N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine com

Details N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine com N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine com

1993-12-14

1995-12-05

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 285, 536 2852, A61K 3170, C07H 1906

Patent

active

054729491

ABSTRACT:
The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.
Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,
or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

REFERENCES:
patent: 4966891 (1990-10-01), Fujiu et al.
Umeda et al., "Synthesis and antitumor activity of 5'-deoxy-5-fluorocytidine (5'-DFCR) derivatives", J. Pharmacobio-Dyn., 13:s-144 (1990).

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