公开(公告)号：EP3302486A1

公开(公告)日：2018-04-11

申请号：EP16804194.5

申请日：2016-05-31

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

Inventor： SHEN, Dong-Ming ,  DWYER, Michael P. ,  SINZ, Christopher J. ,  WANG, Deping ,  STACHEL, Shawn ,  PAONE, Daniel V. ,  FORSTER, Ashley ,  BERGER, Richard ,  CHEN, Yili ,  QIAN, Yimin ,  XU, Shimin ,  HU, Chunmei

IPC: A61K31/519 ,  A61P25/28 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28

Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

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：EP3302486B1

公开(公告)日：2020-09-30

申请号：EP16804194.5

申请日：2016-05-31

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

Inventor： SHEN, Dong-Ming ,  DWYER, Michael P. ,  SINZ, Christopher J. ,  WANG, Deping ,  STACHEL, Shawn ,  PAONE, Daniel V. ,  FORSTER, Ashley ,  BERGER, Richard ,  CHEN, Yili ,  QIAN, Yimin ,  XU, Shimin ,  HU, Chunmei

IPC: A61K31/519 ,  A61P25/28 ,  C07D487/04

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：EP3270926A1

公开(公告)日：2018-01-24

申请号：EP16765473.0

申请日：2016-03-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： SHEN, Dong-Ming ,  SINZ, Christopher J. ,  CRESPO, Alejandro ,  WILSON, Jonathan E. ,  MCCRACKEN, Troy ,  XU, Shimin ,  LI, Haitang

IPC: A61K31/513 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D403/04 ,  A61P25/00 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention is directed to 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). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：EP3204363A1

公开(公告)日：2017-08-16

申请号：EP15849713.1

申请日：2015-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  CRESPO, Alejandro ,  WANG, Ming ,  CHEN, Yili ,  CAI, Jiaqiang ,  WU, Fan ,  DU, Xiaoxing

IPC: C07D239/26

CPC classification number: C07D239/36 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

Abstract: The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

公开(公告)号：EP3204385A1

公开(公告)日：2017-08-16

申请号：EP15848373.5

申请日：2015-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  WANG, Ming ,  CHEN, Yili ,  CAI, Jiaqiang

IPC: C07D471/20 ,  C07D401/14 ,  C07D471/04

CPC classification number: C07D239/36 ,  A61P7/06 ,  C07D413/06

Abstract: The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Abstract translation: 本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，它们用于增强促红细胞生成素的内源产生的用途，以及用于治疗与促红细胞生成素内源性产生减少有关的疾病如贫血等疾病的药物组合物，以及包含这种化合物 和药物载体。

公开(公告)号：EP3204384A1

公开(公告)日：2017-08-16

申请号：EP15848319.8

申请日：2015-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  WANG, Ming ,  CAI, Jiaqiang ,  DU, Xiaoxing ,  CHEN, Yili

IPC: C07D471/20 ,  C07D401/14 ,  C07D471/04

CPC classification number: C07D213/82 ,  A61P7/08 ,  C07D401/04

Abstract: The present invention concerns compounds of formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

Abstract translation: 本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，它们用于增强促红细胞生成素的内源性产生的用途，以及用于治疗与促红细胞生成素的内源性产生减少有关的疾病如贫血等疾病的药物组合物以及包含这种化合物 和药物载体。