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.

公开(公告)号：US10519147B2

公开(公告)日：2019-12-31

申请号：US16061815

申请日：2016-12-15

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

发明人： Thomas J. Greshock ,  James Mulhearn ,  Liangqin Guo ,  Ting Zhang ,  Deping Wang ,  Ronald M. Kim ,  Mark E. Layton ,  Michael J. Kelly, III ,  Rajan Anand ,  Philippe Nantermet ,  Tianying Jian ,  Anthony J. Roecker ,  Walter Won ,  Gang Zhou

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07D277/52 ,  C07D285/135 ,  A61P25/02 ,  A61P25/04 ,  A61P11/14 ,  A61P17/04

摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting 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 pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

公开(公告)号：US20230227441A1

公开(公告)日：2023-07-20

申请号：US18009306

申请日：2021-06-14

申请人： Ashok ARASAPPAN ,  Ian M. BELL ,  Christopher James BUNGARD ,  Christopher S. BURGEY ,  Jason M. COX ,  Deodial Guy GUIADEEN ,  Michael J. KELLY ,  Mark E. LAYTON ,  Hong LIU ,  Jian LIU ,  James T. OLSEN ,  James J. PERKINS ,  Jeffrey W. SCHUBERT ,  Akshay A. SHAH ,  Michael D. VANHEYST ,  Zhe WU ,  Shawn J. STACHEL ,  MERCK SHARP & DOHME CORP.

发明人： Ashok Arasappan ,  Ian M. Bell ,  Christopher James Bungard ,  Christopher S. Burgey ,  Jason Michael Cox ,  Deodial Guy Guiadeen, III ,  Michael J. Kelly, III ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  James T. Olsen ,  James J. Perkins ,  Jeffrey W. Schubert ,  Akshay A. Shah ,  Shawn J. Stachel ,  Michael David VanHeyst ,  Zhe Wu

IPC分类号： C07D413/12 ,  C07D263/24 ,  C07D417/12

CPC分类号： C07D413/12 ,  C07D263/24 ,  C07D417/12

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：US20220305035A1

公开(公告)日：2022-09-29

申请号：US17615769

申请日：2020-06-08

申请人： Anthony J. ROECKER ,  Mark E. LAYTON ,  Deping WANG ,  Xiu WANG ,  Xuanjia PENG ,  Merck Sharp & Dohme Corp.

发明人： Anthony J. Roecker ,  Mark E. Layton ,  Deping Wang ,  Xiu Wang ,  Xuanjia Peng

IPC分类号： A61K31/635 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are compounds of Formula A, or a salt thereof: Wherein “A1”, R1, R2, R3, R6, and R7 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 or their salts, and methods of treating cough, itch and neuropathic pain disorders using the same.

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：US20220000844A1

公开(公告)日：2022-01-06

申请号：US17296601

申请日：2019-12-02

申请人： Merck Sharp & Dohme Corp.

发明人： Christopher J. Bungard ,  Helen Y. Chen ,  Jason M. Cox ,  Liangqin Guo ,  Michael J. Kelly, III ,  Ronald M. Kim ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  Mehul F. Patel ,  James J. Perkins ,  Deping Wang ,  Walter Won ,  Younong Yu ,  Ting Zhang

IPC分类号： A61K31/433 ,  C07D285/08 ,  C07D417/12 ,  C07D239/42 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/167

摘要： Disclosed are compounds of Formula (I), Formula (II), or a salt thereof: Formula (I) Formula (II) which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (I), Formula (II) or their salts, and methods of treating pain disorders, cough, and itch using the same.

公开(公告)号：US20190092738A1

公开(公告)日：2019-03-28

申请号：US16086654

申请日：2017-03-17

申请人： Merck Sharp & Dohme Corp.

发明人： Anthony J. Roecker ,  Mark E. Layton ,  Thomas J. Greshock ,  Joseph E. Pero ,  Michael J. Kelly, III ,  Ting Zhang

IPC分类号： C07D277/52 ,  C07D285/08 ,  A61K31/635 ,  A61K45/06

CPC分类号： C07D277/52 ,  A61K31/18 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/635 ,  A61K45/06 ,  C07D285/08 ,  C07F7/0812 ,  A61K2300/00

摘要： Disclosed are compounds of Formula A-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-1 or their salts, and methods of treating pain (e.g. chronic pain), or cough or itch disorders using the same.

公开(公告)号：US08952005B2

公开(公告)日：2015-02-10

申请号：US14048608

申请日：2013-10-08

申请人： Merck Sharp & Dohme Corp.

发明人： Mark E. Layton ,  Michael J. Kelly, III

IPC分类号： A61K31/54 ,  C07D261/20

CPC分类号： C07D417/10 ,  A61K31/425 ,  C07D277/68 ,  C07D411/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

摘要： The present invention is directed to benzothiazol-one and thiazolo pyridine-one 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受体的增强剂的苯并噻唑-1-酮和噻唑并吡啶一种衍生物，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及其中 涉及代谢型谷氨酸受体。 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：US11802122B2

公开(公告)日：2023-10-31

申请号：US17347639

申请日：2021-06-15

申请人： Merck Sharp & Dohme Corp.

发明人： Ashok Arasappan ,  Ian M. Bell ,  Christopher James Bungard ,  Christopher S. Burgey ,  Jason M. Cox ,  Michael J. Kelly, III ,  Mark E. Layton ,  Hong Liu ,  Jian Liu ,  James J. Perkins ,  Akshay A. Shah ,  Michael David VanHeyst ,  Zhe Wu

IPC分类号： C07D403/12 ,  C07D233/32 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D513/04 ,  A61K31/4166 ,  A61P25/00 ,  A61P25/04 ,  A61P29/00

CPC分类号： C07D403/12 ,  C07D233/32 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D513/04

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：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.