公开(公告)号：WO2022109161A1

公开(公告)日：2022-05-27

申请号：PCT/US2021/059930

申请日：2021-11-18

申请人： MERCK SHARP & DOHME CORP. ,  BAO, Jianming ,  CERNAKA, Natalija ,  CHENG, Alan, C. ,  GAO, Ying-Duo ,  JABRI, Salman ,  LOPEZ, Jovan Alexander ,  MERCHANT, Rohan ,  OGAWA, Anthony Ken ,  OSLER, Skylar, K. ,  SINZ, Christopher, J. ,  SHARP, Phillip Patrick ,  TANG, Haiqun ,  TIAN, Maoqun ,  XIAO, Dong ,  YANG, Song

发明人： BAO, Jianming ,  CERNAKA, Natalija ,  CHENG, Alan, C. ,  GAO, Ying-Duo ,  JABRI, Salman ,  LOPEZ, Jovan Alexander ,  MERCHANT, Rohan ,  OGAWA, Anthony Ken ,  OSLER, Skylar, K. ,  SINZ, Christopher, J. ,  SHARP, Phillip Patrick ,  TANG, Haiqun ,  TIAN, Maoqun ,  XIAO, Dong ,  YANG, Song

IPC分类号： A61K31/4439 ,  A61P7/02 ,  C07D403/12

摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：WO2016057753A1

公开(公告)日：2016-04-14

申请号：PCT/US2015/054626

申请日：2015-10-08

申请人： MERCK SHARP & DOHME CORP ,  UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  WANG, Ming ,  CHEN, Yili ,  CAI, Jiaqiang

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

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

CPC分类号： C07D239/36 ,  A61P7/06 ,  C07D413/06

摘要： 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.

摘要翻译： 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的内源性产生减少有关的疾病如贫血等疾病， 以及包含这种化合物和药物载体的药物组合物。

公开(公告)号：WO2016057743A1

公开(公告)日：2016-04-14

申请号：PCT/US2015/054605

申请日：2015-10-08

申请人： MERCK SHARP & DOHME CORP ,  UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  WANG, Ming ,  CAI, Jiaqiang ,  DU, Xiaoxing ,  CHEN, Yili

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

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

CPC分类号： C07D213/82 ,  A61P7/08 ,  C07D401/04

摘要： 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.

摘要翻译： 本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，其用于增强促红细胞生成素的内源性产生的用途，以及用于治疗与减少红细胞生成素的内源性产生如贫血和类似病症相关的病症，以及包含这种化合物 和药用载体。

公开(公告)号：WO2016196417A1

公开(公告)日：2016-12-08

申请号：PCT/US2016/034928

申请日：2016-05-31

申请人： MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD. ,  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

发明人： 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分类号： A61K31/519 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28

摘要： 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.

摘要翻译： 本发明涉及式（I）的二氢吡唑并嘧啶酮化合物，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的治疗剂。 本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症以及与纹状体功能不全或基底神经节功能障碍相关的神经和精神疾病的用途。

公开(公告)号：WO2016054804A1

公开(公告)日：2016-04-14

申请号：PCT/CN2014/088318

申请日：2014-10-10

申请人： MERCK SHARP & DOHME CORP. ,  UJJAINWALLA, Fez ,  TAN, John Qiang ,  DANG, Qun ,  SINZ, Christopher J. ,  CRESPO, Alejandro ,  WANG, Ming ,  CHEN, Yili ,  CAI, Jiaqiang ,  WU, Fan ,  DU, Xiaoxing

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

IPC分类号： C07D239/36 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  A61K31/505 ,  A61K31/506 ,  A61K31/66 ,  A61P7/00

CPC分类号： C07D239/36 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

摘要： 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.

摘要翻译： 本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，其用于促进促红细胞生成素的内源性产生的用途，以及用于治疗与减少红细胞生成素的内源产生如贫血和类似病症相关的病症，以及包含这种化合物 和药用载体。

公开(公告)号：WO2010099054A2

公开(公告)日：2010-09-02

申请号：PCT/US2010/024853

申请日：2010-02-22

申请人： MERCK SHARP & DOHME CORP. ,  KIM, Ronald, M. ,  PARMEE, Emma, R. ,  SINZ, Christopher Joseph ,  ZIOUZINA, Olga, A.

发明人： KIM, Ronald, M. ,  PARMEE, Emma, R. ,  SINZ, Christopher Joseph ,  ZIOUZINA, Olga, A.

IPC分类号： C07D401/04

CPC分类号： C07D401/04 ,  C07D401/14

摘要： This inventions relates to compounds having the structure Formula I I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.

摘要翻译： 本发明涉及具有结构式I I的化合物及其可药用盐，它们是可溶性鸟苷酸环化酶活化剂。 该化合物可用于治疗或预防心血管疾病，内皮功能障碍，舒张功能障碍，动脉粥样硬化，高血压，肺动脉高压，心绞痛，血栓形成，再狭窄，心肌梗死，中风，心功能不全，肺性高血压，勃起功能障碍，支气管哮喘，慢性 肾功能不全，糖尿病或肝硬化。

公开(公告)号：WO2022010828A1

公开(公告)日：2022-01-13

申请号：PCT/US2021/040420

申请日：2021-07-06

申请人： MERCK SHARP & DOHME CORP. ,  HICKS, Jacqueline, D. ,  KUANG, Rongze ,  SINZ, Christopher, J. ,  LOMBARDO, Matthew, J. ,  LOPEZ, Jovan Alexander ,  MERCHANT, Rohan ,  SHARP, Phillip Patrick ,  WU, Zhicai ,  ZHAO, Zhiqiang ,  CHENG, Alan, C. ,  YANG, Song ,  BAO, Jianming ,  TIAN, Maoqun ,  SHEARN-NANCE, Galen Paul

发明人： HICKS, Jacqueline, D. ,  KUANG, Rongze ,  SINZ, Christopher, J. ,  LOMBARDO, Matthew, J. ,  LOPEZ, Jovan Alexander ,  MERCHANT, Rohan ,  SHARP, Phillip Patrick ,  WU, Zhicai ,  ZHAO, Zhiqiang ,  CHENG, Alan, C. ,  YANG, Song ,  BAO, Jianming ,  TIAN, Maoqun ,  SHEARN-NANCE, Galen Paul

IPC分类号： A61K47/02 ,  A61K47/12 ,  A61K47/22

摘要： The present invention provides a compound of Formula (I), and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

公开(公告)号：WO2017003895A1

公开(公告)日：2017-01-05

申请号：PCT/US2016/039479

申请日：2016-06-27

申请人： MERCK SHARP & DOHME CORP. ,  STACHEL, Shawn, J. ,  SINZ, Christopher, J. ,  CHEN, Yili ,  WILSON, Jonathan, E. ,  DWYER, Michael, P. ,  PAONE, Daniel, V. ,  XU, Shimin

发明人： STACHEL, Shawn, J. ,  SINZ, Christopher, J. ,  CHEN, Yili ,  WILSON, Jonathan, E. ,  DWYER, Michael, P. ,  PAONE, Daniel, V. ,  XU, Shimin

IPC分类号： C07D487/04 ,  A61K31/53 ,  C07D231/56 ,  C07D253/06 ,  C07D253/065 ,  C07D253/075

CPC分类号： C07D487/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28

摘要： The present invention is directed to dihydropyrazolopyrimidinone compounds of formulas (I) and (II) 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.

摘要翻译： 本发明涉及式（I）和（II）的二氢吡唑并嘧啶酮化合物，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的治疗剂。 本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症等神经和精神疾病以及与纹状体功能不全或基底神经节功能障碍相关的疾病的用途。

公开(公告)号：WO2016196071A1

公开(公告)日：2016-12-08

申请号：PCT/US2016/033861

申请日：2016-05-24

申请人： MERCK SHARP & DOHME CORP. ,  MSD R&D (CHINA) CO., LTD. ,  SHEN, Dong-Ming ,  DWYER, Michael, P. ,  SINZ, Christopher, J. ,  WANG, Deping ,  STACHEL, Shawn, J. ,  PAONE, Daniel, V. ,  FORSTER, Ashley ,  BERGER, Richard ,  SHIPE, William, D. ,  CHEN, Yili ,  QIAN, Yimin ,  XU, Shimin ,  HU, Chunmei ,  FU, Jianmin ,  GUO, Zhigang ,  LI, Haitang ,  BO, Yingjian

发明人： SHEN, Dong-Ming ,  DWYER, Michael, P. ,  SINZ, Christopher, J. ,  WANG, Deping ,  STACHEL, Shawn, J. ,  PAONE, Daniel, V. ,  FORSTER, Ashley ,  BERGER, Richard ,  SHIPE, William, D. ,  CHEN, Yili ,  QIAN, Yimin ,  XU, Shimin ,  HU, Chunmei ,  FU, Jianmin ,  GUO, Zhigang ,  LI, Haitang ,  BO, Yingjian

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

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

摘要： The present invention is directed to 6-alkyl 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.

摘要翻译： 本发明涉及式（I）的6-烷基二氢吡唑并嘧啶酮化合物，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的治疗剂。 本发明还涉及这类化合物用于治疗神经和精神疾病如精神分裂症，精神病，帕金森氏病，帕金森病痴呆（PDD）或亨廷顿病的用途，以及与纹状体功能减退或基底节功能障碍相关的那些化合物。 / p>

公开(公告)号：WO2016145614A1

公开(公告)日：2016-09-22

申请号：PCT/CN2015/074396

申请日：2015-03-17

申请人： MERCK SHARP & DOHME CORP. ,  SHEN, Dong-Ming ,  SINZ, Christopher J. ,  CRESPO, Alexander ,  WILSON, Jonathan E. ,  MCCRACKEN, Troy ,  XU, Shimin ,  LI, Haitang

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

IPC分类号： C07D239/36 ,  C07D249/06 ,  C07D249/08 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/505 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24

CPC分类号： C07D498/04 ,  A61P25/00 ,  C07D403/04 ,  C07D471/04 ,  C07D487/04

摘要： 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.

摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的式I的嘧啶甲酰胺化合物。 本发明还涉及这些化合物用于治疗精神分裂症，精神病，帕金森病，帕金森病痴呆（PDD）或亨廷顿舞蹈症等神经和精神疾病以及与纹状体功能不全或基底神经节功能障碍相关的疾病的用途。