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公开(公告)号：US4678806A
公开(公告)日：1987-07-07
申请号：US902895
申请日：1986-09-02
IPC分类号： C07D207/08 , A61K31/195 , A61K31/22 , A61K31/415 , A61P3/06 , A61P9/10 , A61P43/00 , C07C67/00 , C07C231/00 , C07C233/45 , C07C235/26 , C07C235/30 , C07C313/00 , C07C323/59 , C07D209/14 , C07D233/64 , A61K31/235 , C07C101/72
CPC分类号： A61K31/22 , C07C233/45
摘要： Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.
摘要翻译： 可用作抗高胆固醇血症药的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂的前药，其由以下通式（I）表示：其中（I）其酰氨基部分位于 公开了L-构型及其药学上可接受的盐。
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公开(公告)号：US4943588A
公开(公告)日：1990-07-24
申请号：US305060
申请日：1989-02-01
IPC分类号： C07D319/06 , C07H15/26
CPC分类号： C07D319/06 , C07H15/26
摘要： Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## are disclosed.
摘要翻译： 公开了可用作抗高胆固醇血症药物并由以下一般结构式（I）表示的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂的前药：
（I）。 -
公开(公告)号：US4837205A
公开(公告)日：1989-06-06
申请号：US902894
申请日：1986-09-02
IPC分类号： A61K31/335 , A61K31/357 , A61K31/70 , A61K31/7028 , A61P3/06 , C07D319/06 , C07H15/26
CPC分类号： C07H15/26 , C07D319/06
摘要： Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## are disclosed.
摘要翻译： 公开了可用作抗高胆固醇血症药物并由以下一般结构式（I）表示的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂的前药：
（I）。 -
公开(公告)号：US4736064A
公开(公告)日：1988-04-05
申请号：US912867
申请日：1986-09-29
申请人： John J. Baldwin , Wasyl Halczenko , George Hartman
发明人： John J. Baldwin , Wasyl Halczenko , George Hartman
IPC分类号： C07D295/14 , A61K31/22 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P3/06 , A61P9/10 , A61P43/00 , C07C67/00 , C07C227/00 , C07C229/06 , C07D295/15 , C07C69/76
CPC分类号： C07D295/15
摘要： Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## and pharmaceutically acceptable salts thereof are disclosed.
摘要翻译： 公开了可用作抗高胆固醇血症药物并由以下一般结构式（I）表示的3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂的前药：其中药学上可接受的盐和其药学上可接受的盐。
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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
申请人： Mark Fraley , George Hartman
发明人： Mark Fraley , George Hartman
IPC分类号： A61K31/496 , A61K31/4155 , A61K31/5377 , C07D401/06 , C07D413/06 , C07D403/06 , A61P35/00 , A61K31/454
CPC分类号： C07D231/06 , C07D487/08
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：US20060142178A1
公开(公告)日：2006-06-29
申请号：US10510068
申请日：2003-04-04
申请人： Stanley Barnett , Deborah DeFeo-Jones , George Hartman , Kathleen Haskell , Hans Huber , Craig Lindsley , Zhijian Zhao
发明人： Stanley Barnett , Deborah DeFeo-Jones , George Hartman , Kathleen Haskell , Hans Huber , Craig Lindsley , Zhijian Zhao
IPC分类号： A61K38/00 , A61K31/415
CPC分类号： A61K45/06 , A61K31/415 , A61K31/495 , A61K31/50 , A61K31/53 , A61K38/45 , A61K2300/00
摘要： The present invention is directed to a method of treating cancer which comprises administration of a compound which selectively inhibits the activity of one or two of the isoforms of Akt, a serine/threonine protein kinase. The invention is particularly directed to the method wherein the compound is dependent on the presence of the pleckstrin homology domain of Akt for its inhibitory activity.
摘要翻译： 本发明涉及一种治疗癌症的方法，其包括施用选择性抑制一种或两种Akt，丝氨酸/苏氨酸蛋白激酶同工型的活性的化合物。 本发明特别涉及其中化合物取决于Akt的pleckstrin同源结构域的抑制活性的方法。
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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：US20050171122A1
公开(公告)日：2005-08-04
申请号：US10497414
申请日：2002-12-02
申请人： Mark Fraley , George Hartman , William Hoffman
发明人： Mark Fraley , George Hartman , William Hoffman
IPC分类号： 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分类号： C07D513/04
摘要： 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：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：US20050015043A1
公开(公告)日：2005-01-20
申请号：US10739872
申请日：2003-12-18
CPC分类号： A61B17/3421 , A61B17/3423 , A61B17/3474 , A61B2017/00265 , A61B2090/064 , A61M37/00
摘要： A trocar assembly for use in surgery in a patient, comprising an elongated outer tubular member having a first or proximal end and a second or distal end. The proximal end has a housing enclosing a fluid pressure chamber therein. The distal end of the outer tubular member has a gaseous fluid discharge arrangement therethrough, through which a medical instrument is disposed for surgical manipulation of the patient.
摘要翻译： 一种用于患者手术的套管针组件，包括具有第一或近端和第二或远端的细长外管状构件。 近端具有在其中包围流体压力室的壳体。 外管状构件的远端具有穿过其中的气体流体排放装置，医疗器械通过该远处设置用于患者的手术操作。
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