公开(公告)号：US07847100B2

公开(公告)日：2010-12-07

申请号：US11578559

申请日：2005-04-15

申请人： James C. Barrow ,  Georgia B. McGaughey ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Craig A. Coburn

发明人： James C. Barrow ,  Georgia B. McGaughey ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Craig A. Coburn

IPC分类号： A61K31/4245 ,  C07D271/10 ,  C07D271/06

CPC分类号： C07D271/10 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/62 ,  C07D271/06 ,  C07D285/12 ,  C07D307/14 ,  C07D307/42 ,  C07D307/44 ,  C07D307/52 ,  C07D307/54 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： The present invention is directed to 1,3,5-phenyl substituted 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1,3,5-苯基取代的衍生物化合物。 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。

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。

公开(公告)号：US20080153846A1

公开(公告)日：2008-06-26

申请号：US11795283

申请日：2006-01-13

申请人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

发明人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

IPC分类号： A61K31/496 ,  C07C211/00 ,  A61K31/13 ,  A61K31/4245 ,  A61P25/28 ,  C07D271/06 ,  C07D413/06

CPC分类号： C07D413/06 ,  C07D271/10

摘要： The present invention is directed to aminomethyl 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涉及β-分泌酶的疾病如阿尔茨海默氏病的氨基甲基化合物。 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。

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。

公开(公告)号：US07820674B2

公开(公告)日：2010-10-26

申请号：US11795283

申请日：2006-01-13

申请人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

发明人： Craig A. Coburn ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer

IPC分类号： A61K31/4245 ,  A61K31/496 ,  A61K31/454 ,  A61K31/5377 ,  C07D271/10 ,  C07D271/00 ,  C07D271/06 ,  C07D413/06

CPC分类号： C07D413/06 ,  C07D271/10

摘要： The present invention is directed to aminomethyl 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涉及β-分泌酶的疾病如阿尔茨海默氏病的氨基甲基化合物。 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。

公开(公告)号：US08114887B2

公开(公告)日：2012-02-14

申请号：US11663388

申请日：2005-10-12

申请人： James C. Barrow ,  Craig A. Coburn ,  Melissa S. Egbertson ,  Georgia B. McGaughey ,  Melody A. McWherter ,  Lou Anne Neilson ,  Kenneth E. Rittle ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： James C. Barrow ,  Craig A. Coburn ,  Melissa S. Egbertson ,  Georgia B. McGaughey ,  Melody A. McWherter ,  Lou Anne Neilson ,  Kenneth E. Rittle ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D411/02

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of 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： 本发明涉及作为β-分泌酶的抑制剂并且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式（I）的哌啶哌啶化合物。 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。

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。

公开(公告)号：US07354942B2

公开(公告)日：2008-04-08

申请号：US10578953

申请日：2004-11-19

申请人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Mary Beth Young

发明人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Shaun R. Stauffer ,  Mary Beth Young

IPC分类号： C07D213/02 ,  A61K31/44

CPC分类号： C07C255/46 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D207/06 ,  C07D213/76 ,  C07D295/192 ,  C07D401/06

摘要： The present invention is directed to benzylether and benzylamino derivative compounds of 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： 本发明涉及式（I）的苄基醚和苄基氨基衍生物化合物，其是β-分泌酶的抑制剂，其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。

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。

公开(公告)号：US07951949B2

公开(公告)日：2011-05-31

申请号：US11791465

申请日：2005-11-18

申请人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Keith P. Moore

发明人： Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Harold G. Selnick ,  Keith P. Moore

IPC分类号： C07D519/06 ,  A61K31/4353

CPC分类号： C07D491/08

摘要： The present invention is directed to macrocyclic aminopyridyl 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）表示的大环氨基吡啶基化合物，其是β-分泌酶的抑制剂，并且其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。