Novel 2'-deoxy-5-substituted uridine derivatives, processes for
preparing the same and antitumor agent containing the same
    6.
    发明授权
    Novel 2'-deoxy-5-substituted uridine derivatives, processes for preparing the same and antitumor agent containing the same 失效
    新的2'-脱氧-5-取代的尿苷衍生物,其制备方法和含有它们的抗肿瘤剂

    公开(公告)号:US4886877A

    公开(公告)日:1989-12-12

    申请号:US163237

    申请日:1988-02-26

    IPC分类号: C07D405/04 C07H19/06

    CPC分类号: C07H19/06

    摘要: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.

    摘要翻译: 由通式表示的新型2'-脱氧-5-取代的尿苷衍生物,其中R1是氢原子,苯甲酰基或四氢呋喃基; R2是氟原子或三氟甲基; R 3和R 4中的任一个为氢原子,另一个为碳原子数1〜10的烷基,碳原子数为2〜6的烯基,作为取代基的苄基,选自 卤原子,碳原子数为1〜4的烷基,碳原子数为1〜4的烷氧基,硝基,碳原子数为1〜3的烷基,具有一个或两个苯基作为取代基。 新型2'-脱氧-5-取代尿苷衍生物具有优异的抗肿瘤活性,毒性低,因此可用作抗肿瘤剂。

    2'-deoxy-5-substituted uridine derivatives
    8.
    发明授权
    2'-deoxy-5-substituted uridine derivatives 失效
    2'-脱氧-5-取代的尿苷衍生物

    公开(公告)号:US5250673A

    公开(公告)日:1993-10-05

    申请号:US422721

    申请日:1989-10-17

    IPC分类号: C07H19/06 C07H19/073

    CPC分类号: C07H19/06

    摘要: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.

    摘要翻译: 由通式表示的新型2'-脱氧-5-取代的尿苷衍生物,其中R1是氢原子,苯甲酰基或四氢呋喃基; R2是氟原子或三氟甲基; R 3和R 4中的任一个为氢原子,另一个为碳原子数1〜10的烷基,碳原子数为2〜6的烯基,作为取代基的苄基,选自 卤原子,碳原子数为1〜4的烷基,碳原子数为1〜4的烷氧基,硝基,碳原子数为1〜3的烷基,具有一个或两个苯基作为取代基。 新型2'-脱氧-5-取代尿苷衍生物具有优异的抗肿瘤活性,毒性低,因此可用作抗肿瘤剂。

    Anti-cancer composition for delivering 5-fluorouracil
    9.
    发明授权
    Anti-cancer composition for delivering 5-fluorouracil 失效
    用于递送5-氟尿嘧啶的抗癌组合物

    公开(公告)号:US4719213A

    公开(公告)日:1988-01-12

    申请号:US901202

    申请日:1986-08-28

    CPC分类号: C07D239/553 A61K31/505

    摘要: An anti-cancer composition for delivering a 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil. The composition comprises uracil or a pharmaceutically acceptable salt thereof, and a 5-fluorouracil pro drug selected from the group consisting of 1, 3-bis (2-tetrahydrofuryl)-5-fluorouracil and 3-(2-tetrahydrofuryl)-5-fluorouracil in a small amount of about 0.1 to less than 0.1 mole per mole of uracil or salt thereof.

    摘要翻译: 一种用于将5-氟尿嘧啶递送至温血动物的癌症组织的抗癌组合物,其中所述癌症是对5-氟尿嘧啶敏感的癌症。 该组合物包含尿嘧啶或其药学上可接受的盐,和5-氟尿嘧啶前药,其选自1,3-双(2-四氢呋喃基)-5-氟尿嘧啶和3-(2-四氢呋喃基)-5-氟尿嘧啶 其量为每摩尔尿嘧啶或其盐约0.1至小于0.1摩尔的少量。