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    • 2. 发明授权
    • Sphingolipids polyalkylamine conjugates for use in transfection
    • 用于转染的鞘脂聚烷基胺共轭物
    • US08242089B2
    • 2012-08-14
    • US10560932
    • 2004-06-17
    • Yechezkel BarenholzDmitri Simberg
    • Yechezkel BarenholzDmitri Simberg
    • A61K48/00A61K9/127C12N15/00C12N15/88
    • A61K31/132A61K9/1272A61K38/47A61K39/39A61K48/0041A61K2039/543A61K2039/55555A61K2039/55561C07C271/20C12N15/88A61K2300/00
    • The present invention concerns the use of a sphingoid-polyalkylamine conjugate comprising a sphingoid backbone carrying, via a carbamoyl bond, at least one polyalkylamine chains as a capturing agent of nucleic acid molecules. The present invention also provides the use of the sphingoid polyalkylamine conjugate for the preparation of a pharmaceutical composition for the delivery of a nucleic acid molecule into a target cell. In a further aspect the invention provides a method for transfecting a nucleic acid into a target cell, the method comprises contacting said target cell with the sphingoid-polyalkylamine conjugate associated with a nucleic acid molecule, thereby transfecting said target cell with said nucleic acid molecule. Other aspects of the invention concern pharmaceutical compositions comprising said conjugate, therapeutic methods as well as kits, making use of the said conjugate. A preferred conjugate according to the invention is N-palmitoyl D-erythrosphingosyl-1-carbamoyl spermine.
    • 本发明涉及包含通过氨基甲酰键携带至少一个聚烷基胺链作为核酸分子的捕获剂的鞘氨醇主链的鞘氨醇 - 多烷基胺缀合物的用途。 本发明还提供了鞘氨醇多烷基胺缀合物用于制备用于将核酸分子递送至靶细胞的药物组合物的用途。 在另一方面,本发明提供了将核酸转染到靶细胞中的方法,所述方法包括使所述靶细胞与与核酸分子相关联的类鞘氨醇 - 多烷基胺缀合物接触,由此用所述核酸分子转染所述靶细胞。 本发明的其它方面涉及包含所述缀合物的药物组合物,治疗方法以及使用所述缀合物的试剂盒。 根据本发明的优选的缀合物是N-棕榈酰基D-赤藻酰基-1-氨基甲酰基精胺。
    • 8. 发明申请
    • COMPOSITIONS AND DEVICES FOR THE DETECTION OF BIOMARKERS IN THE GASTROINTESTINAL TRACT AND METHODS FOR MAKING AND USING THEM
    • 用于检测气体诱导物中生物标志物的组合物和装置及其制备和使用它们的方法
    • US20140288398A1
    • 2014-09-25
    • US14238189
    • 2012-08-17
    • Dmitri SimbergYu-Tsueng Liu
    • Dmitri SimbergYu-Tsueng Liu
    • A61B5/00A61B5/1473A61B5/145A61B10/00
    • A61B5/6861A61B5/14546A61B5/1473A61B5/4848A61B10/0045A61B2010/0061C12Q1/6806C12Q2563/143C12Q2563/155
    • In alternative embodiments, the invention provides compositions such as devices, pills, beads, capsules, products of manufacture, particles, microparticles, nanoparticles, gels, liquid gels, liquid gel capsules, capsules, tablets, geltabs, liquids, sprays, emulsions, suspensions, pastes or yogurts, for the detection and isolation of biomarkers, nucleic acids, proteins or peptides, proteoglycans, lipids, fats, sugars or polysaccharides in the gastrointestinal tract for e.g., detecting the presence of particular exogenous or endogenous nucleic acids, e.g., DNA or RNA, or proteins, in the gastrointestinal tract, for example, to diagnose the presence of an infectious or exogenous agent such as a virus, a fungus, a parasite, a bacteria, intestinal helminths and protozoan parasites, and the like, or a biomarker such as a cancer-causing or cancer-predisposing allele, e.g., mutations of the KRAS2 oncogene in pancreatic cancer. In alternative embodiments, compositions of the invention comprise magnetic particles such as a magnetically-responsive microparticle or nanoparticle; a superparamagnetic bead or polystyrene bead; a superparamagnetic fine particle; a ferrimagnetic particle; or, a magnetic microsphere, nanosphere, microbead or nanobeads. In alternative embodiments, the invention provides methods for detecting, retrieving, capturing or isolating a sample of a nucleic acid, or an anionic, cationic or hydrophobic protein or peptide, a mucin, a phosphoprotein, a proteoglycan or a polysaccharide, in vivo.
    • 在替代实施方案中,本发明提供组合物,例如装置,丸剂,珠粒,胶囊,制造产品,颗粒,微粒,纳米颗粒,凝胶,液体凝胶,液体凝胶胶囊,胶囊,片剂,凝胶胶囊,液体,喷雾剂,乳液,悬浮液 用于检测和分离胃肠道中的生物标志物,核酸,蛋白质或肽,蛋白聚糖,脂质,脂肪,糖或多糖的例如检测特定的外源或内源核酸的存在,例如DNA 或RNA或蛋白质,例如诊断感染性或外源性药物如病毒,真菌,寄生虫,细菌,肠蠕虫和原生动物寄生虫等的存在,或 生物标志物如癌症或癌症易感性等位基因,例如胰腺癌中KRAS2致癌基因的突变。 在替代实施方案中,本发明的组合物包含磁性颗粒,例如磁响应微粒或纳米颗粒; 超顺磁珠或聚苯乙烯珠; 超顺磁细粒; 亚铁磁颗粒; 或磁性微球,纳米球,微珠或纳米棒。 在替代实施方案中,本发明提供了用于在体内检测,检索,捕获或分离核酸或阴离子,阳离子或疏水蛋白或肽,粘蛋白,磷蛋白,蛋白多糖或多糖的样品的方法。