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20 条记录 (耗时 0.062 秒)

    Fragment Ligated Inhibitors Selective for the Polo Box Domain of PLK1
    3.
    发明申请
    Fragment Ligated Inhibitors Selective for the Polo Box Domain of PLK1 有权
    片段缩合抑制剂选择性PLK1的Polo框域

    公开(公告)号：US20120202970A1

    公开(公告)日：2012-08-09

    申请号：US13365707

    申请日：2012-02-03

    申请人： Campbell McInnes ,  Doaa Boshra Farag

    发明人： Campbell McInnes ,  Doaa Boshra Farag

    IPC分类号： C07K5/00

    CPC分类号： G01N33/573 ,  A61K38/06 ,  A61K38/08 ,  A61K47/48023 ,  A61K47/48038 ,  A61K47/48061 ,  A61K47/54 ,  A61K47/542 ,  A61K47/545 ,  C07K5/081 ,  C07K7/06 ,  C07K2317/34 ,  C12N9/12 ,  C12N9/16 ,  C12Y207/11021 ,  C12Y301/03048 ,  G01N2333/912 ,  G01N2500/02 ,  G06F19/18

    摘要： Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.

    摘要翻译： 描述了开发靶向PLK1蛋白质的polo-box结构域的非肽抑制剂的方法。 方法包括开发肽抑制剂的结构活性关系，随后开发部分肽抑制剂的非肽片段替代物。 非肽片段可以提供与取代的肽类似的结构活性关系。 通过理解肽结构 - 活性关系促进的迭代计算和合成过程中鉴定了关键结合决定簇的片段替代。 该方法由通过合成和测试已知PBD结合基序的截短和突变的类似物获得的肽结构 - 活性数据通知。

    Benzthiazole-3 oxides useful for the treatment of proliferative disorders
    6.
    发明申请
    Benzthiazole-3 oxides useful for the treatment of proliferative disorders 审中-公开

    公开(公告)号：US20060040997A1

    公开(公告)日：2006-02-23

    申请号：US11192893

    申请日：2005-07-28

    申请人： Campbell McInnes ,  Christopher Meades ,  Mokdad Mezna ,  Peter Fischer

    发明人： Campbell McInnes ,  Christopher Meades ,  Mokdad Mezna ,  Peter Fischer

    IPC分类号： A61K31/428

    CPC分类号： C07D277/68 ,  A61K31/428 ,  Y02A50/411

    摘要： The present invention relates to the use of a compound of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and R4 are each independently H, NO2, CF3, SCF3, CN, halo, OH, OR6, NH2, NHR6, NR6R7, N+R6R7R8, COOH, COOR6, CONH2, CONHR6, CONR6R7, COH, COR6, SR6, SOR6, SO2R6, SO2OH, SO2OR6, SO2NH2, SO2NHR6, SO2NR6R7, alkyl, cycloalkyl, cycloheteroalkyl, aryl, or heteroaryl, with the proviso that at least one of R1, R2, R3, and R4 is other than H; or R1 and R2, R2 and R3, or R3 and R4, may together form part of a fused or unfused saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; R5 is OH, OR9, CN, CONH2, CONHNH2, CONHOH, CONHR9, CONR9R10, NH2, NHR9, or NR9R10; each R6, R7 and R8 is independently hydrocarbyl, or two of R6, R7 and R8 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; each R9 and R10 is independently hydrocarbyl, or R9 and R10 together form part of a saturated or unsaturated ring system, optionally containing up to two heteroatoms selected from N, O, and S; in the preparation of a medicament for treating a proliferative disorder.

    CYCLIN BASED INHIBITORS OF CDK2 AND CDK4
    8.
    发明申请
    CYCLIN BASED INHIBITORS OF CDK2 AND CDK4 有权
    基于CYCLIN的CDK2和CDK4抑制剂

    公开(公告)号：US20140316107A1

    公开(公告)日：2014-10-23

    申请号：US14017988

    申请日：2013-09-04

    申请人： Campbell McInnes ,  Shu Liu

    发明人： Campbell McInnes ,  Shu Liu

    IPC分类号： C07K7/06

    CPC分类号： C07K7/06 ,  G01N2500/02 ,  G06F19/16 ,  G06F19/18

    摘要： Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

    摘要翻译： 已经研究了肽抑制剂与细胞周期蛋白D1凹槽结合的结构和功能分析，并用于设计提供结构 - 活性关系的基础的肽，具有改进的结合并具有作为化学生物学探针的发展潜力，作为潜在诊断和治疗 用于治疗包括癌症和炎症在内的增殖性疾病。

    Cyclin Based Inhibitors of CDK2 and CDK4
    9.
    发明申请
    Cyclin Based Inhibitors of CDK2 and CDK4 审中-公开

    公开(公告)号：US20130289240A1

    公开(公告)日：2013-10-31

    申请号：US13851661

    申请日：2013-03-27

    申请人： Campbell McInnes ,  Shu Liu

    发明人： Campbell McInnes ,  Shu Liu

    IPC分类号： G06F19/12 ,  C07K5/11

    CPC分类号： G16B5/00 ,  C07K5/1019 ,  C07K14/4738

    摘要： Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

    Cyclin based inhibitors of CDK2 and CDK4
    10.
    发明授权
    Cyclin based inhibitors of CDK2 and CDK4 有权
    基于细胞周期蛋白的CDK2和CDK4抑制剂

    公开(公告)号：US08566072B2

    公开(公告)日：2013-10-22

    申请号：US13088694

    申请日：2011-04-18

    申请人： Campbell McInnes ,  Shu Liu

    发明人： Campbell McInnes ,  Shu Liu

    IPC分类号： G06K19/16 ,  G06K19/18 ,  C07K7/06

    CPC分类号： C07K7/06 ,  G01N2500/02 ,  G06F19/16 ,  G06F19/18

    摘要： Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.

    摘要翻译： 已经研究了肽抑制剂与细胞周期蛋白D1凹槽结合的结构和功能分析，并用于设计提供结构 - 活性关系的基础的肽，具有改进的结合并具有作为化学生物学探针的发展潜力，作为潜在诊断和治疗 用于治疗包括癌症和炎症在内的增殖性疾病。