公开(公告)号：US20070088165A1

公开(公告)日：2007-04-19

申请号：US10578953

申请日：2004-11-19

申请人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Mary Beth Young

发明人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Mary Beth Young

IPC分类号： C07D213/56 ,  C07D213/57 ,  C07C255/29

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：US20080015233A1

公开(公告)日：2008-01-17

申请号：US11547994

申请日：2005-04-20

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

IPC分类号： A61K31/4439 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

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：US20070293497A1

公开(公告)日：2007-12-20

申请号：US11791204

申请日：2005-11-18

申请人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  James Barrow ,  Shaun Stauffer ,  Joseph Vacca ,  Keith Moore ,  Shawn Stachel ,  Mattahew Stanton

发明人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  James Barrow ,  Shaun Stauffer ,  Joseph Vacca ,  Keith Moore ,  Shawn Stachel ,  Mattahew Stanton

IPC分类号： A61K31/44 ,  A61K31/497 ,  A61K31/5377 ,  A61P25/28 ,  C07D413/14

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：US20070244119A1

公开(公告)日：2007-10-18

申请号：US11578559

申请日：2005-04-15

申请人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

发明人： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Craig Coburn

IPC分类号： A61K31/4245 ,  A61K31/341 ,  A61K31/433 ,  A61K31/5377 ,  C07D263/30 ,  C07D285/12 ,  C07D413/04 ,  C07D307/02 ,  C07D271/10 ,  C07D253/02 ,  A61K31/4418 ,  A61K31/421

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：US20060293380A1

公开(公告)日：2006-12-28

申请号：US10573232

申请日：2004-09-29

申请人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick

发明人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick

IPC分类号： A61K31/4025 ,  A61K31/381 ,  A61K31/18

CPC分类号： C07D213/81 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07D207/06 ,  C07D207/08 ,  C07D213/76 ,  C07D295/192 ,  C07D333/20 ,  C07D405/04

摘要： The present invention is directed to 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-分泌酶的抑制剂的式（I）化合物，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：US20080015213A1

公开(公告)日：2008-01-17

申请号：US11791465

申请日：2005-11-18

申请人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Keith Moore

发明人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Keith Moore

IPC分类号： A61K31/4353 ,  A61P25/28 ,  C07D221/06 ,  C07D267/00

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：US20060149092A1

公开(公告)日：2006-07-06

申请号：US10562470

申请日：2004-06-25

申请人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick

发明人： Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick

IPC分类号： C07C255/50 ,  C07C309/51

CPC分类号： C07D207/08 ,  C07C233/66 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07D207/06 ,  C07D295/192 ,  C07D401/04

摘要： The present invention is directed to 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 prevention or 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预防或治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070142634A1

公开(公告)日：2007-06-21

申请号：US10582856

申请日：2004-12-15

申请人： James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

发明人： James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

IPC分类号： A61K31/5377 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  C07D213/72

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：US20070197571A1

公开(公告)日：2007-08-23

申请号：US11663388

申请日：2005-10-12

申请人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： James Barrow ,  Craig Coburn ,  Melissa Egbertson ,  Georgia McGaughey ,  Melody McWherter ,  Lou Neilson ,  Kenneth Rittle ,  Harold Selnick ,  Shaun Stauffer ,  Zhi-Qiang Yang ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

IPC分类号： A61K31/4747 ,  C07D471/10

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：US20170119912A1

公开(公告)日：2017-05-04

申请号：US15317333

申请日：2015-06-09

申请人： Abbas W. Walji ,  Eric Hostetler ,  Thomas J. Greshock ,  Jing Li ,  Keith P. Moore ,  Idriss Bennacef ,  James Mulhearn ,  Harold Selnick ,  Yaode Wang ,  Kun Yang ,  Jianmin Fu ,  MERCK SHARP & DOHME CORP.

发明人： Abbas W. Walji ,  Eric Hostetler ,  Thomas J. Greshock ,  Jing Li ,  Keith P. Moore ,  Idriss Bennacef ,  James Mulhearn ,  Harold Selnick ,  Yaode Wang ,  Kun Yang ,  Jianmin Fu

IPC分类号： A61K51/04 ,  C07D519/00 ,  C07D471/04

CPC分类号： A61K51/0455 ,  A61K51/0459 ,  C07B2200/05 ,  C07D471/04 ,  C07D519/00

摘要： The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.