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公开(公告)号：US07294640B2
公开(公告)日：2007-11-13
申请号：US11040522
申请日：2005-01-21
IPC分类号： A61K31/426 , C07D277/22 , C07D277/28 , C07D277/26 , C07D277/24
CPC分类号： C07D277/22 , C07D277/24 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/56 , C07D417/04
摘要： The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. 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驱动蛋白和MCAK活性相关的疾病以及用于抑制KSP驱动蛋白和MCAK的取代的噻唑衍生物。 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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公开(公告)号：US20130253135A1
公开(公告)日：2013-09-26
申请号：US13885737
申请日：2011-11-16
申请人： Stephanie E. Barrett , Marina Busuek , Steven L. Colletti , Robert M. Garbaccio , Erin N. Guidry , Robert A. Kowtoniuk , Jing Liao , Craig A. Parish , Rubina G. Parmar , Tao Pei , Kevin M. Schlosser , David M. Tellers , Sandra C. Tobias , Quang T. Truong , Jacob H. Waldman , Weimin Wang , J. Michael Williams
发明人： Stephanie E. Barrett , Marina Busuek , Steven L. Colletti , Robert M. Garbaccio , Erin N. Guidry , Robert A. Kowtoniuk , Jing Liao , Craig A. Parish , Rubina G. Parmar , Tao Pei , Kevin M. Schlosser , David M. Tellers , Sandra C. Tobias , Quang T. Truong , Jacob H. Waldman , Weimin Wang , J. Michael Williams
IPC分类号： A61K47/48
CPC分类号： A61K47/48092 , A61K47/549 , C08G69/10 , C08G73/028 , C08L79/02
摘要： The present invention provides poly(amide) polymers, polyconjugates, compositions and methods for the delivery of oligonucleotides for therapeutic purposes.
摘要翻译： 本发明提供用于递送用于治疗目的的寡核苷酸的聚（酰胺）聚合物，多偶联物，组合物和方法。
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公开(公告)号：US20110124661A1
公开(公告)日：2011-05-26
申请号：US12992439
申请日：2009-05-08
申请人： Edward J. Brnardic , Antonella Converso , Mark E. Fraley , Robert M. Garbaccio , Shaei Y. Huang
发明人： Edward J. Brnardic , Antonella Converso , Mark E. Fraley , Robert M. Garbaccio , Shaei Y. Huang
IPC分类号： A61K31/497 , C07D413/14 , C07D491/147 , C07D401/14 , A61K31/4439 , A61K31/437 , A61P25/18
CPC分类号： C07D498/04
摘要： The present invention is directed to oxazolobenzimidazole 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.
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公开(公告)号：US07485649B2
公开(公告)日：2009-02-03
申请号：US11794861
申请日：2006-01-05
IPC分类号： A61K31/4745 , C07D471/06
CPC分类号： A61K31/00
摘要： The instant invention provides for compounds which comprise fused pyrazoles 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活性的稠合吡唑的化合物。 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：US20080280902A1
公开(公告)日：2008-11-13
申请号：US11795005
申请日：2006-01-24
IPC分类号： A61K31/5377 , C07D401/04 , A61K31/497 , C07D401/14 , A61P35/00 , C07D413/14 , A61K31/4709
CPC分类号： C07D401/14 , C07D401/04
摘要： The instant invention provides for compounds which comprise substituted quinolinones 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活性的取代的喹啉酮的化合物。 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：US20080214594A1
公开(公告)日：2008-09-04
申请号：US11794861
申请日：2006-01-05
IPC分类号： A61K31/437 , C07D471/04 , A61P35/04
CPC分类号： A61K31/00
摘要： The instant invention provides for compounds which comprise fused pyrazoles 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活性的稠合吡唑的化合物。 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：US09139576B2
公开(公告)日：2015-09-22
申请号：US14115123
申请日：2012-04-30
申请人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
发明人： Douglas C. Beshore , Robert M. Garbaccio , Scott D. Kuduk , Adam W. Johnson , Jason W. Skudlarek
IPC分类号： C07D413/12 , C07D401/14 , C07D403/10 , C07D249/18 , C07D401/10 , C07D401/12 , C07D413/10
CPC分类号： C07D413/12 , C07D249/18 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D413/10
摘要： The present invention is directed to aminomethyl biaryl 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受体的增效剂的氨基甲基联芳基苯并三唑衍生物，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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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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20.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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