Mitotic kinesin inhibitor
    32.
    发明申请
    Mitotic kinesin inhibitor 失效
    有丝分裂驱动蛋白抑制剂

    公开(公告)号:US20070155804A1

    公开(公告)日:2007-07-05

    申请号:US10553222

    申请日:2004-04-16

    摘要: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.

    摘要翻译: 一种有丝分裂驱动蛋白Eg5抑制剂,其包含由通式(I)表示的噻二唑啉衍生物或其药理学上可接受的盐作为有效成分:[其中R 1表示氢原子等, O 2表示氢原子,-C(-W)R 6(其中W表示氧原子或硫原子,R 6表示 取代或未取代的低级烷基等)等,R 3表示-C(-Z)R 19(其中Z表示氧原子或硫原子, 和R 19表示取代或未取代的低级烷基等)等,R 4表示取代或未取代的低级烷基等,R 5, / SUP>表示取代或未取代的芳基等〕等。

    Radicicol derivatives
    34.
    发明授权
    Radicicol derivatives 失效
    蓝霉素衍生物

    公开(公告)号:US5977165A

    公开(公告)日:1999-11-02

    申请号:US958285

    申请日:1997-10-27

    IPC分类号: C07D313/00 A61K31/335

    CPC分类号: C07D313/00

    摘要: The present invention relates to radicicol derivatives represented by the following formula (I) or pharmacologically acceptable salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents hydrogen, alkanoyl, alkenoyl or tert-butyldimethylsilyl; (1) when X represents halogen, Y represents an oxygen atom or R.sup.4 --O--N (wherein R.sup.4 represents hydrogen or substituted or unsubstituted lower alkyl); and R.sup.3 represents hydrogen, alkanoyl, alkenoyl or the like; and (2) when X and R.sup.3 are combined with each other to represent a single bond; Y represents R.sup.4B --O--N (wherein R.sup.4B has the same meaning as R.sup.4). The radicicol derivatives of the present invention demonstrate tyrosine kinase inhibition activity and pharmacological activities such as antitumor, antimicrobial or immunosuppression effects.

    摘要翻译: 本发明涉及由下式(I)表示的根赤壳菌素衍生物或其药理学上可接受的盐:其中R1和R2相同或不同,各自代表氢,烷酰基,烯酰基或叔丁基二甲基甲硅烷基; (1)当X表示卤素时,Y表示氧原子或R4-O-N(其中R4表示氢或取代或未取代的低级烷基); 和R3表示氢,烷酰基,烯酰基等; 和(2)当X和R 3相互结合以表示单键时; Y表示R4B-O-N(其中R4B与R4相同)。 本发明的根皮霉素衍生物显示出酪氨酸激酶抑制活性和药理活性,如抗肿瘤,抗微生物或免疫抑制作用。

    Revolution controller for a continuously variable transmission
    38.
    发明授权
    Revolution controller for a continuously variable transmission 失效
    用于无级变速器的革命控制器

    公开(公告)号:US5012697A

    公开(公告)日:1991-05-07

    申请号:US443720

    申请日:1989-11-29

    摘要: A continuously variable transmission includes a driving side pulley and a driven side pulley each having a fixed pulley part and having a movable pulley part supported for movement toward and away from the fixed pulley part, the width of a groove between the pulley parts of each pulley being increased and decreased to increase the decrease at each pulley the rotating radius of a belt wound around both of the pulleys to change a belt ratio. A revolution controller for the transmission limits the rate of change of a target number of revolutions for an engine driving the transmission to a rate limit lower than a prescribed rate when the target number of revolutions of the engine specified by a speed change schedule map based on a throttle opening and a vehicle speed is changed during travel of the vehicle.

    摘要翻译: 无级变速器包括驱动侧滑轮和从动侧滑轮,每个滑轮和从动侧滑轮均具有固定皮带轮部分,并且具有被支撑以朝向和远离固定皮带轮部分运动的可动滑轮部分,每个滑轮的滑轮部分之间的槽宽度 增加和减少,以增加每个滑轮上减少缠绕在两个滑轮上的皮带的旋转半径以改变皮带的比例。 用于变速器的转速控制器将发动机驱动变速器的目标转数的变化速度限制在基于由速度变化进度表映射的发动机的目标转数基于基于 在车辆行驶期间改变节气门开度和车速。