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公开(公告)号：US07329762B2
公开(公告)日：2008-02-12
申请号：US10559857
申请日：2004-06-08
IPC分类号： C07D207/00 , C07D405/00 , C07D295/00 , A01N43/36 , A61K31/40
CPC分类号： C07D401/12 , C07D207/20 , C07D209/48 , C07F9/572 , C07F9/65586
摘要： The present invention relates to phosphate ester prodrugs of 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： 本发明涉及二氢吡咯化合物的磷酸酯前体药物，其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。 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：US07732472B2
公开(公告)日：2010-06-08
申请号：US11660349
申请日：2005-08-15
IPC分类号： A61K31/42 , C07D261/04
CPC分类号： C07D261/04 , C07D413/12
摘要： The present invention relates to dihydroisoxazoles 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疾病和用于抑制KSP驱动蛋白的二氢异恶唑。 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：US07632833B2
公开(公告)日：2009-12-15
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： C07D498/04 , A61K31/5383 , A61K31/551 , A61K31/542
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：US07348440B2
公开(公告)日：2008-03-25
申请号：US10517559
申请日：2003-06-12
申请人： Kenneth L. Arrington , Paul J. Coleman , Christopher D. Cox , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , William F. Hoffman , Edward S. Tasber
发明人： Kenneth L. Arrington , Paul J. Coleman , Christopher D. Cox , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , William F. Hoffman , Edward S. Tasber
IPC分类号： C07D207/00 , C07D403/00 , C07D213/00 , C07D401/00 , C07D271/00 , C07D277/20 , C07D261/06 , C07D285/14 , C07D249/08 , C07D231/00 , A61K31/535 , A61K31/497 , A01N43/40 , A01N43/82 , A01N43/80 , A01N43/64 , A01N43/56 , A01N43/36
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：US20090258852A1
公开(公告)日：2009-10-15
申请号：US11988394
申请日：2006-06-30
申请人： Kenneth L. Arrington , Vadim Y. Dudkin , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Shaei Y. Huang , Constantine Kreatsoulas , Edward S. Tasber
发明人： Kenneth L. Arrington , Vadim Y. Dudkin , Mark E. Fraley , Robert M. Garbaccio , George D. Hartman , Shaei Y. Huang , Constantine Kreatsoulas , Edward S. Tasber
IPC分类号： A61K31/5377 , A61K31/473 , C07D413/14 , C07D401/02
CPC分类号： C07D401/06 , C07D221/12 , C07D401/04 , C07D401/12 , C07D413/04 , C07D498/06
摘要： The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的苯并异喹啉酮和氮杂衍生物的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US20090005418A1
公开(公告)日：2009-01-01
申请号：US11660349
申请日：2005-08-15
IPC分类号： A61K31/454 , C07D261/04 , A61K31/42 , A61P35/00 , C07D401/12
CPC分类号： C07D261/04 , C07D413/12
摘要： The present invention relates to dihydroisoxazoles 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疾病和用于抑制KSP驱动蛋白的二氢异恶唑。 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：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：US08975286B2
公开(公告)日：2015-03-10
申请号：US13391315
申请日：2010-08-16
申请人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
发明人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
IPC分类号： C07D409/14 , C07D405/14 , C07D401/14 , C07D401/12 , C07D403/12 , C07D249/18 , A61K31/506 , A61K31/497 , A61K31/496 , A61K31/454 , A61K31/4545 , A61K31/444 , A61K31/4439 , A61K31/4192 , C07D417/14 , C07D403/14 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04
CPC分类号： C07D417/14 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , C07D249/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04 , C07D498/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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9.发明授权公开(公告)号：US07192949B2
公开(公告)日：2007-03-20
申请号：US11410341
申请日：2006-04-24
IPC分类号： C07D239/70 , C07D401/12 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06
摘要： The present invention relates to cycloalkylpyrimidinone 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疾病和用于抑制KSP驱动蛋白的环烷基嘧啶酮化合物。 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：US08785481B2
公开(公告)日：2014-07-22
申请号：US13247009
申请日：2011-09-28
申请人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
发明人： Douglas C. Beshore , Vadim Dudkin , Robert M. Garbaccio , Adam W. Johnson , Scott D. Kuduk , Jason W. Skudlarek , Cheng Wang , Mark E. Fraley
IPC分类号： A61K31/4245 , C07D249/04
CPC分类号： C07D249/18 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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