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131.发明授权Fluorinated 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP 失效有丝分裂驱动蛋白KSP的氟化2,4-二芳基-2,5-二氢吡咯抑制剂公开(公告)号：US07465746B2
公开(公告)日：2008-12-16
申请号：US10915743
申请日：2004-08-11
IPC分类号： A61K31/4468
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.
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：US20080287414A1
公开(公告)日：2008-11-20
申请号：US11630231
申请日：2005-06-27
申请人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
发明人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Chunze Li , Lou Anne Neilson , Christy M. Olson , Edward S. Tasber
IPC分类号： A61K31/5383 , A61P35/00 , A61K31/551 , A61K31/542 , C07D498/04
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to tricyclic pyrazoles according to Formula (I) 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驱动蛋白的根据式（I）的三环吡唑。 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：US20080274107A1
公开(公告)日：2008-11-06
申请号：US12148649
申请日：2008-04-21
申请人： Mark E. Fraley , Kenneth L. Arrington , Mark T. Bilodeau , George D. Hartman , William F. Hoffman , Yuntae Kim , Randall W. Hungate
发明人： Mark E. Fraley , Kenneth L. Arrington , Mark T. Bilodeau , George D. Hartman , William F. Hoffman , Yuntae Kim , Randall W. Hungate
IPC分类号： A61K39/395 , C07D215/20 , A61K31/337 , A61K31/445 , A61K31/47 , A61P43/00
CPC分类号： C07D401/14 , A61K31/495 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： 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.
摘要翻译： 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化的方法 ，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。
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公开(公告)号：US07378411B2
公开(公告)日：2008-05-27
申请号：US10497553
申请日：2002-12-02
IPC分类号： C07D495/04 , C07D413/06 , C07D413/08 , C07D243/08 , C07D243/14 , C07D245/02 , C07D245/06 , A61K31/519 , A61K31/5355 , A61K31/551 , A61K31/5513 , A61P35/04
CPC分类号： C07D495/04 , C07D519/00
摘要： 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.
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：US07265134B2
公开(公告)日：2007-09-04
申请号：US10486574
申请日：2002-08-13
申请人： George D. Hartman , Thomas J. Tucker , John T. Sisko , Anthony M. Smith , William C. Lumma, Jr.
发明人： George D. Hartman , Thomas J. Tucker , John T. Sisko , Anthony M. Smith , William C. Lumma, Jr.
IPC分类号： A61K31/426 , A61K31/4535 , C07D417/12 , C07D401/12 , C07D277/38
CPC分类号： C07D417/12 , A61K31/427 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D277/48 , C07D417/14 , A61K2300/00
摘要： 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：US06586424B2
公开(公告)日：2003-07-01
申请号：US10062351
申请日：2002-02-01
IPC分类号： C07D41312
CPC分类号： C07D417/12 , C07D417/14
摘要： 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：US06420382B2
公开(公告)日：2002-07-16
申请号：US09788718
申请日：2001-02-20
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： 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：US06117842A
公开(公告)日：2000-09-12
申请号：US264736
申请日：1999-03-09
CPC分类号： C07K5/0205 , C07K5/0202 , A61K38/00 , Y10S514/822
摘要： Compounds of this invention have the formula:X--(CH.sub.2).sub.n --C(O)NH--A--C(COOR.sup.5)R.sup.3 R.sup.4or a pharmaceutically acceptable salt thereof, e.g. ##STR1## which are useful for inhibiting fibrinogen binding to blood platelets, thereby inhibiting platelet aggregation.
摘要翻译： 本发明的化合物具有下式：X-（CH 2）n -C（O）NH-A-C（COOR 5）R 3 R 4或其药学上可接受的盐，例如 其可用于抑制血纤维蛋白原与血小板结合，从而抑制血小板聚集。
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公开(公告)号：USRE36481E
公开(公告)日：2000-01-04
申请号：US188158
申请日：1998-11-04
申请人： Edward S. Inamine , Otto D. Hensens , David R. Houck , Ta J. Lee , Robert L. Smith , Wasyl Halczenko , George D. Hartman , Gerald E. Stokker
发明人： Edward S. Inamine , Otto D. Hensens , David R. Houck , Ta J. Lee , Robert L. Smith , Wasyl Halczenko , George D. Hartman , Gerald E. Stokker
IPC分类号： C07C69/732 , C07D309/30 , A61K31/335 , C07D315/00
CPC分类号： C07D309/30 , C07C69/732
摘要： Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##
摘要翻译： 新型3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂可用作抗高血胆固醇血症药，并由以下一般结构式（I）和（II）表示：
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公开(公告)号：US5856326A
公开(公告)日：1999-01-05
申请号：US600728
申请日：1996-03-01
申请人： Neville J. Anthony , Terrence M. Ciccarone , Christopher J. Dinsmore , Robert P. Gomez , Theresa M. Williams , George D. Hartman
发明人： Neville J. Anthony , Terrence M. Ciccarone , Christopher J. Dinsmore , Robert P. Gomez , Theresa M. Williams , George D. Hartman
IPC分类号： C07D233/54 , C07D241/08 , C07D295/192 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , A61K31/495 , C07D241/04
CPC分类号： C07D233/64 , C07D241/08 , C07D295/192 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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