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    Programmable genotoxic agents and uses therefor
    13.
    发明授权
    Programmable genotoxic agents and uses therefor 失效
    可编程的遗传毒理剂及其用途

    公开(公告)号：US07169611B2

    公开(公告)日：2007-01-30

    申请号：US10299029

    申请日：2002-11-18

    申请人： John M. Essigmann ,  Robert G. Croy ,  Kevin J. Yarema ,  Marshall Morningstar

    发明人： John M. Essigmann ,  Robert G. Croy ,  Kevin J. Yarema ,  Marshall Morningstar

    IPC分类号： C12N15/00 ,  C12N15/01 ,  C12Q1/00 ,  C12Q1/68 ,  C07J1/00 ,  C07H21/00

    CPC分类号： A61K47/64 ,  A61K47/55 ,  A61K47/554 ,  A61K47/557

    摘要： The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.

    摘要翻译： 本文公开的组合物和方法提供异源双功能可编程遗传毒性化合物，其可被设计为杀死异源细胞群体中存在的所选细胞。 本发明化合物包含对细胞DNA造成损害的第一药剂和吸引大分子细胞成分例如蛋白质的第二药剂，其又将基因组病变屏蔽修复。 因此，未修复的病变在细胞基因组中持续存在，并有助于所选细胞的死亡。 相比之下，缺乏细胞成分的非选择细胞中形成的病变是非屏蔽的，因此被修复。 结果，本文所述的化合物对非选择性细胞的毒性较小。 本发明的化合物可被设计成引起转化细胞，病毒感染细胞等的选择性杀伤。

    Aminopiperidine Quinolines and Their Azaisosteric Analogues with Antibacterial Activity
    15.
    发明申请
    Aminopiperidine Quinolines and Their Azaisosteric Analogues with Antibacterial Activity 审中-公开
    氨基哌啶喹啉及其具有抗菌活性的阿片类兴奋剂类似物

    公开(公告)号：US20090131444A1

    公开(公告)日：2009-05-21

    申请号：US11914799

    申请日：2006-05-23

    申请人： Folkert Reck ,  Marshall Morningstar ,  Hajnalka Hartl

    发明人： Folkert Reck ,  Marshall Morningstar ,  Hajnalka Hartl

    IPC分类号： A61K31/517 ,  A61K31/4709 ,  A61K31/502 ,  A61K31/4745 ,  A61K31/445 ,  C07D475/02 ,  C07D471/02 ,  C07D403/02 ,  C07D401/02 ,  A61K31/525

    CPC分类号： C07D471/04 ,  C07D491/04

    摘要： The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.

    摘要翻译： 本发明涉及显示抗菌活性的化合物，其制备方法，含有它们作为活性成分的药物组合物，它们作为药物的用途及其在制备用于治疗温血细菌感染的药物中的用途 动物如人类。 特别地，本发明涉及可用于治疗温血动物如人的细菌感染的化合物，更具体地涉及这些化合物在制备用于治疗温血动物细菌感染的药物中的用途，例如 人类。