Patent classifications
C08B37/0063
CARBOXYLATED DERIVATIVES OF GLYCOSAMINOGLYCANS AND USE AS DRUGS
A glycosaminoglycan derivative endowed with heparanase inhibitory activity and antitumor activity, bearing carboxylate groups in positions 2 and 3 of at least part of the glycosaminoglycan residues, and to the process for preparing the same. The glycosaminoglycan derivatives of the present invention are generated starting from natural or synthetic glycosaminoglycans, preferably heparin or low molecular weight heparin, optionally 2-O- and 2-N-desulfated by two steps of oxidation. By the first oxidation, adjacent dials and optionally adjacent OH/NH.sub.2 of the glycosaminoglycan residues are converted to aldehydes and by the second oxidation said dialdehydes are converted to carboxylate groups. The first oxidation preferably leads to the cleavage of C2-C3 linkage of the ring of oxidable residues. The invention relates to a process for the preparation of said glycosaminoglycan derivatives and to their use as active ingredients of medicaments.
Methods for making saccharide-protein glycoconjugates
The invention provides a process for the reductive amination of a carbonyl group at the reducing terminus of a polysaccharide, wherein the reductive amination is carried out at a pH between 4 and 5. The invention also provides a process for preparing a conjugate of a polysaccharide and a carrier molecule, comprising the steps of: (a) coupling the polysaccharide to a linker, to form a polysaccharide-linker compound in which the free terminus of the linker is an ester group; and (b) reacting the ester group with a primary amine group in the carrier molecule, to form a polysaccharide-linker-carrier molecule conjugate in which the linker is coupled to the carrier molecule via an amide linkage. The invention also provides a process for reducing contamination of a polysaccharide-linker compound with unreacted linker, comprising a step of precipitating unreacted linker under aqueous conditions at a pH of less than 5. The invention also provides polysaccharide-linker-carrier molecule conjugates and intermediate compounds obtained or obtainable by these processes.
CARBOXYLATED DERIVATIVES OF GLYCOSAMINOGLYCANS AND USE AS DRUGS
A glycosaminoglycan derivative endowed with heparanase inhibitory activity and antitumor activity, bearing carboxylate groups in positions 2 and 3 of at least part of the glycosaminoglycan residues, and to the process for preparing the same. The glycosaminoglycan derivatives of the present invention are generated starting from natural or synthetic glycosaminoglycans, preferably heparin or low molecular weight heparin, optionally 2-O- and 2-N-desulfated by two steps of oxidation. By the first oxidation, adjacent dials and optionally adjacent OH/NH.sub.2 of the glycosaminoglycan residues are converted to aldehydes and by the second oxidation said dialdehydes are converted to carboxylate groups. The first oxidation preferably leads to the cleavage of C2-C3 linkage of the ring of oxidable residues. The invention relates to a process for the preparation of said glycosaminoglycan derivatives and to their use as active ingredients of medicaments.
Preparation and/or formulation of proteins cross-linked with polysaccharides
Therapeutic compositions and/or formulations are provided, comprising: at least one cross-linked protein matrix, wherein the at least one cross-linked protein matrix comprises at least one protein residue and at least one saccharide-containing residue, and methods of producing the same. The cross-linked protein matrix may be derived from cross-linking a full length or substantially full length protein, such as tropoelastin, elastin, albumin, collagen, collagen monomers, immunoglobulins, insulin, and/or derivatives or combinations thereof, with a saccharide containing cross-linking agent, such as a polysaccharide cross-linking agent derived from, for example, hyaluronic acid or a cellulose derivative. The therapeutic compositions may be administered topically or by injection. The present disclosure also provides methods, systems, and/or kits for the preparation and/or formulation of the compositions disclosed herein.
High concentration chitosan-nucleic acid polyplex compositions
The invention provides highly concentrated chitosan-nucleic acid polyplex compositions and dispersions, and methods for producing the compositions and dispersions. Methods of mixing the chitosan-nucleic acid polyplexes include an inline mixing of chitosan solution and nucleic acid solution, followed by further concentrating the dispersion of chitosan-nucleic acid polyplexes, optionally with an aggregation inhibitor. Further provides are methods for altering the diameter of chitosan-nucleic acid polyplexes.
METHOD OF PREPARING A HYDROGEL PRODUCT
A method of preparing a hydrogel product comprising crosslinked glycosaminoglycan molecules, comprising the steps of: (a) providing a mixed solution of glycosaminoglycan molecules, a di- or multinucleophilic functional crosslinker, and a mononucleophilic functional graft chain; (b) activating carboxyl groups on the glycosaminoglycan molecules with a coupling agent to form activated glycosaminoglycan molecules; and (c) simultaneously crosslinking the activated glycosaminoglycan molecules and grafting the graft chain to the activated glycosaminoglycan molecules by reacting the nucleophiles with the activated carboxyl groups.
NOVEL POLYSACCHARIDE AND USES THEREOF
Provided herein is an E. coli O polysaccharide, O25B. Also provided herein are prokaryotic host cells containing enzymes (e.g., glycosyltransferases) used in O25B production. The host cells provided herein produce O25B bioconjugates, wherein said bioconjugates contain O25B linked to a carrier protein. Further provided herein are compositions, e.g., pharmaceutical compositions, including O25B and/or bioconjugates containing O25B. Such compositions can be used as vaccines against infection with ExPEC, and may further include one or more additional bioconjugates.
Hydrophilic copolymer with pendant thiol groups
The invention is related to a class of hydrophilic copolymers comprising loosely dangling thiol-containing pendant groups. The hydrophilic copolymers are highly reactive towards azetidinium groups of an azetidinium-containing polymer upon heating and can find particular use in for producing water-soluble highly-branched hydrophilic polymeric material useful for producing water gradient contact lenses.
EXPEC GLYCOCONJUGATE VACCINE FORMULATIONS
Compositions and methods for inducing an immune response against extra-intestinal pathogenic Escherichia coli (ExPEC) are described. In particular, multivalent vaccines containing O-antigen polysaccharide covalently bound to an exotoxin A of Pseudomonas aeruginosa (EPA) carrier protein that can withstand multiple environmental stresses are described.
Process for isolating fucoidan and laminarin from live, harvested seaweed
The present invention is directed to a process for obtaining at least one of fucoidan and laminarin from live, harvested seaweed, wherein the process comprises the steps of: (i) harvesting seaweed comprising fucoidan and laminarin to obtain live, harvested seaweed, wherein the live, harvested seaweed exudes to form an exudate solution; (ii) collecting the exudate solution from the live, harvested seaweed, wherein the fucoidan and laminarin are dissolved in the exudate solution; and (iii) separating the at least one of fucoidan or laminarin from the exudate solution.