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1.发明授权2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease 有权用作治疗阿尔茨海默病的β-分泌酶抑制剂的2,4,6-取代的吡啶基衍生物化合物公开(公告)号：US07968571B2
公开(公告)日：2011-06-28
申请号：US11547994
申请日：2005-04-20
申请人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
发明人： James C. Barrow , Georgia B. McGaughey , Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Shaun R. Stauffer , Joseph P. Vacca , Shawn J. Stachel , Craig A. Coburn , Matthew G. Stanton
IPC分类号： A61K31/443 , C07D413/04
CPC分类号： C07D413/04 , C07D401/04 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的2,4,6-取代的吡啶衍生物化合物。 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治疗涉及β-分泌酶的疾病中的用途。
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2.发明授权N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的N-烷基苯基卡巴酰胺β-分泌酶抑制剂公开(公告)号：US07291620B2
公开(公告)日：2007-11-06
申请号：US10563538
申请日：2004-06-25
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/40 , A61K31/279 , A61K31/16
CPC分类号： C07C237/10 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/14 , C07D211/38 , C07D295/084 , C07D295/185
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗或预防涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 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治疗涉及β-分泌酶的疾病中的用途。
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3.发明授权2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease 有权用作治疗阿尔茨海默氏病的β-分泌酶抑制剂的2,3,4,6-取代的吡啶衍生物化合物公开(公告)号：US08394837B2
公开(公告)日：2013-03-12
申请号：US11791204
申请日：2005-11-18
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , James C. Barrow , Shaun R. Stauffer , Joseph P. Vacca , Keith P. Moore , Shawn J. Stachel , Mattahew G. Stanton
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及2,3,4,6-取代的吡啶基衍生物化合物，其是β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病，例如阿尔茨海默病 。 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治疗涉及β-分泌酶的疾病中的用途。
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4.发明授权Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权苯酰胺和吡啶酰胺β-分泌酶抑制剂治疗阿尔茨海默病公开(公告)号：US07550481B2
公开(公告)日：2009-06-23
申请号：US10582856
申请日：2004-12-15
申请人： James C. Barrow , Craig A. Coburn , Philippe G. Nantermet , Harold G. Selnick , Shawn J. Stachel , Matthew G. Stanton , Shaun R. Stauffer , Linghang Zhuang , Jennifer R. Davis
发明人： James C. Barrow , Craig A. Coburn , Philippe G. Nantermet , Harold G. Selnick , Shawn J. Stachel , Matthew G. Stanton , Shaun R. Stauffer , Linghang Zhuang , Jennifer R. Davis
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07D213/81 , C07D213/75 , C07D257/04 , C07D401/04 , C07D409/12 , C07D413/12
摘要： The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及苯酰胺和吡啶酰胺衍生物化合物，其是β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US20110021516A1
公开(公告)日：2011-01-27
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： A61K31/5365 , C07D471/04 , A61K31/496 , A61P25/06
CPC分类号： C07D471/10 , C07D403/06 , C07D471/20 , C07D519/00
摘要： The present invention is directed to compounds of the formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, G1, G2, G3, G4, J, Q, Ea, Eb, Ec, R6, R7, 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 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： 本发明涉及式（I）的化合物：（其中变量A1，A2，A3，A4，A5，A6，A7，A8，G1，G2，G3，G4，J，Q，Ea，Eb，Ec ，R6，R7，RPG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，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。
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6.发明申请Macrocyclic Tertiary Amine Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease 有权用于治疗阿尔茨海默病的大环叔胺β-分泌酶抑制剂公开(公告)号：US20080269302A1
公开(公告)日：2008-10-30
申请号：US11667913
申请日：2005-11-14
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
IPC分类号： A61K31/365 , C07D267/00 , C07D313/00 , A61K31/395 , A61P25/28 , C07D498/00 , C07D321/00
CPC分类号： C07D273/01 , C07D267/00 , C07D313/00 , C07D321/00 , C07D323/00 , C07D413/04 , C07D498/08
摘要： The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及由通式（I）表示的大环叔胺化合物，其为β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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治疗涉及β-分泌酶的疾病中的用途。
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7.发明申请公开(公告)号：US20110190329A1
公开(公告)日：2011-08-04
申请号：US13059361
申请日：2009-08-11
IPC分类号： A61K31/437 , C07D471/10 , C07D471/20 , C07D235/02 , A61K31/4184 , A61P29/00 , A61P25/06 , A61P9/12 , A61P25/08
CPC分类号： C07D471/04 , C07D235/02 , C07D471/20
摘要： The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and 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： 本发明涉及具有支链末端衍生物的新型非酰胺接头，其为CGRP受体的拮抗剂，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。
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8.发明授权Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease 有权用于治疗阿尔茨海默病的大环叔胺β-分泌酶抑制剂公开(公告)号：US07678783B2
公开(公告)日：2010-03-16
申请号：US11667913
申请日：2005-11-14
申请人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
发明人： Philippe G. Nantermet , Hemaka A. Rajapakse , Harold G. Selnick , Stacey Lindsley , Keith P. Moore , Shawn J. Stachel
IPC分类号： A01N43/00 , A61K31/33 , C07D513/00
CPC分类号： C07D273/01 , C07D267/00 , C07D313/00 , C07D321/00 , C07D323/00 , C07D413/04 , C07D498/08
摘要： The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及由通式（I）表示的大环叔胺化合物，其为β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 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治疗涉及β-分泌酶的疾病中的用途。
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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。
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10.发明授权公开(公告)号：US08552023B2
公开(公告)日：2013-10-08
申请号：US13059361
申请日：2009-08-11
IPC分类号： A61K31/437 , C07D471/10 , C07D471/20 , A61P29/00 , A61P25/06 , A61P9/12
CPC分类号： C07D471/04 , C07D235/02 , C07D471/20
摘要： The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and 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： 本发明涉及具有支链末端衍生物的新型非酰胺接头，其为CGRP受体的拮抗剂，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。
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