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    SUSTAINED RELEASE FORMULATION CONTAINING DFMO
    1.
    发明申请
    SUSTAINED RELEASE FORMULATION CONTAINING DFMO 审中-公开
    含有DFMO的持续释放配方

    公开(公告)号：WO1998019667A1

    公开(公告)日：1998-05-14

    申请号：PCT/US1997020424

    申请日：1997-10-31

    Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  MCGINITY, James

    Inventor： ILEX ONCOLOGY, INC.

    IPC: A61K09/20

    CPC classification number: A61K31/198 ,  A61K9/2081 ,  A61K9/209 ,  A61K9/5084

    Abstract: Preparations comprising a capsule, tablet or other dosage form containing a core of different types of DFMO are provided. These preparations are capable of providing for the direct and constant delivery of DFMO to the entire GI tract or just the colon and rectum. The DFMO-containing granules include granules specially formulated to achieve rapid DFMO release, and granules formulated to achieve slower DFMO release and/or granules formulated for gastric, enteric or colorectal release. Methods of using the preparations to flood the GI tract with relatively constant levels of DFMO may thus be provided. The ratio of the (+) to the (-)-enantiomeric forms of DFMO in the granules will be controlled so as to enhance the pharmacological profile and reduce toxicity of the preparation relative to racemic DFMO. Preparations and methods for achieving systemic delivery as well as direct colon delivery of DFMO are also described.

    Abstract translation: 提供了包含含有不同类型DFMO的核心的胶囊，片剂或其它剂型的制剂。 这些制剂能够提供直接和持续的DFMO输送到整个胃肠道或只是结肠和直肠。 含有DFMO的颗粒包括特殊配制以实现快速DFMO释放的颗粒，以及配制用于实现慢性DFMO释放和/或配制用于胃肠，肠或结肠直肠释放的颗粒的颗粒。 因此可以提供使用制剂以相对恒定水平的DFMO来淹没胃肠道的方法。 将控制颗粒中DFMO的（+）与（ - ） - 对映体形式的比例，以增强制剂相对于外消旋DFMO的药理学特性和降低毒性。 还描述了用于实现系统递送以及DFMO的直接结肠递送的制备和方法。

    NITROXIDE FREE RADICAL DUAL INDICATOR AGENTS
    3.
    发明申请
    NITROXIDE FREE RADICAL DUAL INDICATOR AGENTS 审中-公开
    NITROXIDE自由基双指示剂

    公开(公告)号：WO9950244A9

    公开(公告)日：1999-12-09

    申请号：PCT/US9906688

    申请日：1999-03-26

    Applicant: LIPITEK INC ,  MARTIN VLADIMIR V ,  WEIS ALEXANDER

    Inventor： MARTIN VLADIMIR V ,  WEIS ALEXANDER

    IPC: C07D207/22 ,  C07D233/54 ,  C07D233/88 ,  C07D233/90 ,  C07D403/12 ,  C07D498/04 ,  C07D207/46 ,  C07D213/89 ,  C07D261/20

    CPC classification number: C07D233/54 ,  C07D207/22 ,  C07D233/88 ,  C07D233/90 ,  C07D403/12

    Abstract: Dual indicator agents having synergistically enhanced fluorescent properties are provided that include a nitroxide moiety and a nitroxide free radical center. The indicator molecule may include any variety of chemical or biochemical marking agents, such as a fluorescent molecule. The dual agent may further include a spacer molecule or linker, that will function to attach the indicator molecule, such as a fluorescent moiety, to the nitroxide moiety. These may be used to measure the redox potential in living cells, as well as to determine redox potentials in diagnostics, as well as in many other applications.

    Abstract translation: 提供了具有协同增强的荧光性质的双指示剂，其包括氮氧自由基部分和氮氧自由基中心。 指示剂分子可以包括任何种类的化学或生物化学标记试剂，例如荧光分子。 双重药剂可以进一步包括间隔分子或连接子，其将起到将指示剂分子例如荧光部分连接至氮氧化物部分的作用。 这些可用于测量活细胞中的氧化还原电位，以及确定诊断中的氧化还原电位以及许多其他应用中的氧化还原电位。

    ISOMERIC PHARMACEUTICAL FORMULATION CONTAINING DFMO FOR THE TREATMENT OF CANCER
    4.
    发明申请
    ISOMERIC PHARMACEUTICAL FORMULATION CONTAINING DFMO FOR THE TREATMENT OF CANCER 审中-公开
    含有DFMO用于治疗癌症的异构药物制剂

    公开(公告)号：WO1998025603A1

    公开(公告)日：1998-06-18

    申请号：PCT/US1997023027

    申请日：1997-12-12

    Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  SHAKED, Ze'ev

    Inventor： ILEX ONCOLOGY, INC.

    IPC: A61K31/195

    CPC classification number: A61K31/198

    Abstract: Preparations comprising a single enantiomer or defined non-racemic ratio of enantiomers of alpha-difluoromethylornithine (DFMO) are provided for treating, preventing, controlling the growth of and/or reducing the risk of cancers, tumors and other related neoplastic disorders. The preparations containing a substantially pure preparation of (-)-DFMO or a defined non-racemic ratio of DFMO enantiomers will provide an enhanced pharmacological activity relative to a preparation comprising racemic DFMO.

    Abstract translation: 提供包含单一对映异构体或α-二氟甲基鸟氨酸（DFMO）的对映异构体的限定非外消旋比例的制剂用于治疗，预防，控制癌症，肿瘤和其他相关的肿瘤性疾病的风险和/或降低其风险。 包含（ - ） - DFMO或DFMO对映异构体的限定非外消旋比的基本上纯的制剂的制剂相对于包含外消旋DFMO的制剂将提供增强的药理学活性。

    AMPLIFIED FLUORESCENT MATERIALS AND USES THEREOF
    6.
    发明申请
    AMPLIFIED FLUORESCENT MATERIALS AND USES THEREOF 审中-公开
    放大荧光材料及其用途

    公开(公告)号：WO9949831A3

    公开(公告)日：2000-01-27

    申请号：PCT/US9900203

    申请日：1999-01-05

    Applicant: MARTIN VLADIMIR V ,  WEIS ALEXANDER

    Inventor： MARTIN VLADIMIR V ,  WEIS ALEXANDER

    IPC: C09K11/06 ,  G01N33/533 ,  C07C13/28

    CPC classification number: G01N33/533 ,  C09K11/06

    Abstract: Compositions of fluorescent amplifier molecules are provided, as well as synthetic methods for their preparation. The procedures provide for the preparation of gram quantities of fluorescent molecules from available precursors. The fluorescent amplifier molecules include a multi-dimensional, rigid core (C), to which at least two fluorescent moieties are attached by way of a linker (L). Amplifier molecules that further include a "targeting" molecule (a molecule that functions to direct the fluorescent amplifier to a particular binding site) are also presented, the targeting molecule being attached to the rigid, multi-dimensional core. Signal amplification without steric restrictions of fluorophore mobility is provided, hence reducing and/or avoiding interactions between moieties as well as fluorescence quenching. The advantage of the derivatives of the present invention, in addition to other things, over conventional fluorescent labels is due to the ability to amplify signal upon accumulation of the fluorescent moieties. The new amplified molecules are further disclosed to have the capability to quantitate the fluorescence signal. the compositions may also be employed as nucleic acid fluorescent -in-situ-hybridization probes.

    Abstract translation: 提供荧光放大器分子的组成，以及其制备的合成方法。 该程序提供从可用前体制备克量的荧光分子。 荧光放大器分子包括多维刚性芯（C），其中至少两个荧光部分通过连接体（L）连接到其上。 进一步包括“靶向”分子（用于将荧光放大器引导到特定结合位点的分子）的放大器分子也被提供，靶向分子附着于刚性多维核心。 提供没有荧光团迁移率的空间限制的信号放大，因此减少和/或避免部分之间的相互作用以及荧光猝灭。 本发明的衍生物除了其它方面优于常规荧光标记物的优点是由于在荧光部分积累时扩增信号的能力。 进一步公开了新的扩增分子以具有定量荧光信号的能力。 该组合物也可以用作核酸荧光原位杂交探针。

    DFMO AND TAXOL FOR THE TREATMENT OR PREVENTION OF BREAST CANCER
    7.
    发明申请
    DFMO AND TAXOL FOR THE TREATMENT OR PREVENTION OF BREAST CANCER 审中-公开
    DFMO和TAXOL用于治疗或预防乳腺癌

    公开(公告)号：WO1998014188A1

    公开(公告)日：1998-04-09

    申请号：PCT/US1997018252

    申请日：1997-10-03

    Applicant: ILEX ONCOLOGY, INC. ,  WEIS, Alexander ,  LOVE, Richard ,  MANGOLD, Gina

    Inventor： ILEX ONCOLOGY, INC.

    IPC: A61K31/335

    CPC classification number: A61K31/198 ,  A61K31/335 ,  A61K2300/00

    Abstract: Preparations comprising a single enantiomer or defined ratio of enantiomers of alphadifluoromethylornithine (DFMO) are provided for treating, preventing, controlling the growth of and/or reducing the risk of developing estrogen independent breast cancer or tumor. The preparations containing a single DFMO enantiomer or defined nonracemic ratio of DFMO enantiomers will provide an enhanced pharmacological activity relative to a preparation comprising racemic DFMO. Methods for treating a patient having estrogen independent breast cancer, which methods comprise administering DFMO alone or in combination with taxol, are also provided.

    Abstract translation: 提供了包含单一对映异构体或定义比例的对甲氧基甲基鸟氨酸（DFMO）的制剂，用于治疗，预防和/或降低发展与雌激素无关的乳腺癌或肿瘤的风险。 含有单一DFMO对映异构体或DFMO对映异构体定义的非微量比的制剂相对于包含外消旋DFMO的制剂将提供增强的药理学活性。 还提供了治疗患有雌激素不依赖性乳腺癌的患者的方法，该方法包括单独或与紫杉醇组合施用DFMO。

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