TAXANES COVALENTLY BONDED WITH HYALURONIC ACID OR HYALURONIC ACID DERIVATIVES Russian patent published in 2010 - IPC C08L5/08 C08B37/00 A61K47/36 A61P35/00 

Abstract RU 2384593 C2

FIELD: chemistry.

SUBSTANCE: invention relates to taxane, especially to paclitaxel and docetaxel covalently bonded with hyaluronic acid or a hyaluronic acid derivative, used as active substance in pharmaceutical compositions which are used in oncology, for treating tumours, autoimmune diseases and restenosis, as well as a coating for stents and medical devices. The covalent bond is formed between hydroxyl groups of taxane and carboxyl groups or hydroxyl groups of hyaluronic acid or hyaluronic acid derivatives, or amino groups of deacetylated hyaluronic acid. Bonding can take place using a linking compound (spacer compound) which bonds taxane with hyaluronic acid or hyaluronic acid derivative under the condition that, the linking compound is different from hydrazide.

EFFECT: proposed taxane has high therapeutic effectiveness when treating oncological diseases, autoimmune diseases and restenosis, dissolves in water without reduction of its pharmacological activity and is not toxic, which leads to overcoming hypersensitivity and anaphylaxis.

46 cl, 20 ex, 4 dwg

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RU 2 384 593 C2

Authors

De Luka Dzhil'Da

Marini Bettolo Rinal'Di

Min'Eko Luiza Marija

Dates

2010-03-20Published

2003-10-10Filed