Abstract: The present disclosure relates to synthesis of heparin, which may be bioequivalent to porcine USP Heparin Sodium. The synthesis may involve three intermediates starting from heparosan.

Abstract: The present invention provides improved processes of preparing Fondaparinux sodium comprising converting a compound of formula ABCDE4 to Fondaparinux sodium at a reaction pH of no more than about 9.0. In some embodiments, the intermediates for the synthesis of Fondaparinux sodium, are also provided.

Abstract: Methods and systems for synthesizing heparin compounds are provided. The chemoenzymatic synthesis of structurally homogeneous low molecular weight heparins that have a reversible anticoagulant activity is provided. Also disclosed are heparin compounds having anticoagulant activity, including a binding affinity to antithrombin and an anti-Xa activity, but no detectable anti-lla activity. Additionally, provided are synthetic, low-molecular weight heparin compounds with reversible anticoagulant activity, where the anticoagulant activity is reversible by protamine.

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 ratio 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 ratio as that of the conventionally known gel.

Abstract: A prodrug comprising a heparin and a drug is provided. The prodrug can be used to form a coating on a medical device. The prodrug can also be used with a polymeric material to form a coating on a medical device. The polymeric material can be a hydrophobic polymer, a hydrophilic polymer, a non-fouling polymer, or combinations thereof. The medical device can be implanted in a human being for the treatment of a disease such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, or combinations thereof.

Abstract: Methods of evaluating heparin preparations, e.g., for suitability for use as a drug or for use in making a drug, by determining the absence, presence or amount of a structural signature, wherein, e.g., the structural signature is indicative of the methods used to make the heparin preparation.

Abstract: The present invention provides; a novel gene introduction method which enables a gene to be introduced more safely and more freely, particularly a method for introducing a gene into a specified site in the brain safely and freely; a carrier for gene introduction use, which comprises a nano-particle and a substance capable of binding to a vector for gene introduction and has functional groups involved in the induction of phagocytosis by cells, wherein the substance capable of binding to a vector for gene introduction can bind to the surface of the nano-particle through some of the functional groups and another some of the functional groups remain unbound to the substance capable of binding to a vector for gene introduction; and a gene introduction agent, in which a vector for gene introduction is bound to the substance capable of binding to a vector for gene introduction in the carrier for gene introduction.

Abstract: Compositions containing conjugates of heparosan polymer with at least one drug are disclosed, along with methods of production and use thereof.

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 provides a high purity heparin useful to be a pharmaceutical product, cosmetics, research reagent, or the like, and a method for producing the same, more specifically, a heparin which does not substantially contain a nitrous acid degradation-resistant impurity and a method for producing a heparin, comprising mixing an aqueous solution of 5 to 30% by weight of the heparin with ethanol having an amount (volume) 0.2 to 1 times the amount (volume) of the aqueous heparin solution to obtain a colloidal precipitate of heparin.

Abstract: The present invention relates to immobilized biologically active entities that retain significant biological activity following mechanical manipulation of a substrate material to which the entities are immobilized.

Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.

Abstract: The present invention relates to a method of treating or preventing transthyretin amyloidosis, pharmaceutical composition for use in said treatment or prevention, as well as to a diagnostic method and a kit.

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 present invention relates to a chemically modified glycosaminoglycan with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw, weight average) from about 4.6 to 6.9 kDa. Also disclosed is a method of preparing the modified glycosaminoglycan and its medical uses.

Abstract: The present invention relates to chemically modified heparin for use in the treatment of sickle cell disease, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa.

Abstract: The present invention provides methods for the production of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, compounds thus obtained and compositions comprising same. This invention also provides applications of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides, and compositions comprising same, for use in controlling coagulation and treating thrombosis.

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: The present invention relates to pharmaceutical preparations comprising one or more Factor VIII and a sulfated glycosaminoglycan for increasing the bioavailability of Factor VIII upon non-intravenous administration. The invention further relates to the combined use of Factor VIII and a sulfated glycosaminoglycan for the treatment and prevention of bleeding disorders, whereby the bioavailability of Factor VIII is increased, and to a method for increasing the bioavailability after non-intravenous administration of Factor VIII by coadminstration of a sulfated glycosaminoglycan.

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: In one embodiment, the invention provides a method of treating, reducing the incidence, reducing the severity or pathogenesis of an eye disease or disorder in a subject, including, inter alia, retinal detachment, macular degeneration, glaucoma or retinopathy, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof. This invention also provides a contact lens solution comprising a lipid or phospholipid moiety bound optionally via a spacer to a physiologically acceptable monomer, dimer, oligomer, or polymer via an ester or amide bond, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.

Abstract: According to the present invention, treatment of prion protein related diseases, and in particular cancer tumours, is effected by providing to a subject in need thereof a therapeutically effective amount of an agent capable of modulating binding of a prion protein and/or a prion-like protein to a disease related GAG and/or HSPG.

Abstract: Procedure for the synthesis of deprotected pentasaccharides from a protected precursor pentasaccharide through a reaction procedure having five stages whereamong is included an N-sulphation of amino groups and a hydrogenolysis of benzyl groups. Through this procedure a drastic reduction is achieved in the total synthesis time in comparison with the process traditionally employed, together with increased reproducibility thereof, permitting the standardization thereof.

Abstract: There is provided inter alia a substrate with a surface having a hydrophilic coating comprising a cross-linked copolymer of components A and B, and optional components C and D; wherein component A comprises one or more C2-C16 hydrophilic monomers each bearing one or more alkene and/or alkyne groups; component B comprises one or more hydrophilic polymers each bearing two or more alkene and/or alkyne groups; component C, if present, comprises one or more beneficial agents each bearing one or more alkene or alkyne groups; and component D, if present, comprises one or more low molecular weight cross-linking agents each bearing two or more functional groups independently selected from thiol, alkene and alkyne groups; wherein the cross-linked copolymer is formed by radical polymerisation involving the alkene and/or alkyne groups of components A, B and C (if present) and involving the functional groups of component D (if present); wherein the hydrophilic coating optionally comprises component E which comprises on

Abstract: Biomaterial compositions that include an isolated heparosan polymer are disclosed, as well as kits containing such biomaterial compositions and methods of producing and using such biomaterial compositions.

Abstract: The present disclosure provides polymer compounds binding with lipoamide produced by the reaction of the primary amine group of lipoamide with the carboxy group of polysaccharide compounds such as chondroitin sulfates, carboxymethyl celluloses, or hyaluronic acids; functional compounds such as peptides, proteins, growth factors; or drugs; or biocompatible polymers such as poly(ethylene oxide), poly(vinyl alcohol), or poly(vinyl pyrrolidone). The present disclosure also provides their synthesis methods, products of hydrogels and films using the same as and methods for manufacturing the products.

Abstract: The present invention relates to a method for preparation of heparin silver, to use of heparin silver in manufacture of medicine for treating burns and/or scalds, to a method of using heparin silver to treat burns and/or scalds, and to a topical preparation containing heparin silver for treating burns and/or scalds. The heparin silver product prepared according to the method of the present invention has a high purity and less impurity. The animal test proved that the medicine made by using heparin silver exhibited effects of accelerating wound healing and reducing scar formation.

Abstract: A multi-arm polyethylene glycol (I) having different kinds of reactive groups and the uses thereof are disclosed, which is formed by polymerizing ethylene oxide with oligo-pentaerythritol as an initiator, wherein, PEG is same or different and is —(CH2CH2O)m—, the average value of m is an integer of 2-250; l is an integer of 1 or more. The method for producing the multi-arm polyethylene glycol having different kinds of reactive groups, the multi-arm polyethylene glycol active derivatives comprising linking groups X attached to PEG and terminal reactive groups F attached to X, the gels formed by the multi-arm polyethylene glycol active derivatives, the drug conjugates formed by the multi-arm polyethylene glycol active derivatives and drug molecules, and the uses thereof in preparing drugs are also disclosed.

Abstract: The present invention relates to immobilized biologically active entities that retain a significant biological activity following manipulation. The invention also comprises a medical substrate comprising a heparin entity bound onto a substrate via at least one heparin molecule, wherein said bound heparin entity is heparinase-1 sensitive.

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: Methods of evaluating heparin preparations, e.g., for suitability for use as a drug or for use in making a drug, by determining the absence, presence or amount of a structural signature, wherein, e.g., the structural signature is indicative of the methods used to make the heparin preparation.

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 present invention relates to a device for extracorporeal removal of harmful agents from blood or blood components, comprising full length heparin immobilized on a solid substrate by covalent end point attachment. The present invention also relates to a method for extracorporeal removal of a harmful agent from mammalian blood or blood components. The present invention further relates to a process for covalent end point attachment of full length heparin to a solid substrate.

Abstract: Disclosed are glycan immobilized metal nanoparticles and a method used thereof for detecting HIV-1 in a saliva sample at early stages of viral infection. The method comprises the steps of: (A) providing glycan immobilized metal nanoparticles which can recognize HIV-1; (B) contacting the glycan immobilized metal nanoparticles with the saliva sample and a mixture is obtained; (C) concentrating the mixture; and (D) determining HIV-1 in the concentrated mixture by an appropriate detecting method.

Abstract: The invention relates to sulphated polysaccharides which have the general structure of the constituent polysaccharides of heparin and which have a molecular weight of less than 8000 Daltons, comprising two antithrombin III-binding hexasaccharide sequences corresponding to formula (I) in which: R1 represents an OH group when the hexasaccharide of formula (I) is located at the reducing end of the polysaccharide, or else R1 represents a bond with another saccharide unit of said polysaccharide; R2 represents a hydrogen atom when the hexasaccharide of formula (I) is located at the non-reducing end of the polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit of said hexasaccharide is a double bond, or else R2 represents a bond with another saccharide unit of said polysaccharide, in which case the bond between carbon atoms 4 and 5 of the first saccharide unit is a single bond.

Abstract: Polysaccharide preparations lacking substantial anticoagulant activity are provided herein. Methods of making and using such preparations are provided.

Abstract: Methods for preparing synthetic heparins are provided. Synthetic heparin compounds, including ultralow molecular weight heparin compounds are provided. Also provided are methods of chemoenzymatically synthesizing structurally homogeneous ultra-low molecular weight heparins. Heparin compounds provided herein can have anticoagulant activity.

Abstract: The invention concerns novel biotinylated hexadecasaccharides of general formula (I) wherein: Biot is a biotin derivative; R, R1 and R2, represent independently of one another a C1-C6 alkoxy or and —OSO3; R3 represents a C1-C6 alkoxy or an —OSO3, or R3 constitutes a —O—CH2— bridge; Pe represents a saccharide concatenation; as well as their pharmaceutically acceptable salts, and their use as medicines.

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: This disclosure relates to methods and compositions for treating cancer with platinum particles. In certain embodiments, the disclosure relates to platinum particle coated with a polysaccharide, such as a heparin or modified heparin, conjugated to a polypeptide that has affinity for a cell surface cancer marker and uses related thereto.

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 present invention is related to compositions which can undergo targeted degradation under certain physiological reducing conditions. The compositions may, for example, be hydrogels in which maleimide-functionalized low molecular weight heparin is cross-linked with various thiol-functionalized polyethylene glycol multi-arm star polymers. Both the gelation and degradation of the hydrogels can be modified by careful selection of the thiol. For example, hydrogels prepared from aryl thiol-maleimide adducts can undergo a retro Michael addition-type reaction, leading to degradation of the composition and release of the bioactive molecule.

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 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: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.

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: The present invention provides a high purity heparin useful to be a pharmaceutical product, cosmetics, research reagent, or the like, and a method for producing the same, more specifically, a heparin which does not substantially contain a nitrous acid degradation-resistant impurity and a method for producing a heparin, comprising mixing an aqueous solution of 5 to 30% by weight of the heparin with ethanol having an amount (volume) 0.2 to 1 times the amount (volume) of the aqueous heparin solution to obtain a colloidal precipitate of heparin.

Abstract: Methods and compositions related to promoting hair growth are described.

Abstract: The embodiments provide a carbon nanocapsule conjugated with at least one of the anticoagulants on the surface and an antithrombotic drug containing the anticoagulant-conjugated carbon nanocapsule as an active ingredient. The anticoagulant-conjugated carbon nanocapsule has less cytotoxicity and good biocompatibility. A method for preparing the anticoagulant-conjugated carbon nanocapsule is also provided.

Abstract: Methods of evaluating heparin preparations, e.g., for suitability for use as a drug or for use in making a drug, by determining the absence, presence or amount of a structural signature that is indicative of the methods used to make the heparin preparation.