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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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公开(公告)号：US20120149677A1
公开(公告)日：2012-06-14
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： A61K31/4439 , C07D403/12 , C07D495/04 , C07D403/14 , C07D401/14 , C07D417/14 , A61K31/497 , A61K31/4709 , A61K31/506 , A61K31/519 , A61K31/444 , A61K31/541 , A61K31/438 , A61P25/00 , A61P25/18 , C07D401/12
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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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：US20090233896A1
公开(公告)日：2009-09-17
申请号：US11921598
申请日：2006-06-05
申请人： Kenneth L. Arrington , Vadim Y. Dudkin , Mark E. Fraley , Jacob M. Hoffman , Constantine Kreatsoulas , Cheng Wang
发明人： Kenneth L. Arrington , Vadim Y. Dudkin , Mark E. Fraley , Jacob M. Hoffman , Constantine Kreatsoulas , Cheng Wang
IPC分类号： A61K31/397 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/506 , C07D403/00 , A61K31/496 , A61P35/00
CPC分类号： C07D417/14 , C07D417/04 , C07D417/12
摘要： The instant invention provides for compounds which comprise substituted pyridyl aminothiazoles 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活性的取代的吡啶基氨基噻唑的化合物。 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：US20070254879A1
公开(公告)日：2007-11-01
申请号：US11789288
申请日：2007-04-24
申请人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
发明人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/4745 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The instant invention provides for compounds which comprise substituted triazoloquinazolinones 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活性的取代的三唑并喹唑啉酮的化合物。 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：US07501435B2
公开(公告)日：2009-03-10
申请号：US11789288
申请日：2007-04-24
申请人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
发明人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
IPC分类号： A61K31/4738 , C07D471/06
CPC分类号： C07D471/04 , C07D487/04
摘要： The instant invention provides for compounds which comprise substituted triazoloquinazolinones 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活性的取代的三唑并喹唑啉酮的化合物。 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：US08993779B2
公开(公告)日：2015-03-31
申请号：US13814870
申请日：2011-08-05
申请人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
发明人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
IPC分类号： C07D235/26 , C07D417/14 , C07D403/04 , C07D403/14 , C07D401/04 , C07D401/14 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/06 , C07D453/02 , C07D513/14 , C07D405/10 , C07D409/10 , C07D413/10 , C07D471/04
CPC分类号： C07D235/26 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D513/14
摘要： The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的苯并咪唑酮衍生物，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2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如精神分裂症中的用途。
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公开(公告)号：US20130143880A1
公开(公告)日：2013-06-06
申请号：US13814870
申请日：2011-08-05
申请人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
发明人： Vadim Y. Dudkin , Mark E. Fraley , Kenneth L. Arrington , Mark E. Layton , Alexander J. Reif , Kevin J. Rodzinak , Joseph E. Pero
IPC分类号： A61K31/4745 , C07D235/26 , A61K31/4439 , C07D417/14 , C07D405/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D413/10 , C07D409/10 , C07D405/10 , A61K31/4184 , C07D413/02 , C07D401/02 , C07D403/02 , A61K31/4709 , C07D471/04
CPC分类号： C07D235/26 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/14 , C07D453/02 , C07D471/04 , C07D513/14
摘要： The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.
摘要翻译： 本发明涉及作为mGluR2受体的正变构调节剂的苯并咪唑酮衍生物，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神障碍以及涉及mGluR2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如精神分裂症中的用途。
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公开(公告)号：US09062059B2
公开(公告)日：2015-06-23
申请号：US14239603
申请日：2012-08-20
IPC分类号： C07D487/04 , C07D239/47 , C07D401/14 , C07D417/14 , A61K31/506
CPC分类号： C07D487/04 , A61K31/506 , C07D239/47 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的嘧啶化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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公开(公告)号：US20140228368A1
公开(公告)日：2014-08-14
申请号：US14239603
申请日：2012-08-20
IPC分类号： C07D487/04 , C07D417/14 , C07D401/14
CPC分类号： C07D487/04 , A61K31/506 , C07D239/47 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的嘧啶化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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