公开(公告)号：US11377438B2

公开(公告)日：2022-07-05

申请号：US16669598

申请日：2019-10-31

申请人： Merck Sharp & Dohme Corp.

发明人： Ashok Arasappan ,  Ian M. Bell ,  Michael J. Breslin ,  Christopher James Bungard ,  Christopher S. Burgey ,  Harry R. Chobanian ,  Jason M. Cox ,  Anthony T. Ginnetti ,  Deodial Guy Guiadeen ,  Kristen L. G. Jones ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  James J. Perkins ,  Shawn J. Stachel ,  Linda M. Suen-Lai ,  Zhe Wu

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

公开(公告)号：US20220119363A1

公开(公告)日：2022-04-21

申请号：US17289152

申请日：2019-10-28

申请人： Merck Sharp & Dohme Corp.

发明人： Michael J. Breslin ,  Christopher James Bungard ,  Harry R. Chobanian ,  Kristen L. G. Jones ,  Mark E. Layton ,  Jian Liu ,  James J. Perkins ,  Jeffrey William Schubert ,  Shawn J. Stachel ,  Linda M. Suen-Lai ,  Zhe Wu

IPC分类号： C07D401/04 ,  C07D213/82 ,  C07D401/14 ,  C07D487/18 ,  C07D498/08 ,  C07D513/04 ,  C07D413/04 ,  C07D417/04 ,  C07D487/08 ,  C07D491/107 ,  C07D498/04 ,  C07D491/048 ,  C07D417/14 ,  C07D409/14 ,  C07D405/14 ,  C07D403/04 ,  C07D451/02

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

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：US20210387966A1

公开(公告)日：2021-12-16

申请号：US17289123

申请日：2019-10-31

申请人： Merck Sharp & Dohme Corp.

发明人： Ashok Arasappan ,  Ian M. Bell ,  Michael J. Breslin ,  Christopher James Bungard ,  Christopher S. Burgey ,  Harry R. Chobanian ,  Jason M. Cox ,  Anthony T. Ginnetti ,  Deodial Guy Guiadeen ,  Kristen L. G. Jones ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  James J. Perkins ,  Shawn J. Stachel ,  Linda M. Suen-Lai ,  Zhe Wu

IPC分类号： C07D401/14 ,  C07D471/04 ,  C07D413/14 ,  C07D471/08 ,  C07D495/04 ,  C07D401/12 ,  C07D487/04 ,  C07D491/048

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.

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。