8-fluoro-anthracyclines processes for their preparation and pharmaceutical compositions containing them

摘要

PCT No. PCT/EP95/03061 Sec. 371 Date Apr. 21, 1997 Sec. 102(e) Date Apr. 21, 1997 PCT Filed Aug. 1, 1995 PCT Pub. No. WO96/04292 PCT Pub. Date Feb. 15, 19968-fluoro-anthracyclines of formula (I) have anti-tumor activity. (I) wherein: R is chosen in the group consisting of H, OH, OR4 wherein R4 is chosen in the group consisting of CHO, COCH3, acyl derivative of a carboxylic acid containing up to 6 carbon atoms; R1 is chosen in the group consisting of: H, OH, OCH3; R2 is chosen in the group consisting of: H, OH, NH2 R3 is chosen in the group consisting of: H, OH, NH2, residue of formula (A) The compounds are characterized by having cis-stereochemistry between the groups 8-F and 9-OH. Their preparation and pharmaceutical compositions containing them are also described.