C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
167/125, 167/182
C07H 15/252 (2006.01) A61K 31/70 (2006.01) C07H 23/00 (2006.01)
Patent
CA 1340690
The invention relates to novel cytostatic anthracyclines of the general formula I, if appropriate as the salt of an inorganic or organic acid (see formula I) in which the radicals R1 are hydrogen or hydroxyl, R2 is hydrogen, a structure of the formula II or IV or, together with R3, a structure of the formula III, R3 is hydrogen, a structure of the formula II or IV or, together with R2, a structure of the formula III, R4 is hydrogen, an acyl group, trimethylsilyl, a structure of the formula II or a structure of the formula IV (see formula II, III, IV) and in these R5 is hydrogen, methyl, hydroxymethyl, acyloxymethyl or alkoxymethyl, R6 is hydrogen, hydroxyl, acyloxy, alkoxy, allyloxy, benzyloxy or halogen, R7 has the same meaning as R6 and can also additionally be NH2, NHacyl, N(alkyl)3, N(CH2CN)2, HN(CH2CN) or 2/2 azido, and R8 has the same meaning as R6, X is alkylboronyl, phenylboronyl, an alkyl ortho-carboxylate or a ketal or acetal, the following compounds of the formula I being excluded: 1. R1=R3=R4=H, R2=.alpha.-L-daunosaminyl, 2. R1=R3=R4=H, R2=.alpha.-L-rhodosaminyl or its 4'-acyl derivatives 3. R1=R3=H, R2=R4=.alpha.-L-rhodosaminyl or its 4'-acyl derivatives 4. R1=OH, R3=H, R2=R4=.alpha.-L-rhodosaminyl or its 4'-acyl derivatives 5. R1=R2=R3=H, R4=.alpha.-L-rhodosaminyl or its 4'-acyl derivatives. The invention also relates to a process for the preparation of the compounds and their use in medicaments. The compounds of the invention exhibit cytostatic activity and accordingly may be used for the therapy of tumors.
563694
Gerken Manfred
Hermentin Peter
Hoffmann Dieter
Kolar Cenek
Kraemer Hans Peter
Behringwerke Aktiengesellschaft
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
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