Novel aminopyrimidine derivatives as PLK1 inhibitors
    1.
    发明申请
    Novel aminopyrimidine derivatives as PLK1 inhibitors 有权
    新型氨基嘧啶衍生物作为PLK1抑制剂

    公开(公告)号:US20080305081A1

    公开(公告)日:2008-12-11

    申请号:US12002546

    申请日:2007-12-18

    CPC分类号: C07D471/04

    摘要: The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R3 and R4, which may be the same or different, are each a hydrogen atom, a lower alkyl group, NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group, or the like; and R5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.

    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R 1和R 2可以相同或不同,分别为氢原子,低级烷基,环烷基 ,等等; R 3和R 4可以相同或不同,分别为氢原子,低级烷基,NR a R b,苯基,被苯基取代的低级烷基,4-至7-元脂族杂环基, 被4-至7-元脂族杂环基取代的低级烷基,5或6元芳族杂环基,被5或6元芳族杂环基取代的低级烷基等; R5为氢原子,氰基,卤素原子或低级烷基。

    Novel 2-pyridinecarboxamide derivatives
    3.
    发明申请
    Novel 2-pyridinecarboxamide derivatives 有权
    新型2-吡啶甲酰胺衍生物

    公开(公告)号:US20060258701A1

    公开(公告)日:2006-11-16

    申请号:US10545424

    申请日:2004-02-13

    CPC分类号: C07D471/04 C07D417/14

    摘要: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物,其由式(I)表示:其中X 1表示氮原子, 硫原子,氧原子等; R 1表示6至10元芳基,5至7元杂芳基等; D表示氧原子或硫原子; R和R 3相同或不同,各自表示氢原子,低级烷基等; 式(II)表示任选取代的5〜7元杂芳基等; 式(III)表示单环或双环杂芳基]或其药学上可接受的盐。

    Substituted imidazole derivative
    6.
    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。

    2-pyridine carboxamide derivatives
    7.
    发明授权
    2-pyridine carboxamide derivatives 有权
    2-吡啶甲酰胺衍生物

    公开(公告)号:US07629362B2

    公开(公告)日:2009-12-08

    申请号:US10545424

    申请日:2004-02-13

    CPC分类号: C07D471/04 C07D417/14

    摘要: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及具有葡糖激酶活化作用并可用作糖尿病治疗剂的化合物,其由式(I)表示:[其中X1表示氮原子,硫原子,氧原子等 ; R1表示6-至10-元芳基,5-至7-元杂芳基等; D表示氧原子或硫原子; R2和R3相同或不同,各自表示氢原子,低级烷基等; 式(II)表示任选取代的5〜7元杂芳基等; 式(III)表示单环或双环杂芳基]或其药学上可接受的盐。

    Aminopyrimidine derivatives as PLK1 inhibitors
    10.
    发明授权
    Aminopyrimidine derivatives as PLK1 inhibitors 有权
    氨基嘧啶衍生物作为PLK1抑制剂

    公开(公告)号:US07977336B2

    公开(公告)日:2011-07-12

    申请号:US12002546

    申请日:2007-12-18

    IPC分类号: C07D403/04 A61K31/506

    CPC分类号: C07D471/04

    摘要: The present invention relates to a compound represented by Formula [I]: or a pharmaceutically acceptable salt or ester thereof, wherein R1 and R2, which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R3 and R4, which may be the same or different, are each a hydrogen atom, a lower alkyl group, NRaRb, a phenyl group, a lower alkyl group substituted with a phenyl group, a 4-to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5-or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5-or 6-membered aromatic heterocyclic group, or the like; and R5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.

    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R 1和R 2可以相同或不同,分别为氢原子,低级烷基,环烷基 ,等等; R 3和R 4可以相同或不同,分别为氢原子,低级烷基,NR a R b,苯基,被苯基取代的低级烷基,4-至7-元脂族杂环基, 被4〜7元脂肪族杂环基取代的低级烷基,5元或6元芳族杂环基,被5元或6元芳族杂环基取代的低级烷基等。 R5为氢原子,氰基,卤素原子或低级烷基。