公开(公告)号：US5472949A

公开(公告)日：1995-12-05

申请号：US167392

申请日：1993-12-14

申请人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

发明人： Motohiro Arasaki ,  Hideo Ishitsuka ,  Isami Kuruma ,  Masanori Miwa ,  Chikako Murasaki ,  Nobuo Shimma ,  Isao Umeda

IPC分类号： A61K31/70 ,  A61K31/305 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61P35/00 ,  C07D239/00 ,  C07H19/06

CPC分类号： C07H19/06 ,  Y02P20/55

摘要： The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors.Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions,or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

摘要翻译： 本发明涉及可用作治疗肿瘤的药物的N4-（取代 - 氧代羰基）-5'-脱氧-5-氟胞苷衍生物，包含其的药物组合物，治疗肿瘤的方法和制备N4-（ 取代氧羰基）-5'-脱氧-5-氟胞苷衍生物用于治疗肿瘤。 式（I）化合物，其中R1是饱和或不饱和的直链或支链烃基，其中该烃基的最长直链中的碳原子数范围为3-7，或者是 基团 - （CH 2）n Y其中Y是环己基，C 1 -C 4烷氧基或苯基，并且其中当Y是环己基时，n是0-4的整数，当Y是C 1 -C 4 烷氧基或苯基n是2〜4的整数，R2是氢原子或在生理条件下易水解的基团，或其水合物或溶剂合物。 式（I）化合物可用于治疗肿瘤。