The tetracyclic anthraquinones possessing anti-cancer effect

A - Human Necessities – 61 – K

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A61K 31/704 (2006.01) A61K 9/02 (2006.01) A61K 9/06 (2006.01) A61K 9/08 (2006.01) A61K 9/107 (2006.01) A61K 9/127 (2006.01) A61K 9/19 (2006.01) A61K 9/70 (2006.01) A61K 38/14 (2006.01) A61P 35/00 (2006.01) C07H 15/252 (2006.01)

Patent

CA 2676105

The present invention provides aminoside tetracyclic anthraquinones represented by formula I or II, wherein the piptides are introduced to connect tetracyclic anthraquinones and fatty acid saturated or unsaturated in order to make the anticancer agents to be absorbed and released selectively; meanwhile some water-solubility groups are also introduced into the branched chain, aminosaccharide and tetracyclic moiety of the compounds to improve the water-solubility. The present invention also provides the preparative method and the use thereof as pharmaceutically active components for treating the diseases cured by aminoside tetracyclic anthraquinone, for example cancer, such as intestines, liver, gastric, breast, lung, ovary, prostate, brain glioma, lymph, skin, pigment, thyroid gland, multiple bone marrow cancer and leukemia.

La présente invention concerne des anthraquinones tétracycliques d'aminoside de formule I et II, dans lesquels des peptides sont introduits pour lier les anthraquinones tétracycliques et un acide gras saturé ou insaturé afin de produire des agents anticancéreux destinés à être adsorbés et libérés de manière sélective ; des groupes à caractère hydrosoluble sont également introduits dans la chaîne ramifiée, un aminosaccharide et un groupe fonctionnel tétracyclique des composés pour améliorer le caractère hydrosoluble. La présente invention concerne également un procédé de préparation et d'utilisation desdits composés en tant que constituants pharmaceutiquement actifs pour traiter des maladies soignées par l'anthraquinone tétracyclique d'aminoside, telles que le cancer de l'intestin, du foie, gastrique, du sein, du poumon, de l'ovaire, de la prostate, le gliome cérébral, de la lymphe, de la peau, pigmentaire, de la glande thyroïde, le cancer multiple de la moelle osseuse et la leucémie.

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