Taiho Pharmaceutical Company Limited

Junji Uchida

Koyo Shudo

Mitsugi Yasumoto

Yuji Yamada

Setsuo Takeda

Konstanty Wierzba

Junichi Yamashita

Tadafumi Terada

Katsuhiko Fujimoto

Teiji Takechi

Katsuhisa Koizumi

Mamoru Nukatsuka

The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect. The antitumor effect potentiator comprising at least one member selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof. The present invention also provides a method for enhancing an antitumor effect of an antitumor agent comprising the step of administering to a patient the aforementioned antitumor effect potentiator; a method for inhibiting the growth of a tumor comprising the step of administering to a patient the aforementioned antitumor effect potentiator and a method for cancer treatment comprising the step of administering to a patient the aforementioned antitumor agent.

Antitumor effect potentiator and antitumor agent

The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect. The antitumor effect potentiator comprising at least one member selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof. The present invention also provides a method for enhancing an antitumor effect of an antitumor agent comprising the step of administering to a patient the aforementioned antitumor effect potentiator; and a method for cancer treatment comprising the step of administering to a patient the aforementioned antitumor agent.

This invention provides a 5-substituted uridine derivative of the formula ##STR1## wherein X is F or CF.sub.3, R.sub.1 and R.sub.2 each represent a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6) (wherein R.sub.4, R.sub.5 and R.sub.6 represent C.sub.1 -C.sub.10 alkyl or the like), OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group or carboxylalkylcarbonyloxy group, R.sub.3 is a group --OSi(R.sub.4)(R.sub.5)(R.sub.6), H, OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group, or carboxylalkylcarbonyloxy group, and at least one of R.sub.1, R.sub.2 and R.sub.3 is a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6), with the proviso that when X is fluorine atom, R.sub.3 is not hydrogen, and an intermediate for the preparation thereof, preparation processes of the derivative and anti-tumor agent containing the derivative as an active ingredient.

5-substituted uridine derivatives

Growing community of inventors

Tokushima, Japan

Junji Uchida