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1. 发明授权

US07704987B1 β-amyloid peptide inhibitors 有权
标题翻译：淀粉样蛋白肽抑制剂
公开(公告)号：US07704987B1
公开(公告)日：2010-04-27
申请号：US10031478
申请日：2000-07-21
申请人： Kevin Jeffrey Barnham , Thomas David McCarthy , Susanne Pallich , Barry Ross Matthews , Robert Alan Cherny
发明人： Kevin Jeffrey Barnham , Thomas David McCarthy , Susanne Pallich , Barry Ross Matthews , Robert Alan Cherny
IPC分类号： A61K31/555 , A61K31/4745 , C07D471/14
CPC分类号： C07K14/4711 , A61K38/00 , A61K47/54 , A61K47/547
摘要： The present invention relates to compounds which inhibit the binding of metal ions to a region in the N-terminal loop of the β-amyloid peptide which includes a cluster of histidine residues. In addition, the invention relates to pharmaceutical compositions including these compounds as the active agent, and to methods of treatment involving the administration of these compounds. The compounds of the invention are useful in the treatment of Alzheimer's Disease and other amyloid-related conditions. In a first aspect the present invention provides a compound which interacts with the β-amyloid peptide in such a way that the N-terminal loop of the peptide (amino acid residues 1-15) is blocked or destabilised, thereby inhibiting the binding of one or more metal ions to at least one histidine residue within the N-terminal loop. Preferably the compound inhibits binding of Cu2+, Zn2+ and Fe3+ ions, but not Mg2+ or Ca2+ ions.
摘要翻译：本发明涉及抑制金属离子与包含一组组氨酸残基的β-淀粉状蛋白肽的N-末端环区域的结合的化合物。此外，本发明涉及包含这些化合物作为活性剂的药物组合物以及涉及施用这些化合物的治疗方法。本发明的化合物可用于治疗阿尔茨海默病和其他淀粉样蛋白相关病症。在第一方面，本发明提供了一种与β-淀粉样蛋白肽相互作用的化合物，使得肽（氨基酸残基1-15）的N-末端环被阻断或不稳定，从而抑制一个或多个金属离子至N末端环内的至少一个组氨酸残基。优选地，化合物抑制Cu 2+，Zn 2+和Fe 3+离子而不是Mg 2+或Ca 2+离子的结合。

2. 发明申请

US20120302730A1 MACROMOLECULAR COMPOUNDS HAVING CONTROLLED STOICHIOMETRY 有权
标题翻译：具有控制性分析的大分子化合物
公开(公告)号：US20120302730A1
公开(公告)日：2012-11-29
申请号：US13570058
申请日：2012-08-08
申请人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
发明人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
IPC分类号： C07K1/00 , C07K1/06
CPC分类号： C08G83/003 , A61K31/785
摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.
摘要翻译：以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

3. 发明授权

US08586705B2 Macromolecular compounds having controlled stoichiometry 有权
标题翻译：具有受控化学计量的大分子化合物
公开(公告)号：US08586705B2
公开(公告)日：2013-11-19
申请号：US13570058
申请日：2012-08-08
申请人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
发明人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
IPC分类号： A61K38/00 , A61K9/00 , A61K31/74
CPC分类号： C08G83/003 , A61K31/785
摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.
摘要翻译：以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

4. 发明授权

US08258259B2 Macromolecular compounds having controlled stoichiometry 有权
标题翻译：具有受控化学计量的大分子化合物
公开(公告)号：US08258259B2
公开(公告)日：2012-09-04
申请号：US12091233
申请日：2006-10-25
申请人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
发明人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
IPC分类号： C07K7/00 , A61K31/74 , A61K9/00
CPC分类号： C08G83/003 , A61K31/785
摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.
摘要翻译：以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

5. 发明申请

US20090118467A1 Macromolecular Compounds Having Controlled Stoichiometry 有权
标题翻译：控制化学计量学的大分子化合物
公开(公告)号：US20090118467A1
公开(公告)日：2009-05-07
申请号：US12091233
申请日：2006-10-25
申请人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
发明人： Guy Yeoman Krippner , Gottfried Lichti , Pasquale Razzino , Brian Devlin Kelly , Susanne Pallich , Scott Andrew Henderson , Angela Michelle Scheppokat , Charlotte Claire Williams , Christopher John Hamilton Porter , Benjamin James Boyd , Lisa Michelle Kaminskas , Phillip Martin Rendle , Ben William Greatrex
IPC分类号： C07K5/00
CPC分类号： C08G83/003 , A61K31/785
摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.
摘要翻译：以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

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