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60 条记录 (耗时 0.032 秒)

    Modulators of β-amyloid peptide aggregation
    1.
    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。

    Pharmaceutical formulations for sustained drug delivery
    3.
    发明申请
    Pharmaceutical formulations for sustained drug delivery 审中-公开

    公开(公告)号：US20070185032A1

    公开(公告)日：2007-08-09

    申请号：US11265520

    申请日：2005-11-02

    申请人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    发明人： Malcolm Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher Molineaux

    IPC分类号： A61K38/09 ,  A61K38/08 ,  A61K9/14

    CPC分类号： A61K38/09 ,  A61K47/61

    摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

    Pharmaceutical formulations for sustained drug delivery
    7.
    发明授权
    Pharmaceutical formulations for sustained drug delivery 失效
    用于持续给药的药物制剂

    公开(公告)号：US5968895A

    公开(公告)日：1999-10-19

    申请号：US762747

    申请日：1996-12-11

    申请人： Malcolm L. Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher J. Molineaux

    发明人： Malcolm L. Gefter ,  Nicholas Barker ,  Gary Musso ,  Christopher J. Molineaux

    IPC分类号： A61K47/30 ,  A61K9/22 ,  A61K38/04 ,  A61K38/09 ,  A61K38/22 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/48 ,  A61P15/00 ,  A61P15/18 ,  A61P35/00 ,  A61R38/00

    CPC分类号： B82Y5/00 ,  A61K38/09 ,  A61K47/4823 ,  A61K47/48961 ,  Y10S514/80

    摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptide and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide for prolonged periods, e.g., one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptide of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.

    摘要翻译： 公开了包含肽和载体大分子的水不溶性络合物的持续递送制剂。 本发明的制剂允许在施用复合物之后以较小的体积装载高浓度的肽并延长药物活性肽的递送时间，例如一个月。 本发明的络合物可以研磨或粉碎成细粉末。 以粉末形式，络合物形成稳定的水性悬浮液和分散体，适于注射。 在优选的实施方案中，复合物的肽是LHRH类似物，优选LHRH拮抗剂，载体大分子是阴离子聚合物，优选羧甲基纤维素。 还公开了制备本发明复合物的方法，以及使用含LHRH类似物的复合物治疗可用LHRH类似物治疗的病症的方法。