Staurosporin derivatives
    1.
    发明授权
    Staurosporin derivatives 失效
    星孢菌素衍生物

    公开(公告)号:US06806266B1

    公开(公告)日:2004-10-19

    申请号:US10030618

    申请日:2002-01-11

    IPC分类号: C07D49822

    CPC分类号: C07D498/22 A61K31/553

    摘要: The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.

    摘要翻译: 本发明提供包含星形孢菌素衍生物或其药学上可接受的盐作为活性成分的抗肿瘤剂,其由通式(I)表示:其中R 1表示氢,羟基或低级烷氧基,R 2 和R 3相同或不同,表示氢,取代或未取代的烷基,取代或未取代的低级烯基,取代或未取代的低级炔基,取代或未取代的芳基,取代或未取代的杂环基,卤素,硝基,甲酰基, 等等,R 4表示氢等,R 5表示NR 11A R 12A(其中R 11A和R 12A表示氢,取代或未取代的低级烷基等), 条件是R 2和R 3不同时为氢。

    Mitotic Kinesin Inhibitor
    2.
    发明申请

    公开(公告)号:US20110275827A1

    公开(公告)日:2011-11-10

    申请号:US13188819

    申请日:2011-07-22

    IPC分类号: C07D285/135

    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.

    Hsp90 Family protein Inhibitors
    3.
    发明申请
    Hsp90 Family protein Inhibitors 有权
    Hsp90家族蛋白抑制剂

    公开(公告)号:US20070265268A1

    公开(公告)日:2007-11-15

    申请号:US11718079

    申请日:2005-11-09

    摘要: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoic acid derivative represented by General Formula (I): [wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aroyl, or the like; R2 represents —NR14R15 (wherein R14 and R15 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R3 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; and R4 and R6 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like] or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoic acid derivative or said prodrug.

    摘要翻译: 本发明提供Hsp90家族蛋白抑制剂,其包含通式(I)表示的苯甲酸衍生物作为活性成分:[其中,n表示0〜10的整数, R 1表示取代或未取代的低级烷氧基羰基,取代或未取代的芳酰基等; R 2表示-NR 14 R 15(其中R 14和R 15) 可以相同或不同,各自表示氢原子,取代或未取代的低级烷基,取代或未取代的芳烷基等); R 3和R 5可以相同或不同,各自表示氢原子,取代或未取代的低级烷基等; R 4和R 6可以相同或不同,各自表示氢原子,卤素,取代或未取代的低级烷基等]或其前药,或 所述苯甲酸衍生物或所述前药的药学上可接受的盐。

    Mitotic Kinesin Inhibitor
    5.
    发明申请
    Mitotic Kinesin Inhibitor 审中-公开
    有丝分裂驱动蛋白抑制剂

    公开(公告)号:US20110004000A1

    公开(公告)日:2011-01-06

    申请号:US12883338

    申请日:2010-09-16

    IPC分类号: C07D285/135

    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活性成分:[其中R 1表示氢原子等,R 2表示氢原子,-C(= W)R6(其中W表示氧原子或硫原子,R6表示取代或未取代的低级烷基等)等,R3表示-C(= Z)R19(其中Z表示氧原子或硫原子 原子,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表示取代或未取代的芳基等〕等。