公开(公告)号：US20090176757A1

公开(公告)日：2009-07-09

申请号：US12085005

申请日：2006-11-14

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

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

IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4747

CPC分类号： C07D487/10 ,  C07D471/10

摘要： Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 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，B，E1，E2，E3，E4，E5，G1，G2和R6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：US20080214511A1

公开(公告)日：2008-09-04

申请号：US11662246

申请日：2005-09-06

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

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

IPC分类号： A61K31/437 ,  C07D471/06 ,  C07D487/06 ,  A61P25/00 ,  A61K31/55 ,  A61K31/53 ,  A61K31/4985 ,  A61K31/616 ,  A61K31/5415

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A 1，A 2，B 1，B 2， B，S 4，B 4，D 1，D 2，J，K，T， U，V，W，X，Y，Z，R 4，R 5a，R 5b，R 5c， >，m和n在本文中定义）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：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：US20120122911A1

公开(公告)日：2012-05-17

申请号：US13293186

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley

发明人： Ian M. Bell ,  Mark E. Fraley

IPC分类号： A61K31/438 ,  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：US08481556B2

公开(公告)日：2013-07-09

申请号：US13293186

申请日：2011-11-10

申请人： Ian M. Bell ,  Mark E. Fraley

发明人： Ian M. Bell ,  Mark E. Fraley

IPC分类号： C07D471/14 ,  C07D471/20 ,  A61K31/438 ,  A61P25/06

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：US09409916B2

公开(公告)日：2016-08-09

申请号：US14005673

申请日：2012-03-14

申请人： Ian M. Bell ,  Justin Belardi

发明人： Ian M. Bell ,  Justin Belardi

IPC分类号： C07D487/10 ,  C07D471/10

CPC分类号： C07D487/10 ,  C07D471/10

摘要： The present invention is directed to piperidinone carboxamide spirohydantoin 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甲酰胺螺乙内酰脲衍生物，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：US08143266B2

公开(公告)日：2012-03-27

申请号：US12595704

申请日：2008-04-11

申请人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump

发明人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump

IPC分类号： A61K31/437 ,  C07D221/20

CPC分类号： C07D471/20

摘要： Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, 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.

摘要翻译： 式I化合物（其中变量A1，A2，B，m，n，J，X，R4，G1，G2，G3和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或 预防CGRP涉及的疾病，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：US20120065190A1

公开(公告)日：2012-03-15

申请号：US12520146

申请日：2007-12-14

申请人： Ian M. Bell ,  Harold G. Selnick

发明人： Ian M. Bell ,  Harold G. Selnick

IPC分类号： A61K31/55 ,  C07D487/04 ,  A61P25/08 ,  A61P25/06 ,  A61P9/12 ,  C07D519/00 ,  A61P29/00

CPC分类号： C07D487/04 ,  A61K31/55 ,  A61K45/06 ,  C07D471/10 ,  C07D471/20 ,  C07D498/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 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.

摘要翻译： 式I化合物（其中变量A1，m，R1，R2，R3，R4和Z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， 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：US20100120809A1

公开(公告)日：2010-05-13

申请号：US12595704

申请日：2008-04-11

申请人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump

发明人： Ian M. Bell ,  Harold G. Selnick ,  Craig A. Stump

IPC分类号： A61K31/437 ,  C07D221/20 ,  A61P25/06

CPC分类号： C07D471/20

摘要： Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, 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.

摘要翻译： 式I化合物（其中变量A1，A2，B，m，n，J，X，R4，G1，G2，G3和Y如本文所述），其是CGRP受体的拮抗剂，其可用于治疗或 预防CGRP涉及的疾病，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。