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公开(公告)号：US20080027118A1
公开(公告)日：2008-01-31
申请号：US11630303
申请日：2005-06-27
申请人： Paul Coleman , Christopher Cox , George Hartman
发明人： Paul Coleman , Christopher Cox , George Hartman
IPC分类号： A61K31/415 , A61P35/00 , C07D231/02
CPC分类号： C07D231/06 , C07F9/65031
摘要： The present invention relates to prodrugs of 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，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的二氢吡唑化合物的前药。 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：US20060105997A1
公开(公告)日：2006-05-18
申请号：US10517559
申请日：2003-06-12
申请人： Kenneth Arrington , Paul Coleman , Christopher Cox , Mark Fraley , Robert Garbaccio , George Hartman , William Hoffman , Edward Tasber
发明人： Kenneth Arrington , Paul Coleman , Christopher Cox , Mark Fraley , Robert Garbaccio , George Hartman , William Hoffman , Edward Tasber
IPC分类号： A61K31/675 , A61K31/4025 , C07D43/02
CPC分类号： C07D401/12 , C07D207/14 , C07D207/20 , C07D207/48 , C07D265/30 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12
摘要： The present invention relates to dihydropyrrole 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，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的二氢吡咯化合物。 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：US20050084875A1
公开(公告)日：2005-04-21
申请号：US10821653
申请日：2004-04-09
申请人： Paul Coleman , Nienwen Chow , Christopher Cox
发明人： Paul Coleman , Nienwen Chow , Christopher Cox
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6883 , C12Q2600/158
摘要： The present invention provides methods for profiling mRNA production in single cells, in particular, during disease stages. The invention also provides a method for monitoring gene expression in a single cell which has been isolated from tissue. The methods of the present invention may be used to diagnose or monitor the progression of disease.
摘要翻译： 本发明提供了在单细胞中，特别是在疾病阶段期间分析mRNA产生的方法。 本发明还提供了一种用于监测从组织中分离的单细胞中的基因表达的方法。 本发明的方法可用于诊断或监测疾病的进展。
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公开(公告)号：US20050043357A1
公开(公告)日：2005-02-24
申请号：US10915743
申请日：2004-08-11
IPC分类号： A61P35/00 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/454 , C07D43/02
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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公开(公告)号：US20080027058A1
公开(公告)日：2008-01-31
申请号：US11630224
申请日：2005-06-27
申请人： Paul Coleman , Christopher Cox , Mark Fraley , George Hartman , John Schreier
发明人： Paul Coleman , Christopher Cox , Mark Fraley , George Hartman , John Schreier
IPC分类号： A61K31/4155 , A61K31/454 , A61K31/496 , A61P35/00 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
CPC分类号： C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/14 , C07D487/08 , C07D491/107 , C07D491/113
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.
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公开(公告)号：US20060100191A1
公开(公告)日：2006-05-11
申请号：US10531495
申请日：2003-10-14
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/4025 , A61K31/401 , C07D413/02 , C07D403/02
CPC分类号： C07D405/12 , C07D207/20 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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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：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：US20050038074A1
公开(公告)日：2005-02-17
申请号：US10916096
申请日：2004-08-11
IPC分类号： A61P35/00 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/454 , C07D43/02
CPC分类号： C07D413/14 , C04B35/632 , C07D401/12 , C07D401/14 , C07D417/14
摘要： The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is 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，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的二氢吡咯化合物。 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：US20060287302A1
公开(公告)日：2006-12-21
申请号：US10568000
申请日：2004-08-11
申请人： Paul Coleman , Christopher Cox
发明人： Paul Coleman , Christopher Cox
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4025 , A61K31/454 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D403/12
摘要： The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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