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    Treatment of cancer with mefloquine, its purified enantiomers, and mefloquine analogs
    4.
    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。

    USE OF ETODOLAC TO TREAT HYPERPLASIA
    6.
    发明申请
    USE OF ETODOLAC TO TREAT HYPERPLASIA 审中-公开

    公开(公告)号：US20070299042A1

    公开(公告)日：2007-12-27

    申请号：US11615396

    申请日：2006-12-22

    申请人： Dennis Carson ,  Lorenzo Leoni ,  Mary Corr

    发明人： Dennis Carson ,  Lorenzo Leoni ,  Mary Corr

    IPC分类号： A61K31/407 ,  A61K31/496 ,  A61K31/56 ,  A61P35/00

    CPC分类号： A61K31/12 ,  A61K31/18 ,  A61K31/40 ,  A61K31/407 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/50 ,  A61K31/56 ,  A61K31/675 ,  A61K31/7052

    摘要： The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I):formula (I): wherein R1 is lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R2, R3, R4 and R5 are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, —(CH2)1-3—, —(C1-C3)alkyl(CO)—, or —(CH2)1-3SO2—; Z is hydroxy, lower alkoxy, (C2-C4)acyloxy, —N(R8)(R9), phenylamino, (ω-(4-pyridyl)(C2-C4 alkoxy), (ω-((R8)(R9) amino)(C2-C4 alkoxy), an amino acid ester of (ω-(HO)(C2-C4))alkoxy, —N(R8)CH(R8)CO2H, 1′-D-glucuronyloxy, —SO3H, —PO4H2, —N(NO)(OH), —SO2NH2, —PO(OH)(NH2), —OCH2CH2N(CH3)3+, or tetrazolyl; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; n is 0, 1, 2, or 3; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; each alkyl or phenyl group of R1, R2, R3, R4,R5, R6, R7 and Z is optionally substituted with 1, 2, or 3 (C1-C4)alkyl groups; or a pharmaceutically acceptable salt thereof.

    Alanosine formulations and methods of use
    8.
    发明申请
    Alanosine formulations and methods of use 审中-公开
    阿诺糖苷配方及使用方法

    公开(公告)号：US20060041013A1

    公开(公告)日：2006-02-23

    申请号：US11153640

    申请日：2005-06-14

    申请人： Jason Brittain ,  Joe Franklin ,  Lorenzo Leoni ,  Christina Niemeyer ,  Gary Elliott

    发明人： Jason Brittain ,  Joe Franklin ,  Lorenzo Leoni ,  Christina Niemeyer ,  Gary Elliott

    IPC分类号： A61K31/21

    CPC分类号： A61K31/70 ,  A61K31/21 ,  A61K45/06 ,  A61K2300/00

    摘要： Stable liquid formulations of the anti-tumor agent L-alanosine are described. These formulations preferably comprise L-alanosine in an aqueous environment having a basic pH, preferably in the range of about pH 8-9. The alanosine formulations and compositions disclosed herein can be used for various purposes, including the treatment of various cancers, particularly those that are deficient in methylthioadenosine phophorylase (MTAP) enzymatic activity. Also described are methods for the treatment of diseases susceptible to treatment with alanosine, e.g., certain cancers, particularly those characterized by tumor cells that are MTAP deficient, wherein a patient is administered L-alanosine, alone or as part of a combination therapy with a second chemotherapeutic agent.

    摘要翻译： 描述了抗肿瘤剂L-肌氨酸的稳定的液体制剂。 这些制剂优选在具有碱性pH，优选在约pH8-9的范围内的水性环境中包含L-肌氨酸。 本文公开的肌苷制剂和组合物可以用于各种目的，包括治疗各种癌症，特别是那些缺乏甲基硫代腺苷磷酸化酶（MTAP）酶活性的那些。 还描述了用于治疗易于用阿那诺膦治疗的疾病的方法，例如某些癌症，特别是MTAP缺陷型肿瘤细胞特征的那些癌症，其中单独或作为联合治疗的一部分给予患者L-肌氨酸 第二化疗剂。