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    Amino acid and peptide conjugates of amiloride and methods of use thereof
    2.
    发明授权
    Amino acid and peptide conjugates of amiloride and methods of use thereof 有权
    阿米洛利的氨基酸和肽缀合物及其使用方法

    公开(公告)号：US07863415B2

    公开(公告)日：2011-01-04

    申请号：US11040831

    申请日：2005-01-21

    申请人： Fredric A. Gorin ,  Michael H. Nantz

    发明人： Fredric A. Gorin ,  Michael H. Nantz

    IPC分类号： A61K38/04 ,  A61K38/00

    CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/542 ,  A61K47/555 ,  A61K47/64

    摘要： The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the amiloride conjugates of the present invention for treating cancer or a central nervous system disease or disorder or for preventing or reducing ischemia-reperfusion injury. Further, kits are provided for the treatment of a central nervous system disease or disorder or for the prevention or reduction of ischemia-reperfusion injury using the amiloride conjugates of the present invention.

    摘要翻译： 本发明提供了包含阿米洛利氨基酸和肽缀合物的组合物。 还提供了有效的方法用于施用本发明的用于治疗癌症或中枢神经系统疾病或病症或用于预防或减少缺血再灌注损伤的阿米洛利共轭物。 此外，提供了用于治疗中枢神经系统疾病或病症或使用本发明的阿米洛利共轭物预防或减少缺血再灌注损伤的试剂盒。

    Polyfunctional cationic cytofectins, formulations and methods for generating active cytofectin: polynucleotide transfection complexes
    3.
    发明授权
    Polyfunctional cationic cytofectins, formulations and methods for generating active cytofectin: polynucleotide transfection complexes 失效
    多功能阳离子细胞增生素，用于产生活性细胞色素的制剂和方法：多核苷酸转染复合物

    公开(公告)号：US5824812A

    公开(公告)日：1998-10-20

    申请号：US710350

    申请日：1996-09-17

    申请人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

    发明人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

    IPC分类号： A61K9/127 ,  A61K47/48 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08 ,  C07H21/00 ,  C07C101/00

    CPC分类号： C07H21/00 ,  A61K47/48023 ,  A61K47/48046 ,  A61K9/1272 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08

    摘要： Amine containing compounds and their use in the generation of cytofectin:polynucleotide complexes for transfection of cells, formulations, counterions, and reaction conditions for maximizing the transfection include using cationic amine compounds that have the general structure: ##STR1## wherein R.sub.4 and R.sub.5 are a pair of same or different lipoyl moieties selected from a group consisting of an alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, or alkynoyl groups and for R.sub.1, R.sub.2, and R.sub.3 at least two are hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl groups or at least one amine bonded halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group or a mixture of at least one halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group and at least one hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl group, and X.sup.- is an oxyanion or halide counterion or ##STR2## wherein a, b, or d are the same or different and are from 0-10, usually between 0 and 3, preferably 0 or 1; R.sub.4 and R.sub.5 are the same or different with each an alkyl group, an alkenyl group, an alkynyl group, or an alkyl, alkenyl, or alkynyl containing acyl group; R.sub.8, R.sub.9, or R.sub.10 are the same or different with each an alkyl, alkenyl, or alkynyl group or halogenated alkyl, alkenyl, or alkynyl group as long as one is halogen containing; and X.sup.- is an anion, usually an oxyanion or halide counterion.

    摘要翻译： 含胺化合物及其在产生细胞分裂素中的用途：用于转染细胞的多核苷酸复合物，制剂，抗衡离子和用于使转染最大化的反应条件包括使用具有以下通用结构的阳离子胺化合物：其中R 4和R 5为 一对相同或不同的选自烷基，烯基，炔基，烷酰基，烯酰基或炔酰基的脂酰基部分，对于R1，R2和R3至少两个是羟基化的，含醚的或含酰氧基的烷基，烯基 ，或炔基或至少一个与胺键合的含卤素的部分，其选自卤代烷基，烯基或炔基，或至少一种含卤素部分的混合物，所述部分选自卤代烷基，烯基， 或炔基和至少一个羟基化的含醚或含酰氧基的烷基，烯基或炔基，X是氧阴离子或卤化物 其中a，b或d相同或不同，为0-10，通常为0至3，优选为0或1; R4和R5与烷基，烯基，炔基或含酰基的烷基，链烯基或炔基相同或不同; R8，R9或R10与烷基，烯基或炔基或卤代烷基，烯基或炔基相同或不同，只要一个为含卤素; X-是阴离子，通常是氧阴离子或卤离子抗衡离子。

    NANOPARTICLES FOR DRUG DELIVERY
    5.
    发明申请
    NANOPARTICLES FOR DRUG DELIVERY 有权
    用于药物递送的纳米颗粒

    公开(公告)号：US20150374849A1

    公开(公告)日：2015-12-31

    申请号：US14766726

    申请日：2014-02-07

    申请人： Ralph J. KNIPP ,  Michael H. NANTZ ,  UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.

    发明人： Ralph J. KNIPP ,  Michael H. NANTZ

    IPC分类号： A61K47/48

    CPC分类号： A61K47/6923 ,  A61K41/0028 ,  A61K47/52 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  A61K47/6929

    摘要： The invention provides nanoparticles, methods for making nanoparticles, and methods for using nanoparticles. An important attribute of a drug delivery system is its ability to allow for spatial and temporal regulated drug release, thereby minimizing side effects and improving therapeutic efficacy of conventional pharmaceuticals. Iron oxide nanoparticles (NPs), specifically Fe304 nanoparticles, possess many appropriate qualities that make them a viable choice for drug delivery.

    摘要翻译： 本发明提供纳米颗粒，制备纳米颗粒的方法和使用纳米颗粒的方法。 药物递送系统的一个重要特征是其能够允许空间和时间调节的药物释放，从而最小化副作用并改善常规药物的治疗功效。 氧化铁纳米粒子（NPs），特别是Fe304纳米粒子，具有许多合适的品质，使其成为药物递送的可行选择。

    Extracellular superoxide dismutase (EC-SOD) gene delivery to prevent oxidative injury
    7.
    发明申请
    Extracellular superoxide dismutase (EC-SOD) gene delivery to prevent oxidative injury 审中-公开
    细胞外超氧化物歧化酶（EC-SOD）基因传递，以防止氧化损伤

    公开(公告)号：US20080125382A1

    公开(公告)日：2008-05-29

    申请号：US11040489

    申请日：2005-01-20

    申请人： Jian Wu ,  Michael H. Nantz

    发明人： Jian Wu ,  Michael H. Nantz

    IPC分类号： A61K31/70 ,  A01N1/00 ,  A61N1/30 ,  A61P43/00 ,  C07H21/04 ,  C12N15/87

    CPC分类号： A01N1/0226 ,  A61K38/446 ,  C12N9/0089 ,  C12Y115/01001

    摘要： The present invention relates to compositions and methods for preventing oxidative injury to a cell. The compositions comprise a lipid formulation and a recombinant nucleic acid encoding an extracellular superoxide dismutase (EC-SOD), which upon transfection of a target cell is expressed by the cell and acts as an enzymatic antioxidant. The invention also provides for an isolated organ treated with the claimed composition or method.

    摘要翻译： 本发明涉及用于预防细胞氧化损伤的组合物和方法。 组合物包含脂质制剂和编码细胞外超氧化物歧化酶（EC-SOD）的重组核酸，其在转染靶细胞时由细胞表达并用作酶促抗氧化剂。 本发明还提供了用所要求保护的组合物或方法处理的分离的器官。

    Method for nucleic acid transfection of cells
    8.
    发明授权
    Method for nucleic acid transfection of cells 失效
    核酸转染细胞的方法

    公开(公告)号：US06372722B1

    公开(公告)日：2002-04-16

    申请号：US09487089

    申请日：2000-01-19

    申请人： Michael J. Bennett ,  Stephan S. Rothman ,  Michael H. Nantz

    发明人： Michael J. Bennett ,  Stephan S. Rothman ,  Michael H. Nantz

    IPC分类号： A61K4800

    CPC分类号： A61K48/00 ,  C12N15/87

    摘要： The present invention describes methods for introducing nucleic acids into a target cell using a transition metal enhancer. A mixture containing nucleic acid and a transition metal enhancer is exposed to cells. The nucleic acid is taken up into the interior of the cell with the aid of the transition metal enhancer. Since nucleic acids can encode a gene, the method can be used to replace a missing or defective gene in the cell. The method can also be used to deliver exogenous nucleic acids operatively coding for proteins that are secreted or released from target cells, thus resulting in a desired biological effect outside the cell. Alternatively, the methods of the present invention can be used to deliver exogenous nucleic acids into a target cell that are capable of regulating the expression of a predetermined endogenous gene. This can be accomplished by encoding the predetermined endogenous gene on the nucleic acid or by encoding the nucleic acid with a sequence that is the Watson-Crick complement of the mRNA corresponding to the endogenous gene.

    摘要翻译： 本发明描述了使用过渡金属增强剂将核酸引入靶细胞的方法。 含有核酸和过渡金属增强剂的混合物暴露于细胞。 借助过渡金属增强剂将核酸吸收到细胞的内部。 由于核酸可以编码基因，所以该方法可用于替代细胞中缺失或缺陷的基因。 该方法还可用于递送外源核酸，可操作地编码从靶细胞分泌或释放的蛋白质，从而在细胞外产生所需的生物效应。 或者，本发明的方法可以用于将外源核酸递送到能够调节预定内源基因表达的靶细胞中。 这可以通过在核酸上编码预定的内源基因或通过用对应于内源基因的mRNA的Watson-Crick补体的序列编码核酸来实现。

    Polyfunctional cationic cytofectins
    9.
    发明授权
    Polyfunctional cationic cytofectins 失效
    多官能阳离子细胞增生素

    公开(公告)号：US5869715A

    公开(公告)日：1999-02-09

    申请号：US534471

    申请日：1995-09-27

    申请人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam

    发明人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam

    IPC分类号： A61K9/127 ,  A61K47/48 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08 ,  C07H21/00 ,  C07C101/00

    CPC分类号： C07H21/00 ,  A61K47/48023 ,  A61K47/48046 ,  A61K9/1272 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08

    摘要： For use in transporting biologically active species into and through membrane barriers, a cationic amine compound is utilized that has the general structure: ##STR1## wherein R.sub.4 and R.sub.5 are a pair of same or different lipoyl moieties selected from a group consisting of an alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, or alkynoyl groups and for R.sub.1 R.sub.2, and R.sub.3 at least two are hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl groups or at least one amine bonded halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group or a mixture of at least one halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group and at least one hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl group, and X.sup.- is an anion.

    摘要翻译： 为了用于将生物活性物质输送到膜屏障中并通过膜屏障，使用具有以下一般结构的阳离子胺化合物：其中R 4和R 5是一对相同或不同的脂酰基部分，其选自烷基， 烯基，炔基，烷酰基，烯酰基或炔炔基，对于R 1 R 2，并且R 3至少两个被羟基化，含醚或含酰氧基的烷基，烯基或炔基或至少一个与胺键合的含卤素的部分， 由卤代烷基，烯基或炔基组成，或至少一种选自卤代烷基，烯基或炔基的含卤素部分和至少一个羟基化的，含醚的或含酰氧基的烷基的混合物， 烯基或炔基，X-是阴离子。

    Site specific fluorescence and contrast marker for same
    10.
    发明授权
    Site specific fluorescence and contrast marker for same 有权
    场地特异性荧光和对比度标记相同

    公开(公告)号：US08758727B2

    公开(公告)日：2014-06-24

    申请号：US12935336

    申请日：2009-03-31

    申请人： Kyung A. Kang ,  Michael H. Nantz

    发明人： Kyung A. Kang ,  Michael H. Nantz

    IPC分类号： A61B5/00 ,  C12Q1/02

    CPC分类号： A61K49/0065 ,  A61K47/54 ,  A61K47/6923 ,  A61K49/0034

    摘要： A contrast marker for indicating a presence of a target cell in an environment comprises a fluorophore, an NMP, and a short spacer and a long spacer linking the fluorophore to the NMP. The short spacer holds the fluorophore at a quenching distance from the NMP and the long spacer holds the fluorophore at a fluorescence enhancing distance from the NMP. The short spacer is configured to be cleaved by a molecule characterizing the target cells.

    摘要翻译： 用于指示环境中靶细胞存在的对比标记物包括荧光团，NMP和短间隔物以及将荧光团连接到NMP的长间隔物。 短间隔物将荧光团保持在与NMP的淬灭距离处，并且长间隔物使荧光团保持与NMP的荧光增强距离。 短间隔物被构造成被表征靶细胞的分子裂解。