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    • 85. 发明公开
    • POLYMERIC PHARMACEUTICAL AGENT FOR TREATMENT OF CANCER AND PROCESS FOR PRODUCTION OF THE SAME
    • POLYMERES PHARMAZEUTISCHES MITTEL ZUR BEHANDLUNG VON KREBS UND HERSTELLUNGSVERFAHRENDAFÜR
    • EP1873204A1
    • 2008-01-02
    • EP06731788.3
    • 2006-04-13
    • Maeda, Hiroshi
    • GREISH, Khaled
    • C08L25/04A61K31/704A61K31/409A61K31/7048A61K33/24A61K47/48A61P35/00
    • A61K41/0071A61K9/0019A61K9/107A61K31/409A61K31/704A61K31/7048A61K47/58A61K47/60C08K5/0091C08L35/06
    • [PROBLEMS] To provide a polymeric pharmaceutical agent which can contain the active ingredient in a larger amount, which can be highly accumulated in tumor tissues, and which has a molecular size that is large enough not to undergo the renal excretion.
      [MEANS FOR SOLVING PROBLEMS] The polymeric pharmaceutical agent capable of containing the active ingredient in a large amount can be produced by forming a styrene-maleic acid copolymer (SMA) micelle complex comprising a metalloporphyrin derivative (e.g., zinc protoporphyrin) and an SMA conjugated to each other via non-covalent bonding. This SMA micelle complex can be produced by reacting a metalloporphyrin derivative with an SMA in the absence of a condensing agent under alkaline conditions, solubilizing the resulting product, adjusting the reaction to pH 6 to 8, and collecting a polymeric micelle complex component having the active ingredient contained therein by a procedure for separating a polymeric component.
    • [问题]提供可以含有更多量的活性成分的聚合物药剂,其可以高度积累在肿瘤组织中,并且具有足够大的分子尺寸,不能进行肾脏排泄。 [能够解决问题的手段]能够大量含有活性成分的聚合物药剂可以通过形成包含金属卟啉衍生物(例如锌原卟啉锌)和SMA共轭体系的苯乙烯 - 马来酸共聚物(SMA)胶束复合物 通过非共价结合彼此。 该SMA胶束复合物可以通过在碱性条件下在不存在缩合剂的情况下使金属卟啉衍生物与SMA反应,使所得产物溶解,将反应调节至pH6至8,并收集具有活性的聚合物胶束复合物组分 通过分离聚合物组分的方法含有的成分。
    • 86. 发明公开
    • ON-LINE INTERNAL QUALITY EXAMINING METHOD AND DEVICE
    • 互联网在线 - QUALITÄTSUNTERSUCHUNGSVERFAHRENUND VORRICHTUNG
    • EP1746409A1
    • 2007-01-24
    • EP05739011.4
    • 2005-04-28
    • Maeda, Hiroshi
    • Maeda, Hiroshi
    • G01N21/27G01N21/01G01N21/35G01N21/85
    • G01N21/31B07C5/3416B07C2501/009G01N21/3563G01N21/85G01N21/88G01N21/8806G01N2021/8845
    • To provide a method and an apparatus for inspecting, in a non-destructive manner, internal qualities such as diseases and defects and physiological defects, which cannot be seen in an appearance, along with measurement of taste component values such as a sugar degree and an acid degree of fruits, which are agricultural products. An object is conveyed by conveying means that has a transmitted light path piercing in the vertical direction in the center thereof and is provided with a seat adhering to an object in an annular shape, with a predetermined position on a conveyance path set as an inspection position, a light shielding cylinder, which vertically lowers to, adheres to, and covers an upper part of the object, is advanced synchronously with the object, and beams are projected toward the object from both left and right sides using small lamps. Upper condensing means for condensing transmitted light through the light shielding cylinder downward over the inspection position and upper spectroscopic means connected to the upper condensing means by an optical fiber are provided. Lower condensing means for condensing transmitted light upward below a transmitted light exit of the seat and lower spectroscopic means connected to the lower side condensing means by an optical fiber are provided. An analyzer that subjects spectroscopic spectrum data SA obtained from the upper side spectroscopic means and spectroscopic spectrum SB obtained from the lower side spectroscopic means to spectrum analysis, respectively, and calculates taste component values such as a sugar degree and an acid degree from the upper and the lower spectrum and detects various physiological defects and diseases and defects to output a defect degree is provided.
    • 提供一种用于以非破坏性方式检查外观上看不到的内部品质,如外观上看不到的内容,以及味道成分值如糖度和 水果的酸度,这是农产品。 物体由具有在其中心沿垂直方向穿透的透射光路的输送装置输送,并且设置有附接到环状物体的座位,在作为检查位置的输送路径上具有预定位置 垂直地降低,粘附并覆盖物体的上部的遮光筒与物体同步地前进,并且使用小的灯将光束从左右两侧投影到物体上。 上聚光装置用于将透过的光通过遮光筒向下聚集在检查位置上,而上分光装置通过光纤连接到上聚光装置。 提供用于将透射光向上聚集在座椅的透射光出口下方的下聚光装置和通过光纤连接到下侧聚光装置的下分光装置。 将从上侧分光装置得到的分光光谱数据SA和从下侧分光装置得到的分光光谱SB分别进行光谱分析的分析装置,分别从上部和下部计算诸如糖度和酸度的味成分值 提供较低的光谱并检测各种生理缺陷和疾病和缺陷以输出缺陷程度。
    • 87. 发明公开
    • ANTITUMOR AGENT AND PROCESS FOR PRODUCING THE SAME
    • VERFAHREN ZU SEINER HERSTELLUNG的抗菌剂
    • EP1627645A1
    • 2006-02-22
    • EP04707295.4
    • 2004-02-02
    • Maeda, Hiroshi
    • MAEDA, HiroshiGREISH, Khaled
    • A61K47/48A61K45/06A61K47/18A61K47/32A61P35/00
    • A61K33/24A61K9/1075A61K47/58A61K47/6907
    • The present invention relates to polymeric antitumor agent which is formed in polymeric micelle complex by intermolecular bonding or mutual interaction between styrene maleic acid copolymer (SMA) and low molecule antitumor agent which is anthracyclins drug such as pirarubicin, doxorubicin, epirbicin, daunorbicin, acralbicin, or alkaloid antitumor agent such as cis-platinum, and taxol.
      These polymeric antitumor agents may improve specificity to cancer cells so that it improves antitumor effect, while it may not be concentrated at normal organ or tissue, so that adverse effect may be diminished.
      These polymeric antitumor agents may be prepared by dissolving SMA and low molecule antitumor agent in aqueous solution, then in the presence of aqueous soluble carbodiimide, amino acids, or polyamine, adjusting pH to form micelle complex and recovering polymer fraction.
    • 本发明涉及通过苯乙烯马来酸共聚物(SMA)和低分子抗肿瘤剂之间的分子间键合或相互作用形成聚合物胶束复合物的聚合物抗肿瘤剂,其是蒽环类药物,例如吡柔比星,多柔比星,表赤霉素,柔红霉素, 或生物碱抗肿瘤剂如顺铂和紫杉醇。 这些聚合物抗肿瘤剂可以提高对癌细胞的特异性,从而提高抗肿瘤作用,而不会将其集中在正常的器官或组织上,从而可能减少不利影响。 这些聚合物抗肿瘤剂可以通过将SMA和低分子抗肿瘤剂溶解在水溶液中,然后在水溶性碳二亚胺,氨基酸或多胺的存在下,调节pH以形成胶束复合物并回收聚合物级分来制备。