EP0260057A2 — 2-Oxo-4-carboxy-pyrimidines

USPTO Abstract

A compound for use as an inhibitor for the enzyme dihydroorotase and which is of general formula (I) where either (i) A and B together are =S or (ii) A is -H, and B is -COR₂ or -SR₆; and R₁ and R₂ which may be the same or different are -OH; alkyloxymethyl, a di-, tri- or polypeptide group, -OR where R is saturated or unsaturated C 1-16 alkyl, C 1-16 alkyloxymethyl, or 4-alkyl-piperidinyl-alkyl, -NRʹRʹ where each Rʹ is independently selected from -H, saturated or unsaturated C 1-16 alkyl, or any group able to be hydrolysed in vivo to hydroxy; R₃ and R₄ which may be the same or different are -H, C 1-6 alkyl, hydroxy C 1-16 alkyl, hydroxy C 1-6 ether group, tetrahydrofuranyl, tetrahydropyranyl, a sugar or acetylated sugar group, hexylcarbamyl, methylglycine-N-carbonyl, or any group able to be hydrolysed in vivo to -H; R₅ is -H, halo, or C 1-6 alkyl; R₆ is C 1-6 alkyl or 1-methyl-4-nitroimidazol-5-yl; and the dotted line represents a double bond which may be absent or present in the 4-5 position. The compounds are useful as anti-cancer and anti-malarial drugs.