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：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：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：US20180362518A1

公开(公告)日：2018-12-20

申请号：US16061815

申请日：2016-12-15

申请人： 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.

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 ,  C07D285/135 ,  C07D277/52 ,  A61P11/14 ,  A61P17/04 ,  A61P25/04 ,  A61P25/02

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

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 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.

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：US20190233406A1

公开(公告)日：2019-08-01

申请号：US16246068

申请日：2019-01-11

申请人： Merck Sharp & Dohme Corp.

发明人： 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分类号： C07D417/12 ,  A61K31/426 ,  A61K31/433 ,  A61K31/427 ,  A61K31/551 ,  C07D277/52 ,  C07D285/08 ,  A61K45/06

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

摘要： 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：US20230391758A1

公开(公告)日：2023-12-07

申请号：US18043413

申请日：2021-09-15

申请人： MERCK SHARP & DOHME CORP.

发明人： Michael J. Breslin ,  Mark E. Fraley ,  Melissa C. Ford ,  Kristen L.G. Jones, SR. ,  Anthony J. Roecker ,  Kathy M. Schirripa ,  Ling Tong

IPC分类号： C07D405/12 ,  C07D471/04 ,  C07D307/85 ,  C07D405/06 ,  C07D453/02 ,  C07D405/14 ,  C07D413/12

CPC分类号： C07D405/12 ,  C07D471/04 ,  C07D307/85 ,  C07D405/06 ,  C07D453/02 ,  C07D405/14 ,  C07D413/12

摘要： The present invention relates to Compounds of Formula I: and pharmaccutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).