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：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。

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：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：US20110034483A1

公开(公告)日：2011-02-10

申请号：US12919277

申请日：2009-02-18

申请人： Ivory D. Hills ,  Craig A. Coburn ,  Samuel L. Graham ,  Keith P. Moore ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Shawn J. Stachel ,  Hong Zhu

发明人： Ivory D. Hills ,  Craig A. Coburn ,  Samuel L. Graham ,  Keith P. Moore ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Shawn J. Stachel ,  Hong Zhu

IPC分类号： A61K31/506 ,  C07D233/88 ,  A61K31/4174 ,  C07D403/10 ,  A61K31/4178 ,  C07D403/06 ,  C07D413/10 ,  A61K31/42 ,  C07D401/10 ,  A61K31/4439 ,  A61K31/422 ,  A61P25/28

CPC分类号： C07D233/88 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10

摘要： The present invention is directed to 2-aminoimidazole 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-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。 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：US08492387B2

公开(公告)日：2013-07-23

申请号：US12919277

申请日：2009-02-18

申请人： Ivory D. Hills ,  Craig A. Coburn ,  Samuel L. Graham ,  Keith P. Moore ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Shawn J. Stachel ,  Hong Zhu

发明人： Ivory D. Hills ,  Craig A. Coburn ,  Samuel L. Graham ,  Keith P. Moore ,  Philippe G. Nantermet ,  Hemaka A. Rajapakse ,  Shawn J. Stachel ,  Hong Zhu

IPC分类号： A61K31/506 ,  A61K31/42 ,  A61K31/4174 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/422 ,  C07D233/88 ,  C07D403/10 ,  C07D403/06 ,  C07D413/10 ,  C07D401/10

CPC分类号： C07D233/88 ,  C07D401/04 ,  C07D401/06 ,  C07D401/08 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10

摘要： The present invention is directed to 2-aminoimidazole 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-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。 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：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。

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：US08211904B2

公开(公告)日：2012-07-03

申请号：US11487229

申请日：2006-07-14

申请人： Craig A. Coburn ,  Melissa S. Egbertson ,  Samuel L. Graham ,  Georgia B. McGaughey ,  Shaun R. Stauffer ,  Hemaka A. Rajapakse ,  Philippe G. Nantermet ,  Shawn J. Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Craig A. Coburn ,  Melissa S. Egbertson ,  Samuel L. Graham ,  Georgia B. McGaughey ,  Shaun R. Stauffer ,  Hemaka A. Rajapakse ,  Philippe G. Nantermet ,  Shawn J. Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, 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）的螺哌啶化合物及其互变异构体，其是β-分泌酶的抑制剂，并且其可用于治疗涉及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：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。