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    • 4. 发明申请
    • Convalent conjugates of biologically-active compounds with amino acids and amino acid derivatives for targeting to physiologically-protected sites
    • 生物活性化合物与氨基酸和氨基酸衍生物的共价缀合物用于靶向生理保护部位
    • US20070129312A1
    • 2007-06-07
    • US11436972
    • 2006-05-16
    • Milton YatvinRichard Pederson
    • Milton YatvinRichard Pederson
    • A61K38/05A61K31/55A61K31/5513A61K31/498A61K31/522A61K31/445A61K31/19A61K31/525A61K31/137A61K31/195
    • A61K47/542
    • This invention herein describes a method of facilitating the entry of drugs into cells and tissues at physiologically protected sites at pharmacokinetically useful levels and also a method of targeting drugs to physiologically protected sites in vivo. Also provided are drug conjugates with an amino acid or derivative thereof for facilitating such targeted drug delivery. The conjugates and methods of this invention provide 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, neurological, antibiotic, antibacterial, antimycotic, antiviral, antiproliferative or antineoplastic drugs, agents and conjugates, for rapid and efficient introduction of such agents across, e.g., the blood-brain barrier. Further, the invention provides means for retention and prolonged enzymatic release of such drugs, agents and conjugates comprising the conjugates of the invention, in the brain and central nervous system and other physiologically-protected sites.
    • 本发明在此描述了一种促进药物进入生理保护部位的细胞和组织的药代动力学有用水平的方法,还包括将药物靶向体内生理保护部位的方法。 还提供了具有氨基酸或其衍生物的药物缀合物,用于促进这种靶向药物递送。 本发明的缀合物和方法提供了与现有技术中已知的其它药物靶向方法相比的进步,因为本发明提供在这样的生理保护位点中的药物浓度,其在施用远低于目前施用的系统水平之后可达到治疗有效水平 达到治疗剂量。 该技术适用于精神药物,神经营养因子,神经系统,抗生素,抗细菌剂,抗真菌药,抗病毒药,抗增殖药或抗肿瘤药物,药物和缀合物,用于快速有效地将这些药物引入例如血脑屏障。 此外,本发明提供了在脑和中枢神经系统和其他生理保护部位中包含本发明缀合物的这类药物,试剂和缀合物的保留和延长的酶促释放的方法。