首页> 外国专利> Use of 1,4-di:hydro:pyridine derivs. - to potentiate activity of antitumoural compounds, e.g. mitoxantrone

Use of 1,4-di:hydro:pyridine derivs. - to potentiate activity of antitumoural compounds, e.g. mitoxantrone

机译:使用1,4-二:氢:吡啶衍生物。 -增强抗肿瘤化合物的活性,例如米托蒽醌

摘要

1,4-Dihydropyridine derivs. of formula (I), which have no calcium channel blocking activity, are used to increase the activity of antitumour agents. R1, R2 - opt. substd. methyl; R2, R3 = alkoxy, alkoxyalkoxy, dialkylaminoalkoxy, aryloxy, alkyalmino, HO(CH2)xNH, arylamine, 2-methoxyphenylamine, 2-chlorophenylamine, (2-methyl-5-chlorophenyl) amine, (2,5-dimethoxy-4'- chlorophenyl)amine or 2,4-dimethylphenylamine; X is not defined. USE/ADVANTAGE - Combinations of Ca antogonists (e.g. Nifedipine) with antitumour agents are known to increase the activity of antitumour agents. However, when used in the doses necessary to achieve this increase in activity, the antagonists cause undesirable side effects. Use of (I) achieves an increase of activity against resistant tumour without causing the undesirable side effects. They may also be prepd. by conventional methods. (I) are administered orally, rectally, parenterally or intraperitoneally in doses of 300-100 mg.
机译:1,4-二氢吡啶衍生物。不具有钙通道阻滞活性的式(I)的抗肿瘤药被用于增加抗肿瘤剂的活性。 R1,R2-选择取代甲基; R 2,R 3 =烷氧基,烷氧基烷氧基,二烷基氨基烷氧基,芳氧基,烷基氨基,HO(CH 2)x NH,芳基胺,2-甲氧基苯胺,2-氯苯胺,(2-甲基-5-氯苯基)胺,(2,5-二甲氧基-4' -氯苯基)胺或2,4-二甲基苯基胺; X未定义。用途/优势-已知钙拮抗剂(例如硝苯地平)与抗肿瘤药的组合会增加抗肿瘤药的活性。但是,当以实现这种活性增加所需的剂量使用时,拮抗剂会引起不良的副作用。 (I)的使用在不引起不希望的副作用的情况下提高了抗药性的活性。他们也可以准备。通过常规方法。 (I)以300-100mg的剂量经口服,直肠,肠胃外或腹膜内给药。

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