公开(公告)号：US08754096B2

公开(公告)日：2014-06-17

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： A61K31/4545 ,  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：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：US08148390B2

公开(公告)日：2012-04-03

申请号：US12530898

申请日：2008-03-07

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

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

IPC分类号： A61K31/513 ,  A61K31/4184 ,  A61K31/437 ,  A61P25/06 ,  C07D403/12 ,  C07D471/10 ,  C07D491/107 ,  C07D471/20

CPC分类号： C07D471/20 ,  C07D403/12 ,  C07D471/10 ,  C07D519/00

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。

公开(公告)号：US20110224201A1

公开(公告)日：2011-09-15

申请号：US13121784

申请日：2009-09-29

申请人： Donnette D. Staas ,  Ian M. Bell ,  Harold G. Selnick

发明人： Donnette D. Staas ,  Ian M. Bell ,  Harold G. Selnick

IPC分类号： A61K31/537 ,  C07D498/20 ,  C07D498/04 ,  A61P25/06 ,  A61P25/00

CPC分类号： C07D498/20 ,  C07D498/04 ,  C07D498/10

摘要： Compounds of Formula (I), (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, L, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG, W, Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular 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 receptors are involved.

摘要翻译： 式（I）化合物（其中变量A1，A2，A3，A4，A5，A6，A7，A8，L，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf， W，Y和Z如本文所述）可用作CGRP受体的拮抗剂，并且可用于治疗或预防涉及CGRP受体的疾病，例如头痛，特别是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受体的疾病中的用途。

公开(公告)号：US07989624B2

公开(公告)日：2011-08-02

申请号：US11662424

申请日：2005-09-06

申请人： Ian M. Bell ,  Craig A. Stump ,  Cory R. Theberge

发明人： Ian M. Bell ,  Craig A. Stump ,  Cory R. Theberge

IPC分类号： A61K31/438 ,  C07D401/14 ,  C07D209/54 ,  C07D209/04

CPC分类号： C07D209/96 ,  C07D471/04 ,  C07D487/04

摘要： The present invention is directed to compounds of Formula (I): where variables A1, A2, B, J, K, m, n, R4, R5a, R5b, R5c and X 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）的化合物：其中变量A1，A2，B，J，K，m，n，R4，R5a，R5b，R5c和X如本文所定义，可用作CGRP受体的拮抗剂， 在治疗或预防涉及CGRP的疾病中，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：US07947677B2

公开(公告)日：2011-05-24

申请号：US12085054

申请日：2006-11-14

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

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

IPC分类号： C07D403/06 ,  C07D401/06 ,  A61K31/55 ,  A61K31/4985 ,  A61K31/4355 ,  A61K31/395 ,  A61P25/06

CPC分类号： C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, 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.

摘要翻译： 式I化合物（其中变量A1，A2，A3，A4，A5，A6，A7，B1，B2，B3，B4，D1，D2，E1，E2，E3，E4，E5，G1，G2， K，T，U，V，W，X，Y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，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：US20100324023A1

公开(公告)日：2010-12-23

申请号：US12867332

申请日：2009-02-06

申请人： Howard G. Selnick ,  Ian M. Bell

发明人： Howard G. Selnick ,  Ian M. Bell

IPC分类号： A61K31/55 ,  C07D487/14 ,  C07D498/20 ,  A61P25/06

CPC分类号： C07D519/00 ,  C07D487/14

摘要： Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular 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 receptors are involved.

摘要翻译： 式I化合物（其中变量R1A，R1B，R2，R3，R4，A和Z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受体的疾病 ，如头痛，尤其是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受体的疾病中的用途。

公开(公告)号：US20100152216A1

公开(公告)日：2010-06-17

申请号：US12530898

申请日：2008-03-07

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

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

IPC分类号： A61K31/513 ,  C07D403/12 ,  A61K31/4184 ,  C07D471/10 ,  A61K31/437 ,  A61P25/06 ,  C07D491/107 ,  C07D471/20

CPC分类号： C07D471/20 ,  C07D403/12 ,  C07D471/10 ,  C07D519/00

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。

公开(公告)号：US07659300B2

公开(公告)日：2010-02-09

申请号：US11660821

申请日：2005-09-06

申请人： Ian M. Bell ,  Craig A. Stump

发明人： Ian M. Bell ,  Craig A. Stump

IPC分类号： A61K31/4015 ,  C07D209/54

CPC分类号： C07D471/04 ,  C07D209/96 ,  C07D487/04

摘要： The present invention is directed to compounds of Formula I: I (where 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： 本发明涉及用作CGRP受体的拮抗剂的式I化合物：其中A1（A2，B，J，K，m，n，R4，R5a，R5b和R5c如本文所定义） 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。

公开(公告)号：US20090325991A1

公开(公告)日：2009-12-31

申请号：US12085131

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： A61K31/437 ,  C07D471/04 ,  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, B, 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，B，E1，E2，E3，E4，E5，G1，G2，J和K如本文所述） CGRP受体，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。