Nyegaard & Co A/s

Mikkel J Gacek

Kjell Undheim

Tore Benneche

Reidar Oftebro

Soren Laland

Compounds of general formula: ##STR1## (wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, or a C.sub.1-4 alkyl group, and R.sup.3 represents a hydrogen atom or a C.sub.1-5 saturated or unsaturated, straight or branched acyclic aliphatic group; a C.sub.3-8 saturated or unsaturated cyclic aliphatic group; a heterocyclic substituted aliphatic group; an araliphatic group; or a heterocyclic or carbocyclic aryl group; any of said groups optionally carrying one or more substituents selected from halogen, oxo, hydroxy, mercapto, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkanoyloxy and amino) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation. The compounds of formula I may be prepared by reaction of a 5-halo- or 5-trifluoromethyl-pyrimidin-2-one with an appropriate isocyanate.

Substituted pyrimid-2-ones, the salts thereof, processes for their

Compounds of the formula ##STR1## (wherein X represents a halogen atom; n is 0, 1 or 2; R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a carboxyl, esterified carboxyl, amido or mono- or di-C.sub.1-4 alkylamido group or a C.sub.1-4 alkyl group which may if desired carry a carboxyl or esterified carboxyl group; and R.sup.3 represents a C.sub.1-32 saturated or unsaturated, straight or branched, cyclic or acyclic aliphatic group or an araliphatic or heterocyclic substituted aliphatic group, a heterocyclic group or an aryl group which groups may if desired carry one or more substituents selected from halogen atoms and oxo, nitro, hydroxy, etherified hydroxy, esterified hydroxy, primary, secondary or tertiary amino, acylamino etherified mercapto or S.dbd.O or --SO.sub.2 derivatives thereof and esterified phosphonic acid groups) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation. The compounds are prepared inter alia by oxidation of the corresponding sulfide, displacement of a leaving atom or group from the 2-position of the pyrimidine by reaction with a sulfinic acid or by ring closure of the pyrimidine ring.

Pyrimidine-2-sulphides and their S-oxides for use in medicine and

Compounds of the formula: ##STR1## wherein X represents a halogen atom;

5-Halo-pyrimidin-2-ones, the salts thereof

Novel derivatives of pyrimid-2-one having interesting pharmacological properties are described. The compounds of the invention have been found to be of use in the control of, and in particular in the inhibition of the metaphase of malignant tumours and leukaemias. Processes for the preparation of the novel compounds and pharmaceutical compositions containing them are also described.

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Oslo, Norway

Mikkel J Gacek