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    • 125. 发明申请
    • MOLECULAR ASSEMBLY USING BRANCHED AMPHIPHILIC BLOCK POLYMER, AND DRUG TRANSPORTATION SYSTEM
    • 使用分支的胶囊聚合物和药物运输系统的分子装配
    • US20150202327A1
    • 2015-07-23
    • US14425429
    • 2013-09-03
    • SHIMADZU CORPORATIONKYOTO UNIVERSITY
    • Isao HaraEiichi OzekiShunsaku KimuraAkira Makino
    • A61K49/00A61K9/51
    • A61K49/0054A61K9/5153A61K47/50A61K47/51A61K47/593A61K49/0034A61K49/0089A61K49/12A61K49/124A61K51/0404A61K51/06
    • The present invention provides a molecular assembly whose retention time in a target site is adjusted depending on the kind or purpose of a labeling agent or drug encapsulated therein, and a molecular assembly that can suppress the ABC phenomenon and that can be administered more than once within a short span. A molecular assembly comprising: a branched-type amphiphilic block polymer A comprising a branched hydrophilic block comprising sarcosine and a hydrophobic block comprising a polylactic acid chain; and a functional substance F comprising a functional site and a polylactic acid chain, wherein the polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises L-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises D-lactic acid units, or the polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises D-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises L-lactic acid units.
    • 本发明提供一种分子组合物,其取决于包封在其中的标记试剂或药物的种类或目的在靶位点的保留时间,以及可抑制ABC现象并且可以多次施用的分子组装 短跨度 一种分子组合物,其包含:支链型两亲嵌段聚合物A,其包含含有肌氨酸的支链亲水嵌段和包含聚乳酸链的疏水嵌段; 和包含功能部位和聚乳酸链的功能性物质F,其中构成所述两亲性嵌段聚合物A的疏水性嵌段的聚乳酸链包含L-乳酸单元,所述功能性物质F中所含的聚乳酸链包含D 或者构成两亲性嵌段聚合物A的疏水性嵌段的聚乳酸链包含D-乳酸单元,功能性物质F中所含的聚乳酸链包含L-乳酸单元。
    • 126. 发明申请
    • Formulation of Stable Recombinant Alpha-Fetoprotein Conjugated with Anti-Tumor Substance in Target-Delivery System for Treatment of Cancer and Autoimmune Disease
    • 在用于治疗癌症和自身免疫疾病的靶向递送系统中制备与抗肿瘤物质结合的稳定的重组甲胎蛋白
    • US20150141414A1
    • 2015-05-21
    • US14455249
    • 2014-08-08
    • Nana Legrand
    • Nana Legrand
    • A61K47/48A61K47/34C07K14/47A61K31/538
    • C07K14/4715A61K9/19A61K9/5153A61K31/538A61K47/26
    • Disclosed is a stable formulation based on rAFP conjugated with drug delivery system of various classes of pharmacological agents such as dactinomycin, cardionolide, and bufadinolide, among others. In another embodiment, the invention discloses a method of producing rAFP in a strain of methylotrophic Pichia pastoris yeast, allowing the yeast to replicate, and extracting the newly created rAFP. The method provides a nonpyrogenic, highly stable, recombinant, fully refolded rAFP and its fragments that are free from stable folding intermediates caused by non-native disulfide bridges and irreversible aggregates. The newly created rAFP is purified using a two-step chromatographic purification process in the presence of 0.5% polysorbate-20 and 10 mM inosine that prevents aggregation of the monomers of the target protein, increasing the yield of biologically active rAFP. The invented formulation of rAFP is conjugated with active pharmacological substances or target drug delivery system for prevention or treatment of oncological and autoimmune-diseases.
    • 公开了一种基于与药物递送系统结合的rAFP的稳定制剂,所述药物递送系统包括各种类型的药理学试剂,例如放线菌素,cardionolide和bufadinolide等。 在另一个实施方案中,本发明公开了一种在甲基营养型巴斯德毕赤酵母菌株中生产rAFP的方法,允许酵母复制并提取新产生的rAFP。 该方法提供非致死性,高度稳定,重组,完全重折叠的rAFP及其片段,其不含由非天然二硫键和不可逆聚集体引起的稳定折叠中间体。 在0.5%聚山梨醇酯-20和10mM肌苷存在下,使用两步色谱纯化方法纯化新产生的rAFP,以防止靶蛋白单体的聚集,提高生物活性rAFP的产量。 本发明的rAFP制剂与活性药理物质或靶药物递送系统结合,用于预防或治疗肿瘤和自身免疫疾病。