公开(公告)号：WO2016164286A3

公开(公告)日：2017-01-05

申请号：PCT/US2016025810

申请日：2016-04-04

Applicant: MERCK SHARP & DOHME ,  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: A61K31/166 ,  A61K31/437 ,  C07D471/04

CPC classification number: C07D417/12 ,  C07D403/12 ,  C07D471/04 ,  C07D473/04

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：WO2015148350A3

公开(公告)日：2015-11-26

申请号：PCT/US2015021944

申请日：2015-03-23

Applicant: MERCK SHARP & DOHME ,  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

Inventor： 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: A61K31/166

CPC classification number: 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

Abstract: 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.

Abstract translation: 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，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的功能障碍。

公开(公告)号：WO2015148373A2

公开(公告)日：2015-10-01

申请号：PCT/US2015/022004

申请日：2015-03-23

Applicant: MERCK SHARP & DOHME CORP. ,  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

Inventor： 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: A61K31/5025 ,  C07D487/04

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，与神经生长因子（NGF）受体TrkA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病症。

公开(公告)号：WO2015148350A2

公开(公告)日：2015-10-01

申请号：PCT/US2015/021944

申请日：2015-03-23

Applicant: MERCK SHARP & DOHME CORP. ,  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

Inventor： 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: A61K31/501 ,  A61K31/4439

CPC classification number: 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

Abstract: 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.

Abstract translation: 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 治疗与神经生长因子（NGF）受体TrkA的异常活性有关的疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，疾病，病症，损伤或与dysmyelination或脱髓鞘相关的功能障碍或疾病或病症。

公开(公告)号：WO2015042088A1

公开(公告)日：2015-03-26

申请号：PCT/US2014/055979

申请日：2014-09-17

Applicant: MERCK SHARP & DOHME CORP ,  COOKE, Andrew, J. ,  STUMP, Craig, A. ,  ZHANG, Xu-Fang ,  LI, Chun Sing ,  MAO, Qinghua

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

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

CPC classification number: 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

Abstract: 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.

公开(公告)号：WO2010033421A1

公开(公告)日：2010-03-25

申请号：PCT/US2009/056507

申请日：2009-09-10

Applicant: MERCK SHARP & DOHME CORP. ,  STUMP, Craig, A.

Inventor： STUMP, Craig, A.

IPC: A01N43/50 ,  A61K31/405 ,  A61K31/415

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/107

Abstract: Compounds of formula (I): wherein variables B, G 1 , G 2 , G 3 , G 4 , E a , E b , E c , A 1 , A 2 , A 3 , A 4 , R 6 and R PG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: 式（I）化合物：其中变量B，G1，G2，G3，G4，Ea，Eb，Ec，A1，A2，A3，A4，R6和RPG和Y如本文所述，它们是CGRP受体的拮抗剂， 其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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：WO2008130524A1

公开(公告)日：2008-10-30

申请号：PCT/US2008/004786

申请日：2008-04-11

Applicant: MERCK & CO., INC. ,  BELL, Ian, M. ,  SELNICK, Harold, G. ,  STUMP, Craig, A.

Inventor： BELL, Ian, M. ,  SELNICK, Harold, G. ,  STUMP, Craig, A.

IPC: A61K31/44

CPC classification number: C07D471/20

Abstract: Compounds of formula I: I (wherein variables A 1 , A 2 , B, m, n, J, X, R 4 , G 1 , G 2 , G 3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: 式I化合物I（其中变量A 1，A 2，B，m，n，J，X，R 4，G 其中CGRP受体是拮抗剂，它们可用于治疗或预防，其中，SEQ ID NO：1，SEQ ID NO：3，SEQ ID NO：3和SEQ ID NO： 涉及CGRP的疾病，如偏头痛。 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：WO2007061696A3

公开(公告)日：2007-11-15

申请号：PCT/US2006044212

申请日：2006-11-14

Applicant: MERCK & CO INC ,  BELL IAN M ,  SELNICK HAROLD G ,  STUMP CRAIG A ,  THEBERGE CORY R ,  ZARTMAN C BLAIR

Inventor： BELL IAN M ,  SELNICK HAROLD G ,  STUMP CRAIG A ,  THEBERGE CORY R ,  ZARTMAN C BLAIR

IPC: A61K31/421 ,  C07D413/02

CPC classification number: C07D471/20 ,  C07D519/00

Abstract: Compounds of formula (I): (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , B, E 1 , E 2 , E 3 , E 4 , E 5 , G 1 , G 2 , J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: 式（I）的化合物：其中变量A 1，A 2，A 3，A 4， A，B，E，E，E，B，E，B，E， >，E 3，E 4，E 5，G 1，G 2， >，J和K如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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：WO2007061694A2

公开(公告)日：2007-05-31

申请号：PCT/US2006/044190

申请日：2006-11-14

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

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

IPC: A61K31/55 ,  C07D487/10

CPC classification number: C07D519/00

Abstract: Compounds of formula I: (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , B 1 , B 2 , B 3 , B 4 , D 1 , D 2 , E 1 , E 2 , E 3 , E 4 , E 5 , G 1 , G 2 , R 6 , T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: 式I化合物:(其中变量A 1，A 2，A 3，A 4，A 5，A 5，A 5， 4，A 5，A 6，A 7，B 1，B 4，B 5，B 5，B 5， 2，B 3，B 4，D 1，D 2，E 3， 1，E 2，E 3，E 4，E 5，G 5，E 5，E 5，E 5， 1，G 2，R 6，T，U，V，W，X，Y和Z如本文所述），它们是CGRP受体的拮抗剂 并且可用于治疗或预防其中涉及CGRP的疾病，如偏头痛。 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其中涉及CGRP的此类疾病中的用途。

公开(公告)号：WO2007061677A3

公开(公告)日：2007-05-31

申请号：PCT/US2006/044088

申请日：2006-11-14

Applicant: MERCK & CO., INC. ,  BELL, Ian, M. ,  SELNICK, Harold, G. ,  WOOD, Michael, R. ,  THEBERGE, Cory, R. ,  STUMP, Craig, A. ,  GALLICCHIO, Steven, N. ,  ZARTMAN, C., Blair

Inventor： BELL, Ian, M. ,  SELNICK, Harold, G. ,  WOOD, Michael, R. ,  THEBERGE, Cory, R. ,  STUMP, Craig, A. ,  GALLICCHIO, Steven, N. ,  ZARTMAN, C., Blair

IPC: A01N43/42 ,  A61K31/44

Abstract: Compounds of formula (I): (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , E 1 , E 2 , E 3 , E 4 , E 5 , G 1 , G 2 , J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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.