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    • 9. 发明授权
    • 5'deoxycytidine derivatives
    • 5'-脱氧胞苷衍生物
    • US6005098A
    • 1999-12-21
    • US234200
    • 1999-01-20
    • Kazuo HattoriTohru IshikawaHideo IshitsukaYasunori KohchiNobuhiro OikawaNobuo ShimmaHitomi Suda
    • Kazuo HattoriTohru IshikawaHideo IshitsukaYasunori KohchiNobuhiro OikawaNobuo ShimmaHitomi Suda
    • C07H19/06A61K31/513A61K31/70A61K31/7042A61K31/7052A61K31/7064A61K31/7068A61K31/7072A61P35/00A61P43/00C07H19/067C07H19/16C07H19/167
    • C07H19/16
    • Compounds of the formula (I) ##STR1## wherein R.sup.1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions;R.sup.2 is --(CH.sub.2).sub.n -cycloalkyl wherein cycloalkyl contains 3 to 5 carbon atoms and n is an integer from 0 to 4, heteroaryl-(lower-alkyl), (lower-alkoxy)-(lower-alkyl), aryloxy-(lower-alkyl), aralkyloxy-(lower-alkyl), (lower-alkylthio)-(lower-alkyl), arylthio-(lower-alkyl), aralkylthio-(lower-alkyl), oxo-(lower-alkyl), acylamino-(lower-alkyl), cyclic amino-(lower-alkyl), (2-oxocyclic amino)-(lower-alkyl) wherein the alkylene chain is unsubstituted or substituted with one or two lower-alkyl group(s); andR.sup.3 is iodo, or a vinyl or ethynyl group which group is unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, C.sub.1-4 alkyl, cycloalkyl, aralkyl, carbocyclic aromatic ring and heteorcyclic aromatic ring.The compounds of formula I are useful in the treatment of malignant diseases and can also be administered together with 5-fluorouracil or derivatives thereof to enhance the antitumour activity of the latter.
    • 式(I)的化合物,其中R 1各自独立地为氢或在生理条件下易于水解的基团; R 2为 - (CH 2)n - 环烷基,其中环烷基含有3至5个碳原子,n为0至4的整数,杂芳基 - (低级 - 烷基),(低级 - 烷氧基) - (低级 - 烷基),芳氧基 - ( 低级烷基),芳烷氧基 - (低级烷基),(低级 - 烷硫基) - (低级 - 烷基),芳硫基 - (低级烷基),芳烷硫基 - (低级烷基),氧代(低级烷基) - (低级烷基),环状氨基 - (低级 - 烷基),(2-氧代环氨基) - (低级烷基),其中亚烷基链未被取代或被一个或两个低级烷基取代; 或R 3为碘,或乙烯基或乙炔基,该基团是未取代的或被一个或多个选自卤素,C 1-4烷基,环烷基,芳烷基,碳环芳环和杂环芳环的取代基取代。 式I化合物可用于治疗恶性疾病,也可与5-氟尿嘧啶或其衍生物一起施用以增强后者的抗肿瘤活性。