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

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：EP3046553A2

公开(公告)日：2016-07-27

申请号：EP14845789.8

申请日：2014-09-17

申请人： Merck Sharp & Dohme Corp.

发明人： COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  LI, Chun Sing ,  MAO, Qinghua

IPC分类号： A61K31/17 ,  A61K31/41 ,  A61P29/00 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D471/04 ,  C07D213/16 ,  C07D231/40 ,  C07D239/42 ,  C07D261/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.

摘要翻译： 本发明涉及式（I）苄基脲化合物，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，牛皮癣，血栓形成 与神经生长因子（NGF）受体Trk-A，Trk-B和/或Trk-C的异常活性有关的疾病，病症，损伤或与功能障碍或脱髓鞘相关的疾病或障碍。

公开(公告)号：EP2421370A1

公开(公告)日：2012-02-29

申请号：EP10767743.7

申请日：2010-04-22

申请人： Merck Sharp & Dohme Corp.

发明人： MERCER, Swati, P. ,  ROECKER, Anthony, J. ,  WILLIAMS, Theresa ,  ZHANG, Xu-Fang

IPC分类号： A01N43/82 ,  A61K31/41

CPC分类号： C07D413/04 ,  C07D413/14

摘要： The present invention is directed to 2-alkylpiperidines which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

摘要翻译： 本发明涉及2-代烷基哌啶，其为代谢型谷氨酸受体的正变构调节剂，特别是mGluR5受体，并且其可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及其中代谢型谷氨酸受体为 参与其中。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：EP3122345A2

公开(公告)日：2017-02-01

申请号：EP15769224.5

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. ,  CHEN, Yi Heng ,  BESHORE, Douglas, C. ,  ZHANG, Xu-Fang ,  MCCOMAS, Casey, C. ,  SCHIRRIPA, Kathy ,  MCWHERTER, Melody ,  MERCER, Swati, P. ,  MOORE, Keith, P. ,  LIU, Ping ,  WOOD, Harold, B. ,  LI, Chun Sing ,  MAO, Qinghua

IPC分类号： A61K31/166

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.

摘要翻译： 本发明涉及式（I）的双环杂芳基苯甲酰胺化合物，其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，牛皮癣， 与神经生长因子（NGF）受体TrkA的异常活动相关的血栓形成，疾病，障碍，损伤或与异常髓鞘或脱髓鞘相关的疾病或障碍。

公开(公告)号：EP2855477A1

公开(公告)日：2015-04-08

申请号：EP13796299.9

申请日：2013-05-24

申请人： Merck Sharp & Dohme Corp.

发明人： ALTMAN, Michael, D. ,  FISCHER, Christian ,  KATZ, Jason, D. ,  WILLIAMS, Theresa, M. ,  ZHANG, Xu-Fang ,  ZHOU, Hua

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D231/12 ,  C07D471/08

摘要： The present invention is directed to isotopically labeled biaryl urea compounds which possess high affinity to neurofibrillary tangles (NFTs), and thus are useful to determine the amount and distribution of NFTs in brain. The isotopically labeled biaryl urea compounds may also be useful as PET tracers and in competition assays to identify other compounds that may serve as PET tracers.

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：EP1606264B1

公开(公告)日：2012-05-02

申请号：EP04719323.0

申请日：2004-03-10

申请人： Merck Sharp & Dohme Corp.

发明人： BELL, Ian, M. ,  THEBERGE, Cory, R. ,  WILLIAMS, Theresa, M. ,  ZARTMAN, C. Blair ,  ZHANG, Xu-Fang ,  GALLICCHIO, Steven, N.

IPC分类号： C07D233/78

CPC分类号： C07D235/02 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12

摘要： The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

公开(公告)号：EP1605936B1

公开(公告)日：2011-07-20

申请号：EP04719322.2

申请日：2004-03-10

申请人： Merck Sharp & Dohme Corp.

发明人： BELL, Ian, M. ,  THEBERGE, Cory, R. ,  ZHANG, Xu-Fang ,  ZARTMAN, C. Blair

IPC分类号： A61K31/415 ,  C07D233/02 ,  C07D233/28

CPC分类号： C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

公开(公告)号：EP3046554A1

公开(公告)日：2016-07-27

申请号：EP14845934.0

申请日：2014-09-17

申请人： Merck Sharp & Dohme Corp.

发明人： COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  LI, Chun Sing ,  MAO, Qinghua

IPC分类号： A61K31/17 ,  A61K31/41 ,  A61P29/00

CPC分类号： C07D213/75 ,  C07C275/28 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D249/08 ,  C07D257/04 ,  C07D261/14 ,  C07D263/32 ,  C07D271/10 ,  C07D277/44 ,  C07D277/48 ,  C07D285/12 ,  C07D295/135 ,  C07D311/88 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.