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US 5,294,701 AGranted
Anthracycline compounds and intermediates
AssigneePharmachemie B.V.
InventorsJohan W. Scheeren, Joannes F. M. de Bie, Dirk de Vos
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Abstract
This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.
Claims15
A compound of formula (1):
- ##STR53## wherein R is --COCH.sub.3 or --C.tbd.C--R.sub.4 ;
- R.sub.4 is H or --Si(CH.sub.3).sub.3 ;
- R.sub.1 and R.sub.2 represent H or together form a group --CR.sub.5 .dbd.CR.sub.6 --CR.sub.7 .dbd.CR.sub.8 --, --CR.sub.9 .dbd.CR.sub.10 --CR.sub.11 .dbd.N-- or --N.dbd.CR.sub.9 --CR.sub.10 .dbd.CR.sub.11 ;
- each of the symbols R.sub.5, R.sub.6, R.sub.7, and R.sub.8 represents H or a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or an --OH group;
- each of the symbols R.sub.9, R.sub.10 and R.sub.11 represents H or a C.sub.1 -C.sub.3 alkyl group;
- R.sub.12 is H or ##STR54## R.sub.3 is H or --COCF.sub.3 ;
- R.sub.13 is H or ##STR55## or a pharmaceutically acceptable acid addition salt thereof;
- with the exclusion of compounds where
- R is --COCH.sub.3 or --C.tbd.CH and R.sub.1 and R.sub.2 form a group --CR.sub.5 .dbd.CR.sub.6 --CR.sub.7 .dbd.CR.sub.8 --, or an acid addition salt of an excluded compound.
6 more elements
Dependencies are inferred from the claim text.