公开(公告)号：EP2443124A1

公开(公告)日：2012-04-25

申请号：EP10789936.1

申请日：2010-06-07

Applicant: Merck Sharp & Dohme Corp.

Inventor： PIERCE, Joan, M. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  VACHAL, Petr

IPC: C07D491/10 ,  A61K31/44

CPC classification number: A61K31/44 ,  C07D471/10

Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

Abstract translation: 本发明涉及用作HIF脯氨酰羟化酶抑制剂以治疗贫血和类似病症的取代的1,3,8-三氮杂螺[4.5]十-2,4-二酮。

公开(公告)号：EP3463362A1

公开(公告)日：2019-04-10

申请号：EP17803324.7

申请日：2017-05-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： ADAMS, Gregory, L. ,  COX, Jason, M. ,  DEBENHAM, John, S. ,  EDMONDSON, Scott ,  GILBERT, Eric, J. ,  GUO, Yan ,  JIANG, Yu ,  JOSIEN, Hubert ,  KIM, Hyunjin, M. ,  LAN, Ping ,  MIAO, Shouwu ,  PLUMMER, Christopher, W. ,  RAJAGOPALAN, Murali ,  SHAH, Unmesh ,  SUN, Zhongxiang ,  TRUONG, Quang, T. ,  UJJAINWALLA, Feroze ,  VELAZQUEZ, Francisco ,  VENKATRAMAN, Srikanth ,  SUZUKI, Takao ,  WANG, Nengxue

IPC: A61K31/472 ,  A61K31/4725 ,  A61P3/10 ,  C07D217/02

公开(公告)号：EP3394067A1

公开(公告)日：2018-10-31

申请号：EP16823455.7

申请日：2016-12-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： BERGER, Raphelle ,  CHEN, Yi-Heng ,  LI, Guoqing ,  GARFUNKLE, Joie ,  LI, Hong ,  MIAO, Shouwu ,  RAGHAVAN, Subharekha ,  SMITH, Cameron, J. ,  STELMACH, John ,  WHITEHEAD, Alan ,  ZHANG, Rui ,  ZHANG, Yong ,  FU, Jianmin ,  JI, Gang ,  JIANG, Falong

IPC: C07D487/04 ,  A61K31/519 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04

Abstract: or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.

公开(公告)号：EP2160187B1

公开(公告)日：2013-05-22

申请号：EP08769441.0

申请日：2008-05-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： FLETCHER, Joan, M. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  VACHAL, Petr

IPC: A61K31/44 ,  C07D401/00 ,  A61P7/06

CPC classification number: C07D471/10

公开(公告)号：EP2575473B1

公开(公告)日：2016-01-20

申请号：EP11787236.6

申请日：2011-05-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： RAGHAVAN, Subharekha ,  STELMACH, John, E. ,  SMITH, Cameron, J. ,  LI, Hong ,  WHITEHEAD, Alan ,  WADDELL, Sherman, T. ,  CHEN, Yi-Heng ,  MIAO, Shouwu ,  ORNOSKI, Olga, A. ,  GARFUNKLE, Joie ,  LIAO, Xibin ,  CHANG, Jiang ,  HAN, Xiaoqing ,  GUO, Jian ,  GROEPER, Jonathan, A. ,  BROCKUNIER, Linda, L. ,  ROSAUER, Keith ,  PARMEE, Emma, R.

IPC: A01N43/90 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D519/00

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：EP2575473A1

公开(公告)日：2013-04-10

申请号：EP11787236.6

申请日：2011-05-24

Applicant: Merck Sharp & Dohme Corp.

Inventor： RAGHAVAN, Subharekha ,  STELMACH, John, E. ,  SMITH, Cameron, J. ,  LI, Hong ,  WHITEHEAD, Alan ,  WADDELL, Sherman, T. ,  CHEN, Yi-Heng ,  MIAO, Shouwu ,  ORNOSKI, Olga, A. ,  GARFUNKLE, Joie ,  LIAO, Xibin ,  CHANG, Jiang ,  HAN, Xiaoqing ,  GUO, Jian ,  GROEPER, Jonathan, A. ,  BROCKUNIER, Linda, L. ,  ROSAUER, Keith ,  PARMEE, Emma, R.

IPC: A01N43/90 ,  A61K31/519

CPC classification number: C07D487/04 ,  A61K31/519 ,  C07D519/00

Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract translation: 式（I）化合物或其药学上可接受的盐能够调节身体产生环磷酸鸟苷（“cGMP”），并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病 。 本发明还涉及制备式I化合物或其药学上可接受的盐用于治疗和预防上述疾病和制备用于该目的的药物的方法，以及涉及包含式 I）或其药学上可接受的盐。

公开(公告)号：EP2285375A2

公开(公告)日：2011-02-23

申请号：EP09743278.5

申请日：2009-04-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： FLETCHER, Joan, M. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  VACHAL, Petr

IPC: A61K31/44 ,  A61K31/40 ,  A61K31/235

CPC classification number: C07D471/20

Abstract: The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

Abstract translation: 本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似疾病的螺氮杂吲哚化合物。

公开(公告)号：EP2160187A1

公开(公告)日：2010-03-10

申请号：EP08769441.0

申请日：2008-05-12

Applicant: Merck Sharp & Dohme Corp.

Inventor： FLETCHER, Joan, M. ,  HALE, Jeffrey, J. ,  MIAO, Shouwu ,  VACHAL, Petr

IPC: A61K31/44 ,  C07D401/00

CPC classification number: C07D471/10

Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.

Abstract translation: 本发明涉及可用作HIF脯氨酰羟化酶抑制剂治疗贫血和类似疾病的螺吲哒酮化合物。

公开(公告)号：EP3394067B1

公开(公告)日：2020-04-01

申请号：EP16823455.7

申请日：2016-12-20

Applicant: Merck Sharp & Dohme Corp.

Inventor： BERGER, Raphelle ,  CHEN, Yi-Heng ,  LI, Guoqing ,  GARFUNKLE, Joie ,  LI, Hong ,  MIAO, Shouwu ,  RAGHAVAN, Subharekha ,  SMITH, Cameron, J. ,  STELMACH, John ,  WHITEHEAD, Alan ,  ZHANG, Rui ,  ZHANG, Yong ,  FU, Jianmin ,  JI, Gang ,  JIANG, Falong

IPC: C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/04