NEW ADRIAMYCIN DERIVATIVE

PURPOSE:To obtain a new, lowly toxic and sustainedly releasable adriamycin derivative excellent in carcinostatic activity in a wide dose range by chemically combining adriamycin with cyclodextrin through a dicarboxylate. CONSTITUTION:An adriamycin derivative of formula I (wherein R is a bivalent hyd...

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Main Authors TANAKA HIROSHI, OKAMOTO ROKURO, YOSHIOKA TAKEO, YAMAMOTO REIKO, TONE HIROSHI, HIRANO SHINICHI, IGUCHI HIROSHI, OKAJIMA YASUO, KOMINATO KAICHIRO, NISHIDA HIROSHI, SHIRAI MASATAKA
Format Patent
LanguageEnglish
Published 19.01.1993
Subjects
CHEMISTRY
COMPOSITIONS BASED THEREON
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
ORGANIC MACROMOLECULAR COMPOUNDS
POLYSACCHARIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
THEIR PREPARATION OR CHEMICAL WORKING-UP
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Summary:PURPOSE:To obtain a new, lowly toxic and sustainedly releasable adriamycin derivative excellent in carcinostatic activity in a wide dose range by chemically combining adriamycin with cyclodextrin through a dicarboxylate. CONSTITUTION:An adriamycin derivative of formula I (wherein R is a bivalent hydrocarbon group; CD is a cyclodextrin residue; m is 1-8; and n is 0-8), which can be produced, for example, by acylating cyclodextrin, desirably gamma-cyclodextrin with a dicarboxylic acid of formula II or its acyl-forming derivative and reacting the acylated cyclodextrin of formula III (wherein Y is a cation) with 14- halodaunomycin or its salt. When this derivative is used as a carcinostatic agent for the treatment of a cancer, it is orally or parenterally administered in a dose of usually 0.1-20mg/kg/day (in terms of the weight of adriamycin).
Bibliography:Application Number: JP19910268608