Anthracycline derivatives having cytostatic activity

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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C07H 1524

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active

052604250

ABSTRACT:
The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.7 is an organic substituent which has 2 to 6 carbon atoms and which contains at least one oxygen, nitrogen or sulfur atom or a C--C double bond or a C--C triple bond, it being possible for the double bond also to be a constituent of a heteroaromatic system and for the oxygen, nitrogen or sulfur atom to be a constituent of an open-chain or heterocyclic system, to a process for the preparation thereof and to the use thereof in a pharmaceutical.

REFERENCES:
patent: 4591637 (1986-05-01), Acton et al.
patent: 4888418 (1989-12-01), Kawai et al.
patent: 4948880 (1990-08-01), Hermentin et al.
Umezawa et al., "Daunomycin and Adriamycin Derivatives," Chemical Abstracts, vol. 92, No. 17, Item No. 147142f, (1980).
Acton et al., "N-(2-Hydroxyethyl)doxrubicin from Hydrolysis of 3'-Deamino-3'-(3-cyano-4-morpholinyl)doxorubicin", Journal of Medicinal Chemistry, (1986), pp. 2120-2122.
Hermentin et al., 4th European Carbohydrate Symposium, Darmstadt, FRG, Jul. 12-17, 1987.
Tong et al., J. Med. Chem., vol. 22, No. 8, 1979, pp. 912-918.

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