Composition for increasing the anti-cancer activity of an anti-c

Details Composition for increasing the anti-cancer activity of an anti-c Composition for increasing the anti-cancer activity of an anti-c

1989-11-17

1992-10-13

Nutter, Nathan M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514344, A61K 3144, C07D21369, C07D40504

Patent

active

051551136

ABSTRACT:
A composition for increasing the anti-cancer activity of an anti-cancer compound selected from among 5-fluorouracil and a compound capable of producing 5-fluorouracil in vivo, the composition comprising an effective amount of a pyridine derivative represented by the formula ##STR1## wherein R.sup.1 is hydroxy or acyloxy, R.sup.2 and R.sup.4 are each hydrogen, halogen, amino, carboxyl, carbamoyl, cyano, nitro, lower alkyl, lower alkenyl or lower alkoxycarbonyl, R.sup.3 and R.sup.5 are each hydrogen, hydroxy or acyloxy; when at least one or R.sup.1, R.sup.3 and R.sup.5 is hydroxy, the structure of 1-position on the pyridine ring can be ##STR2## due to the keto-enol tautomerism, said hydrogen attached to nitrogen being optionally substituted with a substituent selected from the group consisting of lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, phthalidyl, carbamoyl, lower alkoxycarbonyl-lower alkylcarbamoyl, phenyl-lower alkoxy-lower alkyl, phenylcarbamoyl which may have a substituent on the phenyl ring, lower alkylcarbamoyl, carboxy-lower alkylcarbamoyl, lower alkylthio-lower alkyl and lower alkenyl, provided that the compound having the following formula is excluded, ##STR3## wherein .alpha. is hydrogen, lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, lower alkylcarbamoyl, lower alkylthio-lower alkyl or lower alkenyl.

REFERENCES:
Fujii et al. (Gann 69, 763-772; Dec., 1978).
Fujii et al. (Gann 70, 209-214; Apr. 1979).
Fujii et al. (Gann 71, 100-106; Feb. 1980).
Kimura et al. Gastroenterologia Japnonica, vol. 15, No. 4, 324-329, Aug. 1980.
Chemical Abstracts 105: 97331f (1986).

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