摘要:
A new method is described for the oversulfation of (epi)KS-N-sulfates to obtain (epi)K5-amine-O-oversulfates at extremely high degree of sulfation and for the transformation of these intermediates into new Nacyl-(epi)K5-amine-O-oversulfates basically free of activity on the coagulation parameters and useful in the cosmetic or pharmaceutical field. Also described are pharmaceutical compositions containing, as one of their active ingredients, an (epi)K5-amine-O-oversulfate.
摘要:
Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. Said glycosaminoglycan derivatives are endowed with antiangiogenic and heparanase-inhibiting acitivity ans are devoid of anticoagulant activity.
摘要:
The invention relates to a process for the depolymerization of glycosaminoglycanes characterized by the use of high-energy radiation in the presence of an organic compound selected from the group consisting of ethers, alcohols, aldehydes, amides and formic acid. The invention also relates to intermediate depolymerized heparin having Mw comprised between 1,000 and 5,500, absorbance at 400 nm below 0.300 and ratio SO 3 - /COO - equal to or higher than in the starting heparin. The intermediate depolymerized heparin can be dissolved in a buffer solution and fractionated by Gel Permeation for obtaining the desired Molecular Weight.
摘要:
The invention concerns cross-linked copolymers with a base of non cross-linked polycarboxylic polymers, said copolymers containing at least one polycarboxylic polysaccharide. The invention also concerns a method for preparing these copolymers and their use in particular as support in pharmaceutical compositions.
摘要:
The present invention relates to a process for preparing surface modifications having an improved antithrombogenic activity, whereby the improvement is achieved by treating heparin at elevated temperature or at elevated pH or in contact with nucleophilic catalysts such as amines, alcohols, thiols or immobilized amino, hydroxyl or thiol groups before attaching said heparin to the surface to be modified.
摘要:
Substances comprising carboxylated and/or sulfated oligosaccharides in substantially purified form, including compositions containing same and methods of using same, are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of Tumor Necrosis Factor Alpha (TNF- alpha ) can be either inhibited or augmented selectively by administration to the host of effective amounts of substances or their compositions comprising specific oligosaccharides in substantially purified form. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF- alpha . The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be daily, at very low effective doses, typically below 0.1 mg/kg human, or at intervals of up to about 5-8 days, preferably once a week.
摘要:
A heparin complex having anticoagulation activity and being insoluble in blood is provided. The preferred complex comprises a cationic alkyldimethylammonium represented by formula (1): wherein R 1 and R 2 are independently an alkyl or alkenyl group, each group is C 12 -C 24 when R 1 and R 2 are the same, the sum of the carbon atoms are 26-38 when R 1 and R 2 are different; and heparin. In this complex, reduction in the anticoagulation activity of the heparin by the formation of the complex is minimized, and ionic bonding of the heparin is quite stable. Dissolution of the cationic alkyldimethylammonium from the coating is also minimized. A medical device coated with such substance is also provided.