Daunosamine nucleosides
AssigneeSocieta' Farmaceutici Italia S.p.A.
InventorsEttore Lazzari, Federico Arcamone, Aurelio DI Marco
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Abstract
The antitumor efficacy of the known antibiotics daunomycin (daunorubicin) and adriamycin (doxorubicin) is synergized by the use of said antibiotics together with a daunosamine nucleoside. The latter compounds are prepared by condensing a reactive protected daunosamine with a reactive protected heterocyclic base.
Claims7
A daunosamine nucleoside of the formula:
- ##STR6## wherein R and R' are both H or R is COCF.sub.3 and R' is COC.sub.6 H.sub.5.
A daunosamine nucleoside of the formula:
- ##STR7## wherein R is H and R' is N(CH.sub.3).sub.2 ;
- R is COCH.sub.3 and R' is Cl or N(CH.sub.3).sub.2.
A daunosamine nucleoside of the formula:
- ##STR8## wherein R and R' are both H, or R is COCF.sub.3 and R' is COC.sub.6 H.sub.5.
A daunosamine nucleoside of the formula:
- ##STR9## wherein R is H or COCF.sub.3.
A composition comprising a therapeutically effective amount of the antitumor antibiotic daunomycin or adriamycin in combination with a synergizing amount of a daunosamine nucleoside selected from the group consisting of 9-(.beta.-daunosaminyl)-adenine, 6-dimethyl-9-(.beta.-daunosaminyl)-adenine, 1-(.beta.-daunosaminyl)-adenine, 1-(.beta.-daunosaminyl)-cytosine and 1-(.beta.-daunosaminyl)-thymine and an inert carrier therefor.
A method of inhibiting the growth of ascites sarcoma 180 which comprises intraperitoneally administering to a host afflicted with said tumor an amount of a compound selected from the group consisting of 9-(.beta.-daunosaminyl)-adenine, 6-dimethyl-9-(.beta.-daunosaminyl)-adenine, 1-(.beta.-daunosaminyl)-cytosine and 1-(.beta.-daunosaminyl)-thymine sufficient to inhibit the growth of said tumor, in combination with a therapeutically effective amount of daunomycin or adriamycin.
Dependencies are inferred from the claim text.