公开(公告)号：US20210395224A1

公开(公告)日：2021-12-23

申请号：US17286591

申请日：2019-10-24

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co. LTD.

Inventor： John J. Acton, III ,  Melissa Egbertson ,  Xiaolei Gao ,  Scott T. Harrison ,  Timothy J. Henderson ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  James Mulhearn ,  Vanessa L. Rada ,  Jeffrey W. Schubert ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang ,  Jianming Bao ,  Chunsing Li

IPC: C07D401/14 ,  C07D405/14

Abstract: The present invention is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US20200069671A1

公开(公告)日：2020-03-05

申请号：US16674546

申请日：2019-11-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： John J. Acton, III ,  Jianming Bao ,  Melissa Egbertson ,  Xiaolei Gao ,  Scott T. Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, JR. ,  Zhaoyang Meng ,  Michael T. Rudd ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Jenny Miu-Chun Wai

IPC: A61K31/4439 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61K31/437 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US20170015633A1

公开(公告)日：2017-01-19

申请号：US15107233

申请日：2014-12-17

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co. Ltd.

Inventor： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhi Qiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC: C07D239/36 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D487/04 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D401/06 ,  C07D403/12

CPC classification number: C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

Abstract: Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.

Abstract translation: 公开了式（I）的嘧啶羧酰胺化合物，其可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病，药物组合物及其用途的治疗剂。

公开(公告)号：US20170002008A1

公开(公告)日：2017-01-05

申请号：US15038805

申请日：2014-11-24

Applicant: Dansu LI ,  Mark E. LAYTON ,  Anthony J. ROECKER ,  Melissa EGBERTSON ,  Kristen L. G. JONES ,  Xiu WANG ,  Xuanjia PENG ,  MERCK SHARP & DOHME CORP.

Inventor： Mark E. Layton ,  Anthony J. Roecker ,  Melissa Egbertson ,  Kristen L. G. Jones ,  Dansu Li ,  Xiu Wang ,  Xuanjia Peng

IPC: C07D487/04 ,  C07D487/10 ,  C07D471/04 ,  C07D285/135 ,  C07D213/76 ,  C07D239/42 ,  C07D237/20 ,  C07D491/20 ,  C07D277/52

CPC classification number: C07D487/04 ,  C07D213/76 ,  C07D237/20 ,  C07D239/42 ,  C07D277/52 ,  C07D285/135 ,  C07D471/04 ,  C07D487/10 ,  C07D491/20

Abstract: 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.

Abstract translation: 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：US11339156B2

公开(公告)日：2022-05-24

申请号：US16621953

申请日：2018-06-22

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co., Ltd.

Inventor： John J. Acton, III ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Timothy J. Henderson ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Meng Na ,  Michael T. Rudd ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang ,  Takao Suzuki

IPC: C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D417/14

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US11149036B2

公开(公告)日：2021-10-19

申请号：US16621959

申请日：2018-06-22

Applicant: John J. Acton, III ,  Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co., Ltd. ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

Inventor： John J. Acton, III ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

IPC: C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D498/04

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US10933056B2

公开(公告)日：2021-03-02

申请号：US16674546

申请日：2019-11-05

Applicant: Merck Sharp & Dohme Corp. ,  MSD R&D (CHINA) CO., LTD.

Inventor： John J. Acton, III ,  Jianming Bao ,  Melissa Egbertson ,  Xiaolei Gao ,  Scott T. Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Michael T. Rudd ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Jenny Miu-Chun Wai

IPC: C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  A61K31/4439 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61K31/437

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US20150141428A1

公开(公告)日：2015-05-21

申请号：US14401941

申请日：2013-05-17

Applicant: Merck Sharp & Dohme Corp.

Inventor： Shawn J. Stachel ,  Melissa Egbertson ,  Edward Brnardic ,  Kristen G. Jones ,  John M. Sanders ,  Darrell Henze

IPC: C07D487/04 ,  C07D277/30 ,  C07D403/04 ,  C07D239/34 ,  C07D239/42 ,  C07D471/04 ,  C07D417/12

CPC classification number: C07D487/04 ,  C07D239/34 ,  C07D239/42 ,  C07D277/28 ,  C07D277/30 ,  C07D277/32 ,  C07D277/66 ,  C07D403/04 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.

Abstract translation: 本发明涉及苄基脲化合物，其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病， 与神经生长因子（NGF）受体Trk-A，Trk-B和/或Trk-C的异常活动相关的疾病或障碍或与脱髓鞘或脱髓鞘相关的疾病，损伤或功能障碍。

公开(公告)号：US20190000824A1

公开(公告)日：2019-01-03

申请号：US16062500

申请日：2016-12-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： John J. Acton, III ,  Jianming Bao ,  Melissa Egbertson ,  Xiaolei Gao ,  Scott T. Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Michael T. Rudd ,  Oleg B. Selyutin ,  David M. Tellers ,  Ling Tong ,  Jenny Miu-Chun Wai

IPC: A61K31/4439 ,  A61K31/437 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC classification number: A61K31/4439 ,  A61K31/437 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US09815796B2

公开(公告)日：2017-11-14

申请号：US15107233

申请日：2014-12-17

Applicant: Merck Sharp & Dohme Corp. ,  MSD R & D (China) Co. Ltd.

Inventor： Dong Ming Shen ,  Melissa Egbertson ,  Richard Berger ,  XiaoXia Qian ,  Yimin Qian ,  Bart Harper ,  Meng Yang ,  Zack Zhiqiang Guo ,  Vanessa L. Rada ,  Deping Wang ,  Timothy A. Cernak ,  Christopher Sinz ,  Ming Wang ,  Jonathan E. Wilson ,  Shimin Xu

IPC: C07D239/36 ,  C07D401/12 ,  C07D401/06 ,  C07D403/04 ,  C07D403/14 ,  C07D487/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D403/12 ,  C07D403/06

CPC classification number: C07D239/36 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D487/04

Abstract: Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.