Novel 2'-deoxy-5-substituted uridine derivatives, processes for
preparing the same and antitumor agent containing the same
    54.
    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。

    Pyrazolotriazine compounds
    56.
    发明授权
    Pyrazolotriazine compounds 失效
    吡唑并三嗪化合物

    公开(公告)号:US4824834A

    公开(公告)日:1989-04-25

    申请号:US105581

    申请日:1987-10-08

    CPC分类号: C07D487/04 Y02P20/582

    摘要: Pyrazolotriazine compounds of the formula: ##STR1## wherein R.sup.1 is OH or alkanoyloxy; R.sup.2 is H, OH, or SH; R.sup.3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) ##STR2## R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) ##STR3## or (xx) ##STR4## (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.

    摘要翻译: 下式的吡唑并三嗪化合物:其中R1是OH或烷酰氧基; R2是H,OH或SH; R3是(1)任选具有1-2个卤素取代基的不饱和N-或S-杂环基,硝基或苯硫基,(2)萘基,(3)任选具有1-3个(i)烷基取代基的苯基,(ii) )苯基,(iii)烷氧基羰基,(iv)氰基,(ⅴ)硝基,(vi)烷氧基,(i)苯基烷氧基(ii)苯硫基烷基,(ix)苯氧基,(Ⅹ) 取代的烷基,任选具有1-3个取代基的苯基或吡啶基,l是0,1或2,(xi)卤素,(xii)苯基烷基,(xiii)羧基,(xiv)烷酰基,(xv) 1-3取代基,(xvi)氨基,(xvii)OH,(xviii)烷酰氧基,(xix)或(xx)(A是亚烷基),所述化合物具有黄嘌呤氧化酶抑制活性, 用于预防和治疗痛风。

    Automatic analyzer for guanase activity
    57.
    发明授权
    Automatic analyzer for guanase activity 失效
    自动分析仪进行鸟类活动

    公开(公告)号:US4788141A

    公开(公告)日:1988-11-29

    申请号:US078009

    申请日:1987-07-24

    CPC分类号: C12Q1/34 G01N2333/978

    摘要: An automatic analyzer comprising a plurality of sample containers for accommodating different blood samples individually, specific sample container moving means, a plurality of reagent containers for accommodating at least a reagent for an assay of guanase activity, a specific reagent container holding means, a plurality of reaction containers, specific reaction container moving means, specific sample pouring means, specific cleaning vessels, specific stirring means, specific measuring means, specific cleaning means, a specific analog-digital converter, specific counting-calculating means, a specific display means, and specific operation control means, so that the display means produces a signal for excluding the measured blood sample corresponding to a display value when the display value is above a predetermined reference value of guanase activity.

    摘要翻译: 一种自动分析装置,其特征在于,包括分别容纳不同的血液样本的多个检体容器,特定的检体容器移动机构,至少容纳用于检测动物活动的试剂的多个试剂容器,特定试剂容器保持机构, 反应容器,特定反应容器移动装置,特定的样品注入装置,特定的清洁容器,特定的搅拌装置,特定的测量装置,特定的清洁装置,特定的模拟数字转换器,特定的计数计算装置,特定的显示装置和特定的 操作控制装置,使得当显示值高于动画活动的预定参考值时,显示装置产生用于排除与显示值相对应的测量血样的信号。

    Sulfonic acid ester derivatives useful as antilipemic agents
    58.
    发明授权
    Sulfonic acid ester derivatives useful as antilipemic agents 失效
    可用作抗脂药的磺酸酯衍生物

    公开(公告)号:US4675428A

    公开(公告)日:1987-06-23

    申请号:US861635

    申请日:1986-05-07

    IPC分类号: C07C309/73 C07C143/68

    CPC分类号: C07C309/00

    摘要: A sulfonic acid ester derivative represented by the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, A is a group represented by the general formula ##STR2## (wherein R.sub.2 and R.sub.3 are each alkyl having 1 to 4 carbon atoms) or by the general formula ##STR3## (wherein R.sub.4 and R.sub.5 are each alkyl having 1 to 4 carbon atoms or, when taken together with the cabon atom to which they are attached, form cycloalkyl having 4 to 6 carbon atoms), and l is an integer of from 1 to 3, and a process for preparing the derivative.

    摘要翻译: PCT No.PCT / JP83 / 00300 Sec。 1984年4月30日 102(e)日期1984年4月30日PCT提交1983年9月6日PCT公布。 第WO84 / 00959号公报 1984年3月15日,由通式表示的磺酸酯衍生物,其中R1是氢原子,具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基,A是由 通式[IMAGE](其中R2和R3各自为具有1至4个碳原子的烷基)或通式为其中R 4和R 5各自为具有1至4个碳原子的烷基,或者当与碳原子一起 与它们相连的原子,形成具有4-6个碳原子的环烷基),和l是1至3的整数,以及制备该衍生物的方法。