公开(公告)号：US06410534B1

公开(公告)日：2002-06-25

申请号：US09347673

申请日：1999-06-29

申请人： Christopher J. Dinsmore ,  Ian M. Bell ,  Douglas C. Beshore ,  Theresa M. Williams

发明人： Christopher J. Dinsmore ,  Ian M. Bell ,  Douglas C. Beshore ,  Theresa M. Williams

IPC分类号： A61K314188

CPC分类号： C07D498/04 ,  A61K31/415 ,  A61K31/335 ,  A61K2300/00

摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

公开(公告)号：US5691323A

公开(公告)日：1997-11-25

申请号：US440153

申请日：1995-05-12

申请人： Wayne J. Thompson ,  Michael F. Sugrue ,  Richard W. Ransom ,  Pierre J. Mallorga ,  Ian M. Bell ,  Anthony M. Smith

发明人： Wayne J. Thompson ,  Michael F. Sugrue ,  Richard W. Ransom ,  Pierre J. Mallorga ,  Ian M. Bell ,  Anthony M. Smith

IPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/38 ,  A61K31/34 ,  C07D403/14

CPC分类号： C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Compounds, 1,3-dihydro-1-{1-�piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

摘要翻译： 化合物，1,3-二氢-1- {1- [哌啶-4-基]哌啶-4-基} -2H-苯并咪唑-2-酮和1,3-二氢-1- {4-氨基-1- 环己基} -2H-苯并咪唑-2-酮及其衍生物，其制备方法，使用方法和药物组合物。 这些化合物具有抗毒蕈碱活性，可用于治疗和/或预防近视（俗称近视）。

公开(公告)号：US08685965B2

公开(公告)日：2014-04-01

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

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：US20140011827A1

公开(公告)日：2014-01-09

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

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.

公开(公告)号：US20140005214A1

公开(公告)日：2014-01-02

申请号：US14005595

申请日：2012-03-14

申请人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Helen J. Mitchell ,  Cheng Wang

发明人： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Helen J. Mitchell ,  Cheng Wang

IPC分类号： C07D401/12

CPC分类号： C07D401/12 ,  A61K31/445

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：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。

公开(公告)号：US07968540B2

公开(公告)日：2011-06-28

申请号：US12085008

申请日：2006-11-14

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

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

IPC分类号： A61K31/55 ,  C07D243/04 ,  C07D487/10

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, R6, 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， 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：US07893079B2

公开(公告)日：2011-02-22

申请号：US12614726

申请日：2009-11-09

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： C07D401/12 ,  A61K31/4355 ,  A61P25/06

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, A3, 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，A3，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：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。