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：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：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：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：US20070021454A1

公开(公告)日：2007-01-25

申请号：US11487229

申请日：2006-07-14

申请人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  Wenjin Yang ,  Wanli Lu ,  Bruce Fahr

发明人： Craig Coburn ,  Melissa Egbertson ,  Samuel Graham ,  Georgia McGaughey ,  Shaun Stauffer ,  Hemaka Rajapakse ,  Philippe Nantermet ,  Shawn Stachel ,  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) 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：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：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：US20110183980A1

公开(公告)日：2011-07-28

申请号：US12886950

申请日：2010-09-21

申请人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Shaun Stauffer ,  Richard Williams ,  Gregor MacDonald ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda

发明人： P. Jeffrey Conn ,  Craig W. Lindsley ,  Charles David Weaver ,  Shaun Stauffer ,  Richard Williams ,  Gregor MacDonald ,  Ya Zhou ,  José Manuel Bartolomé-Nebreda

IPC分类号： A61K31/5377 ,  C07D213/62 ,  C07D213/78 ,  C07D401/12 ,  C07D417/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/444 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/506 ,  A61P25/00

CPC分类号： A61K31/44 ,  C07D213/80 ,  C07D213/85 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

摘要翻译： 一方面，本发明涉及O-苄基烟酰胺类似物，其衍生物和相关化合物，其可用作代谢型谷氨酸受体亚型5（mGluR5）的阳性变构调节剂; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与谷氨酸官能障碍相关的神经和精神障碍的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。