Cationic amphiphiles containing linkers derived from neutral or
positively charged amino acids
    1.
    发明授权
    Cationic amphiphiles containing linkers derived from neutral or positively charged amino acids 失效
    含有源自中性或带正电氨基酸的连接体的阳离子两亲物

    公开(公告)号:US5948925A

    公开(公告)日:1999-09-07

    申请号:US851917

    申请日:1997-05-06

    IPC分类号: C07J41/00 C07J9/00 C07J33/00

    CPC分类号: C07J41/0055

    摘要: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

    摘要翻译: 提供阳离子两亲物,其促进生物活性(治疗性)分子进入细胞。 还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。 根据本发明的实践可以递送到细胞中的治疗分子包括DNA,RNA和多肽。 本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。 关于基因治疗的治疗组合物,通常以与阳离子两亲物络合的质粒的形式提供DNA。

    Imidazole-containing cationic amphiphiles for intracellular delivery of
therapeutic molecules
    3.
    发明授权
    Imidazole-containing cationic amphiphiles for intracellular delivery of therapeutic molecules 失效
    含咪唑的阳离子两亲物用于细胞内递送治疗分子

    公开(公告)号:US5912239A

    公开(公告)日:1999-06-15

    申请号:US833370

    申请日:1997-04-04

    CPC分类号: A61K9/1272 C07J43/003

    摘要: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

    摘要翻译: 提供阳离子两亲物,其促进生物活性(治疗性)分子进入细胞。 还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。 根据本发明的实践可以递送到细胞中的治疗分子包括DNA,RNA和多肽。 本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。 关于基因治疗的治疗组合物,通常以与阳离子两亲物络合的质粒的形式提供DNA。

    Cationic amphiphiles containing amino acid or dervatized amino acid
groups for intracellular delivery of therapeutic molecules
    4.
    发明授权
    Cationic amphiphiles containing amino acid or dervatized amino acid groups for intracellular delivery of therapeutic molecules 失效
    含有氨基酸或衍生化氨基酸基团的阳离子两亲物用于治疗分子的细胞内递送

    公开(公告)号:US5767099A

    公开(公告)日:1998-06-16

    申请号:US546086

    申请日:1995-10-20

    摘要: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile. Novel and highly effective plasmid constructs are also disclosed, including those that are particularly effective at providing gene therapy for clinical conditions complicated by inflammation. Additionally, targeting of organs for gene therapy by intravenous administration of therapeutic compositions is described.

    摘要翻译: 提供了新的阳离子两亲物,其促进生物活性(治疗性)分子进入细胞。 两亲物含有衍生自类固醇的单亲或二烷基胺或烷基或酰基的亲脂基团; 和在生理pH下可质子化的阳离子基团,衍生自胺,烷基胺或多烷基胺。 还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。 根据本发明的实践可以递送到细胞中的治疗分子包括DNA,RNA和多肽。 本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。 关于基因治疗的治疗组合物,通常以与阳离子两亲物络合的质粒的形式提供DNA。 还公开了新型和高效的质粒构建体,包括在为炎症复杂的临床病症提供基因治疗方面特别有效的质粒构建体。 另外,描述了通过静脉内施用治疗组合物靶向用于基因治疗的器官。

    Cationic amphiphiles for intracellular delivery of therapeutic molecules
    5.
    发明授权
    Cationic amphiphiles for intracellular delivery of therapeutic molecules 失效
    阳离子两亲物用于细胞内递送治疗分子

    公开(公告)号:US5650096A

    公开(公告)日:1997-07-22

    申请号:US352479

    申请日:1994-12-09

    摘要: Novel cationic amphiphiles are provided that facilitate transport of biologically active molecules into cells. Typically, the amphiphiles contain lipophilic groups derived from steroids or from mono or dialkylamines, and two cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles, with or without colipids, and therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, polypeptides and low molecular weight organic compounds. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells.

    摘要翻译: 提供了新的阳离子两亲物,其促进生物活性分子进入细胞。 通常,两亲物含有衍生自类固醇或单或二烷基胺的亲脂基团,以及两种阳离子基团,其在生理pH下可质子化,衍生自胺,烷基胺或多烷基胺。 还提供了通常通过使一种或多种阳离子两亲物的分散体与或不与咔啉和治疗分子接触而制备的治疗组合物。 根据本发明的实践可以递送到细胞中的治疗分子包括DNA,RNA,多肽和低分子量有机化合物。 本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。

    Child-resistant/non-child-resistant closure
    8.
    发明授权
    Child-resistant/non-child-resistant closure 失效
    防儿童/非儿童防护闭合

    公开(公告)号:US4281771A

    公开(公告)日:1981-08-04

    申请号:US157534

    申请日:1980-06-09

    申请人: Craig S. Siegel

    发明人: Craig S. Siegel

    CPC分类号: B65D50/068 B65D50/041

    摘要: A child-resistant/non-child-resistant dual function double cap closure with incorporated means for over-ride of conventional normally disengaged torque couplings includes a hole formed in the top surface of the outer cap, a formed plug having a locking protuberance and removal ring, and a plurality of spaced stop lugs formed annularly on the top surface of the inner cap. The free and separate movement of the outer cap is prevented in either direction of rotation by the plug's insertion into the hole of the outer cap as to place the base of the plug in the space between the stop lugs of the inner cap rendering the cap non-child-resistant at the time of consumer purchase. The consumer may use the cap in a non-child-resistant mode or remove the plug thus converting the cap to a child-resistant mode.

    摘要翻译: 具有防止/不耐儿童的双功能双盖封闭件,其具有用于常规常规脱离扭矩联接器的过载的装置,包括形成在外盖顶表面中的孔,形成的塞子,其具有锁定突起和移除 环和在内盖的顶表面上环形地形成的多个间隔的止动凸耳。 外盖的自由和分离的运动通过插头插入外盖的孔中而在任何旋转方向上被阻止,以将插头的底部放置在内盖的止动凸耳之间的空间中, 在消费者购买时抗生素。 消费者可以以非儿童防护模式使用盖子,或者去除插头,从而将盖子转换为防儿童模式。

    Cationic amphiphiles containing spermine or spermidine cationic group
for intracellular delivery of therapeutic molecules
    10.
    发明授权
    Cationic amphiphiles containing spermine or spermidine cationic group for intracellular delivery of therapeutic molecules 失效
    含有精胺或亚精胺阳离子基团的阳离子两亲物用于细胞内递送治疗分子

    公开(公告)号:US5783565A

    公开(公告)日:1998-07-21

    申请号:US595375

    申请日:1996-02-01

    摘要: Novel cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. The amphiphiles contain lipophilic groups derived from steroids, from mono or dialkylamines, or from alkyl or acyl groups; and cationic groups, protonatable at physiological pH, derived from amines, alkylamines or polyalkylamines. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile. Novel and highly effective plasmid constructs are also disclosed, including those that are particularly effective at providing gene therapy for clinical conditions complicated by inflammation. Additionally, targeting of organs for gene therapy by intravenous administration of therapeutic compositions is described.

    摘要翻译: 提供了新的阳离子两亲物,其促进生物活性(治疗性)分子进入细胞。 两亲物含有衍生自类固醇的单亲或二烷基胺或烷基或酰基的亲脂基团; 和在生理pH下可质子化的阳离子基团,衍生自胺,烷基胺或多烷基胺。 还提供了通常通过使一种或多种阳离子两亲物的分散体与治疗分子接触而制备的治疗组合物。 根据本发明的实践可以递送到细胞中的治疗分子包括DNA,RNA和多肽。 本发明治疗组合物的代表性用途包括提供基因治疗以及向细胞递送反义多核苷酸或生物活性多肽。 关于基因治疗的治疗组合物,通常以与阳离子两亲物络合的质粒的形式提供DNA。 还公开了新型和高效的质粒构建体,包括在为炎症复杂的临床病症提供基因治疗方面特别有效的质粒构建体。 另外,描述了通过静脉内施用治疗组合物靶向用于基因治疗的器官。