公开(公告)号：WO2012061019A2

公开(公告)日：2012-05-10

申请号：PCT/US2011/056981

申请日：2011-10-20

Applicant: MERCK SHARP & DOHME CORP. ,  ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  LI, Jing ,  MERCER, Swati, P. ,  ROECKER, Anthony, J. ,  STUMP, Craig, A. ,  WILLIAMS, Theresa, M.

Inventor： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  LI, Jing ,  MERCER, Swati, P. ,  ROECKER, Anthony, J. ,  STUMP, Craig, A. ,  WILLIAMS, Theresa, M.

IPC: A61K31/554

CPC classification number: C07D513/04 ,  C07D471/04 ,  C07D471/14 ,  C07D498/04

Abstract: The present invention is directed to tricyclic compounds 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.

Abstract translation: 本发明涉及三环化合物，其是代谢型谷氨酸受体，特别是mGluR5受体的正性变构调节剂，其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病症以及涉及代谢型谷氨酸受体的疾病 。 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：WO2010077752A1

公开(公告)日：2010-07-08

申请号：PCT/US2009/067412

申请日：2009-12-10

Applicant: MERCK SHARP & DOHME CORP. ,  SELNICK, Harold G. ,  WOOD, Michael R. ,  MCWHERTER, Melody ,  HILLS, Ivory D. ,  STUMP, Craig A.

Inventor： SELNICK, Harold G. ,  WOOD, Michael R. ,  MCWHERTER, Melody ,  HILLS, Ivory D. ,  STUMP, Craig A.

IPC: A01N43/50

CPC classification number: C07D471/10 ,  C07D235/02 ,  C07D471/20 ,  C07D491/10 ,  C07D519/00

Abstract: The present invention is directed to imidazolinone derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which 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: 本发明涉及作为CGRP受体的拮抗剂的咪唑啉酮衍生物，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：WO2008130512A1

公开(公告)日：2008-10-30

申请号：PCT/US2008/004694

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: A01N31/00 ,  A61K31/05

CPC classification number: C07D471/20 ,  C07D519/00

Abstract: Compounds of formula I: I (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 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：I（其中变量A1，A2，B，m，n，J，R4，G1，G2，G3和Y如本文所述）是CGRP受体的拮抗剂，其可用于治疗或预防 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：WO2008112159A3

公开(公告)日：2008-10-30

申请号：PCT/US2008003078

申请日：2008-03-07

Applicant: MERCK & CO INC ,  BELL IAN M ,  STUMP CRAIG A ,  SELNICK HAROLD G

Inventor： BELL IAN M ,  STUMP CRAIG A ,  SELNICK HAROLD G

IPC: A61K31/44 ,  A61K31/40

CPC classification number: C07D471/20 ,  C07D403/12 ,  C07D471/10 ,  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化合物：其中变量A 1，A 2，B，J，K，m，n，R 4 R 5，R 5和R 5c如本文所定义）可用作CGRP受体的拮抗剂并可用于治疗 或预防涉及CGRP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的此类疾病中的用途。

公开(公告)号：WO2008112159A2

公开(公告)日：2008-09-18

申请号：PCT/US2008/003078

申请日：2008-03-07

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

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

IPC: A61K31/401

CPC classification number: C07D471/20 ,  C07D403/12 ,  C07D471/10 ,  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化合物：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：WO2008020902A1

公开(公告)日：2008-02-21

申请号：PCT/US2007/010953

申请日：2007-05-04

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

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

IPC: C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D519/00 ,  A61K31/403 ,  A61K31/407 ,  C07D471/20 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/438 ,  A61K31/4965 ,  A61K31/499

CPC classification number: C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/20 ,  C07D519/00

Abstract: Compounds of formula I: I (wherein variables A 1 , A 2 , A 3 , A 4 , m, n, J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , 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I（其中变量A 1，A 2，A 3，A 4，M ，n，J，Q，R 4，O，A，B，C，O， > 6，R 7，R e，R f，R PG和Y分别为 本文描述），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：WO2007061695A3

公开(公告)日：2007-12-06

申请号：PCT/US2006044194

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: A61K31/4188 ,  C07D413/02

CPC classification number: C07D487/10 ,  C07D471/10

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 and R 6 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 4， 第5类，第6类，第7类，第B类，第1类，第2类， E 3，E 4，E 5，G 1，G 2和 R 6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：WO2005072308A3

公开(公告)日：2007-03-22

申请号：PCT/US2005002199

申请日：2005-01-25

Applicant: MERCK & CO INC ,  BURGEY CHRISTOPHER S ,  PAONE DANIEL V ,  SHAW ANTHONY W ,  STUMP CRAIG A ,  WILLIAMS THERESA M

Inventor： BURGEY CHRISTOPHER S ,  PAONE DANIEL V ,  SHAW ANTHONY W ,  STUMP CRAIG A ,  WILLIAMS THERESA M

IPC: C07D401/14 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P25/06 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: Compounds of Formula (I): and Formula (II), where variables R 1 , R 2 , R 3 , R 4 , A, B, D, G, J, Q, T, W, X and Y 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, pharmaceutical compositions comprising these compounds, use of these compounds and compositions toprevent or treat diseases involving CGRP.

Abstract translation: 式（I）：和式（II）的化合物，其中R 1，R 2，R 3，R 4， A，B，D，G，J，Q，T，W，X和Y如本文所定义，可用作CGRP受体的拮抗剂，可用于治疗或预防涉及CGRP的疾病 ，包含这些化合物的药物组合物，这些化合物和组合物的用途，用于消除或治疗涉及CGRP的疾病。

公开(公告)号：WO2006031610A3

公开(公告)日：2006-03-23

申请号：PCT/US2005/032041

申请日：2005-09-09

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

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

IPC: C07D403/02 ,  C07D221/02 ,  C07D401/00 ,  C07D239/00 ,  C07D241/00 ,  A61K31/4965 ,  A61K31/44 ,  A61K31/517

Abstract: The present invention is directed to compounds of Formula (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.

公开(公告)号：WO2006031610A2

公开(公告)日：2006-03-23

申请号：PCT/US2005032041

申请日：2005-09-09

Applicant: MERCK & CO INC ,  BELL IAN M ,  THEBERGE CORY R ,  STUMP CRAIG A ,  ZHANG XUFANG ,  GALLICCHIO STEVEN N ,  ZARTMAN C BLAIR

Inventor： BELL IAN M ,  THEBERGE CORY R ,  STUMP CRAIG A ,  ZHANG XUFANG ,  GALLICCHIO STEVEN N ,  ZARTMAN C BLAIR

IPC: A61K31/4747

CPC classification number: C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D519/00 ,  Y02P20/582

Abstract: The present invention is directed to compounds of Formula (I): (where variables A

Abstract translation: 本发明涉及式（I）的化合物：（其中变量A