Methods of Inhibiting the Interaction Between S100 and the Receptor for Advanced Glycation End-Products
    3.
    发明申请
    Methods of Inhibiting the Interaction Between S100 and the Receptor for Advanced Glycation End-Products 审中-公开
    抑制S100与高分子糖蛋白终产物受体相互作用的方法

    公开(公告)号:US20080214491A1

    公开(公告)日:2008-09-04

    申请号:US12041112

    申请日:2008-03-03

    摘要: A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.

    摘要翻译: 提供了抑制S100蛋白与用于晚期糖基化终产物的受体之间的相互作用的方法,包括向受试者施用治疗有效量的色甘酸,C5或其盐,水合物或溶剂合物。 在一些实施方案中,S100蛋白是S100P。 在一些实施方案中,S100蛋白是S100P。 此外,本发明提供了一种治疗癌症的方法,包括向哺乳动物施用治疗有效量的色甘酸,C5或其盐,水合物或溶剂合物。 还提供了附加的方法。

    METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS
    4.
    发明申请
    METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS 失效
    与DEHYDRONS包裹相关的方法和组合物

    公开(公告)号:US20130131076A1

    公开(公告)日:2013-05-23

    申请号:US11927329

    申请日:2007-10-29

    IPC分类号: A61K31/506

    CPC分类号: A61K31/506 C07D401/04

    摘要: This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.

    摘要翻译: 该应用描述了药物发现和药物成像/检测中的新技术:包装技术。 该技术基于可溶性蛋白质结构中确定的奇异点。 与基于标准结构考虑的药物设计方法相比,蛋白质的包装,或更准确地说,其脱水剂图案可以用作选择性过滤器来设计小分子抑制剂。 本文描述的包装技术是用于避免药物治疗中的副作用并且锐化药物对肿瘤细胞的抑制作用的合理药物设计的新型形式。

    Methods of inhibiting the interaction between S100 and the receptor for advanced glycation end-products
    5.
    发明授权
    Methods of inhibiting the interaction between S100 and the receptor for advanced glycation end-products 失效
    抑制S100与晚期糖基化终产物受体相互作用的方法

    公开(公告)号:US08252807B2

    公开(公告)日:2012-08-28

    申请号:US12247635

    申请日:2008-10-08

    IPC分类号: A61K31/353 A61K31/513

    摘要: A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided.

    摘要翻译: 提供了抑制S100蛋白与用于晚期糖基化终产物的受体之间的相互作用的方法,包括向受试者施用治疗有效量的色甘酸,C5或其盐,水合物或溶剂合物。 在一些实施方案中,S100蛋白是S100P。 在一些实施方案中,S100蛋白是S100P。 此外,本发明提供了一种治疗癌症的方法,包括向哺乳动物施用治疗有效量的色甘酸,C5或其盐,水合物或溶剂合物。 还提供了附加的方法。

    Methods of Inhibiting the Interaction Between S100P and the Receptor for Advanced Glycation End-Products
    6.
    发明申请
    Methods of Inhibiting the Interaction Between S100P and the Receptor for Advanced Glycation End-Products 审中-公开
    抑制S100P与受体之间高级糖基化终产物相互作用的方法

    公开(公告)号:US20110195924A1

    公开(公告)日:2011-08-11

    申请号:US13122814

    申请日:2009-10-06

    CPC分类号: A61K31/352

    摘要: A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof. In addition, provided herein are methods of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, and/or other analogs, or salts, hydrates, or solvates thereof.

    摘要翻译: 提供抑制S100蛋白与晚期糖基化终产物的受体之间的相互作用的方法,包括向受试者施用治疗有效量的色甘酸,C5和/或其它类似物或其盐,水合物或溶剂合物。 此外,本文提供了治疗癌症的方法,包括向哺乳动物施用治疗有效量的色甘酸,C5和/或其它类似物或其盐,水合物或溶剂化物。

    Method of Cancer Treatment with Naphthol Analogs
    9.
    发明申请
    Method of Cancer Treatment with Naphthol Analogs 审中-公开
    萘酚类似物治疗癌症的方法

    公开(公告)号:US20100152140A1

    公开(公告)日:2010-06-17

    申请号:US12529252

    申请日:2008-01-18

    IPC分类号: A61K31/66

    CPC分类号: A61K31/661

    摘要: In one embodiment, the present invention relates to a method of treating a cancer characterized by overexpression of cyclic adenosine monophosphate response element-binding protein (CREB) or phosphorylated CREB (p-CREB) by administering to a patient suffering from the cancer a pharmaceutically-effective amount of a composition comprising a compound selected from the group consisting of 2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide, naphthol analogs having the structure (I), wherein R1 is selected from the group consisting of —H, —F, —Cl, —Br, and —I; R2 is selected from the group consisting of —H, —F, —Cl, —Br, —I, —C1-6 alkyl, —C1-6alkenyl, and —C1-6 alkynyl; R3 is selected from the group consisting of —H and —NO2; and R4 is selected from the group consisting of —H, —C1-6 alkyl, —C1-6 alkenyl, —C1-6 alkynyl, —OC1-6 alkyl, —OC1-6 alkenyl, and —OC1-6 alkynyl; and salts and esters thereof.

    摘要翻译: 在一个实施方案中,本发明涉及一种治疗癌症的方法,其特征在于通过向患有癌症的患者施用药学上可接受的方法来过表达环腺苷一磷酸应答元件结合蛋白(CREB)或磷酸化CREB(p-CREB) 有效量的包含选自2- {1- [3-(脒基硫代)丙基] -1H-吲哚-3-基} -3-(1-甲基吲哚-3-基)马来酰亚胺的化合物的组合物, 具有结构(I)的萘酚类似物,其中R 1选自-H,-F,-Cl,-Br和-I; R 2选自-H,-F,-Cl,-Br,-I,-C 1-6烷基,-C 1-6烯基和-C 1-6炔基; R3选自-H和-NO 2; 并且R 4选自-H,-C 1-6烷基,-C 1-6烯基,-C 1-6炔基,-OC 1-6烷基,-OC 1-6链烯基和-OC 1-6苯基; 及其盐和酯。