公开(公告)号：US08080544B2

公开(公告)日：2011-12-20

申请号：US12864120

申请日：2009-02-04

申请人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

发明人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

IPC分类号： A61K31/55 ,  A61P25/06 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07F9/6561

摘要： Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are 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.

摘要翻译： 公开了式（I）的前药化合物（其中变量R 1和R 2如本文所述），其是CGRP受体的拮抗剂的类似物，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：US20100298269A1

公开(公告)日：2010-11-25

申请号：US12864120

申请日：2009-02-04

申请人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

发明人： Ian M. Bell ,  Steven N. Gallicchio ,  Valentino J. Stella

IPC分类号： A61K31/675 ,  C07F9/6561 ,  A61P29/00 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P19/02 ,  A61P17/00

CPC分类号： C07D471/04 ,  C07F9/6561

摘要： Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are 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.

摘要翻译： 公开了式（I）的前药化合物（其中变量R 1和R 2如本文所述），其是CGRP受体的拮抗剂的类似物，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：US08912210B2

公开(公告)日：2014-12-16

申请号：US13293177

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/02

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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.

公开(公告)号：US20130231358A1

公开(公告)日：2013-09-05

申请号：US13884632

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  Blair C. Zartman ,  Heather E. Stevenson

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  Blair C. Zartman ,  Heather E. Stevenson

IPC分类号： C07D471/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  A61K31/506 ,  C07D487/04

摘要： The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and 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.

摘要翻译： 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺二氢化茚衍生物，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：US20120122899A1

公开(公告)日：2012-05-17

申请号：US13293166

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Heather E. Stevenson ,  Cheng Wang ,  C. Blair Zartman

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Heather E. Stevenson ,  Cheng Wang ,  C. Blair Zartman

IPC分类号： A61K31/439 ,  A61K31/527 ,  A61P25/06 ,  C07D471/20

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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.

摘要翻译： 本发明涉及作为CGRP受体的拮抗剂的哌啶酮羧酰胺氮杂茚衍生物，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：US08133891B2

公开(公告)日：2012-03-13

申请号：US12718386

申请日：2010-03-05

申请人： Ian M. Bell ,  Steven N. Gallicchio ,  Craig A. Stump ,  Cory R. Theberge ,  Joseph P. Vacca ,  C. Blair Zartman ,  Xufang Zhang

发明人： Ian M. Bell ,  Steven N. Gallicchio ,  Craig A. Stump ,  Cory R. Theberge ,  Joseph P. Vacca ,  C. Blair Zartman ,  Xufang Zhang

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495

CPC分类号： C07D519/00 ,  C07D209/96 ,  C07D471/06 ,  C07D471/16 ,  C07D487/06

摘要： The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are 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.

摘要翻译： 本发明涉及式I化合物：其中A1，A2，B1，B2，B3，B4，D1，D2，J，K，T，U，V，W，X，Y，Z， R5a，R5b，R5c，m和n在本文中定义），其可用作CGRP受体的拮抗剂，并且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：US20090247514A1

公开(公告)日：2009-10-01

申请号：US12085057

申请日：2006-11-14

申请人： Ian M. Bell ,  Harold G. Selnick ,  Michael R. Wood ,  Cory R. Theberge ,  Craig A. Stump ,  Steven N. Gallicchio ,  C. Blair Zartman

发明人： Ian M. Bell ,  Harold G. Selnick ,  Michael R. Wood ,  Cory R. Theberge ,  Craig A. Stump ,  Steven N. Gallicchio ,  C. Blair Zartman

IPC分类号： A61K31/5377 ,  C07D471/10 ,  A61K31/438 ,  A61K31/497 ,  A61P25/00

CPC分类号： C07D471/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, 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.

摘要翻译： 式I化合物（其中变量A1，A2，A3，A4，A5，A6，A7，E1，E2，E3，E4，E5，G1，G2，J和K如本文所述），其是CGRP受体的拮抗剂 并且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：US20080318927A1

公开(公告)日：2008-12-25

申请号：US12214460

申请日：2008-06-19

申请人： Michael R. Wood ,  Steven N. Gallicchio ,  Harold G. Selnick ,  C. Blair Zartman ,  Ian M. Bell ,  Craig A. Stump

发明人： Michael R. Wood ,  Steven N. Gallicchio ,  Harold G. Selnick ,  C. Blair Zartman ,  Ian M. Bell ,  Craig A. Stump

IPC分类号： A61K31/551 ,  A61K31/454 ,  C07D401/12 ,  A61K31/541 ,  A61P25/06 ,  A61K31/501 ,  A61K31/496 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, A2, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG 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.

摘要翻译： 式I化合物（其中变量A1，A2，A2，A4，m，n，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf，RPG和Y如本文所述） 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：US20120122900A1

公开(公告)日：2012-05-17

申请号：US13293177

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC分类号： A61K31/437 ,  A61K31/527 ,  A61P25/06 ,  C07D471/20

CPC分类号： A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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.

公开(公告)号：US08003792B2

公开(公告)日：2011-08-23

申请号：US11662703

申请日：2005-09-09

申请人： Ian M. Bell ,  Cory R. Theberge ,  Craig A. Stump ,  Xufang Zhang ,  Steven N. Gallicchio ,  C. Blair Zartman

发明人： Ian M. Bell ,  Cory R. Theberge ,  Craig A. Stump ,  Xufang Zhang ,  Steven N. Gallicchio ,  C. Blair Zartman

IPC分类号： A61K31/40 ,  A61K31/438 ,  C07D401/04 ,  C07D227/02

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

摘要： The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c 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.

摘要翻译： 本发明涉及式I化合物（其中变量A1，A2，B，J，K，m，n，R4，R5a，R5b和R5c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。