EP0763529A1 — Uracil derivatives, and antitumor effect potentiator and antitumor agent containing the same

USPTO Abstract

Provided are a uracil derivative represented by the following formula (1): wherein R 1 represents a chlorine, bromine or iodine atom or a cyano or lower alkyl group; and R 2 represents a 4-8 membered heterocyclic group having 1-3 nitrogen atoms, which may be substituted by one or more lower alkyl, imino, hydroxyl, hydroxymethyl, methanesulfonyloxy, amino or nitro groups; an amidinothio group, one or more of the hydrogen atom(s) on one or both of the nitrogen atoms of which may each be substituted by a lower alkyl group; a guanidino group, one or more of the hydrogen atom(s) on one, two or all of the nitrogen atoms of which may each be substituted by a lower alkyl or cyano group; a (lower alkyl)amidino group; an amino group, one or both of the hydrogen atoms on the nitrogen atom of which may each be substituted by a lower alkyl group; a group -CH 2 N(R a )R b in which R a and R b may be the same or different and each represents a hydrogen atom or a lower alkyl group or R a and R b may form a pyrrolidine ring together with the nitrogen atom to which R a and R b are bonded; a group -NH-(CH 2 ) m -Z in which Z represents an amino group, one or both of the hydrogen atoms on the nitrogen atom of which may each be substituted by a lower alkyl group, or a cyano group, and m stands for an integer of from 0 to 3; a group NR c (CH 2 ) n -OH in which R c represents a hydrogen atom or a lower alkyl group, and n stands for a natural number of from 1 to 4; a group -X-Y in which X represents S or NH, and Y represents a 2-imidazolin-2-yl, 2-imidazolyl, 1-methylimidazol-2-yl, 1,2,4-triazol-3-yl, 2-pyrimidyl or 2-benzimidazolyl group which may be substituted by one or more lower alkyl groups; or a ureido or thioureido group, one or more of the hydrogen atom(s) on one or both of the nitrogen atoms of which may each be substituted by a lower alkyl group; or a salt thereof; as well as a pharmaceutical, antitumor effect potentiator and antitumor agent containing same as an active ingredient.