abstract |
Invention Patent: <B> "5'-DEOXICITIDINE DERIVATIVES" <D>. Compounds of the general formula (I) in which R¹ is independently hydrogen or a hydrolyzable group with ease under physiological conditions; R² is - (CH ~ 2 ~) ~ n ~ cycloalkyl {where cycloalkyl consists of 3 to 5 carbon atoms, 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), ozo - (lower alkyl), acylamino - ( lower alkyl), cyclic amino - (lower alkyl), (2-amino oxocyclic) - (lower alkyl), in which the alkylene chain can be further substituted with one or more lower alkyl group (s) and R ^ 3 ^ is iodine, a vinyl or ethynyl group [whose groups can be replaced with a halogen atom (s), C ~ 1-4 ~ alkyl, cycloalkyl or an aromatic ring that can have one or more hetero-atom (s)], are useful in the treatment of malignant diseases and can also be administered in conjunction with 5-fluorouracil or derivatives thereof to increase its antitumor activity last. |