公开(公告)号：US09586968B2

公开(公告)日：2017-03-07

申请号：US15038805

申请日：2014-11-24

申请人： Merck Sharp & Dohme Corp. ,  Dansu Li ,  Mark E. Layton ,  Anthony J. Roecker ,  Melissa Egbertson ,  Kristen L. G. Jones ,  Xiu Wang ,  Xuanjia Peng

发明人： Mark E. Layton ,  Anthony J. Roecker ,  Melissa Egbertson ,  Kristen L. G. Jones ,  Dansu Li ,  Xiu Wang ,  Xuanjia Peng

IPC分类号： C07D487/04 ,  A61K31/407 ,  C07D471/04 ,  A61K31/4353 ,  C07D491/20 ,  C07D487/10 ,  C07D277/52 ,  C07D213/76 ,  C07D239/42 ,  C07D237/20 ,  C07D285/135

CPC分类号： C07D487/04 ,  C07D213/76 ,  C07D237/20 ,  C07D239/42 ,  C07D277/52 ,  C07D285/135 ,  C07D471/04 ,  C07D487/10 ,  C07D491/20

摘要： Disclosed are compounds of Formula A-a, or a salt thereof: Where “B1” and “R1” through “R5” are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.

摘要翻译： 公开了式A-a或其盐的化合物：其中“B1”和“R1”至“R5”如本文所定义，这些化合物具有阻断外周和交感神经元中的Nav 1.7离子通道的性质。 还描述了包含式A-a化合物或其盐的药物制剂，以及使用其制备神经性疼痛病症的方法。

公开(公告)号：US20170002008A1

公开(公告)日：2017-01-05

申请号：US15038805

申请日：2014-11-24

申请人： Dansu LI ,  Mark E. LAYTON ,  Anthony J. ROECKER ,  Melissa EGBERTSON ,  Kristen L. G. JONES ,  Xiu WANG ,  Xuanjia PENG ,  MERCK SHARP & DOHME CORP.

发明人： Mark E. Layton ,  Anthony J. Roecker ,  Melissa Egbertson ,  Kristen L. G. Jones ,  Dansu Li ,  Xiu Wang ,  Xuanjia Peng

IPC分类号： C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D285/135 ,  C07D213/76 ,  C07D239/42 ,  C07D237/20 ,  C07D491/20 ,  C07D277/52

CPC分类号： C07D487/04 ,  C07D213/76 ,  C07D237/20 ,  C07D239/42 ,  C07D277/52 ,  C07D285/135 ,  C07D471/04 ,  C07D487/10 ,  C07D491/20

摘要： Disclosed are compounds of Formula A-a, or a salt thereof: Where “B1” and “R1” through “R5” are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.

摘要翻译： 公开了式A-a或其盐的化合物：其中“B1”和“R1”至“R5”如本文所定义，这些化合物具有阻断外周和交感神经元中的Nav 1.7离子通道的性质。 还描述了包含式A-a化合物或其盐的药物制剂，以及使用其制备神经性疼痛病症的方法。

公开(公告)号：US09273040B2

公开(公告)日：2016-03-01

申请号：US14353488

申请日：2012-10-26

申请人： Mark E. Layton ,  Joseph E. Pero ,  Hannah Fiji ,  Michael J. Kelly, III ,  Pablo de Leon ,  Michael A. Rossi ,  Kevin F. Gilbert ,  Anthony J. Roecker ,  Zhijian Zhao ,  Swati I P. Mercer ,  Scott Wolkenberg ,  James Mulhearn ,  Lianyun Zhao ,  Dansu Li

发明人： Mark E. Layton ,  Joseph E. Pero ,  Hannah Fiji ,  Michael J. Kelly, III ,  Pablo de Leon ,  Michael A. Rossi ,  Kevin F. Gilbert ,  Anthony J. Roecker ,  Zhijian Zhao ,  Swati I P. Mercer ,  Scott Wolkenberg ,  James Mulhearn ,  Lianyun Zhao ,  Dansu Li

IPC分类号： A61K31/00 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D491/107 ,  C07D493/10

CPC分类号： C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D491/107 ,  C07D493/10

摘要： Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.

摘要翻译： 公开了式（A）的化合物或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。 还描述了包含式（A）化合物或其盐的药物制剂，以及使用其制备神经性疼痛障碍的方法。

公开(公告)号：US09242995B2

公开(公告)日：2016-01-26

申请号：US14354392

申请日：2012-10-19

申请人： Dansu Li ,  Anthony J. Roecker

发明人： Dansu Li ,  Anthony J. Roecker

IPC分类号： C07D498/04

CPC分类号： C07D498/04

摘要： The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical 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肽受体拮抗剂的异恶唑嘌呤类化合物。 本发明还涉及本文所述的异恶唑嘌呤类化合物在治疗或预防涉及食欲素受体的神经和精神疾病和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US09732077B2

公开(公告)日：2017-08-15

申请号：US15105825

申请日：2014-12-16

申请人： Scott D. Kuduk ,  Thomas S. Reger ,  Anthony J. Roecker

发明人： Scott D. Kuduk ,  Thomas S. Reger ,  Anthony J. Roecker

IPC分类号： C07D413/04 ,  C07D403/04 ,  A61K31/55 ,  C07D417/14 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14 ,  C07D417/04

CPC分类号： C07D417/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： The present invention is directed to diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the diazepane compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：US08710076B2

公开(公告)日：2014-04-29

申请号：US13124901

申请日：2009-10-15

申请人： Michael J. Breslin ,  Paul J. Coleman ,  Christopher D. Cox ,  Izzat T. Raheem ,  Anthony J. Roecker ,  John D. Schreier

发明人： Michael J. Breslin ,  Paul J. Coleman ,  Christopher D. Cox ,  Izzat T. Raheem ,  Anthony J. Roecker ,  John D. Schreier

IPC分类号： A61K31/47 ,  C07D401/14

CPC分类号： A61K31/445 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

摘要： The present invention is directed to 2,5-disubstituted piperidine 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2,5-二取代的哌啶酰胺化合物，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：US20110201591A1

公开(公告)日：2011-08-18

申请号：US13124568

申请日：2009-10-26

申请人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mamio Christa Mattern ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker

发明人： Jeffrey M. Bergman ,  Paul J. Coleman ,  Mamio Christa Mattern ,  Swati P. Mercer ,  Thomas S. Reger ,  Anthony J. Roecker

IPC分类号： A61K31/497 ,  C07D401/14 ,  C07D213/81 ,  C07D401/04 ,  C07D401/12 ,  C07D417/14 ,  A61K31/444 ,  A61K31/4418 ,  A61K31/4439 ,  A61P3/04 ,  A61P25/00

CPC分类号： C07D401/04 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D417/14

摘要： The present invention is directed to isonicotinamide 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异烟酰胺化合物，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：US20100063056A1

公开(公告)日：2010-03-11

申请号：US12528142

申请日：2008-02-29

申请人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

发明人： Paul J. Coleman ,  Swati P. Mercer ,  Anthony J. Roecker

IPC分类号： A61K31/444 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/498 ,  A61P43/00

CPC分类号： C07D213/82 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

摘要： The present invention is directed to bipyridyl 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联吡啶羧酰胺化合物，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：US20090239843A1

公开(公告)日：2009-09-24

申请号：US12309243

申请日：2007-07-13

申请人： Paul J. Coleman ,  Christopher D. Cox ,  Georgia B. McGaughey ,  Anthony J. Roecker ,  John D. Schreir

发明人： Paul J. Coleman ,  Christopher D. Cox ,  Georgia B. McGaughey ,  Anthony J. Roecker ,  John D. Schreir

IPC分类号： A61K31/517 ,  C07D413/14 ,  C07D487/18 ,  A61K31/55 ,  A61P25/00

CPC分类号： C07D471/08 ,  C07D487/08

摘要： The present invention is directed to bridged diazepan 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桥连二氮杂环庚烷化合物，其可用于治疗或预防涉及食欲肽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：US10968210B2

公开(公告)日：2021-04-06

申请号：US16345913

申请日：2017-11-13

申请人： Merck Sharp & Dohme Corp. ,  Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

发明人： Thomas J. Greshock ,  James Mulhearn ,  Anthony J. Roecker ,  Tianying Jian ,  Gang Zhou ,  Liangqin Guo ,  Walter Won ,  Ting Zhang ,  Rajan Anand ,  John E. Stelmach ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Christopher S. Burgey ,  Philippe G. Nantermet

IPC分类号： C07D417/12 ,  C07D417/14 ,  C07D277/52 ,  C07D471/04 ,  C07D487/10 ,  C07D401/12 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.