Derivatives of doxorubicine, their preparation and use

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 17A, 2603457R, A61K 3171, C07H 1524

Patent

active

042961050

ABSTRACT:
New derivatives of doxorubicine of the formula ##STR1## wherein R represents a radical of the formula ##STR2## wherein R.sub.1 represents hydrogen, alkyl (possibly substituted with amino, alkylamino, dialkylamino, hydroxy, mercapto or methylthio), phenyl, benzyl (possibly substituted with one or more hydroxy) and R.sub.2 represents hydrogen or forms with R.sub.1 an alkylene radical, the salts thereof and pharmaceutical compositions containing said compounds.
They are prepared according to methods known in peptidic chemistry by reacting a reactive form of an aminoacid of the formula ##STR3## with doxorubicine.

REFERENCES:
patent: 3665018 (1972-05-01), Jolles
patent: 4012448 (1977-03-01), Smith et al.
patent: 4077988 (1978-03-01), Arcamone et al.

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