公开(公告)号：EP3185865B1

公开(公告)日：2020-07-15

申请号：EP15836358.0

申请日：2015-08-24

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： ARASAPPAN, Ashok ,  BUNGARD, Christopher James ,  FRIE, Jessica L. ,  HAN, Yongxin ,  HOYT, Scott B. ,  MANLEY, Peter J. ,  MEISSNER, Robert S. ,  PERKINS, James J. ,  SEBHAT, Iyassu K. ,  WILKENING, Robert R. ,  LEAVITT, Kenneth J.

IPC: A61K31/4375

公开(公告)号：EP2882754B1

公开(公告)日：2018-10-03

申请号：EP13748245.1

申请日：2013-08-06

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： BARA, Thomas ,  BHAT, Sathesh ,  BISWAS, Dipshika ,  BROCKUNIER, Linda ,  BURNETTE, Duane ,  CHACKALAMANNIL, Samuel ,  CHELIAH, Mariappan, V. ,  CHEN, Austin ,  CLASBY, Martin ,  COLANDREA, Vince, J. ,  GUO, Zhuyan ,  HAN, Yongxin ,  JAYNE, Charles ,  JOSIEN, Hubert ,  MARCANTONIO, Karen ,  MIAO, Shouwu ,  NEELAMKAVIL, Santhosh ,  PINTO, Patrick ,  RAJAGOPALAN, Murali ,  SHAH, Unmesh ,  VELAZQUEZ, Francisco ,  VENKATRAMAN, Srikanth ,  XIA, Yan

IPC: C07D491/22 ,  C07D419/00 ,  A61K45/06 ,  A61K31/343 ,  A61K31/407 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07K5/08 ,  A61K38/06 ,  A61K45/06 ,  C07D419/00 ,  C07D491/22

Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

公开(公告)号：EP2413941A1

公开(公告)日：2012-02-08

申请号：EP10759391.5

申请日：2010-04-01

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： MCKAY, Daniel, J. ,  ARBOUR, Melissa ,  ASPIOTIS, Renee ,  CHEN, Austin ,  DOLMAN, Sarah Jennifer ,  FOURNIER, Pierre-Andre ,  GALLANT, Michel ,  HAN, Yongxin ,  HUGHES, Greg ,  JANEY, Jacob ,  JUTEAU, Helene ,  LACOMBE, Patrick ,  LALIBERTE, Sebastien ,  LAUZON, Sophie ,  MACDONALD, Dwight ,  MACKAY, Bruce ,  MELLON, Christophe ,  MOLINARO, Carmela ,  MORLEY, Krista, L. ,  O'SHEA, Paul ,  RAMTOHUL, Yeeman, K. ,  SIMARD, Daniel ,  TSUI, Chit

IPC: A61K31/535

CPC classification number: C07D211/26 ,  C07D211/22 ,  C07D211/28 ,  C07D211/52 ,  C07D401/04 ,  C07D401/12 ,  C07D413/04 ,  C07D413/14

Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.

Abstract translation: 本发明涉及二芳基哌啶基肾素抑制剂化合物及其在治疗心血管事件和肾功能不全中的用途。

公开(公告)号：EP2780026A2

公开(公告)日：2014-09-24

申请号：EP12850713.4

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc. ,  Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.

Inventor： RUDD, Michael, T. ,  MCCAULEY, John ,  LIVERTON, Nigel ,  GRISE-BARD, Christiane ,  BROUCHU, Marie-Christine ,  CHARRON, Sylvie ,  AULAKH, Virender ,  BACHAND, Benoit ,  BEAULIEU, Patrick ,  ZAGHDANE, Helmi ,  HAN, Yongxin ,  FERRARA, Marco ,  HARPER, Steven ,  SUMMA, Vincenzo ,  CHACKALAMANNIL, Samuel ,  VENKATRAMAN, Srikanth ,  SHAH, Unmesh ,  VELAZQUEZ, Francisco

IPC: A61K38/12

CPC classification number: C07K5/08 ,  A61K31/4745 ,  A61K31/5377 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/005 ,  A61K38/06 ,  A61K38/12 ,  A61K38/21 ,  C07K5/0804 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0821 ,  A61K2300/00

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.

公开(公告)号：EP3185865A1

公开(公告)日：2017-07-05

申请号：EP15836358.0

申请日：2015-08-24

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： ARASAPPAN, Ashok ,  BUNGARD, Christopher James ,  FRIE, Jessica L. ,  HAN, Yongxin ,  HOYT, Scott B. ,  MANLEY, Peter J. ,  MEISSNER, Robert S. ,  PERKINS, James J. ,  SEBHAT, Iyassu K. ,  WILKENING, Robert R. ,  LEAVITT, Kenneth J.

IPC: A61K31/4375

Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.

Abstract translation: 本发明提供式（I）的喹啉甲酰胺和喹啉腈化合物或其药学上可接受的盐，其中R 1，R 2，L，X 1，X 2和X 3如本文所定义。 本发明的药物组合物包含它们的化合物，以及它们的药学上可接受的盐，以及，是非竞争性的mGluR2拮抗剂，或mGluR2的负变构调节剂（NAMs中）是有用的，并在有需要治疗的人，其用于的方法可能是有用的 疾病或病症，其中mGluR2的-NAM受体发挥致病作用，如阿尔茨海默氏症，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍。

公开(公告)号：EP2882754A1

公开(公告)日：2015-06-17

申请号：EP13748245.1

申请日：2013-08-06

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： BARA, Thomas ,  BHAT, Sathesh ,  BISWAS, Dipshika ,  BROCKUNIER, Linda ,  BURNETTE, Duane ,  CHACKALAMANNIL, Samuel ,  CHELIAH, Mariappan, V. ,  CHEN, Austin ,  CLASBY, Martin ,  COLANDREA, Vince, J. ,  GUO, Zhuyan ,  HAN, Yongxin ,  JAYNE, Charles ,  JOSIEN, Hubert ,  MARCANTONIO, Karen ,  MIAO, Shouwu ,  NEELAMKAVIL, Santhosh ,  PINTO, Patrick ,  RAJAGOPALAN, Murali ,  SHAH, Unmesh ,  VELAZQUEZ, Francisco ,  VENKATRAMAN, Srikanth ,  XIA, Yan

IPC: C07D491/107 ,  A61K31/343 ,  A61K31/407 ,  A61P1/16 ,  A61P31/14

CPC classification number: C07K5/08 ,  A61K38/06 ,  A61K45/06 ,  C07D419/00 ,  C07D491/22

Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.

Abstract translation: 本发明涉及含有螺环状的丙型肝炎病毒（HCV）NS3蛋白酶抑制剂，这些化合物的用途以及这些化合物的合成。

公开(公告)号：EP3886845A1

公开(公告)日：2021-10-06

申请号：EP19888409.0

申请日：2019-11-25

Applicant: Merck Sharp & Dohme Corp.

Inventor： CLAUSEN, Dane ,  CHEN, Ping ,  FRADERA, Xavier ,  GUO, Liangqin ,  HAN, Yongxin ,  HE, Shuwen ,  HUANG, Xianhai ,  KOZLOWSKI, Joseph ,  LI, Guoqing ,  MARTINOT, Theodore, A. ,  PASTERNAK, Alexander ,  VERRAS, Andreas ,  XIAO, Li ,  YU, Wensheng ,  ZHANG, Rui

IPC: A61K31/416 ,  C07D231/56

公开(公告)号：EP3710444A1

公开(公告)日：2020-09-23

申请号：EP18807838.0

申请日：2018-11-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： HAN, Yongxin ,  ACHAB, Abdelghani ,  DENG, Yongqi ,  FRADERA, Xavier ,  GIBEAU, Craig ,  HOPKINS, Brett, A. ,  LI, Derun ,  LIU, Kun ,  MCGOWAN, Meredeth, A. ,  SCIAMMETTA, Nunzio ,  SLOMAN, David ,  WHITE, Catherine ,  ZHANG, Hongjun ,  ZHOU, Hua

IPC: C07D405/14 ,  C07D413/14 ,  C07D231/12 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D413/10 ,  C07D241/12 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D263/32 ,  A61K31/443 ,  A61K31/437 ,  A61K31/337 ,  A61P37/00 ,  A61P35/00 ,  A61P31/00

公开(公告)号：EP3694506A1

公开(公告)日：2020-08-19

申请号：EP18866742.2

申请日：2018-10-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： WHITE, Catherine, M. ,  MCGOWAN, Meredeth Ann ,  HAN, Yongxin ,  SCIAMMETTA, Nunzio

IPC: A61K31/337 ,  C07D305/02

公开(公告)号：EP4051678A1

公开(公告)日：2022-09-07

申请号：EP20815976.4

申请日：2020-10-27

Applicant: MERCK SHARP & DOHME CORP.

Inventor： BHARATHAN, Indu ,  GATHIAKA, Symon ,  GRAHAM, Thomas, H. ,  HAN, Yongxin ,  HENDERSON, Timothy ,  HENNESSY, Elisabeth ,  MA, Xiaoshen ,  OTTE, Ryan ,  PALANI, Anandan ,  SLOMAN, David, L.

IPC: C07D471/04 ,  C07D498/04 ,  A61K31/522 ,  A61P35/00