公开(公告)号：US20220396571A1

公开(公告)日：2022-12-15

申请号：US17771527

申请日：2020-10-29

申请人： Ian M. BELL ,  Brendan M. CROWLEY ,  Philippe NANTERMET ,  Merck Sharp & Dohme Corp.

发明人： Ian M. Bell ,  Brendan M. Crowley ,  Phillippe Nantermet

IPC分类号： C07D417/08 ,  A61K31/454 ,  C07D413/14 ,  C07D401/14 ,  A61K31/4545 ,  A61K31/506

摘要： The present disclosure relates to compounds of formula (I) that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.

公开(公告)号：US20200262826A1

公开(公告)日：2020-08-20

申请号：US16646616

申请日：2018-09-14

申请人： Ian M. BELL ,  Brendan M. CROWLEY ,  Peter J. MANLEY ,  William D. SHIPE ,  Merck Sharp & Dohme Corp.

发明人： Ian M. Bell ,  Brendan M. Crowley ,  Peter J. Manley ,  William D. Shipe

IPC分类号： C07D413/08 ,  C07D413/14 ,  C07D417/08 ,  C07D417/14 ,  A61P25/28 ,  A61P25/16 ,  A61P25/18

摘要： The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).

公开(公告)号：US08796260B2

公开(公告)日：2014-08-05

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 ,  C07D487/12

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：US08765759B2

公开(公告)日：2014-07-01

申请号：US12934208

申请日：2009-03-24

申请人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

发明人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

IPC分类号： A61K31/437 ,  A61K31/497 ,  A61K31/4985

CPC分类号： C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

摘要： The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, 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 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： 本发明涉及下式的化合物：其中作为拮抗剂的式（其中变量A1，A2，A3，G1，G2，G3，G4，J，Ea，Eb，Ec，R6，R7和Y如本文所述） 的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：US08362005B2

公开(公告)日：2013-01-29

申请号：US13062540

申请日：2009-08-31

申请人： Ian M. Bell ,  Howard G. Selnick

发明人： Ian M. Bell ,  Howard G. Selnick

IPC分类号： C07D403/14 ,  C07D409/14 ,  C07D401/14 ,  A61K31/553 ,  A61K31/537 ,  A61P25/00 ,  A61P25/06

CPC分类号： C07D471/04 ,  C07D417/14 ,  C07D471/10

摘要： Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, 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B，m，n，J，R4，Ea，Eb，Ec，Re，Rf，RPb和Ec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：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：US08173655B2

公开(公告)日：2012-05-08

申请号：US12595874

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： A61K31/438 ,  A61K31/498

CPC分类号： C07D471/20 ,  C07D519/00

摘要： Compounds of formula I: (wherein variables A1, A2, B, m, n, J, 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，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 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：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：US20110245240A1

公开(公告)日：2011-10-06

申请号：US13122769

申请日：2009-09-30

申请人： Donnette D. Staas ,  Ian M. Bell ,  Michael R. Wood

发明人： Donnette D. Staas ,  Ian M. Bell ,  Michael R. Wood

IPC分类号： A61K31/538 ,  C07D491/20 ,  C07D471/04 ,  C07D491/107 ,  A61K31/499 ,  A61K31/437 ,  A61K31/438 ,  A61P25/00 ,  A61P25/06

CPC分类号： A61K31/00 ,  C07D471/10 ,  C07D491/107 ,  C07D491/20

摘要： Compounds of Formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and 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）的化合物（其中变量A1，A2，A3，A4，A5，A6，A7，A8，J，Q，R4，Ea，Eb，Ec，R6，R7，Re，Rf，RPG和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：US07951795B2

公开(公告)日：2011-05-31

申请号：US12517674

申请日：2007-12-05

申请人： Ian M. Bell ,  Harold G. Selnick

发明人： Ian M. Bell ,  Harold G. Selnick

IPC分类号： C07D521/00 ,  A61K31/5517 ,  A61P25/06

CPC分类号： C07D487/04

摘要： Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 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，G1，G2，G3，J，m，n，p，R1，R2，R3，R4和Y如本文所述），其是CGRP受体的拮抗剂， 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。