Treatment of cancer with mefloquine, its purified enantiomers, and mefloquine analogs
    6.
    发明申请
    Treatment of cancer with mefloquine, its purified enantiomers, and mefloquine analogs 审中-公开
    用梅氟喹,其纯化的对映异构体和甲氟喹类似物治疗癌症

    公开(公告)号:US20050154010A1

    公开(公告)日:2005-07-14

    申请号:US10509693

    申请日:2003-05-16

    IPC分类号: A61K31/4709 A61K31/4745

    CPC分类号: A61K31/4745 A61K31/4709

    摘要: Cancers, particularly solid tumors (e.g., breast, lung, renal, colon and ovarian cancers and melanomas) and cancers of the hematologic system, e.g., hemopoietic cancers such as leukemias, lymphomas or myelomas, are treated by administration of a therapeutically effective amount of a compound having the formula (1): (I)in which the quinoline ring is substituted by from one to three groups selected from halogen and trifluoromethyl (designated in the formula by “A”), and is optionally further substituted by one or more other moieties and R is (a) NR1R2 in which R1 and R2 are independently hydrogen or C1-C4 alkyl; (b) 2-piperidyl, (c) 2-pyridyl, and (d) 5-(ethyl or vinyl)-quinuclidin-4-yl; an enantiomer of such a compound; a pharmaceutically acceptable salts of such a compound or of an enantiomer thereof; a prodrug of such a compound or of an enantiomer thereof; a metabolite of such a compound or of an enantiomer thereof; and mixtures of two or more of the foregoing. A particularly preferred compound is mefloquine.

    摘要翻译: 癌症,特别是实体肿瘤(例如乳腺癌,肺癌,结肠癌,卵巢癌和黑素瘤)和血液系统的癌症,例如造血性癌症如白血病,淋巴瘤或骨髓瘤,通过施用治疗有效量的 具有式(1):(I)的化合物,其中喹啉环被选自卤素和三氟甲基(式中“A”表示)的一至三个基团取代,并且任选进一步被一个或多个 其它部分和R是(a)NR1R2,其中R1和R2独立地是氢或C1-C4烷基; (b)2-哌啶基,(c)2-吡啶基和(d)5-(乙基或乙烯基) - 奎宁环-4-基; 这种化合物的对映异构体; 这种化合物或其对映异构体的药学上可接受的盐; 这种化合物或其对映异构体的前药; 这种化合物或其对映异构体的代谢物; 以及上述两种或更多种的混合物。 特别优选的化合物是甲氟喹。

    LIPOPROTEINS, LIPOPEPTIDES AND ANALOGS, AND METHODS FOR MAKING AND USING THEM
    10.
    发明申请
    LIPOPROTEINS, LIPOPEPTIDES AND ANALOGS, AND METHODS FOR MAKING AND USING THEM 有权
    脂蛋白,脂蛋白和类似物,以及制备和使用它们的方法

    公开(公告)号:US20100266675A1

    公开(公告)日:2010-10-21

    申请号:US12600930

    申请日:2008-05-21

    CPC分类号: C07C323/60 C07C233/47

    摘要: The invention provides novel compositions—lipopeptides and analogs, including somocystinamide A, and somocystinamide A variants and analogs, and pharmaceutical compositions, liposomes and nanoparticles comprising them, and methods of making and using them. In one embodiment, these lipopeptides and analogs are used to induce apoptosis in a cell, which can be a normal cell, a dysfunctional cell and/or a cancer (tumor) cell. In alternative embodiments, the compositions of the invention, including the lipopeptides and analogs of the invention, and the pharmaceutical compositions comprising them, are used to treat or ameliorate (including slowing the progression of) normal, dysfunctional (e.g., abnormally proliferating) and/or tumor associated blood vessels, including endothelial and/or capillary cell growth; including neovasculature related to (within, providing a blood supply to) a tumor.

    摘要翻译: 本发明提供了新颖的组合物 - 脂肽和类似物,包括胞质酰胺A和胞囊酰胺A变体和类似物,以及包含它们的药物组合物,脂质体和纳米颗粒,以及制备和使用它们的方法。 在一个实施方案中,这些脂肽和类似物用于诱导细胞凋亡,细胞可以是正常细胞,功能障碍细胞和/或癌症(肿瘤)细胞。 在替代实施方案中,本发明的组合物,包括本发明的脂肽和类似物以及包含它们的药物组合物用于治疗或改善(包括减缓正常,功能障碍(例如异常增殖)和/ 或肿瘤相关血管,包括内皮细胞和/或毛细胞生长; 包括与肿瘤相关的新血管生成(内部,提供血液供应)。