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    COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISORDERS
    5.
    发明申请
    COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISORDERS 审中-公开
    适用于治疗神经损伤性疾病的化合物

    公开(公告)号：US20110136749A1

    公开(公告)日：2011-06-09

    申请号：US12957551

    申请日：2010-12-01

    申请人： Mark A. Findeis ,  Kollol Pal ,  Frank Schroeder

    发明人： Mark A. Findeis ,  Kollol Pal ,  Frank Schroeder

    IPC分类号： A61K31/704 ,  C12N5/00 ,  A61P25/28 ,  A61P25/16

    CPC分类号： C07J53/00 ,  C07J71/00 ,  C07J71/0005

    摘要： As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.

    摘要翻译： 如本文所述，本发明提供了可用于治疗或减轻神经变性疾病严重程度的化合物。 本发明还提供了治疗或减轻此类疾病严重程度的方法，其中所述方法包括向患者施用本发明化合物或其组合物。 所述方法可用于治疗或减轻例如阿尔茨海默病的严重性。

    Modulators of β-amyloid peptide aggregation
    6.
    发明授权
    Modulators of β-amyloid peptide aggregation 失效
    β-淀粉样肽聚集的调节剂

    公开(公告)号：US07803774B2

    公开(公告)日：2010-09-28

    申请号：US10989763

    申请日：2004-11-15

    申请人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olsen ,  Christopher Self

    发明人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olsen ,  Christopher Self

    IPC分类号： A61K38/00 ,  A61K49/00

    CPC分类号： C07K14/4711 ,  A61K38/00

    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 alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate 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： 调节天然化合物的化合物 提供淀粉样肽聚集。 本发明的调节剂包含肽，优选基于 淀粉样肽，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。 在一个特别优选的实施方案中，该肽是一种反式异构体， 淀粉样蛋白肽，优选A-Bgr; 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是烷基。 优选的羧基末端修饰基团包括酰胺基，乙酸基，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。

    Modulators of &bgr;-amyloid peptide aggregation
    7.
    发明授权
    Modulators of &bgr;-amyloid peptide aggregation 失效
    β-淀粉样肽聚集的调节剂

    公开(公告)号：US06831066B2

    公开(公告)日：2004-12-14

    申请号：US10395290

    申请日：2003-03-24

    申请人： Mark A. Findeis ,  Kathryn Phillips

    发明人： Mark A. Findeis ,  Kathryn Phillips

    IPC分类号： A61K3800

    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 alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate 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是烷基。 优选的羧基末端修饰基团包括酰胺基，乙酸基，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。

    Modulators of &mgr;-amyloid peptide aggregation
    8.
    发明授权
    Modulators of &mgr;-amyloid peptide aggregation 失效
    β-淀粉样肽聚集的调节剂

    公开(公告)号：US06610658B1

    公开(公告)日：2003-08-26

    申请号：US09519019

    申请日：2000-03-03

    申请人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olson ,  Christopher Self

    发明人： Mark A. Findeis ,  Kathryn Phillips ,  Gary L. Olson ,  Christopher Self

    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, carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate 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，肽在以下氨基末端修饰：羧基末端或两者。 优选的氨基末端修饰基团是烷基。 优选的羧基末端修饰基团包括酰胺基，乙酸基，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。