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Anti-tumor bioconjugates of hyaluronic acid or its derivatives obtained by indirect chemical conjugation, and its use in the pharmaceutical field
专利权人:
FIDIA FARMACEUTICI S.P.A.
发明人:
RENIER, Davide,BETTELLA, Fabio
申请号:
ES06762981
公开号:
ES2596877T3
申请日:
2006.08.02
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Chemical-pharmaceutical conjugates of hyaluronic acid and / or its derivatives obtained through an indirect bond between the polysaccharide and a drug with an antitumor action, through a molecular spacer that forms an ester bond with the carboxylic group of HA and / or its derivative, with the proviso that said separator is not a hydrazide or a polypeptide, the drug being a nitrosourea, and the hyaluronic acid derivative being selected from - HA salified with organic and / or inorganic bases having a molecular weight of 50 -730 KDa or a high molecular weight of 750-1230 KDa; - HA esters with aliphatic, araliphatic, cycloaliphatic, aromatic, cyclic and heterocyclic series alcohols, with an esterification percentage that varies depending on the type and length of the alcohol used, from 1 to 75%; - HA amides with aliphatic, araliphatic, cycloaliphatic, aromatic, cyclic and heterocyclic series amines, with an amidation percentage ranging from 1 to 10%; - O-sulfated derivatives of HA up to the 4th degree of sulphation; - internal esters of HA with a percentage of internal esterification ranging from 0.5 to 10% and preferably 5%; - HA deacetylates derived from the deacetylation of the N-acetyl-glucosamine fraction with a percentage of deacetylation preferably varying from 0.1 to 30%; - percarboxylated derivatives of HA obtained from the oxidation of the primary hydroxyl of the N-acetylglucosamine fraction with a degree of percarboxylation ranging from 0.1 to 100%.Conjugados químico-farmacéuticos de ácido hialurónico y/o sus derivados obtenidos a través de un enlazamiento indirecto entre el polisacárido y un fármaco con una acción antitumoral, a través de un espaciador molecular que forma un enlace éster con el grupo carboxílico de HA y/o su derivado, con la condición de que dicho separador no es una hidrazida o un polipéptido, siendo el fármaco una nitrosourea, y el derivado de ácido hialurónico siendo seleccionado de - HA salificado con bases orgánicas y/o inorgánicas qu
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