公开(公告)号：EP2922543A1

公开(公告)日：2015-09-30

申请号：EP13856512.2

申请日：2013-11-15

申请人： Merck Sharp & Dohme Corp.

发明人： MCCOMAS, Casey, C. ,  KUDUK, Scott, D. ,  REGER, Thomas, S.

IPC分类号： A61K31/444

CPC分类号： C07D401/14 ,  A61K31/506 ,  C07D471/04

摘要： The present invention is directed to substituted pyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：EP3122346A2

公开(公告)日：2017-02-01

申请号：EP15769367.2

申请日：2015-03-23

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

发明人： MITCHELL, Helen ,  FRALEY, Mark, E. ,  COOKE, Andrew, J. ,  CHEN, Yi-Heng ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  MERCER, Swati, P. ,  BABAOGLU, Kerim ,  MENG, Dongfang ,  WU, Jane ,  LIU, Ping ,  WOOD, Harold, B. ,  BAO, Jianming ,  LI, Chun Sing ,  MAO, Qinghua ,  QI, Zhiqi

IPC分类号： A61K31/166 ,  C07D471/04

摘要： The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及式（I）的六元杂芳基苯甲酰胺化合物，它们是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，银屑病 ，血栓形成，与神经生长因子（NGF）受体TrkA的异常活性有关的与髓鞘形成障碍或脱髓鞘有关的疾病，病症，损伤或功能障碍或疾病或病症。

公开(公告)号：EP2919781B1

公开(公告)日：2017-06-28

申请号：EP13854671.8

申请日：2013-11-11

申请人： Merck Sharp & Dohme Corp.

发明人： KUDUK, Scott, D. ,  MCCOMAS, Casey, C. ,  REGER, Thomas, S.

IPC分类号： A61K31/506 ,  C07D403/14 ,  A61P25/14

CPC分类号： C07D403/14 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/506

公开(公告)号：EP3013333A1

公开(公告)日：2016-05-04

申请号：EP14816671.3

申请日：2014-06-19

申请人： Merck Sharp & Dohme Corp.

发明人： HE, Shuwen ,  LAI, Zhong ,  DAI, Xing ,  XIAO, Dong ,  LONDON, Clare ,  ZORN, Nicolas ,  NARGUND, Ravi ,  PALANI, Anandan ,  MCCOMAS, Casey, C. ,  LI, Peng ,  PENG, Xuanjia

IPC分类号： A61K31/343

CPC分类号： A61K31/454 ,  A61K31/404 ,  A61K31/423 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K2300/00

摘要： The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

公开(公告)号：EP2922823B1

公开(公告)日：2018-10-31

申请号：EP13856456.2

申请日：2013-11-15

申请人： Merck Sharp & Dohme Corp.

发明人： MCCOMAS, Casey, C. ,  KUDUK, Scott, D. ,  REGER, Thomas, S.

IPC分类号： C07D405/14 ,  C07D413/14 ,  C07D401/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/506 ,  A61P25/18

CPC分类号： C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：EP2922543B1

公开(公告)日：2017-05-24

申请号：EP13856512.2

申请日：2013-11-15

申请人： Merck Sharp & Dohme Corp.

发明人： MCCOMAS, Casey, C. ,  KUDUK, Scott, D. ,  REGER, Thomas, S.

IPC分类号： A61K31/444 ,  C07D401/14 ,  A61K31/506 ,  C07D471/04

CPC分类号： C07D401/14 ,  A61K31/506 ,  C07D471/04

公开(公告)号：EP3122343A2

公开(公告)日：2017-02-01

申请号：EP15767840.0

申请日：2015-03-23

申请人： Merck Sharp & Dohme Corp.

发明人： MITCHELL, Helen ,  FRALEY, Mark, E. ,  COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  LIU, Ping ,  PARKER, Dann ,  LI, Chun Sing ,  MAO, Qinghua

IPC分类号： A61K31/166

CPC分类号： C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

摘要翻译： 本发明涉及作为原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂的式（I）（式（I））的取代的五元杂芳基苯甲酰胺化合物，因此可用于治疗疼痛，炎症，癌症 ，再狭窄，动脉粥样硬化，银屑病，血栓形成，与髓鞘形成障碍或神经生长因子（NGF）受体TrkA异常活性相关的疾病或病症有关的疾病，病症，损伤或功能障碍。

公开(公告)号：EP2968324A1

公开(公告)日：2016-01-20

申请号：EP14768510.1

申请日：2014-03-10

申请人： Merck Sharp & Dohme Corp.

发明人： KUDUK, Scott, D. ,  MCCOMAS, Casey, C. ,  REGER, Thoma, S. ,  QI, Changhe

IPC分类号： A61K31/501 ,  C07D237/02

CPC分类号： C07D417/14 ,  A61K31/50 ,  A61K31/501 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis 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剂以治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的式I的取代的哒嗪酮化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿舞蹈病的用途，以及与纹状体功能减退或基底节功能障碍有关的那些化合物。

公开(公告)号：EP2919781A1

公开(公告)日：2015-09-23

申请号：EP13854671.8

申请日：2013-11-11

申请人： Merck Sharp & Dohme Corp.

发明人： KUDUK, Scott, D. ,  MCCOMAS, Casey, C. ,  REGER, Thomas, S.

IPC分类号： A61K31/4184

CPC分类号： C07D403/14 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/506

摘要： The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis 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10（PDE10）相关的中枢神经系统疾病的治疗剂的取代的环丁基苯并咪唑化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

公开(公告)号：EP3122346B1

公开(公告)日：2020-07-15

申请号：EP15769367.2

申请日：2015-03-23

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

发明人： MITCHELL, Helen ,  FRALEY, Mark, E. ,  COOKE, Andrew, J. ,  CHEN, Yi-Heng ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  MERCER, Swati, P. ,  BABAOGLU, Kerim ,  MENG, Dongfang ,  WU, Jane ,  LIU, Ping ,  WOOD, Harold, B. ,  BAO, Jianming ,  LI, Chun Sing ,  MAO, Qinghua ,  QI, Zhiqi

IPC分类号： A61K31/166 ,  C07D471/04 ,  A61P35/00