公开(公告)号：US20120121508A1

公开(公告)日：2012-05-17

申请号：US13386955

申请日：2010-07-20

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

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

IPC分类号： A61K51/04 ,  A61P25/00 ,  C07D471/10

CPC分类号： C07D471/10 ,  C07B59/002 ,  C07D471/20

摘要： The present invention is directed to radiolabeled CGRP receptor antagonists which are useful for the quantitative imaging of CGRP receptors in mammals.

摘要翻译： 本发明涉及放射性标记的CGRP受体拮抗剂，其可用于哺乳动物中CGRP受体的定量成像。

公开(公告)号：US20110306604A1

公开(公告)日：2011-12-15

申请号：US13059164

申请日：2009-08-14

申请人： Michael R. Wood ,  Ian M. Bell ,  June J. Kim ,  Harold G. Selnick ,  Craig A. Stump

发明人： Michael R. Wood ,  Ian M. Bell ,  June J. Kim ,  Harold G. Selnick ,  Craig A. Stump

IPC分类号： A61K31/551 ,  A61K31/4545 ,  A61P25/00 ,  A61K31/437 ,  A61K31/496 ,  A61P25/06 ,  C07D471/20 ,  A61K31/499

CPC分类号： C07D471/20

摘要： Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are 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）的化合物（其中变量R1A，R1B，R2，R3，R4，A和Z如本文所定义），其可用作CGRP受体的拮抗剂，并且可用于治疗或预防CGRP 涉及受体，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：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：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：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：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：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。

公开(公告)号：US08507477B2

公开(公告)日：2013-08-13

申请号：US13059164

申请日：2009-08-14

申请人： Michael R. Wood ,  Ian M. Bell ,  June J. Kim ,  Harold G. Selnick ,  Craig A. Stump

发明人： Michael R. Wood ,  Ian M. Bell ,  June J. Kim ,  Harold G. Selnick ,  Craig A. Stump

IPC分类号： C07D487/10 ,  A61K31/55 ,  A61P25/06

CPC分类号： C07D471/20

摘要： Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are 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）的化合物（其中变量R1A，R1B，R2，R3，R4，A和Z如本文所定义），其可用作CGRP受体的拮抗剂，并且可用于治疗或预防CGRP 涉及受体，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：US08071771B2

公开(公告)日：2011-12-06

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： C07D211/00 ,  C07D401/00

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。