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：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：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：US20060052615A1

公开(公告)日：2006-03-09

申请号：US10534291

申请日：2003-11-06

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： C07D403/02 ,  C07C255/45

CPC分类号： C07D207/08 ,  C07C255/46 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D211/22 ,  C07D211/32 ,  C07D211/44 ,  C07D211/46 ,  C07D211/74 ,  C07D491/10

摘要： Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and 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： 公开了式（I）的化合物，

公开(公告)号：US20060161020A1

公开(公告)日：2006-07-20

申请号：US10563538

申请日：2004-06-25

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： C07C237/20

CPC分类号： C07C237/10 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/14 ,  C07D211/38 ,  C07D295/084 ,  C07D295/185

摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention 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或预防涉及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治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20060058278A1

公开(公告)日：2006-03-16

申请号：US10541476

申请日：2004-01-02

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： C07D267/00

CPC分类号： C07D273/02

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 or prevention of diseases in which the beta-secretase enzyme in 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： 本发明涉及式（I）化合物，

公开(公告)号：US20070037784A1

公开(公告)日：2007-02-15

申请号：US10568153

申请日：2004-08-10

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： A61K31/395 ,  C07D225/04

CPC分类号： C07D267/00 ,  C07D225/08

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 or prevention 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-分泌酶的抑制剂并可用于治疗或预防其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式I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：US20060264416A1

公开(公告)日：2006-11-23

申请号：US11495123

申请日：2006-07-28

申请人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

发明人： Craig Coburn ,  Shawn Stachel ,  Joseph Vacca

IPC分类号： A61K31/4747 ,  C07D491/10

CPC分类号： C07D207/08 ,  C07C255/46 ,  C07C255/57 ,  C07C311/08 ,  C07C2601/02 ,  C07C2601/08 ,  C07D211/22 ,  C07D211/32 ,  C07D211/44 ,  C07D211/46 ,  C07D211/74 ,  C07D491/10

摘要： Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and 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： 公开了作为β-分泌酶的抑制剂并可用于治疗或预防其中涉及β-分泌酶的疾病（例如阿尔茨海默病）和包含这些化合物的药物组合物的式（I）化合物和 这些化合物和组合物在预防或治疗涉及β-分泌酶的疾病中的应用。

公开(公告)号：US20070203147A1

公开(公告)日：2007-08-30

申请号：US10593808

申请日：2005-03-25

申请人： Craig Coburn ,  Amy Espeseth ,  Shawn Stachel ,  David Olsen ,  Daria Hazuda ,  M. Holloway

发明人： Craig Coburn ,  Amy Espeseth ,  Shawn Stachel ,  David Olsen ,  Daria Hazuda ,  M. Holloway

IPC分类号： A61K31/506 ,  A61K31/501 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/426 ,  C07D417/02

CPC分类号： C07D417/14 ,  C07D277/40 ,  C07D277/60 ,  C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08

摘要： The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. 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 and HIV protease are involved.

摘要翻译： 本发明涉及作为天冬氨酰蛋白酶抑制剂的2-氨基噻唑化合物，并且是β-分泌酶和HIV蛋白酶的抑制剂，并且其可用于治疗其中涉及β-分泌酶和HIV的疾病 ，如阿尔茨海默病，艾滋病毒感染和艾滋病。 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-分泌酶和HIV蛋白酶的疾病的用途中的用途。