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11 条记录 (耗时 0.026 秒)

    Treatment of cancer with mefloquine, its purified enantiomers, and mefloquine analogs
    5.
    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

    申请人： Dennis Carson ,  Lorenzo Leoni ,  Howard Cottam

    发明人： Dennis Carson ,  Lorenzo Leoni ,  Howard Cottam

    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。

    Compounds for inhibition of ceramide-mediated signal transduction
    10.
    发明授权
    Compounds for inhibition of ceramide-mediated signal transduction 失效

    公开(公告)号：US06562819B2

    公开(公告)日：2003-05-13

    申请号：US09951198

    申请日：2001-09-13

    申请人： Dennis A. Carson ,  Howard Cottam

    发明人： Dennis A. Carson ,  Howard Cottam

    IPC分类号： C07D21724

    CPC分类号： C07D239/545 ,  C07D213/76 ,  C07D217/24 ,  C07D239/96 ,  C07D473/06 ,  C07D473/10 ,  C07D475/02 ,  C07D513/04

    摘要： Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.