公开(公告)号：WO2006031606A2

公开(公告)日：2006-03-23

申请号：PCT/US2005/032036

申请日：2005-09-09

Applicant: MERCK & CO., INC. ,  WILLIAMS, Theresa, M. ,  BURGEY, Christopher, S. ,  TUCKER, Thomas, J. ,  STUMP, Craig, A. ,  BELL, Ian, M.

Inventor： WILLIAMS, Theresa, M. ,  BURGEY, Christopher, S. ,  TUCKER, Thomas, J. ,  STUMP, Craig, A. ,  BELL, Ian, M.

IPC: A61K31/55

CPC classification number: C07D471/04 ,  C07D401/12 ,  C07D413/12 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP receptors and 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.

Abstract translation: 本发明涉及式I的化合物：I（其中变量A 1，A 2，B，J，K，m，n，R 4 R 5c，R 5b和R 5c如本文所定义）可用作CGRP受体的拮抗剂并且可用于治疗 或预防CGRP所涉及的疾病，如头痛，偏头痛和丛集性头痛。 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CGRP的疾病中的用途。

公开(公告)号：WO2004087649A2

公开(公告)日：2004-10-14

申请号：PCT/US2004007715

申请日：2004-03-10

Applicant: MERCK & CO INC ,  BELL IAN M ,  GRAHAM SAMUEL L ,  WILLIAMS THERESA M ,  STUMP CRAIG A

Inventor： BELL IAN M ,  GRAHAM SAMUEL L ,  WILLIAMS THERESA M ,  STUMP CRAIG A

IPC: A61K31/55 ,  C07D20060101 ,  C07D403/12 ,  C07D

CPC classification number: C07D403/12 ,  C07D235/02

Abstract: 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.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的化合物，其可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 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CGRP的疾病中的用途。

公开(公告)号：WO2004082602A2

公开(公告)日：2004-09-30

申请号：PCT/US2004/007226

申请日：2004-03-10

Applicant: MERCK & CO. INC. ,  BELL, Ian, M. ,  GALLICCHIO, Steven, N. ,  STUMP, Craig, A. ,  ZARTMAN, Blair, C.

Inventor： BELL, Ian, M. ,  GALLICCHIO, Steven, N. ,  STUMP, Craig, A. ,  ZARTMAN, Blair, C.

IPC: A61K

CPC classification number: C07D233/78 ,  C07D235/02 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D471/10 ,  C07D513/04

Abstract: 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.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的化合物，其可用于治疗或预防涉及CGRP的疾病，例如头痛，偏头痛和丛集性头痛。 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CGRP的疾病中的用途。

公开(公告)号：WO2003086395A1

公开(公告)日：2003-10-23

申请号：PCT/US2003/010737

申请日：2003-04-08

Applicant: MERCK & CO., INC. ,  KIM, Annette ,  STUMP, Craig, A. ,  DINSMORE, Christopher, J. ,  GRAHAM, Samuel, L. ,  WILLIAMS, Theresa, M. ,  NGUYEN, Diem, N. ,  TROTTER, B. Wesley

Inventor： KIM, Annette ,  STUMP, Craig, A. ,  DINSMORE, Christopher, J. ,  GRAHAM, Samuel, L. ,  WILLIAMS, Theresa, M. ,  NGUYEN, Diem, N. ,  TROTTER, B. Wesley

IPC: A61K31/439

CPC classification number: C07D471/08 ,  A01M31/06

Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a benzazocine moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.

Abstract translation: 本发明涉及能够抑制，调节和/或调节受体型和非受体型酪氨酸激酶的信号转导的化合物。 本发明的化合物具有包含苯并佐菌酮部分的核心结构。 本发明还涉及这些化合物的药学上可接受的盐，水合物和立体异构体。

公开(公告)号：WO2017222952A1

公开(公告)日：2017-12-28

申请号：PCT/US2017/038068

申请日：2017-06-19

Applicant: MERCK SHARP & DOHME CORP. ,  WALJI, Abbas ,  BERGER, Richard ,  STUMP, Craig, A. ,  SCHLEGEL, Kelly Ann, S. ,  MULHEARN, James, J. ,  GRESHOCK, Thomas, J. ,  FRALEY, Mark, E. ,  JONES, Kristen, G.

Inventor： WALJI, Abbas ,  BERGER, Richard ,  STUMP, Craig, A. ,  SCHLEGEL, Kelly Ann, S. ,  MULHEARN, James, J. ,  GRESHOCK, Thomas, J. ,  FRALEY, Mark, E. ,  JONES, Kristen, G.

IPC: C07D413/14 ,  A61K31/4245 ,  A61K31/444

CPC classification number: A61K45/06 ,  A61P9/00 ,  A61P11/06 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.

Abstract translation: 本发明涉及通式（I）（I）的取代的5-三氟甲基恶二唑化合物或其药学上可接受的盐。 特别地，本发明涉及一类式I的杂芳基取代的5-三氟甲基恶二唑化合物，其可用作HDAC6抑制剂以治疗细胞增殖性疾病，包括癌症，神经退行性疾病如精神分裂症和中风以及其他 疾病。

公开(公告)号：WO2017222951A1

公开(公告)日：2017-12-28

申请号：PCT/US2017/038067

申请日：2017-06-19

Applicant: MERCK SHARP & DOHME CORP. ,  WALJI, Abbas ,  BERGER, Richard ,  STUMP, Craig, A. ,  SCHLEGEL, Kelly Ann, S. ,  MULHEARN, James, J. ,  GRESHOCK, Thomas, J. ,  WANG, Deping ,  FRALEY, Mark, E. ,  JONES, Kristen, G.

Inventor： WALJI, Abbas ,  BERGER, Richard ,  STUMP, Craig, A. ,  SCHLEGEL, Kelly Ann, S. ,  MULHEARN, James, J. ,  GRESHOCK, Thomas, J. ,  WANG, Deping ,  FRALEY, Mark, E. ,  JONES, Kristen, G.

IPC: C07D413/14 ,  A61K31/4245 ,  A61K31/444

CPC classification number: C07D413/10 ,  A61K45/06 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  C07D271/06 ,  C07D271/113 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D498/04 ,  C07D513/04 ,  C07F7/0807

Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.

Abstract translation: 本发明涉及通式（I）的取代的5-三氟甲基恶二唑化合物或其药学上可接受的盐。 特别地，本发明涉及一类式I的芳基和杂芳基取代的5-三氟甲基恶二唑化合物，其可用作HDAC6抑制剂用于治疗细胞增殖性疾病，包括癌症，神经变性疾病，例如精神分裂症和中风，以及 作为其他疾病。

公开(公告)号：WO2016164286A2

公开(公告)日：2016-10-13

申请号：PCT/US2016/025810

申请日：2016-04-04

Applicant: MERCK SHARP & DOHME CORP. ,  STUMP, Craig, A. ,  CHEN, Yi Heng ,  LIU, Ping ,  MENG, Dongfang ,  WU, Jane ,  LI, Chun Sing ,  QI, Zhiqi

Inventor： STUMP, Craig, A. ,  CHEN, Yi Heng ,  LIU, Ping ,  MENG, Dongfang ,  WU, Jane ,  LI, Chun Sing ,  QI, Zhiqi

IPC: G06F1/08

CPC classification number: C07D471/04 ,  A61P7/02 ,  A61P9/10 ,  A61P17/06 ,  A61P25/00 ,  A61P35/00 ,  C07D403/12 ,  C07D417/12 ,  C07D473/04 ,  C07D487/04

Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (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.

Abstract translation: 本发明涉及式（I）的双环杂芳基苯甲酰胺化合物：其为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，损伤或与脱髓鞘或脱髓鞘相关的疾病或障碍。

公开(公告)号：WO2015143652A8

公开(公告)日：2015-12-10

申请号：PCT/CN2014074143

申请日：2014-03-26

Applicant: MERCK SHARP & DOHME ,  MITCHELL HELEN ,  FRALEY MARK E ,  COOKE ANDREW J ,  STUMP CRAIG A ,  BESHORE DOUGLAS C ,  MCCOMAS CASEY C ,  SCHIRRIPA KATHY ,  MCWHERTER MELODY ,  ZHANG XU-FANG ,  MERCER SWATI P ,  MOORE KEITH ,  LIU CHUNGSING ,  MAO QINGHAU

Inventor： MITCHELL HELEN ,  FRALEY MARK E ,  COOKE ANDREW J ,  STUMP CRAIG A ,  BESHORE DOUGLAS C ,  MCCOMAS CASEY C ,  SCHIRRIPA KATHY ,  MCWHERTER MELODY ,  ZHANG XU-FANG ,  MERCER SWATI P ,  MOORE KEITH ,  LIU CHUNGSING ,  MAO QINGHAU

IPC: C07D235/00 ,  A61K31/16 ,  A61P29/00 ,  C07D263/52 ,  C07D275/04 ,  C07D277/60 ,  C07D285/14 ,  C07D291/08

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: 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.

Abstract translation: 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，损伤或与脱髓鞘或脱髓鞘相关的疾病或障碍。

公开(公告)号：WO2015148344A2

公开(公告)日：2015-10-01

申请号：PCT/US2015021936

申请日：2015-03-23

Applicant: MERCK SHARP & DOHME ,  MSD R & D CHINA CO LTD ,  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

Inventor： 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: C07D471/04

CPC classification number: 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

Abstract: 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.

Abstract translation: 本发明涉及式（I）的六元杂芳基苯甲酰胺化合物，其为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，疾病，障碍，损伤或与神经生长因子（NGF）受体TrkA的异常活动相关的疾病或病症相关的异常髓鞘或脱髓鞘相关的功能障碍。

公开(公告)号：WO2015143654A8

公开(公告)日：2015-10-01

申请号：PCT/CN2014/074145

申请日：2014-03-26

Applicant: MERCK SHARP & DOHME CORP. ,  MITCHELL, Helen ,  FRALEY, Mark E. ,  COOKE, Andrew J. ,  STUMP, Craig A. ,  SCHIRRIPA, Kathy ,  ZHANG, Xu-Fang ,  MCWHERTER, Melody ,  LIU, Chungsing ,  MAO, Qinghau

Inventor： MITCHELL, Helen ,  FRALEY, Mark E. ,  COOKE, Andrew J. ,  STUMP, Craig A. ,  SCHIRRIPA, Kathy ,  ZHANG, Xu-Fang ,  MCWHERTER, Melody ,  LIU, Chungsing ,  MAO, Qinghau

IPC: C07D213/00 ,  C07D221/00 ,  C07D239/02 ,  C07D241/02 ,  C07D251/02 ,  C07D265/00 ,  C07D279/00 ,  A61K31/16 ,  A61P29/00

Abstract: 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.