公开(公告)号：US20170158698A1

公开(公告)日：2017-06-08

申请号：US15128782

申请日：2015-03-23

申请人： Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Xu-Fang ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Ping LIU ,  Dann PARKER ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

发明人： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Ping Liu ,  Dann Parker ,  Chun Sing Li ,  Qinghua Mao

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

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.

公开(公告)号：US20170114056A1

公开(公告)日：2017-04-27

申请号：US15129206

申请日：2015-03-23

申请人： Helen MITCHELL ,  Mark E. FRALEY ,  Andrew J. COOKE ,  Craig A. STUMP ,  Yi Heng CHEN ,  Douglas C. BESHORE ,  Xu-Fank ZHANG ,  Casey C. MCCOMAS ,  Kathy SCHIRRIPA ,  Melody MCWHERTER ,  Swati P. MERCER ,  Keith P. MOORE ,  Ping LIU ,  Harold B. WOOD ,  Chun Sing LI ,  Qinghua MAO ,  Merck Sharp & Dohme Corp.

发明人： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi- Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Keith P. Moore ,  Ping Liu ,  Harold B. Wood ,  Chun Sing Li ,  Qinghua Mao ,  Douglas C. Beshore

IPC分类号： C07D471/04 ,  C07D513/04

CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is directed to a bicyclic 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.

公开(公告)号：US20150307489A1

公开(公告)日：2015-10-29

申请号：US14443619

申请日：2013-11-15

申请人： Casey C. MCCOMAS ,  Scott D. KUDUK ,  Thomas S. REGER ,  MERCK SHARP & DOHME CORP.

发明人： Scott D. Kuduk ,  Casey C. McComas ,  Thomas S. Reger

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

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.

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嘧啶化合物。 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：US20150307479A1

公开(公告)日：2015-10-29

申请号：US14442963

申请日：2013-11-11

申请人： Scott D. KUDUK ,  Casey C. MCCOMAS ,  Thomas S. REGER ,  MERCK SHARP & DOHME CORP.

发明人： Scott D. Kuduk ,  Casey C. McComas ,  Thomas S. Reger

IPC分类号： C07D403/14

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：US20160016947A1

公开(公告)日：2016-01-21

申请号：US14769829

申请日：2014-03-10

申请人： Scott D. KUDUK ,  Casey C. MCCOMAS ,  Thomas S. REGER ,  Changhe QI ,  MERCK SHARP & DOHME CORP.

发明人： Scott D. Kuduk ,  Casey C. McComas ,  Thomas S. Reger

IPC分类号： C07D417/14 ,  C07D403/12 ,  C07D471/04 ,  C07D413/14 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14

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与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的式I的取代吡啶嗪酮化合物。 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：US09663513B2

公开(公告)日：2017-05-30

申请号：US14443619

申请日：2013-11-15

申请人： Merck Sharp & Dohme Corp.

发明人： Scott D. Kuduk ,  Casey C. McComas ,  Thomas S. Reger

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

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：US09914736B2

公开(公告)日：2018-03-13

申请号：US15128782

申请日：2015-03-23

申请人： Merck Sharp & Dohme Corp.

发明人： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Ping Liu ,  Dann Parker ,  Chun Sing Li ,  Qinghua Mao

IPC分类号： A61K31/40 ,  C07D487/04 ,  C07D277/46 ,  C07D231/40 ,  C07D417/12 ,  C07D401/04 ,  C07D417/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

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.

公开(公告)号：US09364482B2

公开(公告)日：2016-06-14

申请号：US14898768

申请日：2014-06-19

申请人： Merck Sharp & Dohme Corp.

发明人： Xing Dai ,  Hong Liu ,  Anandan Palani ,  Shuwen He ,  Ravi Nargund ,  Dong Xiao ,  Nicolas Zorn ,  Qun Dang ,  Casey C. McComas ,  Xuanjia Peng ,  Peng Li ,  Richard Soll

IPC分类号： A61K31/65 ,  A61K31/519 ,  A61K31/517 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/06 ,  C07D498/04 ,  C07D471/04 ,  C07D405/04 ,  C07D475/02 ,  C07D405/14 ,  A61K31/5365 ,  A61K31/53 ,  A61K45/06

CPC分类号： A61K31/5365 ,  A61K31/437 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D475/02 ,  C07D498/04

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)

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的用途的式I化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产。 （一世）

公开(公告)号：US20150368265A1

公开(公告)日：2015-12-24

申请号：US14766491

申请日：2014-02-03

申请人： MERCK SHARP & DOHME CORP.

发明人： Shuwen He ,  Xing Dai ,  Anandan Palani ,  Ravi Nargund ,  Zhong Lai ,  Nicolas Zorn ,  Dong Xiao ,  Qun Dang ,  Casey C. McComas ,  Peng Li ,  Xuanjia Peng ,  Richard Soll

IPC分类号： C07D498/14 ,  A61K31/5365 ,  A61K31/5377 ,  A61K45/06

CPC分类号： C07D498/14 ,  A61K31/5365 ,  A61K31/5377 ,  A61K45/06 ,  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

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的式（I）化合物 并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒生产。 一世

公开(公告)号：US09815846B2

公开(公告)日：2017-11-14

申请号：US15128689

申请日：2015-03-23

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

发明人： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi-Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Kerim Babaoglu ,  Dongfang Meng ,  Jane Wu ,  Ping Liu ,  Harold B. Wood ,  Jianming Bao ,  Chun Sing Li ,  Qinghua Mao ,  Zhiqi Qi

IPC分类号： C07D491/107 ,  C07C233/66 ,  C07D213/75 ,  C07D403/12 ,  C07D401/12 ,  C07D417/12 ,  C07D239/42 ,  C07D401/04 ,  C07D413/12 ,  C07D417/14 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D401/06 ,  C07D413/06 ,  C07D403/06

CPC分类号： C07D491/107 ,  C07C233/66 ,  C07D213/75 ,  C07D231/12 ,  C07D239/42 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  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.