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    Novel Biphenyl Compounds And Their Use
    4.
    发明申请
    Novel Biphenyl Compounds And Their Use 审中-公开
    新型联苯化合物及其用途

    公开(公告)号：US20070265345A1

    公开(公告)日：2007-11-15

    申请号：US11632331

    申请日：2005-07-27

    申请人： Amita Chaudhari ,  Dashyant Dhanak ,  Steven Knight ,  David Morgans ,  Cynthia Parrish

    发明人： Amita Chaudhari ,  Dashyant Dhanak ,  Steven Knight ,  David Morgans ,  Cynthia Parrish

    IPC分类号： A61K31/17 ,  A61K31/165 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  A61P9/00 ,  C07C233/00 ,  C07C273/18 ,  C07C275/00

    CPC分类号： C07C275/28 ,  C07C233/15 ,  C07C233/43 ,  C07C259/06 ,  C07C275/30 ,  C07C275/40 ,  C07C275/42 ,  C07C275/64 ,  C07C317/24 ,  C07C317/42 ,  C07C323/44 ,  C07C335/16 ,  C07D209/02 ,  C07D307/79 ,  C07D317/66 ,  C07D319/18

    摘要： The invention is directed to certain biphenyl compounds. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Y are as defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are KSP inhibitors, particularly human KSP inhibitors, and can be useful for the treatment for a variety of diseases and conditions, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders, fungal disorders, and inflammation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting KSP and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. In an additional aspect, the invention provides methods of screening for compounds that will bind to a KSP kinesin, for example compounds that will displace or compete with the binding of the compounds of the invention. The methods comprise combining a labeled compound of the invention, a KSP kinesin, and at least one candidate agent and determining the binding of the candidate bioactive agent to the KSP kinesin. In a further aspect, the invention provides methods of screening for modulators of KSP kinesin activity. The methods comprise combining a compound of the invention, a KSP kinesin, and at least one candidate agent and determining the effect of the candidate bioactive agent on the KSP kinesin activity.

    摘要翻译： 本发明涉及某些联苯化合物。 具体地说，本发明涉及式Ⅰ化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Y如下所定义，及其药学上可接受的盐。 本发明的化合物是KSP抑制剂，特别是人KSP抑制剂，并且可用于治疗各种疾病和病症，例如癌症，增生，再狭窄，心脏肥大，免疫疾病，真菌病症和炎症。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制KSP和治疗与其相关的病症的方法。 在另一方面，本发明提供筛选将结合KSP驱动蛋白的化合物的方法，例如将取代或与本发明化合物结合竞争的化合物。 所述方法包括组合本发明的标记化合物，KSP驱动蛋白和至少一种候选试剂，并确定候选生物活性剂与KSP驱动蛋白的结合。 另一方面，本发明提供筛选KSP驱动蛋白活性调节剂的方法。 所述方法包括组合本发明的化合物，KSP驱动蛋白和至少一种候选试剂，并确定候选生物活性剂对KSP驱动蛋白活性的影响。