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2. 发明申请

WO2008103276A2 COMPOSITIONS AND METHODS FOR POTENTIATED ACTIVITY OF BIOLOGICALY ACTIVE MOLECULES 审中-公开
标题翻译：生物活性分子的潜在活性的组合物和方法
公开(公告)号：WO2008103276A2
公开(公告)日：2008-08-28
申请号：PCT/US2008002006
申请日：2008-02-15
申请人： MERCK & CO INC , JADHAV VASANT , VARGEESE CHANDRA , SHAW LUCINDA , MORRISSEY DAVID , JENSEN KRISTI
发明人： JADHAV VASANT , VARGEESE CHANDRA , SHAW LUCINDA , MORRISSEY DAVID , JENSEN KRISTI
IPC分类号： A61K48/00
CPC分类号： C12N15/88
摘要： The present invention relates to novel compositions and methods for potentiating the activity of biologically active molecules in conjunction with one or more delivery vehicles and one or more carrier molecules. Specifically, the invention features the use of a carrier molecule in combination with a delivery vehicle and a biologically active molecule of interest to potentiate the activity of the biologically active molecule. The carrier molecule can be biologically inert, inactive, or attenuated; or can alternately be biologically active in the same or different manner than the biologically active molecule of interest. Specifically, the invention features novel particle forming delivery agents including cationic lipids, microparticles, and nanoparticles that are useful for delivering various biologically active molecules to cells in conjunction with a carrier molecule. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism that are delivered intracellularly in conjunction with a carrier molecule. In various embodiments, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism, in conjunction with one or more carrier molecules. Such novel cationic lipids, microparticles, nanoparticles and transfection agents that are used in conjuction with one or more carrier molecules are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism.
摘要翻译：本发明涉及用于增强生物活性分子与一种或多种递送载体和一种或多种载体分子结合的活性的新型组合物和方法。具体地，本发明的特征在于使用载体分子与递送载体和感兴趣的生物活性分子组合以增强生物活性分子的活性。载体分子可以是生物惰性的，无活性的或减毒的; 或者可以以与感兴趣的生物活性分子相同或不同的方式交替地具有生物活性。具体地，本发明的特征在于新颖的颗粒形成递送剂，其包括阳离子脂质，微粒和纳米颗粒，其可用于将各种生物活性分子与载体分子结合递送至细胞。本发明还特征在于用于研究，诊断和治疗响应基因表达和/或活性的基因表达和/或活性在细胞内与载体结合递送的研究，诊断和治疗的组合物和方法分子。在各种实施方案中，本发明涉及有效转染或递送生物活性分子的新型阳离子脂质，微粒，纳米颗粒和转染剂，例如抗体（例如单克隆抗体，嵌合型，人源化等），胆固醇，激素，抗病毒剂，肽，蛋白质，化学治疗剂，小分子，维生素，辅因子，核苷，核苷酸，寡核苷酸，酶核酸，反义核酸，形成三链体的寡核苷酸，2,5-A嵌合体，异构酶，适体，诱饵及其类似物，以及小核酸酸分子，如短干扰核酸（siNA），短干扰RNA（siRNA），双链RNA（dsRNA），微RNA（miRNA）和短发夹RNA（shRNA）分子）相关细胞和/或组织，例如受试者或生物体，与一种或多种载体分子结合。用于与一种或多种载体分子结合使用的这种新型阳离子脂质，微粒，纳米颗粒和转染剂可用于例如提供预防，抑制或治疗细胞，受试者或疾病中的疾病，病症或性状的组合物生物。

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