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Antiallergic and antiulcer 1-oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides and intermediates therefor
2-[4-[(4,4 -Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyrimidines
9-(1,3-Dihydroxy-2-propoxymethyl)guanine as antiviral agent
4-[(Cycloalkyl or cycloalkenyl substituted) amino, alkylamino or alkenylamino]benzoic acids, salts and derivatives thereof
1,4-Dihydropyridine-3,5-dicarboxylic acid ester derivatives
Derivatives of 2-amino-5-(o-sulphamidophenyl)-1,3,4-thiadiazol as antiviral agents and a process for the preparation thereof
Antihypertensive 4-thiazolidinecarboxylic acids (substituted alkyl derivatives)
6-Substituted-hydrocarbon-2-(substituted-thio)penem-3-carboxylic acids
5(Aminomethyl)-4,5,6,7-tetrahydro[d]thiazole containing compositions for and medical use in treating circulatory insufficiencies
Methods of use of 1-[(substituted-naphthyl)ethyl]-imidazole derivatives
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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 SO 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:
| 2876224 | March, 1959 | Grant et al. | 544/316 | Basic esters of substituted pyrimidine-4-carboxylic acids and their preparation | | 3112316 | November, 1963 | Westphal et al. | 544/317 | | | 4248618 | February, 1981 | Serban et al. | 544/318 | Derivatives of (pyrimidyloxy)phenoxy-alkanecarboxylic acid and herbicidal compositions thereof |
Other Refs:
EP0001187| March, 1979 | 2-phenoxy-pyrimidines and their use as pesticides. | | | EP0015124September, 1980 | PARASITICIDAL HETEROCYCLIC ETHER DERIVATIVES, PROCESSES FOR THE MANUFACTURE THEREOF AND COMPOSITIONS | | | DE2455582May, 1976 | | | | DE2820032November, 1978 | | | | GB1561290February, 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
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