulodexide and its composition are useful for the treatment of pathologies wherein the MMPs are involved, such as cardiovascular disease, cardiovascular disease caused by diabetes, varicose veins, chronic venous insufficiency (CVI), gastrointestinal ulcers, pulmonary disease, and neoplastic pathologies.

Abstract: Heparan sulphate HS/BMP2 is disclosed, together with the use of HS/BMP2 in the repair and regeneration of bone tissue.

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

Abstract: A method for targeted delivery of therapeutic compounds from hydrogels is presented. The method involves administering to a cell a hydrogel in which a therapeutic compound is noncovalently bound to heparin. The hydrogel may contain covalent and non-covalent crosslinks.

Abstract: The present invention relates to novel silyl-derivatives of polysaccharides and their salts, the processes for their preparation and their use in cosmetic/pharmaceutical field.

Abstract: Embodiments presented herein relate to various polymers. Some of the polymer embodiments are heparin binding polymers. Some embodiments of the heparin binding polymers can be employed to bind to heparin for methods such as separating, purifying, removing, and/or isolating heparin and heparin like molecules.

Abstract: Processes are disclosed for the synthesis of the Factor Xa anticoagulant fondaparinux and related compounds. Protected pentasaccharide intermediates and efficient and scalable processes for the industrial scale production of fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions are provided.

Abstract: A functionalized electrospun matrix for the controlled-release of biologically active agents, such as growth factors, is presented. The functionalized matrix comprises a matrix polymer, a compatibilizing polymer and a biomolecule or other small functioning molecule. In certain aspects the electrospun polymer fibers comprise at least one biologically active molecule functionalized with low molecular weight heparin.

Abstract: An inhibiting heart failure disease pharmaceutical composition is provided. The pharmaceutical composition includes: an effective amount of a KMUP-3 amine salt of formula (I); wherein RX contains a carboxylic group donated from one selected from a group consisting of a sodium carboxyl methylcellulose (sodium CMC), a ?-polyglutamic acid derivative, and co-polymer salt; RX? is an anion form of the carboxylic group; and a pharmaceutically accepted carrier.

Abstract: Disclosed are polysaccharides containing residues of glucosamine or galactosamine in the repetitive unit, characterized by the presence of esters on the hydroxyls or amides on the amine functions, with lipoic acid or with mixtures of lipoic acid and formic acid.

Abstract: We provide methods and compositions for the treatment of dysregulation of blood vessel growth by regulation of neovascularization. Embodiments accomplish this by restricting the diffusion and transport of therapeutic agents through conjugating them to polymers or polymer constructs while retaining the binding affinities and functions of the therapeutic agents.

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 invention relates to composition comprising a dextran-tyramine conjugate and a conjugate selected from the group consisting of chondroitin sulphate-tyramine, collagen-tyramine, chitosan-tyramine, chitosan-phloretic acid, gelatine-tyramine, heparan sulphate-tyramine, keratin sulphate-tyramine, hyaluronic acid-tyramine and heparin-tyramine.

Abstract: Processes for the synthesis of the Factor Xa anticoagulent Fondaparinux, and related compounds are described. Also described are protected pentasaccharide intermediates as well as efficient and scalable processes for the industrial scale production of Fondaparinux sodium by conversion of the protected pentasaccharide intermediates via a sequence of deprotection and sulfonation reactions.

Abstract: The synthesized piperazium salt of KMUPs disclosed in the present invention is characterized by presented pharmaceutics having functions to improve 5-HT function and eNOS expression of KMUPS in lung diseases, such as proliferation, obliteration, pulmonary artery hypertension. The pharmaceutical composition for inhibiting monocrotaline (MCT)-induced proliferation of pulmonary artery includes an effective amount of a complex salt of formula (I): wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; RX contains a carboxylic group donated from one selected from a group consisting of a Statin, a Co-polymer, a poly-?-polyglutamic acid (?-PGA) derivative and sodium CMC; and ?RX substituent is an anion of the carboxylic group carrying a negative charge; and a pharmaceutically accepted carrier.

Abstract: Methods to generate a distinctive fingerprint (pattern of migration) for a sample of complex, polydisperse heparins are provided. The methods involve adding resolving agents such as polyamines to a heparin sample and then analyzing the sample with a technique that separates macromolecules according to charge to mass ratio (e.g. capillary electrophoresis). The resulting electropherogram is unique to and characteristic of the heparin sample. The methods may be used, for example, to monitor the quality and consistency of various heparin preparations.

Abstract: The present invention is directed to compositions comprising a polymer backbone with protective chain and anionic groups, and a cationic therapeutic agent. The present invention is directed to compositions for treating infections, inflammatory diseases, excess growth, and damaged cells and organs.

Abstract: A method for the production of heparosan from fermentation culture of E. coli K5 suitable for industrial production, exhibiting superior yield and purity, smaller culture volumes, faster growth, and lower costs.

Abstract: Described herein are compounds such as macromolecules that have been modified in order to facilitate crosslinking and methods of making and using thereof.

Abstract: The invention provides an efficient modular chemical synthesis for heparan sulfate oligosaccharides based on orthogonal protection strategies. Modular disaccharide building blocks, themselves the product of a novel combinatorial synthesis, are combined in numerous ways to produce a range of oligosaccharides.

Abstract: A new method is described for the oversulfation of epiK5-N-sulfate to obtain an epiK5-amine-O-oversulfate with very high sulfation degree which, by subsequent N-sulfation, provides new epiK5-N,O-oversulfate-derivatives with a sulfation degree of at least 4, basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are new low molecular weight epiK5-N-sulfates useful as intermediates in the preparation of the corresponding LMW-epiK5-N,O-oversulfate-derivatives.

Abstract: The present invention relates to a process for the synthesis of the Factor Xa anticoagulent Fondaparinux and related compounds. The invention relates, in addition, to efficient and scalable processes for the synthesis of various intermediates useful in the synthesis of Fondaparinux and related compounds.

Abstract: The instant invention relates to decasaccharides of formula (I): wherein Ac represents an acetyl group and R represents a group of formula —OH or —OSO3?, in their acid form or in the form of any one of their pharmaceutically acceptable salts, and to their process of preparation. The oligosaccharides of formula (I) are useful as antithrombotic agents.

Abstract: The instant invention relates to the octasaccharide of formula (I): in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.

Abstract: The instant invention relates to the decasaccharide of formula (I), wherein Ac represents an acetyl group: in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.

Abstract: A methodology for polymer grafting by a polysaccharide synthase allows the creation of a variety of glycosaminoglycan oligosaccharides that have a natural, chimeric, hybrid and/or unnatural sugar structure and/or a targeted size (i.e., substantially monodisperse in size).

Abstract: The instant invention relates to the heptasaccharide of formula (I): in its acid form or in the form of any one of its pharmaceutically acceptable salts, and to its process of preparation. The oligosaccharide of formula (I) is useful as an antithrombotic agent.

Abstract: Heparan sulphate from bone marrow stroma is disclosed together with the use of heparan sulphate from bone marrow stroma in the differentiation and/or lineage commitment of stem cells.

Abstract: The invention provides an intermediate and the process for making the same. This intermediate is useful in the process for making polysaccharides, and more particularly fondaparinux.

Abstract: This invention relates to a dose of 10 mg of AVE5026 for the treatment of venous thromboembolism in patients with severe renal impairment.

Abstract: Compositions and methods of using the compositions are provided for forming an embolus within a region of an anatomical lumen for a transitory period in order to achieve a therapeutic effect.

Abstract: Methods for analyzing mixtures of polysaccharides, for example heparin or a LMWH, using reduce end labeling are described. In general, the mixture of polysaccharides includes polysaccharides having a desired structural moiety. In some instances, one or more polysaccharides in the mixture are chemically modified prior to analysis.

Abstract: Provided are a photosensitizer-metal nanoparticle charge complex and a composition for photodynamic therapy or diagnosis containing the same. The complex includes a metal nanoparticle, a photosensitizer charged with a first charge, and a linker bound to the metal nanoparticle and charged with a second charge having an opposite polarity to the first charge. During circulation in blood, the photosensitizer-metal nanoparticle charge complex is maintained in a complex type, and thus duration of a side effect of photosensitivity can be reduced. In a tumor tissue, the complex is specifically accumulated, but in a normal tissue, it is difficult for the complex to penetrate. Thus, the complex can selectively destroy the tumor tissue. Moreover, selective fluorescence in the tumor tissue can provide further improvement in accuracy of diagnosing a tumor using the complex.

Abstract: The invention relates to a bonding product comprising at least the polysaccharides T1 and T2, characterized in that a) the monosaccharides from which the polysaccharides T1 and T2 are constructed are partially or completely bonded to each other alpha-1,4-glycosidically and b) at least one of the polysaccharides T1 and/or T2 comprises at least one amino group and c) T1 and T2 are chemically bonded to each other covalently by at least one linker Z and d) T1 and/or T2 carries m groups -(L-A), wherein A is an active pharmaceutical ingredient and/or a fluorescence label, L is a second linker, by which T1 and/or T2 is covalently bonded to A, and m is an integer, which is 0 or at least 1.

Abstract: The present invention relates to mixtures of polysaccharides derived from heparin having a mean molecular weight of 1500 to 3000 Daltons and an anti-Xa/anti-IIa ratio greater than 30, their method of preparation and pharmaceutical compositions containing them.

Abstract: Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.

Abstract: The present invention relates to cosmetological and dermatological compositions comprising heparan sulfate. The invention further discloses a process for the purification of heparan sulfate for dermatological and cosmetological applications, which process comprises the following steps: solubilization of heparan sulfate in water, adsorption on an anion exchange resin, desorption from the resin by using conditions which result in selective desorption of hepar an sulfate. The cosmetological and dermatological compositions according to the invention show, inter alia, anti-age, lenitive, and whitening effect.

Abstract: The invention provides a process for the production of a composition comprising a glycosaminoglycan, said process comprising subjecting a homogenate of glycosaminoglycan-containing animal material to chromatography using a chromatographic matrix in the form of a membrane adsorber.

Abstract: The invention relates to methods and products associated with analyzing and monitoring heterogeneous populations of sulfated polysaccharides. In particular therapeutic heparin products including low molecular weight heparin products and methods of analyzing and monitoring these products are described.

Abstract: Glycosaminoglycans derived from K5 polysaccharide having high anticoagulant and antithrombotic activity and useful for the control of coagulation and as antithrombotic agents are obtained starting from an optionally purified K5 polysaccharide by a process comprising the steps of N-deacetylation/N-sulfation, C5 epimerization, O-oversulfation, selective O-desulfation, 6-O-sulfation, N-sulfation, and optional depolymerization, in which said epimerization is performed with the use of the enzyme glucoronosyl C5 epimerase in solution or in immobilized form in the presence of divalent cations. New, particularly interesting antithrombin compounds are obtained by controlling the reaction time in the selective O-desulfation step and submitting the product obtained at the end of the final N-sulfation step to depolymerization.

Abstract: Described herein are composites useful in tissue and organ engineering. In one aspect, the composite comprises the reaction product between a macromolecule comprising at least one thiol group and a gold nanoparticle. The thiolated macro-molecule crosslinks with the gold nanoparticle to produce a composite that is useful in anchoring cells. The composites can be used to form multi-layer 3-D structures, where the cells in each layer can aggregate and fuse with one another to form tissues and organs.

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: The present invention relates to pharmaceutical compositions which are useful in the treatment of diseases where excess mucus is present in the respiratory tract, such as cystic fibrosis and chronic obstructive pulmonary disease. In particular, the invention relates to pharmaceutical compositions for administration by pulmonary inhalation.

Abstract: Neutrophil elastase (NE) is a protease secreted by neutrophils during inflammation. Aberrant expression of NE such as in chronic respiratory inflammatory diseases, results in tissue destruction and decline in lung function. Compositions including an NE-targeting agent that targets the pathologic elements of respiratory inflammation are provided. Non-anticoagulant heparin derivatives or fragments are exemplary NE-targeting agents. The compositions preferably include a carrier, such as chitosan, to facilitate delivery of the active agent. Methods of manufacturing non-anticoagulant heparin are also provided. Methods of administering the disclosed compositions to treat respiratory diseases are also disclosed. In preferred methods, an effective amount of the pharmaceutical composition is administered to subject in need thereof to reduce, inhibit, or alleviate one or more symptoms of chronic respiratory inflammation.