CAMPTOTHECIN DERIVATIVE

PROBLEM TO BE SOLVED: To obtain the subject compound which can manifest antitumor action without side-effect and is useful for treatment of solid tumors such as lung cancer by bonding a polysaccharide bearing a carboxyl group through an amino acid or a peptide to camptothecin acid bearing a reactive...

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Bibliographic Details
Main Authors KAWAGUCHI TAKAYUKI, TSUJIHARA KENJI, YANO TOSHIRO, OKUNO SATORU
Format Patent
LanguageEnglish
Published 17.03.1998
Edition6
Subjects
CHEMISTRY
COMPOSITIONS BASED THEREON
DERIVATIVES THEREOF
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
ORGANIC MACROMOLECULAR COMPOUNDS
PEPTIDES
POLYSACCHARIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
THEIR PREPARATION OR CHEMICAL WORKING-UP
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Summary:PROBLEM TO BE SOLVED: To obtain the subject compound which can manifest antitumor action without side-effect and is useful for treatment of solid tumors such as lung cancer by bonding a polysaccharide bearing a carboxyl group through an amino acid or a peptide to camptothecin acid bearing a reactive group. SOLUTION: This compound has a moiety of (A) a compound of formula I [R is a (substituted) lower alkyl; X is a group of the formula: NHR (R is H, a lower alkyl), OH; Alk is a (branched) alkylene which may be bridged with O atoms] and another moiety of (B) a polysaccharide bearing a carboxyl group in which the moieties (A) and (B) are linked to each other through (C1 ) an amino acid or (C2 ) a peptide and also may be in the salt form, typically exemplified by formula II (CM is carboxymethyl). The typified compound is prepared is prepared by reaction of sodium carboxymethylated dextran with 7-ethyl-10- 2'-[2''-(glycyl-glycyl-L-phenyl-alanyglycylamino)ethyloxy]ethyloxy}-(20 S)-camptothecin hydrochloride.
Bibliography:Application Number: JP19960198939