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：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：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：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：US20120202852A1

公开(公告)日：2012-08-09

申请号：US13500097

申请日：2010-10-25

申请人： James Barrow ,  Kelly-Ann Schlegel ,  Yoheng Shu ,  Zhi-Qiang Yang

发明人： James Barrow ,  Kelly-Ann Schlegel ,  Yoheng Shu ,  Zhi-Qiang Yang

IPC分类号： A61K31/4439 ,  C07D249/04 ,  A61K31/4192 ,  C07D277/30 ,  A61K31/426 ,  C07D263/34 ,  A61K31/421 ,  C07D257/04 ,  A61K31/41 ,  C07D413/04 ,  A61P25/08 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/22 ,  A61P25/30 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D233/64 ,  C07D249/04 ,  C07D257/04 ,  C07D263/32 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14

摘要： The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.

摘要翻译： 本发明涉及作为T型钙通道拮抗剂的杂环酰胺化合物，其可用于治疗或预防涉及T型钙通道的疾病和疾病。 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预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US08987310B2

公开(公告)日：2015-03-24

申请号：US13500097

申请日：2010-10-25

申请人： James Barrow ,  Kelly-Ann Schlegel ,  Yoheng Shu ,  Zhi-Qiang Yang

发明人： James Barrow ,  Kelly-Ann Schlegel ,  Yoheng Shu ,  Zhi-Qiang Yang

IPC分类号： C07D401/12 ,  A61K31/4439 ,  C07D401/06 ,  C07D233/64 ,  C07D249/04 ,  C07D257/04 ,  C07D271/10 ,  C07D277/28 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14 ,  C07D263/32

CPC分类号： C07D401/06 ,  C07D233/64 ,  C07D249/04 ,  C07D257/04 ,  C07D263/32 ,  C07D271/10 ,  C07D271/113 ,  C07D277/28 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14

摘要： The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.

摘要翻译： 本发明涉及作为T型钙通道拮抗剂的杂环酰胺化合物，其可用于治疗或预防涉及T型钙通道的疾病和疾病。 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预防或治疗涉及T型钙通道的疾病中的用途。

公开(公告)号：US06387911B1

公开(公告)日：2002-05-14

申请号：US09717566

申请日：2000-11-21

申请人： Christopher Burgey ,  Richard C. Isaacs ,  Bruce D. Dorsey ,  Kyle A. Robinson ,  Donnette Staas ,  Philip E. Sanderson ,  James Barrow

发明人： Christopher Burgey ,  Richard C. Isaacs ,  Bruce D. Dorsey ,  Kyle A. Robinson ,  Donnette Staas ,  Philip E. Sanderson ,  James Barrow

IPC分类号： A61K31497

CPC分类号： C07D401/12 ,  C07D401/14

摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein A is

摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：或其药学上可接受的盐，其中A为