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    • 2. 发明申请
    • COVALENT POLAR LIPID CONJUGATES WITH BIOLOGICALLY-ACTIVE COMPOUNDS FOR USE IN SALVES
    • 具有生物活性化合物的共价极性脂质与SALVES一起使用
    • WO1998003204A1
    • 1998-01-29
    • PCT/US1996012124
    • 1996-07-23
    • OREGON HEALTH SCIENCES UNIVERSITY
    • OREGON HEALTH SCIENCES UNIVERSITYYATVIN, Milton, B.STOWELL, Michael, H., B.
    • A61K47/48
    • A61K47/62A61K47/544
    • This invention herein describes a method of facilitating the entry of drugs into cells and tissues at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative, antibiotic, antimycotic, antiviral and antineoplastic drugs, in particular in combination with a multiplicity of other emollients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of such agents through the epidermis for treatment of skin diseases and other disorders.
    • 本发明在此描述了一种促进药物进入细胞和组织的药学上有用水平的方法,还涉及将药物靶向细胞内的特定细胞器的方法。 这种极性脂质/药物共轭靶向发明体现了其他药物靶向方法的进步,因为通过该方法,细胞内药物浓度可达到比其它药物浓度高数量级的水平。 此外,它通过使治疗剂被引导到某些细胞内结构来改善药物递送过程。 该技术适用于抗增生,抗生素,抗真菌,抗病毒和抗肿瘤药物,特别是与多种其他润肤剂和药剂组合以组合局部活性物质如药膏,以快速有效地引入这些药剂通过 用于治疗皮肤病和其他疾病的表皮。
    • 8. 发明申请
    • A cDNA CLONE ENCODING A HUMAN NOREPINEPRHINE TRANSPORTER
    • A cDNA克隆编码人类肾上腺素转运蛋白
    • WO1992017568A1
    • 1992-10-15
    • PCT/US1992001376
    • 1992-02-20
    • OREGON HEALTH SCIENCES UNIVERSITY
    • OREGON HEALTH SCIENCES UNIVERSITYAMARA, Susan, G.PACHOLCZYK, TadeuszBLAKELY, Randy, D.
    • C12N05/10
    • C07K14/70571
    • A cDNA encoding human norepinephrine transporter isolated from human neuroblastoma cells is disclosed. Determination of the nucleotide sequence thereof permitted a putative amino-acid sequence of the transporter protein to be determined. Mammalian cells transfected with the cDNA produced an mRNA species similar in size to that produced by norepinephrine-producing neurons. Such transfected cells also became capable of norepinephrine uptake. The uptake was inhibitable by various uptake-inhibiting drugs, including cocaine, to a degree similar to the effect of such drugs on noradrenergic neurons. The cloned cDNA makes possible well-controlled studies of transporter function in non-neuronal cells without the obfuscating influence of other transporters in the same cells. Such studies include the relative effects of various drugs such as antidepressants.
    • 公开了编码从人神经母细胞瘤细胞分离的人去甲肾上腺素转运蛋白的cDNA。 其核苷酸序列的确定允许确定转运蛋白的推定氨基酸序列。 用cDNA转染的哺乳动物细胞产生与去甲肾上腺素产生的神经元产生的大小相似的mRNA。 这样的转染细胞也能够去甲肾上腺素摄取。 各种吸收抑制药物(包括可卡因)的吸收可以与类似药物对去甲肾上腺素能神经元的作用类似。 克隆的cDNA使得在非神经元细胞中转运蛋白功能的良好控制研究成为可能,而没有其他转运蛋白在相同细胞中的混淆影响。 这些研究包括各种药物如抗抑郁药的相对作用。
    • 9. 发明申请
    • COVALENT POLAR LIPID CONJUGATES FOR TARGETING
    • 有价值的极乐团队
    • WO1998017325A2
    • 1998-04-30
    • PCT/US1997019486
    • 1997-10-27
    • OREGON HEALTH SCIENCES UNIVERSITYYATVIN, Milton, B.STOWELL, Michael, H., B.MEREDITH, Michael, J.
    • OREGON HEALTH SCIENCES UNIVERSITY
    • A61K97/48
    • C07H19/06A61K31/00A61K47/543A61K47/544B82Y5/00C07H19/10
    • This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmicokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods known in the prior art, because the invention provides drug concentrations in such physiologically protected sites that can reach therapeutically-effective levels after administration of systemic levels much lower than are currently administered to achieve a therapeutic dose. This technology is appropriate for use with psychotropic, neurotropic and neurological drugs, agents and compounds, for rapid and efficient introduction of such agents across the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of psychotropic, neurotropic and neurological drugs, agents and compounds comprising the conjugates of the invention, in the brain and central nervous system.
    • 本发明在此描述了一种促进药物进入生理学保护部位的细胞和组织的药学上有用水平的方法,以及将药物靶向细胞内的特定细胞器的方法。 这种极性脂质/药物共轭靶向发明体现了先前技术中已知的其它药物靶向方法的进步,因为本发明提供了在这样的生理保护部位中的药物浓度,其在施用远低于目前的系统水平后达到治疗有效水平 施用以达到治疗剂量。 该技术适用于精神药物,神经营养因子和神经药物,药剂和化合物,用于快速有效地将这些药物引入血脑屏障。 此外,本发明提供了在脑和中枢神经系统中保留和延长酶促释放精神药物,神经营养因子和神经药物,包含本发明缀合物的药剂和化合物的方法。