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公开(公告)号:US20080032980A1
公开(公告)日:2008-02-07
申请号:US11630302
申请日:2005-06-27
Applicant: Mark Fraley , George Hartman
Inventor: Mark Fraley , George Hartman
IPC: A61K31/496 , A61K31/4155 , A61K31/5377 , C07D401/06 , C07D413/06 , C07D403/06 , A61P35/00 , A61K31/454
CPC classification number: C07D231/06 , C07D487/08
Abstract: 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:US20060134767A1
公开(公告)日:2006-06-22
申请号:US10520492
申请日:2003-07-03
Applicant: 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
Inventor: 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 classification number: C07K14/47 , C07K2299/00 , C12N9/14 , G01N33/6803 , G01N2500/04 , G16B15/00 , G16B20/00
Abstract: 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.
Abstract translation: 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:US20050171122A1
公开(公告)日:2005-08-04
申请号:US10497414
申请日:2002-12-02
Applicant: Mark Fraley , George Hartman , William Hoffman
Inventor: Mark Fraley , George Hartman , William Hoffman
IPC: A61K31/519 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P1/04 , A61P9/00 , A61P13/08 , A61P13/10 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P43/00 , C07D487/02 , C07D498/02 , C07D513/04 , C07D519/00
CPC classification number: C07D513/04
Abstract: The present invention relates to azolopyrimidinone 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:US20080027058A1
公开(公告)日:2008-01-31
申请号:US11630224
申请日:2005-06-27
Applicant: Paul Coleman , Christopher Cox , Mark Fraley , George Hartman , John Schreier
Inventor: Paul Coleman , Christopher Cox , Mark Fraley , George Hartman , John Schreier
IPC: A61K31/4155 , A61K31/454 , A61K31/496 , A61P35/00 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
CPC classification number: C07D231/12 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/14 , C07D487/08 , C07D491/107 , C07D491/113
Abstract: 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:US20050228003A1
公开(公告)日:2005-10-13
申请号:US10497553
申请日:2002-12-02
Applicant: Mark Fraley , George Hartman , William Hoffman
Inventor: Mark Fraley , George Hartman , William Hoffman
IPC: A61K31/138 , A61K31/337 , A61K31/4465 , A61K31/4535 , A61K31/519 , A61K31/551 , A61K31/5513 , A61K39/395 , A61K45/00 , A61P35/00 , C07D495/04 , C07D498/02 , C07D519/00
CPC classification number: C07D495/04 , C07D519/00
Abstract: The present invention relates to thienopyrimidinone 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.
Abstract translation: 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驱动蛋白的噻吩并嘧啶酮化合物。 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:US20050176737A1
公开(公告)日:2005-08-11
申请号:US10497385
申请日:2002-12-02
Applicant: Mark Fraley , George Hartman , William Hoffman
Inventor: Mark Fraley , George Hartman , William Hoffman
IPC: A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/5513 , A61K45/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07D487/04 , C07D519/00 , C07D491/02 , C07D498/02
CPC classification number: C07D487/04 , C07D519/00
Abstract: The present invention relates to azolopyrimidinone 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.
Abstract translation: 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驱动蛋白的偶氮嘧啶酮化合物。 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:US20050096344A1
公开(公告)日:2005-05-05
申请号:US10900662
申请日:2004-07-28
Applicant: Mark Fraley , Kenneth Arrington , Mark Bilodeau , George Hartman , William Hoffman , Yuntae Kim , Randall Hungate
Inventor: Mark Fraley , Kenneth Arrington , Mark Bilodeau , George Hartman , William Hoffman , Yuntae Kim , Randall Hungate
IPC: A61K31/495 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/02 , A61K31/4745 , C07D491/02 , C07D498/02
CPC classification number: C07D401/14 , A61K31/495 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K2300/00
Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号:US20070129356A1
公开(公告)日:2007-06-07
申请号:US10582826
申请日:2004-12-15
Applicant: Kenneth Arrington , Mark Fraley , George Hartman
Inventor: Kenneth Arrington , Mark Fraley , George Hartman
IPC: A61K31/541 , A61K31/5377 , A61K31/513 , C07D239/36
CPC classification number: C07D239/36
Abstract: The present invention relates to 2-phenylpyrimidinone 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.
Abstract translation: 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2-苯基嘧啶酮化合物。 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:US20050032817A1
公开(公告)日:2005-02-10
申请号:US10497382
申请日:2002-12-02
Applicant: Mark Fraley , George Hartman
Inventor: Mark Fraley , George Hartman
IPC: A61K31/138 , A61K31/4465 , A61K31/4535 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5517 , A61K39/395 , A61K45/00 , A61P35/00 , C07D491/04 , C07D491/048 , C07D519/00 , C07D491/02
CPC classification number: C07D491/04
Abstract: The present invention relates to furanopyrimidinone 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.
Abstract translation: 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驱动蛋白的呋喃并嘧啶酮化合物。 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:US20070149553A1
公开(公告)日:2007-06-28
申请号:US10582825
申请日:2004-12-15
Applicant: Kenneth Arrington , Mark Fraley , George Hartman
Inventor: Kenneth Arrington , Mark Fraley , George Hartman
IPC: A61K31/519 , C07D498/02
CPC classification number: C07D498/02 , A61K41/00 , C07D495/04
Abstract: The present invention relates to 2-phenylthienylpyrimidinone 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.
Abstract translation: 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疾病和用于抑制KSP驱动蛋白的2-苯基噻吩基嘧啶酮化合物。 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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