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    METHODS OF PROMOTING UPTAKE AND NUCLEAR ACCUMULATION OF POLYAMIDES IN EUKARYOTIC CELLS
    1.
    发明申请
    METHODS OF PROMOTING UPTAKE AND NUCLEAR ACCUMULATION OF POLYAMIDES IN EUKARYOTIC CELLS 审中-公开
    促肾上腺皮质激素摄取和核聚集的方法

    公开(公告)号：WO03041128A2

    公开(公告)日：2003-05-15

    申请号：PCT/US0235587

    申请日：2002-11-07

    Applicant: PHARMACIA CORP ,  CROWLEY KATHLEEN S ,  BASHKIN JAMES K ,  SCHWEITZER BARBARA A ,  PHILLION DENNIS P

    Inventor： CROWLEY KATHLEEN S ,  BASHKIN JAMES K ,  SCHWEITZER BARBARA A ,  PHILLION DENNIS P

    IPC: C12N1/00 ,  A61K31/275 ,  A61K31/40 ,  A61K31/495 ,  A61K38/00 ,  A61K45/00 ,  A61K48/00 ,  A61P43/00 ,  C12N15/63 ,  H01L

    CPC classification number: C12N15/63 ,  A61K31/275 ,  A61K31/40 ,  A61K31/495

    Abstract: A method for enhancing cellular uptake and redistributing gene regulating polyamides from the extranuclear areas in eukaryotic cells to the nucleus thereof. The method consists of administering to the eukaryotic cells a molecular trafficking compound. The administered molecular trafficking compound affects cellular pathways and mechanisms that accumulate polyamides in cytoplasmic vessicles and/or efflux polyamides from the intracellular regions of cell. The method also includes modifying polyamides to contain negatively-charged or acidic moieties wherein the moieties inhibit the accumulation of polyamides in cellular lysosomes. By affecting the cellular pathways and mechanisms, the polyamides are redistributed throughout the cell, whereby nuclear accumulation of the polyamides is enhanced.

    Abstract translation: 一种用于增强细胞摄取并将基因调节聚酰胺从真核细胞的核外区重新分布到其核的方法。 该方法包括向真核细胞施用分子运输化合物。 所施用的分子运输化合物影响细胞途径和机制，其在细胞质容器中积聚聚酰胺和/或从细胞的细胞内区域流出聚酰胺。 该方法还包括改性聚酰胺以含有带负电荷或酸性部分，其中所述部分抑制聚酰胺在细胞溶酶体中的积聚。 通过影响细胞途径和机制，聚酰胺在整个细胞中重新分布，从而增强了聚酰胺的核聚集。

    COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THE MINOR GROOVE OF DSDNA
    3.
    发明申请
    COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THE MINOR GROOVE OF DSDNA 审中-公开
    具有融合的双链体系的化合物用于与DSDNA的小型细胞结合

    公开(公告)号：WO2004099131A3

    公开(公告)日：2005-02-17

    申请号：PCT/US2004013285

    申请日：2004-04-29

    Applicant: PHARMACIA CORP ,  PHILLION DENNIS P ,  BASHKIN JAMES K

    Inventor： PHILLION DENNIS P ,  BASHKIN JAMES K

    IPC: C07D20060101 ,  C07D235/04 ,  C07D401/00 ,  C07D403/02 ,  C07H19/04 ,  C07H21/04 ,  C12Q1/68

    CPC classification number: C07D417/14 ,  C07D403/14 ,  C07D471/04 ,  C07H19/04 ,  C07H21/04

    Abstract: The present invention is directed to the means by which to alter the binding affinity and/or specificity of a compound with a sequence of DNA in the minor groove of a double-strand thereof. More particularly, the present invention is directed to a synthetic and/or non-naturally occurring compound (e.g., an analog of a polyamide oligomer or polymer) which contains at least one hydrogen bond donor moiety and at least one hydrogen bond acceptor moiety, wherein the latter moiety or "building block" has a fused, bicyclic structure which is heteroaromatic, said structure having a heteroatom therein which acts as a hydrogen bond acceptor to bind guanine in the minor groove of the dsDNA sequence, and which is incapable of forming a tautomer. In one particular embodiment of the synthetic and/or non-naturally occurring compound, the fused, bicyclic structure occupies an initial or first terminal position within the compound.

    Abstract translation: 本发明涉及在双链的小槽中改变化合物与DNA序列的结合亲和力和/或特异性的方法。 更具体地，本发明涉及含有至少一个氢键供体部分和至少一个氢键受体部分的合成和/或非天然存在的化合物（例如，聚酰胺低聚物或聚合物的类似物），其中 后一部分或“构建块”具有杂芳族化合物的稠合双环结构，所述结构在其中具有杂原子，其作为氢键受体以在dsDNA序列的小沟中结合鸟嘌呤，并且不能形成 互变异构体。 在合成和/或非天然存在的化合物的一个具体实施方案中，稠合双环结构占据化合物内的初始或第一末端位置。

    COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THEMINOR GROOVE OF DSDNA
    6.
    发明专利
    COMPOUNDS HAVING A FUSED, BICYCLIC MOIETY FOR BINDING TO THEMINOR GROOVE OF DSDNA 未知

    公开(公告)号：CA2531869A1

    公开(公告)日：2004-11-18

    申请号：CA2531869

    申请日：2004-04-29

    Applicant: PHARMACIA CORP

    Inventor： BASHKIN JAMES K ,  PHILLION DENNIS P

    IPC: C07H19/04 ,  C07D20060101 ,  C07D235/04 ,  C07D401/00 ,  C07D403/02 ,  C07H21/04 ,  C12Q1/68

    Abstract: The present invention is directed to the means by which to alter the binding affinity and/or specificity of a compound with a sequence of DNA in the mino r groove of a double-strand thereof. More particularly, the present invention is directed to a synthetic and/or non-naturally occurring compound (e.g., an analog of a polyamide oligomer or polymer) which contains at least one hydrogen bond donor moiety and at least one hydrogen bond acceptor moiety, wherein the latter moiety or "building block" has a fused, bicyclic structur e which is heteroaromatic, said structure having a heteroatom therein which ac ts as a hydrogen bond acceptor to bind guanine in the minor groove of the dsDNA sequence, and which is incapable of forming a tautomer. In one particular embodiment of the synthetic and/or non-naturally occurring compound, the fused, bicyclic structure occupies an initial or first terminal position within the compound.

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