Substituted imidazole derivative
    12.
    发明授权
    Substituted imidazole derivative 有权
    取代的咪唑衍生物

    公开(公告)号:US07718801B2

    公开(公告)日:2010-05-18

    申请号:US11661486

    申请日:2005-08-30

    IPC分类号: C07D239/00 C07D239/02

    CPC分类号: C07D471/04 C07D487/04

    摘要: The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1′, R2, R2′, R3, R3′, R4, and R4′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8′, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.

    摘要翻译: 本发明涉及由式[I]表示的化合物或其药学上可接受的盐或酯:其中:X 1,X 2,X 3和X 4可以相同或不同,各自为C或N,条件是 X1,X2,X3和X4中的两个为N; Y是CH或N; R1,R1',R2,R2',R3,R3',R4和R4'可以相同或不同,分别为氢原子,低级烷基等; R5是氢原子或甲基; R 6和R 7可以相同或不同,分别为氢原子,低级烷基等; R 8和R 8'可以相同或不同,分别为氢原子,低级烷基等; R9是可以被取代的芳基或杂芳基; n为1〜3的整数,PLK1抑制剂或含有该PLK1抑制剂的抗癌剂。

    Pyrimidopyrimidoindazole derivative
    14.
    发明授权
    Pyrimidopyrimidoindazole derivative 失效
    嘧啶并嘧啶并吲唑衍生物

    公开(公告)号:US08288396B2

    公开(公告)日:2012-10-16

    申请号:US13202773

    申请日:2010-02-18

    IPC分类号: A61K31/519 C07D487/14

    CPC分类号: C07D487/14 C07D519/00

    摘要: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): R1 means a —(C═O)aOb(C1-C6)alkyl group, a —(C═O)aOb(C2-C6)alkenyl group, a —(C═O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C═O)aOb(C1-C6)alkyl group or a group of —(C═O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.

    摘要翻译: 本发明提供一种用于癌症化疗或放射治疗的新型抗癌剂或敏化剂。 通式(I)的化合物:其中A表示芳基或杂芳基,或式(a)的基团:R 1表示 - (C = O)a O b(C 1 -C 6)烷基, - (C = O)a O b(C 2 -C 6)烯基, - (C = O)a O b(C 3 -C 6)环烷基,芳基或杂芳基; R2和R3各自表示氢原子,卤素原子,羟基,羧基, - (C = O)aOb(C1-C6)烷基或 - (C = O)aN(R1e) R2e; R4表示氢原子或(C1-C6)烷基等具有优异的Wee1激酶抑制作用,因此可用于医学领域,特别是在各种癌症治疗领域。

    Novel indolopyrrolocarbazole derivative with antitumor activity
    17.
    发明申请
    Novel indolopyrrolocarbazole derivative with antitumor activity 审中-公开
    具有抗肿瘤活性的新型吲哚并吡咯并咔唑衍生物

    公开(公告)号:US20070042975A1

    公开(公告)日:2007-02-22

    申请号:US10571861

    申请日:2004-09-14

    IPC分类号: A61K31/7056 C07H19/22

    CPC分类号: A61K31/7056

    摘要: The present invention relates to a novel indolopyrrolocarbazole derivative which is represented by the formula [I]: wherein: A represents O, NH, or CH2; R1 represents a single bond, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, etc.; R2 represents a phenyl group, a naphthyl group, or a five- or six-membered aromatic or aliphatic heterocyclic ring having at least one atom selected from N, S, or O, wherein the phenyl group, naphthyl group, aromatic or aliphatic heterocyclic ring may be substituted; and G represents a hexose group or a pentose group, or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及由式[I]表示的新型吲哚并吡咯并唑衍生物:其中:A表示O,NH或CH 2。 R 1表示单键,低级烷基,低级烯基,低级炔基等; R 2表示具有至少一个选自N,S或O的原子的苯基,萘基或五元或六元芳族或脂族杂环,其中苯基, 萘基,芳族或脂肪族杂环可以被取代; G表示己糖基或戊糖基,或其药学上可接受的盐。