Use of 1,4-benzothiazepine derivatives as drugs for...

A - Human Necessities – 61 – K

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A61K 31/554 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2373484

The present invention relates to use of compounds represented by the following general formula [1] or salts or prodrugs thereof: <see formula I> [where R1 represents hydrogen atom or lower alkoxy group; RZ represents hydrogen atom, lower alkoxy group, optionally substituted phenyl group, <see formula> (where R3 represents acyl group); X represents -CO- or -CH2-; and n-represents 1 or 2], as drugs for overcoming a resistance to anticancer drugs or drugs for enhancing an effect of anticancer drugs. The compounds represented by the general formula [1] have not only a function of overcoming the resistance to various anticancer drugs but also a function of enhancing the effect of various anticancer drugs to anticancer-drug sensitive cells. Thus, these compounds have excellent effects on resistant cells and also on sensitive cells, and in particular effective in the treatment of a cancer having an acquired resistance to an anticancer drug.

L'invention concerne l'utilisation de composés représentés par la formule générale (I), des sels ou des promédicaments de ceux-ci, en tant que médicaments contre la tolérance carcinostatique ou en tant que médicaments augmentant l'effet d'agents cancérostatiques. Dans ladite formule (I), R<1> représente hydrogène ou alcoxy inférieur; R<2> représente hydrogène, alcoxy inférieur, phényle éventuellement substitué (1), (dans laquelle R<3> représente acyle); X représente -CO- ou -CH2-; et n vaut 1 ou 2. Les composés de formule générale (I) agissent contre la tolérance à divers agents cancérostatiques mais peuvent également augmenter les effets de divers agents cancérostatiques sur des cellules à sensibilité cancérostatique. Ainsi, lesdits composés sont très efficaces sur les cellules tolérantes et les cellules sensibles, notamment dans le traitement de cancer devenu tolérant aux agents cancérostatiques.

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