公开(公告)号：US20150266897A1

公开(公告)日：2015-09-24

申请号：US14638733

申请日：2015-04-03

Applicant: Merck Sharp & Dohme Corp. ,  MSD Italia S.R.L.

Inventor： Nigel J. Liverton ,  Vincenzo Summa ,  Maria Emilia Di Francesco ,  Marco Ferrara ,  Kevin F. Gilbert ,  Steven Harper ,  John A. McCauley ,  Charles J. McIntyre ,  Alessia Petrocchi ,  Marco Pompei ,  Joseph J. Romano ,  Michael T. Rudd ,  John W. Butcher ,  M. Katharine Holloway

IPC: C07D498/22 ,  A61K31/437 ,  A61K31/439 ,  C07D498/08 ,  A61K31/407 ,  A61K31/4192 ,  C07D498/18 ,  A61K45/06

CPC classification number: C07D498/22 ,  A61K31/407 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/439 ,  A61K38/00 ,  A61K45/06 ,  C07D498/08 ,  C07D498/18 ,  C07K5/0804 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/0812

Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。

公开(公告)号：US09624208B2

公开(公告)日：2017-04-18

申请号：US14437315

申请日：2013-10-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Joseph E. Pero ,  Hannah D. G. F. Lehman ,  Michael J. Kelly, III ,  Lianyun Zhao ,  Michael A. Rossi ,  Dansu Li ,  Kevin F. Gilbert ,  Scott Wolkenberg ,  James Mulhearn ,  Mark E. Layton ,  Pablo de Leon

IPC: C07D413/12 ,  C07D413/14 ,  C07D263/58 ,  A61K31/44

CPC classification number: C07D413/14 ,  A61K31/44 ,  C07D263/58 ,  C07D413/12

Abstract: Disclosed are compounds of Formula A: 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.

公开(公告)号：US20150252034A1

公开(公告)日：2015-09-10

申请号：US14437315

申请日：2013-10-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Joseph E. Pero ,  Hannah D.G.F. Lehman ,  Michael J. Kelly, III ,  Lianyun Zhao ,  Michael A. Rossi ,  Dansu Li ,  Kevin F. Gilbert ,  Scott Wolkenberg ,  James Mulhearn ,  Mark E. Layton ,  Pablo de Leon

IPC: C07D413/14 ,  C07D413/12

CPC classification number: C07D413/14 ,  A61K31/44 ,  C07D263/58 ,  C07D413/12

Abstract: Disclosed are compounds of Formula A: 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.

Abstract translation: 公开了式A的化合物：式A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或其盐的化合物的药物制剂，以及使用其制备治疗神经性疼痛障碍的方法。

公开(公告)号：US20140303143A1

公开(公告)日：2014-10-09

申请号：US14353488

申请日：2012-10-26

Applicant: MERCK SHARP & DOHME CORP.

Inventor： 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: C07D417/12 ,  C07D491/107 ,  C07D471/04 ,  C07D493/10 ,  C07D417/14 ,  C07D451/02

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D491/107 ,  C07D493/10

Abstract: 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.

Abstract translation: 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。