Anthracycline derivatives, their preparation and use

Details Anthracycline derivatives, their preparation and use Anthracycline derivatives, their preparation and use

1977-11-14

1979-09-04

Love, Ethel G.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

260463, 260590FB, 536 4, 536 17A, A61K 3170, C07G 1100, C07G 300

Patent

active

041668480

ABSTRACT:
Disclosed are antitumor compounds of the formula: ##STR1## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl; a C.sub.3 -C.sub.6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X--Phe--(CH.sub.2).sub.n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R.sub.2 is hydrogen, hydroxyl or acyloxy (R--COO--), where R is an alkyl having from 1 to 11 carbon atoms; and R.sub.3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids. Compounds I are prepared by condensing the aglycones thereof with 2,3,6-trideoxy-3-trifluoroacetamido-4-O-trifluoro-acetyl-.alpha.-L-lyxopyr anosyl chloride according to a conventional technique.

REFERENCES:
patent: 4067969 (1978-01-01), Penco et al.
patent: 4107423 (1978-08-01), Arcamone et al.
Arcamone et al., Journ. Med. Chem. vol, 17, No. 3, pp. 335-337 (1974).

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