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公开(公告)号:US07528249B2
公开(公告)日:2009-05-05
申请号:US12142145
申请日:2008-06-19
申请人: Richard E. Olson , Michael G. Yang
发明人: Richard E. Olson , Michael G. Yang
IPC分类号: C07D243/12 , C07D243/24
CPC分类号: C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译: 本发明涉及具有式(I)的新型环状丙二酰胺:其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病,例如阿尔茨海默病和唐氏综合征。
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公开(公告)号:US07053081B2
公开(公告)日:2006-05-30
申请号:US10746769
申请日:2003-12-24
申请人: Richard E. Olson , Michael G. Yang
发明人: Richard E. Olson , Michael G. Yang
IPC分类号: A61P25/28
CPC分类号: C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译: 本发明涉及具有式(I)的新型环状丙二酰胺:其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病,例如阿尔茨海默病和唐氏综合征。
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23.
公开(公告)号:US06759404B2
公开(公告)日:2004-07-06
申请号:US09825211
申请日:2001-04-03
申请人: Richard E. Olson , Michael G. Yang
发明人: Richard E. Olson , Michael G. Yang
IPC分类号: C07D40312
CPC分类号: C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要: Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein.
摘要翻译: 具有式(I)的新型环状丙二酰胺及其药物组成。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。
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24.
公开(公告)号:US06632812B2
公开(公告)日:2003-10-14
申请号:US09832455
申请日:2001-04-11
申请人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
发明人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
IPC分类号: C07D24324
CPC分类号: C07D401/04 , C07D223/12 , C07D223/18 , C07D243/12 , C07D243/24 , C07D403/02
摘要: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译: 本发明涉及式(I)的新型内酰胺:具有药物和生物影响性质,其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经障碍,例如阿尔茨海默病和唐氏综合征。
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公开(公告)号:US20110059940A1
公开(公告)日:2011-03-10
申请号:US12990922
申请日:2009-05-07
申请人: Paul J. Gilligan , Michael G. Yang , Jianliang Shi
发明人: Paul J. Gilligan , Michael G. Yang , Jianliang Shi
IPC分类号: A61K31/18 , C07C311/00 , C07D205/04 , C07D233/61 , C07D249/08 , C07D231/12 , C07D213/42 , C07D217/24 , A61K31/24 , A61K31/195 , A61K31/397 , A61K31/4164 , A61K31/4196 , A61K31/415 , A61P25/00 , A61P25/28
CPC分类号: C07D205/04 , C07C311/19 , C07C2601/04 , C07D213/42 , C07D217/24 , C07D231/12 , C07D233/61 , C07D249/08 , C07D263/32 , C07D273/02
摘要: The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了式I化合物,包括其药学上可接受的盐,其药物组合物及其在抑制β-淀粉状蛋白肽(β-bGRAP)生产中的用途。
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26.
公开(公告)号:US20090170831A1
公开(公告)日:2009-07-02
申请号:US12388944
申请日:2009-02-19
申请人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
发明人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
IPC分类号: A61K31/5513 , C07D243/12 , C07D487/04 , A61K31/55 , A61P25/28
CPC分类号: C07D401/04 , C07D223/12 , C07D223/18 , C07D243/12 , C07D243/24 , C07D403/02
摘要: Field of the Invention This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译: 技术领域本发明涉及式(I)的新型内酰胺:具有药物和生物影响性质,其药物组合物和使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病,例如阿尔茨海默病和唐氏综合征。
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公开(公告)号:US07390896B2
公开(公告)日:2008-06-24
申请号:US11841081
申请日:2007-08-20
申请人: Richard E. Olson , Michael G. Yang
发明人: Richard E. Olson , Michael G. Yang
IPC分类号: C07D243/16 , C07D223/16 , C07D403/12
CPC分类号: C07D223/16 , A61K31/4015 , A61K31/445 , A61K31/55 , A61K38/00 , C07D223/10 , C07D223/12 , C07D223/18 , C07D243/14 , C07D243/24 , C07D401/06 , C07D401/12 , C07D403/12 , C07K5/0205 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0812
摘要: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译: 本发明涉及具有式(I)的新型环状丙二酰胺:其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工,更具体地,抑制Aβ肽的产生,从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地,本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病,例如阿尔茨海默病和唐氏综合征。
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公开(公告)号:US07276495B2
公开(公告)日:2007-10-02
申请号:US11005573
申请日:2004-12-06
申请人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
发明人: Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
IPC分类号: C07D487/00 , A61K31/55 , A61P25/28
CPC分类号: C07D401/04 , C07D223/12 , C07D223/18 , C07D243/12 , C07D243/24 , C07D403/02
摘要: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
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公开(公告)号:US07183282B2
公开(公告)日:2007-02-27
申请号:US11375125
申请日:2006-03-14
申请人: Albert J. Robichaud , Taekyu Lee , Wei Deng , Ian S. Mitchell , Michael G. Yang , Simon Haydar , Wenting Chen , Christopher D. McClung , Emilie J. Calvello , David M. Zawrotny
发明人: Albert J. Robichaud , Taekyu Lee , Wei Deng , Ian S. Mitchell , Michael G. Yang , Simon Haydar , Wenting Chen , Christopher D. McClung , Emilie J. Calvello , David M. Zawrotny
IPC分类号: C07D471/04 , A61K31/4985
CPC分类号: C07D471/06 , C07D221/18 , C07D223/32 , C07D471/16 , C07D487/06 , C07D491/06 , C07D495/06 , C07D513/06 , C07D513/16 , C07D519/00
摘要: The present invention is directed to compounds useful for treating addictive behavior and sleep disorders represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.
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公开(公告)号:US07071186B2
公开(公告)日:2006-07-04
申请号:US10787941
申请日:2004-02-26
申请人: Albert J. Robichaud , Taekyu Lee , Wei Deng , Ian S. Mitchell , Michael G. Yang , Simon Haydar , Wenting Chen , Christopher D. McClung , Emilie J. Calvello , David M. Zawrotny
发明人: Albert J. Robichaud , Taekyu Lee , Wei Deng , Ian S. Mitchell , Michael G. Yang , Simon Haydar , Wenting Chen , Christopher D. McClung , Emilie J. Calvello , David M. Zawrotny
IPC分类号: A61P25/00
CPC分类号: C07D471/06 , C07D221/18 , C07D223/32 , C07D471/16 , C07D487/06 , C07D491/06 , C07D495/06 , C07D513/06 , C07D513/16 , C07D519/00
摘要: The present invention is directed to methods of treating addictive behavior and sleep disorders by administering compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.
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