公开(公告)号：US10221167B2

公开(公告)日：2019-03-05

申请号：US15378465

申请日：2016-12-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC: C07D417/12 ,  C07D285/08 ,  C07D277/52 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4168 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06

Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are 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 disorders, cough, and itch using the same.

公开(公告)号：US20220000844A1

公开(公告)日：2022-01-06

申请号：US17296601

申请日：2019-12-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： 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: A61K31/433 ,  C07D285/08 ,  C07D417/12 ,  C07D239/42 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/167

Abstract: 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：US20160194330A1

公开(公告)日：2016-07-07

申请号：US14655572

申请日：2013-12-20

Applicant: Amjad ALI ,  Michael Man-Chu LO ,  Yeon-Hee LIM ,  Andrew STAMFORD ,  Rongze KUANG ,  Paul TEMPEST ,  Younong YU ,  Michael BERLIN ,  Pauline TING ,  Gang ZHOU ,  Tao YU ,  Christopher BOYCE ,  Joseph Michael KELLY ,  Jayaram TAGAT ,  Junying ZHENG ,  Xianhai HUANG ,  Wei ZHOU ,  Jae-Hun KIM ,  Nicolas ZORN ,  Dong XIAO ,  Gioconda V. GALLO ,  Walter WON ,  Heping WU ,  Rajan ANAND ,  MERCK SHARP & DOHME CORP.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Michael Berlin ,  Pauline Ting ,  Gang Zhou ,  Tao Yu ,  Christopher Boyce ,  Joseph Michael Kelly ,  Jayaram R. Tagat ,  Junying Zheng ,  Xianhai Huang ,  Wei Zhou ,  Jae-Hun Kim ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Rajan Anand ,  Qiaolin Deng

IPC: C07D487/04 ,  C07D487/18 ,  C07D487/08 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04

Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Abstract translation: 公开了式A化合物（结构表示），其中“RG1”，“RG2a”，“RG4”，“RG5”，“MG1”，“n”和“m”在本文中定义为哪些化合物是A2A受体的拮抗剂。 本文还公开了本文所述的化合物作为A2a受体的拮抗剂的潜在治疗或预防涉及A2A受体的神经障碍和疾病的用途。 本文还公开了包含这些化合物的药物组合物和这些药物组合物的用途。

公开(公告)号：US20190233406A1

公开(公告)日：2019-08-01

申请号：US16246068

申请日：2019-01-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： Thomas J. Greshock ,  James Mulhearn ,  Junying Zheng ,  Ronald M. Kim ,  Ting Zhang ,  Anthony J. Roecker ,  Walter Won ,  Philippe Nantermet ,  Rajan Anand ,  Gang Zhou ,  Deping Wang ,  Liangqin Guo

IPC: C07D417/12 ,  A61K31/426 ,  A61K31/433 ,  A61K31/427 ,  A61K31/551 ,  C07D277/52 ,  C07D285/08 ,  A61K45/06

CPC classification number: C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/551 ,  A61K45/06 ,  C07D277/52 ,  C07D285/08 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are 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 disorders, cough, and itch using the same.

公开(公告)号：US20180193314A1

公开(公告)日：2018-07-12

申请号：US15815212

申请日：2016-06-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Junying Zheng ,  Walter Won ,  Michael Berlin ,  Pauline Ting ,  Guoqing Li ,  Dong Xiao ,  Hongwu Wang ,  Robert Aslanian

IPC: A61K31/4162 ,  A61K31/519 ,  A61K31/497 ,  A61P25/00

CPC classification number: A61K31/4162 ,  A01N43/80 ,  A61K31/497 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04 ,  C07D487/10 ,  A01N25/04

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US10968210B2

公开(公告)日：2021-04-06

申请号：US16345913

申请日：2017-11-13

Applicant: 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

Inventor： 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: C07D417/12 ,  C07D417/14 ,  C07D277/52 ,  C07D471/04 ,  C07D487/10 ,  C07D401/12 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08

Abstract: 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：US10688082B2

公开(公告)日：2020-06-23

申请号：US15815212

申请日：2016-06-06

Applicant: Merck Sharp & Dohme Corp.

Inventor： Junying Zheng ,  Walter Won ,  Michael Berlin ,  Pauline Ting ,  Guoqing Li ,  Dong Xiao ,  Hongwu Wang ,  Robert Aslanian

IPC: A61K31/4162 ,  A61K31/519 ,  A61K31/497 ,  A61P25/00 ,  A01N43/80 ,  C07D487/04 ,  C07D487/10

Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: “Z”, R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

公开(公告)号：US10519147B2

公开(公告)日：2019-12-31

申请号：US16061815

申请日：2016-12-15

Applicant: 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

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

Abstract: 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：US20170197991A1

公开(公告)日：2017-07-13

申请号：US15423238

申请日：2017-02-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： Amjad Ali ,  Michael Man-Chu Lo ,  Yeon-Hee Lim ,  Andrew Stamford ,  Rongze Kuang ,  Paul Tempest ,  Younong Yu ,  Xianhai Huang ,  Timothy J. Henderson ,  Jae-Hun Kim ,  Christopher Boyce ,  Pauline Ting ,  Junying Zheng ,  Edward Metzger ,  Nicolas Zorn ,  Dong Xiao ,  Gioconda V. Gallo ,  Walter Won ,  Heping Wu ,  Qiaolin Deng

IPC: C07D519/00 ,  C07D487/04

CPC classification number: C07D519/00 ,  C07D487/04

Abstract: Disclosed are compounds of Formula G1: where “RG3”. “Rd1” to “Rd4”, “n”, “m”, “p”, “W”, “X”, “Y”, and “Z” are defined herein, which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

公开(公告)号：US20180362518A1

公开(公告)日：2018-12-20

申请号：US16061815

申请日：2016-12-15

Applicant: Thomas J. GRESHOCK ,  James MULHEARN ,  Liangqin GUO ,  Ting ZHANG ,  Deping WANG ,  Ronald M. KIM ,  Mark E. LAYTON ,  Michael J. KELLY, III ,  Rajan ANAND ,  Tianying JIAN ,  Philippe NANTERMET ,  Anthony J. ROECKER ,  Walter WON ,  Gang ZHOU ,  Merck Sharp & Dohme Corp.

Inventor： 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: C07D417/12 ,  C07D285/135 ,  C07D277/52 ,  A61P11/14 ,  A61P17/04 ,  A61P25/04 ,  A61P25/02

CPC classification number: C07D417/12 ,  A61K45/06 ,  A61P11/14 ,  A61P17/04 ,  A61P25/02 ,  A61P25/04 ,  C07D277/52 ,  C07D285/135

Abstract: 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 Na 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.