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公开(公告)号：US20060134767A1
公开(公告)日：2006-06-22
申请号：US10520492
申请日：2003-07-03
申请人： Carolyn Buser-Doepner , Paul Coleman , Christopher Cox , Mark Fraley , Robert Garbaccio , George Hartman , David Heimbrook , Lawrence Kuo , Hans Huber , Vinod Sardana , Maricel Torrent , Youwei Yan
发明人： Carolyn Buser-Doepner , Paul Coleman , Christopher Cox , Mark Fraley , Robert Garbaccio , George Hartman , David Heimbrook , Lawrence Kuo , Hans Huber , Vinod Sardana , Maricel Torrent , Youwei Yan
CPC分类号： C07K14/47 , C07K2299/00 , C12N9/14 , G01N33/6803 , G01N2500/04 , G16B15/00 , G16B20/00
摘要： The present invention is directed to the identification, characterization and three-dimensional structure of a novel ligand binding site of KSP. Binding of ligands to the novel binding site result in a conformational change in the three-dimensional structure of the protein and a modulation of the activity of KSP. This conformational change in turn results in the formation of a novel binding pocket in the KSP protein, which comprises the novel binding site of the instant invention.
摘要翻译： 本发明涉及KSP新型配体结合位点的鉴定，表征和三维结构。 配体与新结合位点的结合导致蛋白质三维结构的构象变化和KSP活性的调节。 这种构象变化又导致在KSP蛋白质中形成新的结合口袋，其包含本发明的新结合位点。
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公开(公告)号：US20050119484A1
公开(公告)日：2005-06-02
申请号：US10506702
申请日：2003-03-04
申请人： Michael Breslin , Paul Coleman , Christopher Cox , J. christopher Culberson , George Hartman , Brenda Mariano , Maricel Torrent
发明人： Michael Breslin , Paul Coleman , Christopher Cox , J. christopher Culberson , George Hartman , Brenda Mariano , Maricel Torrent
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P35/00 , C07D231/06 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/04 , C07D417/04 , C07D43/02
CPC分类号： C07D401/04 , C04B35/632 , C07D231/06 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/04 , C07D417/04
摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的二氢吡唑化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US07745639B2
公开(公告)日：2010-06-29
申请号：US10506702
申请日：2003-03-04
申请人： Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , J. Christopher Culberson , George D. Hartman , Brenda J. Mariano , Maricel Torrent
发明人： Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , J. Christopher Culberson , George D. Hartman , Brenda J. Mariano , Maricel Torrent
IPC分类号： C07D231/06 , A01N43/56
CPC分类号： C07D401/04 , C04B35/632 , C07D231/06 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/04 , C07D417/04
摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的二氢吡唑化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US07608739B2
公开(公告)日：2009-10-27
申请号：US10593504
申请日：2005-03-18
IPC分类号： C07C211/00
CPC分类号： C07C215/50 , C07C211/53 , C07C215/16 , C07C215/20 , C07C215/24 , C07C229/18 , C07C229/30 , C07C237/06 , C07C237/10 , C07C237/12 , C07C2601/02 , C07D211/26 , C07D231/12 , C07D261/08 , C07D295/04
摘要： The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的N-取代苄基苯胺衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20080234281A1
公开(公告)日：2008-09-25
申请号：US10593504
申请日：2005-03-18
IPC分类号： A61K31/495 , C07C211/52 , C07D241/04 , C07D211/26 , A61K31/445 , A61K31/167
CPC分类号： C07C215/50 , C07C211/53 , C07C215/16 , C07C215/20 , C07C215/24 , C07C229/18 , C07C229/30 , C07C237/06 , C07C237/10 , C07C237/12 , C07C2601/02 , C07D211/26 , C07D231/12 , C07D261/08 , C07D295/04
摘要： The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的N-取代苄基苯胺衍生物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20090149467A1
公开(公告)日：2009-06-11
申请号：US11991862
申请日：2006-09-11
申请人： Christopher J. Dinsmore , David J. Guerin , Barbara Hanney , Yuntae Kim , Keith L. Spencer , Maricel Torrent
发明人： Christopher J. Dinsmore , David J. Guerin , Barbara Hanney , Yuntae Kim , Keith L. Spencer , Maricel Torrent
IPC分类号： A61K31/506 , C07D403/12 , C07D401/14 , A61P35/00 , C07D401/12 , C07D487/04
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04
摘要： The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病的吡啶氧基 - 和嘧啶氧基吲哚衍生物，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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