C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/54 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 239/553 (2006.01) C07D 403/02 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 521/00 (2006.01)
Patent
CA 2191340
Provided are a uracil derivative represented by the following formula (1): (see formula I) wherein R1 represents a chlorine, bromine or iodine atom or a cyano or lower alkyl group; and R2 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 -CH2N(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-(CH2)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(CH2)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.
Dérivés d'uracile représentés par la formule générale (1) ou sels de ces dérivés. Dans la formule (1), R<1> représente chloro, bromo, iodo, cyano ou alkyle inférieur; et R<2> représente un hétérocycle comptant de 4 à 8 éléments facultativement substitué par alkyle inférieur, imino, hydroxy, hydroxyméthyle, méthanesulfonyloxy, amino ou nitro et comportant de un à trois atomes d'azote, amidinothio dans lequel l'hydrogène sur l'azote est facultativement substitué par alkyle inférieur, guanidino dans lequel l'hydrogène sur l'azote est facultativement substitué par alkyle inférieur ou cyano, alkylamidino, amino dans lequel l'hydrogène sur l'azote est facultativement substitué par alkyle inférieur, -CH2N(R<a>)R<b> (dans lequel R<a> et R<b> sont identiques ou différents et représentent l'hydrogène ou un alkyle inférieur ou bien R<a> et R<b>, avec l'atome d'azote auxquels ils sont liés peuvent former de la pyrrolidine), -NH-(CH2)m-Z (où Z représente amino, l'hydrogène sur l'azote étant facultativement substitué par alkyle inférieur ou cyano; et m est un entier de 0 à 3), -NR<c>(CH2)m-OH (où R<c> représente hydrogène ou alkyle inférieur; et n est un entier naturel de 1 à 4), -X-Y (où X représente S ou NH; et Y représente 2-imidazoline-2-yle, 2-imidazolyle, 1-méthylimidazole-2-yle, 1, 2, 4-triasol-3-yle, 2-pyrimidyle ou 2-benzimidazolyle facultativement substitué par alkyle inférieur), ou ureido ou thioureido dans lequel l'hydrogène sur l'azote est facultativement substitué par alkyle inférieur, médicaments renfermant ces substances, tels que des agents de potentialisation d'effet antitumoral et agents antitumoraux.
Asao Tetsuji
Emura Tomohiro
Fukushima Masakazu
Kazuno Hideki
Sato Tsutomu
Gowling Lafleur Henderson Llp
Taiho Pharmaceutical Co. Ltd.
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