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。

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。

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。

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。

公开(公告)号：US20120135977A1

公开(公告)日：2012-05-31

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： A61K31/4192 ,  C07D401/12 ,  A61K31/4439 ,  C07D403/12 ,  A61K31/506 ,  A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/551 ,  A61K31/55 ,  C07D417/12 ,  A61K31/541 ,  A61P25/00 ,  A61P25/18 ,  C07D249/18

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.

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。

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。

公开(公告)号：US08623863B2

公开(公告)日：2014-01-07

申请号：US13125174

申请日：2009-10-15

申请人： Paul J. Coleman ,  Mark E. Fraley ,  John D. Schreier

发明人： Paul J. Coleman ,  Mark E. Fraley ,  John D. Schreier

IPC分类号： A61K31/55 ,  A61P43/00 ,  C07D223/12

CPC分类号： C07D223/12 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14

摘要： The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的二取代氮杂环庚烷和氧氮杂环酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 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食欲肽受体的疾病中的用途。

公开(公告)号：US08003797B2

公开(公告)日：2011-08-23

申请号：US12669909

申请日：2008-08-07

申请人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mark E. Fraley ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker ,  Justin T. Steen

发明人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mark E. Fraley ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker ,  Justin T. Steen

IPC分类号： C07D213/22 ,  C07D213/44

CPC分类号： C07D213/82 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  C07D401/04 ,  C07D401/14

摘要： The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.

摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的吡啶羧酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 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食欲肽受体的疾病中的用途。

公开(公告)号：US07550470B2

公开(公告)日：2009-06-23

申请号：US10540784

申请日：2003-12-05

申请人： Mark E. Fraley

发明人： Mark E. Fraley

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P19/08

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  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, macular edema, retinal ischemia, 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，黄斑水肿，视网膜缺血，炎症性疾病等。