公开(公告)号：EP3087060B1

公开(公告)日：2020-05-13

申请号：EP14873215.9

申请日：2014-12-17

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

Inventor： SHEN, Dong-Ming ,  EGBERTSON, Melissa ,  BERGER, Richard ,  QIAN, XiaoXia ,  QIAN, Yimin ,  HARPER, Bart ,  YANG, Meng ,  GUO, Zack Zhi Qiang ,  RADA, Vanessa L. ,  WANG, Deping ,  CERNAK, Timothy A. ,  SINZ, Christopher J. ,  WANG, Ming ,  WILSON, Jonathan E. ,  XU, Shimin

IPC: C07D239/36 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  A61K31/513 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28

公开(公告)号：EP3873467A2

公开(公告)日：2021-09-08

申请号：EP19879545.2

申请日：2019-10-24

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

Inventor： ACTON, John, J., III ,  EGBERTSON, Melissa ,  GAO, Xiaolei ,  HARRISON, Scott, T. ,  HENDERSON, Timothy, J. ,  LO, Michael Man-Chu ,  MAZZOLA, Robert, D., Jr. ,  MENG, Zhaoyang ,  MULHEARN, James ,  RADA, Vanessa, L. ,  SCHUBERT, Jeffrey, W. ,  SELYUTIN, Oleg, B. ,  TELLERS, David, M. ,  TONG, Ling ,  ZHANG, Fengqi ,  BAO, Jianming ,  LI, Chunsing

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

公开(公告)号：EP3644992A1

公开(公告)日：2020-05-06

申请号：EP18825469.2

申请日：2018-06-22

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

Inventor： ACTON, John, J., III ,  BAO, Jianming ,  DENG, Qiaolin ,  EGBERTSON, Melissa ,  FERGUSON, Ronald, III ,  GAO, Xiaolei ,  HARRISON, Scott Timothy ,  KNOWLES, Sandra L. ,  LI, Chunsing ,  LO, Michael Man-Chu ,  MAZZOLA, Robert D., Jr. ,  MENG, Zhaoyang ,  NA, Meng ,  RUDD, Michael T. ,  SELYUTIN, Oleg B. ,  TELLERS, David M. ,  TONG, Ling ,  ZHANG, Fengqi

IPC: A61K31/4155 ,  C07D231/10

公开(公告)号：EP3393472A1

公开(公告)日：2018-10-31

申请号：EP16879916.1

申请日：2016-12-19

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

Inventor： ACTON, John, J., III ,  BAO, Jianming ,  EGBERTSON, Melissa ,  GAO, Xiaolei ,  HARRISON, Scott T. ,  KNOWLES, Sandra L. ,  LI, Chunsing ,  LO, Michael Man-Chu ,  MAZZOLA, Robert D., Jr. ,  MENG, Zhaoyang ,  RUDD, Michael, T. ,  SELYUTIN, Oleg ,  TELLERS, David, M. ,  TONG, Ling ,  WAI, Jenny Miu-Chun

IPC: A61K31/4155 ,  C07D231/10

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：EP3393472B1

公开(公告)日：2020-08-12

申请号：EP16879916.1

申请日：2016-12-19

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

Inventor： ACTON, John, J., III ,  BAO, Jianming ,  EGBERTSON, Melissa ,  GAO, Xiaolei ,  HARRISON, Scott T. ,  KNOWLES, Sandra L. ,  LI, Chunsing ,  LO, Michael Man-Chu ,  MAZZOLA, Robert D., Jr. ,  MENG, Zhaoyang ,  RUDD, Michael, T. ,  SELYUTIN, Oleg ,  TELLERS, David, M. ,  TONG, Ling ,  WAI, Jenny Miu-Chun

IPC: A61K31/4155 ,  C07D231/10

公开(公告)号：EP3644991A1

公开(公告)日：2020-05-06

申请号：EP18824389.3

申请日：2018-06-22

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

Inventor： ACTON, John, J., III ,  BAO, Jianming ,  DENG, Qiaolin ,  EGBERTSON, Melissa ,  FERGUSON, Ronald, III ,  GAO, Xiaolei ,  HARRISON, Scott Timothy ,  HENDERSON, Timothy, J. ,  KNOWLES, Sandra, L. ,  LO, Michael Man-Chu ,  MAZZOLA, Robert, D., Jr. ,  NA, Meng ,  SELYUTIN, Oleg, B. ,  SUZUKI, Takao ,  ZHANG, Fengqi

IPC: A61K31/4155 ,  C07D231/10 ,  C07D471/04

公开(公告)号：EP3087060A1

公开(公告)日：2016-11-02

申请号：EP14873215.9

申请日：2014-12-17

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

Inventor： SHEN, Dong-Ming ,  EGBERTSON, Melissa ,  BERGER, Richard ,  QIAN, XiaoXia ,  QIAN, Yimin ,  HARPER, Bart ,  YANG, Meng ,  GUO, Zack Zhi Qiang ,  RADA, Vanessa L. ,  WANG, Deping ,  CERNAK, Timothy A. ,  SINZ, Christopher J. ,  WANG, Ming ,  WILSON, Jonathan E. ,  XU, Shimin

IPC: C07D239/36 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  A61K31/513 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28

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：EP1881825B1

公开(公告)日：2013-07-24

申请号：EP06759135.4

申请日：2006-05-05

Applicant: Merck Sharp & Dohme Corp.

Inventor： VACCA, Joseph, P. ,  WAI, John, S. ,  PAYNE, Linda, S. ,  ISAACS, Richard, C., A. ,  HAN, Wei ,  EGBERTSON, Melissa ,  PRACITTO, Richard

IPC: A61K31/40 ,  A61K31/445 ,  C07D498/14 ,  A61K31/4353 ,  A61K31/4375 ,  C07D471/14

CPC classification number: C07D471/14 ,  A61K31/4353 ,  A61K31/4375 ,  C07D498/14

公开(公告)号：EP3074402B1

公开(公告)日：2019-01-16

申请号：EP14866477.4

申请日：2014-11-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： LI, Dansu ,  LAYTON, Mark E. ,  ROECKER, Anthony J. ,  EGBERTSON, Melissa ,  JONES, Kristen L. G. ,  WANG, Xiu ,  PENG, Xuanjia

IPC: C07D487/04 ,  C07D491/20 ,  C07D471/04 ,  C07D455/02 ,  A61K31/433 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/501 ,  A61K31/437 ,  A61K31/4375 ,  A61P25/02

公开(公告)号：EP3074402A1

公开(公告)日：2016-10-05

申请号：EP14866477.4

申请日：2014-11-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： LI, Dansu ,  LAYTON, Mark E. ,  ROECKER, Anthony J. ,  EGBERTSON, Melissa ,  JONES, Kristen L. G. ,  WANG, Xiu ,  PENG, Xuanjia

IPC: C07D487/04

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 "B
1 " and "R
1 " through "R
5 " are as defined herein, which compounds have properties for blocking Na
v 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.