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    ANTI-METASTATIC AGENTS PREDICATED UPON POLYAMINE MACROCYCLIC CONJUGATES
    2.
    发明申请
    ANTI-METASTATIC AGENTS PREDICATED UPON POLYAMINE MACROCYCLIC CONJUGATES 有权
    聚氨酯大分子结合剂预防的抗细菌剂

    公开(公告)号：US20150057361A1

    公开(公告)日：2015-02-26

    申请号：US14388851

    申请日：2013-03-13

    Applicant: Otto Phanstiel, IV ,  Aaron Muth

    Inventor： Otto Phanstiel, IV ,  Aaron Muth

    IPC: C07C211/17 ,  A61K45/06 ,  A61K31/132

    CPC classification number: C07C211/17 ,  A61K31/132 ,  A61K45/06 ,  C07C211/36 ,  C07C2601/18

    Abstract: Disclosed herein are novel motuporamine compounds that act as anti-metastatic agents with low toxicity and high anti-migration activity. The non-toxic, anti-metastatic agents may be given to patients with potential or actual metastatic cancers, such as pancreatic cancers, alone in combination with known and/or new therapies to help block the growth and spread of tumor(s).

    Abstract translation: 本文公开了作为具有低毒性和高抗迁移活性的抗转移剂的新型血浆胺化合物。 可以将具有潜在或实际转移性癌症（例如胰腺癌）的患者单独与已知和/或新疗法结合用于有助于阻止肿瘤生长和扩散的患者进行无毒的抗转移剂。

    ASSAYS AND METHODS FOR CELL PROLIFERATION-TARGETED TREATMENT THERAPIES
    4.
    发明申请
    ASSAYS AND METHODS FOR CELL PROLIFERATION-TARGETED TREATMENT THERAPIES 审中-公开
    细胞增殖指标治疗方法的测定和方法

    公开(公告)号：US20160299149A1

    公开(公告)日：2016-10-13

    申请号：US15074993

    申请日：2016-03-18

    Applicant: Otto Phanstiel, IV ,  Deborah Altomare ,  Laurence von Kalm

    Inventor： Otto Phanstiel, IV ,  Deborah Altomare ,  Laurence von Kalm

    IPC: G01N33/574 ,  A61K31/198 ,  A61K31/404 ,  C12Q1/68 ,  A61K31/137

    CPC classification number: G01N33/57496 ,  A61K31/404 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  C12Q2600/16 ,  C12Y306/03 ,  G01N33/57492 ,  G01N2333/4703

    Abstract: Assays are described which measure polyamine transport activity and markers associated with polyamine transport and metabolism. These data are then used for the selection of treatments using therapies which target polyamine transport and polyamine metabolism. The assay includes a substrate to which a protein-containing cell sample can bind, a solution comprising a first antibody specific against ATP13A3, wherein the first antibody is configured to bind to ATP13A3 protein on the substrate, a solution comprising a second antibody specific against the first antibody, the second antibody comprising an enzyme linked thereto, wherein the second antibody is configured to bind to the first antibody. The assay further includes a substrate specific to the enzyme, wherein upon combining the substrate and the enzyme, the amount of enzyme in the solution can be identified, wherein said amount of enzyme identified is proportional to the amount of ATP13A3 protein in the sample, wherein said ATP13A3 protein is indicative of polyamine transport in the cells of the sample. In addition, primary antibodies covalently attached to respective fluorophores can be used to directly measure the relative expression levels of these biomarkers in histological samples. In addition, several biomarkers are described which allow for therapy selection based upon the expression and relative ratios of specific proteins associated with polyamine transport (c-myc, ATP13A3 Cav-2, and Cav-1 as well as c-Raf).

    Abstract translation: 描述了测定多胺转运活性和与多胺转运和代谢相关的标记的测定。 然后将这些数据用于使用靶向多胺转运和多胺代谢的疗法的治疗选择。 所述测定法包括含有蛋白质的细胞样品可以结合的底物，包含针对ATP13A3特异性的第一抗体的溶液，其中所述第一抗体配置为与所述底物上的ATP13A3蛋白结合，所述溶液包含针对所述底物的第二抗体 第一抗体，所述第二抗体包含与其连接的酶，其中所述第二抗体被配置为结合所述第一抗体。 该测定还包括对酶特异的底物，其中在组合底物和酶时，可以鉴定溶液中的酶的量，其中所鉴定的酶的量与样品中ATP13A3蛋白的量成比例，其中 所述ATP13A3蛋白表明样品细胞中的多胺转运。 此外，共价连接到相应荧光团的一抗可用于直接测量组织学样品中这些生物标志物的相对表达水平。 此外，描述了几种基于与多胺转运（c-myc，ATP13A3Cav-2和Cav-1以及c-Raf）相关的特异性蛋白质的表达和相对比例进行治疗选择的生物标志物。

    FLUORESCENT CYTOTOXIC COMPOUNDS SPECIFIC FOR THE CELLULAR POLYAMINE TRANSPORT SYSTEM
    5.
    发明申请
    FLUORESCENT CYTOTOXIC COMPOUNDS SPECIFIC FOR THE CELLULAR POLYAMINE TRANSPORT SYSTEM 有权
    细胞聚氨酯运输系统的荧光细胞毒素化合物

    公开(公告)号：US20130337494A1

    公开(公告)日：2013-12-19

    申请号：US13835708

    申请日：2013-03-15

    Applicant: Otto Phanstiel, IV

    Inventor： Otto Phanstiel, IV

    IPC: G01N21/64

    CPC classification number: G01N21/6486 ,  C07C255/58 ,  C07C2603/24 ,  G01N33/5008 ,  G01N33/533 ,  G01N33/574 ,  G01N33/582

    Abstract: Cyano-substituted anthracene containing polyamines were synthesized and shown to be efficient polyamine transporter ligands. Moreover, these compounds (3 and 4) had improved fluorescence properties over previously known anthryl-polyamine conjugates, which facilitated their intracellular trafficking by confocal microscopy and fluorescence methods. These cytotoxic fluorescent agents may find use as molecular probes which traffic into cells via the polyamine transport system and may also be viable anticancer drugs which are readily quantified in human tissues due to their excellent fluorescence properties: (excitation: λ405 nm) and emission (420 nm) occurs in the visible light range. The ability to excite and emit in the visible range provides an advantage to these probes as these wavelengths are considered non-toxic to human cells (versus ultraviolet mediated excitations, λ

    Abstract translation: 合成含氰基取代的含多胺的多胺，显示为有效的多胺转运体配体。 此外，这些化合物（3和4）具有比先前已知的蒽基 - 聚胺共轭物更好的荧光性能，这促进了它们通过共焦显微镜和荧光方法的细胞内运输。 这些细胞毒性荧光剂可以用作通过多胺转运系统进入细胞的分子探针，并且还可以是由人体组织中容易定量的活的抗癌药物，因为它们具有优异的荧光性质：（激发：λ405nm）和发射（420 nm）出现在可见光范围内。 在可见光范围内激发和发射的能力为这些探针提供了优势，因为这些波长被认为对人体细胞无毒（相对于紫外线介导的激发，λ<400nm），可见光激光器的购买和操作成本较低 UV激光源。

    Lipophilic polyamines providing enhanced intracellular delivery of agents by a polyamine transport system
    6.
    发明授权
    Lipophilic polyamines providing enhanced intracellular delivery of agents by a polyamine transport system 有权
    亲脂性多胺通过多胺转运系统提供增强的细胞内递送的药剂

    公开(公告)号：US07910363B1

    公开(公告)日：2011-03-22

    申请号：US12113970

    申请日：2008-05-02

    Applicant: Otto Phanstiel, IV ,  Ken Teter

    Inventor： Otto Phanstiel, IV ,  Ken Teter

    IPC: C12N15/00 ,  A01N63/00

    CPC classification number: C12N15/87

    Abstract: Polyamine cationic lipids have been synthesized that have the ability to be transported into cells having an active polyamine transport system. Accordingly, these lipids may be conjugated with various agents and, thereby, act as vectors for transporting the agent into the cell aided by the cell's own polyamine transport system. A method of delivering an agent into a cell includes associating the agent with a polyamine cationic lipid selected from compounds 25, 26, 27, 28, their pharmaceutically acceptable salts and combinations thereof and contacting the cell therewith.

    Abstract translation: 已经合成了具有能够转运到具有活性多胺转运体系的细胞的能力的多胺阳离子脂质。 因此，这些脂质可以与各种试剂缀合，从而作为用于将细胞运送到由细胞本身的多胺转运系统辅助的细胞中的载体。 将试剂递送到细胞中的方法包括将试剂与选自化合物25,26,27,28的多胺阳离子脂质，其药学上可接受的盐及其组合缔合并使细胞接触。

    POLYAMINE TRANSPORTER SELECTIVE COMPOUNDS AS ANTI CANCER AGENTS
    10.
    发明申请
    POLYAMINE TRANSPORTER SELECTIVE COMPOUNDS AS ANTI CANCER AGENTS 有权
    聚氨酯运输选择性化合物作为抗癌剂

    公开(公告)号：US20140057989A1

    公开(公告)日：2014-02-27

    申请号：US13953667

    申请日：2013-07-29

    Applicant: Otto Phanstiel, IV

    Inventor： Otto Phanstiel, IV

    IPC: C07C211/31 ,  C07C211/27 ,  C07C211/30

    CPC classification number: C07C211/27 ,  C07C211/30 ,  C07C211/31 ,  C07C2603/24 ,  C09B1/00

    Abstract: Several aromatic hydrocarbons di-substituted with a polyamine are described according to formulas selected from compounds 4, 7, 10, 15 and pharmaceutically acceptable salts thereof. The novel dimeric polyamines of the present invention demonstrate enhanced penetration into cells having an upregulated polyamine transport system, such as various types of cancer cells. The disclosed aromatic polyamine dimers provide highly efficient drugs for targeting cancer cells with active polyamine transporters.

    Abstract translation: 根据选自化合物4,7,10,15的式及其药学上可接受的盐描述了被多胺二取代的若干芳烃。 本发明的新型二聚多胺显示增强的渗透进入具有上调多胺转运系统的细胞，例如各种类型的癌细胞。 所公开的芳族聚胺二聚体提供了用活性多胺转运蛋白靶向癌细胞的高效药物。

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