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1.发明授权公开(公告)号：US07175828B2
公开(公告)日：2007-02-13
申请号：US10677076
申请日：2003-09-30
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary F. Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
CPC分类号： C07K5/101 , A61K38/00 , C07K5/1027 , C07K7/06 , C07K14/4711 , G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3–5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样肽的逆反异构体，优选Abeta 17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团包括环状，杂环，多环和支链烷基。 优选的羧基末端修饰基团包括酰胺基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。
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2.发明授权公开(公告)号：US06689752B2
公开(公告)日：2004-02-10
申请号：US09895443
申请日：2001-06-29
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
IPC分类号： A61K3807
CPC分类号： C07K5/101 , A61K38/00 , C07K5/1027 , C07K7/06 , C07K14/4711 , G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样肽的逆反异构体，优选Abeta17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团包括环状，杂环，多环和支链烷基。 优选的羧基末端修饰基团包括酰胺基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。
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3.发明授权公开(公告)号：US06277826B1
公开(公告)日：2001-08-21
申请号：US09356931
申请日：1999-07-19
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
IPC分类号： A61K3806
CPC分类号： C07K5/101 , A61K38/00 , C07K5/1027 , C07K7/06 , C07K14/4711 , G01N33/6896 , G01N2333/4709 , G01N2800/2821
摘要： Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样肽的逆反异构体，优选Abeta17-21的逆反异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团包括环状，杂环，多环和支链烷基。 优选的羧基末端修饰基团包括酰胺基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。
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4.发明授权
公开(公告)号：US5985242A
公开(公告)日：1999-11-16
申请号：US920162
申请日：1997-08-27
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate natural .beta. amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a .beta. amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a .beta. amyloid peptide, preferably a retro-inverso isomer of A.beta..sub.17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译： 提供调节天然β淀粉样肽聚集的化合物。 本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。 优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。 在特别优选的实施方案中，肽是β淀粉样蛋白肽的逆反异构体，优选Aβ17-21的逆反式异构体。 在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。 优选的氨基末端修饰基团包括环状，杂环，多环和支链烷基。 优选的羧基末端修饰基团包括酰胺基，烷基酰胺基，芳基酰胺基或羟基。 还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。
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公开(公告)号：US06303567B1
公开(公告)日：2001-10-16
申请号：US08703675
申请日：1996-08-27
申请人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
发明人： Mark A. Findeis , Malcolm L. Gefter , Gary Musso , Ethan R. Signer , James Wakefield , Susan Molineaux , Joseph Chin , Jung-Ja Lee , Michael Kelley , Sonja Komar-Panicucci , Christopher C. Arico-Muendel , Kathryn Phillips , Neil J. Hayward
IPC分类号： A61K3806
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
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公开(公告)号：US07989395B2
公开(公告)日：2011-08-02
申请号：US11584880
申请日：2006-10-23
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
IPC分类号： C40B50/16
CPC分类号： C12N15/1068 , C07H21/00
摘要： The present invention provides a method for identifying a compound of interest by screening libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译： 本发明提供了通过筛选包括编码寡核苷酸标签的分子文库来鉴定感兴趣的化合物的方法。
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公开(公告)号：US08598089B2
公开(公告)日：2013-12-03
申请号：US13040674
申请日：2011-03-04
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffan Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffan Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
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公开(公告)号：US08410028B2
公开(公告)日：2013-04-02
申请号：US13051314
申请日：2011-03-18
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffan Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffan Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
CPC分类号： C12N15/1068 , C07H21/00 , C40B50/10
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
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公开(公告)号：US20120245040A1
公开(公告)日：2012-09-27
申请号：US13040674
申请日：2011-03-04
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译： 本发明提供合成包含编码寡核苷酸标签的分子文库的方法。
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公开(公告)号：US07972992B2
公开(公告)日：2011-07-05
申请号：US11015458
申请日：2004-12-17
申请人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
发明人： Barry Morgan , Stephen Hale , Christopher C. Arico-Muendel , Matthew Clark , Richard Wagner , David I. Israel , Malcolm L. Gefter , Dennis Benjamin , Nils Jakob Vest Hansen , Malcolm J. Kavarana , Steffen Phillip Creaser , George J. Franklin , Paolo A. Centrella , Raksha A. Acharya
IPC分类号： C40B50/00
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides methods of synthesizing a molecule comprising a functional moiety which is operatively linked to an encoding oligonucleotide. The methods include providing an initiator compound comprising an initial functional moiety comprising n building blocks, wherein the initial functional moiety comprises at least one reactive group, and is operatively linked to an initial oligonucleotide; reacting the initiator compound with a building block comprising at least one complementary reactive group, under conditions suitable for reaction of the complementary reactive group to form a covalent bond; and reacting the initial oligonucleotide with an incoming oligonucleotide corresponding to the building block in the presence of an enzyme which catalyzes ligation of the initial oligonucleotide and the incoming oligonucleotide, under conditions suitable for ligation of the incoming oligonucleotide and the initial oligonucleotide to form an encoding oligonucleotide.
摘要翻译： 本发明提供合成包含与编码寡核苷酸有效连接的功能部分的分子的方法。 所述方法包括提供包含起始功能部分的引发剂化合物，其包含n个结构单元，其中所述初始功能部分包含至少一个反应性基团，并且可操作地连接到初始寡核苷酸; 使引发剂化合物与包含至少一个互补反应性基团的构建块在适于互补反应性基团反应以形成共价键的条件下反应; 并在初始寡核苷酸和入侵寡核苷酸的连接酶存在下，使初始寡核苷酸与对应于构建单元的入侵寡核苷酸反应，在适合连接引入寡核苷酸和初始寡核苷酸的条件下形成编码寡核苷酸 。
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