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公开(公告)号:US20080153868A1
公开(公告)日:2008-06-26
申请号:US11951516
申请日:2007-12-06
申请人: Lorin A. Thompson , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
发明人: Lorin A. Thompson , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
IPC分类号: A61K31/437 , C07D217/00 , A61K31/47 , A61P25/00 , A61P25/28 , C07D221/02
CPC分类号: C07K5/06139 , C07D471/04
摘要: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译: 提供一系列式(I)的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐,其中R 8 R 8和R 9如本文所定义,其药物组合物和使用方法。 这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白(APP)的加工,更具体地抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物,例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
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公开(公告)号:US07902218B2
公开(公告)日:2011-03-08
申请号:US11951516
申请日:2007-12-06
申请人: Lorin A. Thompson, III , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
发明人: Lorin A. Thompson, III , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
IPC分类号: C07D217/00 , A61K31/47
CPC分类号: C07K5/06139 , C07D471/04
摘要: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译: 提供一系列式(I)的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐,其中R,R 8和R 9如本文所定义,其药物组合物和使用方法。 这些化合物通过分泌酶抑制淀粉样蛋白前体蛋白(APP)的加工,更具体地,抑制Aβ的生成。 本公开涉及可用于治疗与淀粉样蛋白产生相关的神经系统疾病的化合物,例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
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公开(公告)号:US20110015175A1
公开(公告)日:2011-01-20
申请号:US12683791
申请日:2010-01-07
申请人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
发明人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
IPC分类号: A61K31/55 , C07D487/04 , C07D417/12 , C07D491/20 , A61K31/437 , A61K31/428 , A61K31/4439 , A61P25/28 , A61P25/00 , A61P27/02 , A61P35/00
CPC分类号: C07D487/04 , C07D417/12 , C07D471/04 , C07D513/10
摘要: The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其减少β-淀粉状蛋白肽(&bgr--AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
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4.
公开(公告)号:US08349880B2
公开(公告)日:2013-01-08
申请号:US12683791
申请日:2010-01-07
申请人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
发明人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
IPC分类号: A61K31/41 , A61K31/425 , C07D249/00 , C07D277/82
CPC分类号: C07D487/04 , C07D417/12 , C07D471/04 , C07D513/10
摘要: The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其减少β-淀粉状蛋白肽(&bgr--AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
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公开(公告)号:US08710061B2
公开(公告)日:2014-04-29
申请号:US13358822
申请日:2012-01-26
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/497 , A01N43/54 , A01N43/90
CPC分类号: C07D239/70 , A61K31/517 , A61K31/519 , C07D401/04 , C07D471/04 , C07D487/10 , C07D491/048 , C07D491/10
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
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公开(公告)号:US08637525B2
公开(公告)日:2014-01-28
申请号:US13013373
申请日:2011-01-25
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A01N43/54 , A01N43/90 , A61K31/517 , A61K31/519 , A01N43/64 , A61K31/41
CPC分类号: A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列调节β-淀粉样肽(β-AP)产生的式(I)化合物,并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽(β-AP)产生影响的病症 。
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公开(公告)号:US20110212937A1
公开(公告)日:2011-09-01
申请号:US12845045
申请日:2010-07-28
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/397 , C07D401/12 , A61K31/517 , C07D239/70 , C07D403/12 , C07D403/14 , C07D471/04 , A61K31/519 , C07D491/052 , C07D413/14 , A61K31/5377 , A61K31/496 , A61K31/5386 , A61P25/28
CPC分类号: C07D403/12 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
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公开(公告)号:US07745470B2
公开(公告)日:2010-06-29
申请号:US11370728
申请日:2006-03-08
IPC分类号: A61K31/42 , C07D263/30
CPC分类号: C07D265/30 , C07D207/09 , C07D207/12 , C07D207/27 , C07D265/32 , C07D403/12 , C07D413/12 , C07D413/14
摘要: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译: 提供了一系列取代的式(I)的间苯二甲酸酯或其立体异构体; 或其药学上可接受的盐,其中如本文所定义的W,R 3,R 5和R 6,其药物组合物和使用方法。 这些新化合物通过分泌酶抑制淀粉样蛋白前体蛋白(APP)的加工,更具体地,抑制Aβ的生成。 本公开涉及可用于治疗与淀粉样蛋白产生相关的神经系统疾病的化合物,例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
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公开(公告)号:US20120028994A1
公开(公告)日:2012-02-02
申请号:US13013373
申请日:2011-01-25
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/517 , C07D401/14 , A61P35/00 , A61P25/28 , A61P25/00 , A61P27/02 , C07D403/12 , C07D401/12
CPC分类号: A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
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公开(公告)号:US08486952B2
公开(公告)日:2013-07-16
申请号:US12845045
申请日:2010-07-28
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A01N43/54 , A01N43/90 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/497 , A61K31/00 , A61K31/535 , C07D239/70 , C07D491/00 , C07D495/00 , C07D471/00 , C07D413/00
CPC分类号: C07D403/12 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列调节β-淀粉样肽(β-AP)产生的式(I)化合物,并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽(β-AP)产生影响的病症 。
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