公开(公告)号：US07625901B2

公开(公告)日：2009-12-01

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： C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D471/04 ,  C07D519/00 ,  C07D471/20 ,  A61K31/499 ,  A61K31/4965 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/4188 ,  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：US20090054408A1

公开(公告)日：2009-02-26

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： A61K31/4747 ,  C07D471/20 ,  A61K31/551 ,  A61P25/00 ,  A61P25/06

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 CORP 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） 治疗或预防公司涉及的疾病，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：US06358985B1

公开(公告)日：2002-03-19

申请号：US09342577

申请日：1999-06-29

申请人： Neville J. Anthony ,  Ian M. Bell ,  Douglas C. Beshore ,  Terrence M. Ciccarone ,  S. Jane de Solms ,  Christopher J. Dinsmore ,  Gerald E. Stokker

发明人： Neville J. Anthony ,  Ian M. Bell ,  Douglas C. Beshore ,  Terrence M. Ciccarone ,  S. Jane de Solms ,  Christopher J. Dinsmore ,  Gerald E. Stokker

IPC分类号： A61K314164

CPC分类号： A61K31/4174 ,  A61K31/00

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：US06248756B1

公开(公告)日：2001-06-19

申请号：US09248883

申请日：1999-02-11

申请人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

发明人： Neville J. Anthony ,  Christopher Dinsmore ,  Robert P. Gomez ,  John H. Hutchinson ,  John S. Wai ,  Theresa M. Williams ,  Ian M. Bell ,  Mark W. Embrey ,  Thorsten E. Fisher

IPC分类号： A61K314468

CPC分类号： C07D401/06 ,  C07D211/62 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferas (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

摘要翻译： 本发明涉及抑制法尼基蛋白转移（Fatease-protein transferas，FTase）和致癌基因蛋白Ras的法呢基化的化合物。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。

公开(公告)号：US5718912A

公开(公告)日：1998-02-17

申请号：US736705

申请日：1996-10-28

申请人： Wayne J. Thomspon ,  Pierre Mallorga ,  Richard W. Ransom ,  Ian M. Bell ,  Michael F. Sugrue ,  Peter M. Munson

发明人： Wayne J. Thomspon ,  Pierre Mallorga ,  Richard W. Ransom ,  Ian M. Bell ,  Michael F. Sugrue ,  Peter M. Munson

IPC分类号： C07D401/04 ,  A61F2/00 ,  A01N43/40 ,  A61K31/445

CPC分类号： C07D401/04

摘要： This invention is concerned with novel 1-�cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.

摘要翻译： 本发明涉及新的1- [环烷基吡啶-4-基] -2H-苯并咪唑酮，其组合物和使用方法。 新型化合物是m2亚型的选择性毒蕈碱激动剂，在m3亚型下具有低活性。 该化合物对于治疗与毛果芸香碱治疗相比副作用较小的青光眼有效。

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。