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1.发明授权Macrocyclic beta-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的大环β-分泌酶抑制剂公开(公告)号：US07329746B2
公开(公告)日：2008-02-12
申请号：US10568153
申请日：2004-08-10
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
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2.发明授权2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease 有权用作治疗阿尔茨海默病的β-分泌酶抑制剂的2,4,6-取代的吡啶基衍生物化合物公开(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。
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3.发明授权N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的N-烷基苯基卡巴酰胺β-分泌酶抑制剂公开(公告)号：US07291620B2
公开(公告)日：2007-11-06
申请号：US10563538
申请日：2004-06-25
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。
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4.发明授权Macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease 有权用于治疗阿尔茨海默氏病的大环β-分泌酶抑制剂公开(公告)号：US07371853B2
公开(公告)日：2008-05-13
申请号：US10541476
申请日：2004-01-02
IPC分类号： C07D267/22 , C07D281/18 , C07D291/00 , C07D337/16 , C07D487/00 , C07D498/00 , C07D513/00
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： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗或预防所涉及的β-分泌酶如阿尔茨海默病的疾病的式（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。
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5.发明授权Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease 有权苯甲酰胺β-分泌酶抑制剂治疗阿尔茨海默病公开(公告)号：US07348356B2
公开(公告)日：2008-03-25
申请号：US11495123
申请日：2006-07-28
IPC分类号： A61K31/40 , C07D207/06
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。
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公开(公告)号：US07109217B2
公开(公告)日：2006-09-19
申请号：US10534291
申请日：2003-11-06
IPC分类号： A01N43/40 , A01N43/36 , C07D211/44 , C07D207/08
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.
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7.发明授权Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease 有权Spiropyrrolidineβ-分泌酶抑制剂用于治疗阿尔茨海默氏病公开(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。
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8.发明申请SPIROPYRROLIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的螺旋罗哌啶β-分泌酶抑制剂公开(公告)号：US20110306595A1
公开(公告)日：2011-12-15
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
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。
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9.发明申请2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的2-氨基咪唑β-分泌酶抑制剂公开(公告)号：US20110034483A1
公开(公告)日：2011-02-10
申请号：US12919277
申请日：2009-02-18
申请人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
发明人： Ivory D. Hills , Craig A. Coburn , Samuel L. Graham , Keith P. Moore , Philippe G. Nantermet , Hemaka A. Rajapakse , Shawn J. Stachel , Hong Zhu
IPC分类号： A61K31/506 , C07D233/88 , A61K31/4174 , C07D403/10 , A61K31/4178 , C07D403/06 , C07D413/10 , A61K31/42 , C07D401/10 , A61K31/4439 , A61K31/422 , A61P25/28
CPC分类号： C07D233/88 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10
摘要： The present invention is directed to 2-aminoimidazole 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病的式（I）的2-氨基咪唑化合物。 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。
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10.发明授权Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease 有权用于治疗阿尔茨海默氏病的Spiropiperidineβ-分泌酶抑制剂公开(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。
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