METHOD FOR PREPARING HEPARIN CONJUGATES Russian patent published in 2007 - IPC A61K31/727 A61K31/715 

FIELD: chemistry, biochemistry.

SUBSTANCE: invention relates to a method for preparing novel substances representing derivatives of heparin that can be used in medicine and pharmacology. Method is carried out by interaction of heparin with amino-containing compounds in the presence of 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide (EDC) as a condensing agent in an aqueous medium at room temperature and pH = 4.7-4.8. The following pharmacologically active amines are used a amino-containing compounds: p-aminophenol, p-aminobenzoic and anthranilic acids, 4- and 5-aminosalicylic acids, streptocid, sulfacyl-sodium, anesthesin, novocain, taurine (taufon), 7-aminocephalosporinic acid and isoniazid (isonicotinic acid hydrazide) also. Depending on nature of amino-containing compound and the ratio of reagents method provides preparing modified water-soluble heparins with different conversion of carboxyl groups. The advantage of proposed method involves carrying out reaction for short time providing the high conversion of carboxy-groups of heparin and using small excesses of reagents R-NH₂ : EDC = 1:(1-3):(0.75-3.00), respectively. Variation of the ratio of component provides preparing modified heparins with the required conversion degree of carboxy-groups. Method provides easy purification of conjugates from low-molecular impurities and good water-solubility of synthesized conjugates of heparin. Prepared derivatives of heparin an be used in medicine and pharmacology.

EFFECT: improved preparing method.

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