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Title: Pyrimidine-2-sulphides and their S-oxides for use in medicine and methods of use therefor, pharmaceutical compositions containing them, processes for their preparation and per se novel sulphides and S-oxides

Abstract: Compounds of the formula ##STR1## (wherein X represents a halogen atom; n is 0, 1 or 2; R1 and R2, which may be the same or different, each represents a hydrogen atom or a carboxyl, esterified carboxyl, amido or mono- or di-C1-4 alkylamido group or a C1-4 alkyl group which may if desired carry a carboxyl or esterified carboxyl group; and R3 represents a C1-32 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O or --SO2 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.


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Inventors: Benneche, Tore (Oslo, NO)
Gacek, Mikkel J. (Oslo, NO)
Undheim, Kjell (Oslo, NO)

Application Number: 06/223760
Filing Date: 1981-01-09
Publication_date: 1983-12-27
Assignee: NYEGAARD & CO AS (NO)

Primary Class(es): 514/274 514/252.140, 514/885, 514/210.200, 514/212.080, 544/3
Other Classes: C07C233/07; C07D239/38; C07D239/40; C07F9/6512; C07H17/02; C07C233/00; C07D239/00; C07F9/00; C07H17/00; C07D239/38; A61K31/505
US Patent Ref:
2876224March, 1959Grant et al.544/316Basic esters of substituted pyrimidine-4-carboxylic acids and their preparation
3112316November, 1963Westphal et al.544/317
4248618February, 1981Serban et al.544/318Derivatives of (pyrimidyloxy)phenoxy-alkanecarboxylic acid and herbicidal compositions thereof

Other Refs: EP0001187EP0015124DE2455582DE2820032GB1561290
March, 19792-phenoxy-pyrimidines and their use as pesticides.
September, 1980PARASITICIDAL HETEROCYCLIC ETHER DERIVATIVES, PROCESSES FOR THE MANUFACTURE THEREOF AND COMPOSITIONS
May, 1976
November, 1978
February, 1980
Other References: Budesinsky et al., Coll. Czech. Chem. Commun., vol. 30, pp. 3895-3901, (1965).
Budesinsky et al., Coll. Czech. Chem. Commun., vol. 37, pp. 1721-1733, (1972).
Brown et al., J. Chem. Soc., 1971, pp. 250-256.
Krchnak et al., Coll. Czech. Chem. Commun., vol. 40, pp. 1384-1389, (1975).

Primary Examiner: Lee, Mary C.
Assistant Examiner:
Attorney: Bacon & Thomas
Claims:
We claim: