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：US07329746B2

公开(公告)日：2008-02-12

申请号：US10568153

申请日：2004-08-10

申请人： Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca

发明人： Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca

IPC分类号： C07D225/04 ,  C07D267/22 ,  A61K31/33 ,  A61K31/395 ,  A61P25/28

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：US08865701B2

公开(公告)日：2014-10-21

申请号：US13201570

申请日：2010-02-20

申请人： Kun Liu ,  Shawn J. Stachel ,  Craig A. Coburn ,  Thomas G. Steele ,  Richard Soll ,  Hao Wu ,  Xuanjin Peng ,  Yaxian Cai ,  Xiaoxiang Du ,  Jian Li

发明人： Kun Liu ,  Shawn J. Stachel ,  Craig A. Coburn ,  Thomas G. Steele ,  Richard Soll ,  Hao Wu ,  Xuanjin Peng ,  Yaxian Cai ,  Xiaoxiang Du ,  Jian Li

IPC分类号： A61K31/55 ,  C07D513/20 ,  A61K31/438 ,  A61K31/445 ,  A61P25/28 ,  C07D405/14 ,  C07D413/14 ,  C07D495/10 ,  C07D491/20 ,  C07D209/96 ,  C07D491/10 ,  C07D471/20 ,  C07D513/10 ,  C07D471/10

CPC分类号： C07D401/06 ,  C07D209/96 ,  C07D471/10 ,  C07D471/20 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D495/10 ,  C07D513/10 ,  C07D513/20

摘要： The present invention is directed to spiropyrrolidine 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氏病的式（I）的螺吡咯烷化合物。 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：US08354545B2

公开(公告)日：2013-01-15

申请号：US12747605

申请日：2008-12-10

申请人： Shawn J. Stachel ,  Thomas Steele ,  Alessia Petrocchi

发明人： Shawn J. Stachel ,  Thomas Steele ,  Alessia Petrocchi

IPC分类号： C07D401/06 ,  C07D207/06 ,  C07D403/14 ,  C07D413/06 ,  A61K31/535 ,  A61K31/445 ,  A61K31/415 ,  A61K31/4025

CPC分类号： C07D413/06 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/04 ,  C07D491/10

摘要： The present invention is directed to 3,4-substituted pyrrolidine 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）的3,4-取代吡咯烷化合物，其可用于治疗其中涉及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：US07291620B2

公开(公告)日：2007-11-06

申请号：US10563538

申请日：2004-06-25

申请人： Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca ,  Harold G. Selnick

发明人： Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca ,  Harold G. Selnick

IPC分类号： A61K31/4965 ,  A61K31/445 ,  A61K31/40 ,  A61K31/279 ,  A61K31/16

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：US08765759B2

公开(公告)日：2014-07-01

申请号：US12934208

申请日：2009-03-24

申请人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

发明人： Harold G. Selnick ,  Ian M. Bell ,  Melody McWherter ,  Donnette D. Staas ,  Shawn J. Stachel ,  Thomas Steele ,  Craig Stump ,  Michael R. Wood ,  C. Blair Zartman

IPC分类号： A61K31/437 ,  A61K31/497 ,  A61K31/4985

CPC分类号： C07D471/10 ,  C07D403/06 ,  C07D471/20 ,  C07D519/00

摘要： The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 本发明涉及下式的化合物：其中作为拮抗剂的式（其中变量A1，A2，A3，G1，G2，G3，G4，J，Ea，Eb，Ec，R6，R7和Y如本文所述） 的CGRP受体，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US08552023B2

公开(公告)日：2013-10-08

申请号：US13059361

申请日：2009-08-11

申请人： Michael R. Wood ,  June J. Kim ,  Harold G. Selnick ,  Shawn J. Stachel

发明人： Michael R. Wood ,  June J. Kim ,  Harold G. Selnick ,  Shawn J. Stachel

IPC分类号： A61K31/437 ,  C07D471/10 ,  C07D471/20 ,  A61P29/00 ,  A61P25/06 ,  A61P9/12

CPC分类号： C07D471/04 ,  C07D235/02 ,  C07D471/20

摘要： The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

摘要翻译： 本发明涉及具有支链末端衍生物的新型非酰胺接头，其为CGRP受体的拮抗剂，可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP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：US20080161363A1

公开(公告)日：2008-07-03

申请号：US11666942

申请日：2005-10-25

申请人： Craig A. Coburn ,  M. Katharine Holloway ,  Shawn J. Stachel

发明人： Craig A. Coburn ,  M. Katharine Holloway ,  Shawn J. Stachel

IPC分类号： A61K31/4965 ,  A61K31/501

CPC分类号： C07D213/73

摘要： The present invention is directed to 2-aminopyridine 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-氨基吡啶化合物。 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。