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    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。

    DNA vaccines for eliciting a mucosal immune response
    6.
    发明授权
    DNA vaccines for eliciting a mucosal immune response 失效
    用于引发粘膜免疫应答的DNA疫苗

    公开(公告)号：US6110898A

    公开(公告)日：2000-08-29

    申请号：US862632

    申请日：1997-05-23

    申请人： Robert W. Malone ,  Jill G. Malone

    发明人： Robert W. Malone ,  Jill G. Malone

    IPC分类号： C07K14/005 ,  C07K14/195 ,  C12N15/86 ,  A61K48/00 ,  C12Q1/70 ,  C17N15/00

    CPC分类号： C07K14/005 ,  C07K14/195 ,  C12N15/86 ,  A61K2039/51 ,  C12N2770/36143

    摘要： The invention consists of a method for inducing production of a mucosal immune response in a host by administration of an antigen-encoding polynucleotide preparation, comprising DNA or RNA encoding an antigenic epitope to a mucosal inductor site in the mucosal tissue of the host. Naked DNA may be administered directly to mucosa, for instance in saline drops, or in a recombinant gene expression vector. Preferably, the recombinant gene expression vectors are not capable of replication or dessimination. The invention also includes the use of live viral vaccines wherein the viruses include immunostimulatory polynucleotides of the invention. According to a preferred method of the invention, a target protein antigen is administered through its expression by a recombinant gene expression vector.

    摘要翻译： 本发明包括通过向宿主的粘膜组织中的粘膜感染部位施用包含编码抗原表位的DNA或RNA的抗原编码多核苷酸制剂来诱导宿主中产生粘膜免疫应答的方法。 裸DNA可以直接施用于粘膜，例如在盐水中或重组基因表达载体中。 优选地，重组基因表达载体不能复制或被确定。 本发明还包括使用活病毒疫苗，其中病毒包括本发明的免疫刺激多核苷酸。 根据本发明的优选方法，通过重组基因表达载体的表达来施用靶蛋白抗原。

    Formulations and methods for generating active cytofectin: polynucleotide transfection complexes
    7.
    发明授权
    Formulations and methods for generating active cytofectin: polynucleotide transfection complexes 失效
    产生活性细胞分裂素的制剂和方法：多核苷酸转染复合物

    公开(公告)号：US5925623A

    公开(公告)日：1999-07-20

    申请号：US679971

    申请日：1996-07-15

    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 ,  A01N43/04

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

    摘要： In the generation of cytofectin:polynucleotide complexes for transfection of cells, formulations, counterions, and reaction conditions for maximizing the transfection include using a cationic amine compound 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 oxyanion or halide counterion.

    摘要翻译： 细胞增生素的产生：用于转染细胞的多核苷酸复合物，用于使转染最大化的制剂，抗衡离子和反应条件包括使用具有以下通式结构的阳离子胺化合物：其中R 4和R 5是选中的一对相同或不同的脂酰基部分 由烷基，烯基，炔基，烷酰基，烯酰基或炔酰基组成的组，并且对于R 1，R 2和R 3，至少两个羟基化，含醚或含酰氧基的烷基，烯基或炔基或至少一个 胺键合的含卤素部分，其选自卤代烷基，烯基或炔基，或至少一种含卤素部分的选自卤代烷基，烯基或炔基的部分和至少一个羟基化的 醚，或含酰氧基的烷基，链烯基或炔基，X-是氧阴离子或卤化物的抗衡离子。