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    • 1. 发明授权
    • Glycoproteins and processes for their production
    • 糖蛋白及其生产工艺
    • US4481137A
    • 1984-11-06
    • US467840
    • 1983-02-18
    • Haruo OhnishiKazuo YamaguchiYasuo SuzukiEi MochidaNobuo Mochida
    • Haruo OhnishiKazuo YamaguchiYasuo SuzukiEi MochidaNobuo Mochida
    • A61K38/00C07K14/47C07K14/52C12P21/00C07G7/00
    • C07K14/47C07K14/52A61K38/00Y10S514/908Y10S530/806Y10S530/809Y10S530/828Y10S530/829
    • A glycoprotein obtained from the cells of human or non-human warm-blooded animals having an anti-tumor effect and characterized by the following properties:(a) molecular weight: in the range from 7,000 to 90,000 by Sephadex gel filtration or SDS gel electrophoresis;(b) color reactions: it exhibits a color indicating proteins in the Lowry reaction, exhibits a color indicating peptide bonds and amino acids in the ninhydrin reaction after hydrolysis with hydrochloric acid, and exhibits a color indicating sugars in the phenol-sulfuric acid reaction, the anthrone-sulfuric acid reaction, the indole-sulfuric acid reaction and the tryptophane-sulfuric acid reaction;(c) appearance and solubility: white powder soluble in water, aqueous sodium chloride and phosphate buffer, and sparingly soluble in benzene, hexane and chloroform;(d) sugar content: sugar content is 8-45%, 6-28% of the total sugar being hexoses, 1-11% being hexosamines and 1-6% being sialic acids;(e) stability: stable in an aqueous solution of pH 2.0, pH 7.0 or pH 11.0 at 4.degree. C. for 24 hours or longer and in an aqueous solution of pH 7.0 at 60.degree. C. for 3 hours or longer; and(f) cytotoxicity: it selectively damages tumor cells without substantially damaging normal cells.
    • 从具有抗肿瘤作用的人或非人温血动物的细胞获得的糖蛋白,其特征在于以下性质:(a)分子量:通过Sephadex凝胶过滤或SDS凝胶电泳在7,000至90,000的范围内 ; (b)显色反应:在Lowry反应中表现出表示蛋白质的颜色,在用盐酸水解后,在茚三酮反应中表现出表示肽键和氨基酸的颜色,并表现出苯酚 - 硫酸反应中的糖的颜色, 蒽酮 - 硫酸反应,吲哚 - 硫酸反应和色氨酸 - 硫酸反应; (c)外观和溶解性:白色粉末溶于水,氯化钠水溶液和磷酸盐缓冲液,微溶于苯,己烷和氯仿; (d)糖含量:糖含量为8-45%,总糖的6-28%为己糖,1-11%为己糖胺,1-6%为唾液酸; (e)稳定性:在pH2.0,pH7.0或pH11.0的水溶液中在4℃下稳定24小时以上,在pH7.0的水溶液中在60℃下稳定3小时以上; 和(f)细胞毒性:它选择性地损伤肿瘤细胞,而不会对正常细胞造成实质的损害。
    • 7. 发明授权
    • Intermediates cephalosporin derivatives
    • 中间体CEPHALOSPORIN衍生物
    • US5064953A
    • 1991-11-12
    • US412992
    • 1989-09-26
    • Haruo OhnishiHiroshi KosuzumeMasahiro MizotaYasuo SuzukiEi Mochida
    • Haruo OhnishiHiroshi KosuzumeMasahiro MizotaYasuo SuzukiEi Mochida
    • C07D239/40C07D239/46C07D277/20C07D417/12C07D487/04C07D501/36C07D513/04
    • C07D239/47C07D239/40C07D277/587C07D417/12C07D487/04C07D513/04
    • The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The novel cephalosporin derivatives according to the present invention contain condensed heterocyclic groups, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring as substituents at the 3-position of the cephem skeleton, and a hydroxyimino, an alkyloxyimino or an acyloxyimino moiety as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against gram-negative bacteria and also against gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
    • 本发明涉及新型头孢菌素衍生物,其制备方法,用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物,以及头孢菌素衍生物合成中的中间体化合物及其制备方法。 根据本发明的新型头孢菌素衍生物含有缩合杂环基团,特别是作为头孢烯骨架3位的取代基的三唑并嘧啶环或噻二唑嘧啶环,作为7-位上的取代基的羟基亚氨基,烷氧基亚氨基或酰氧基亚氨基部分, 头脑骨架的位置。 含有上述取代基的本发明化合物对革兰氏阴性细菌和包括耐甲氧西林金黄色葡萄球菌的革兰氏阳性细菌具有很强的抗菌活性。 这些化合物对治疗感染性疾病非常有用。
    • 9. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US4840945A
    • 1989-06-20
    • US838309
    • 1986-03-10
    • Haruo OhnishiHiroshi KosuzumeMasahiro MizotaYasuo SuzukiEi Mochida
    • Haruo OhnishiHiroshi KosuzumeMasahiro MizotaYasuo SuzukiEi Mochida
    • C07D209/48C07D277/20C07D277/40C07D501/20C07D501/36C07D501/46C07D501/59C07D519/00
    • C07D209/48C07D277/587C07D501/36C07D501/46C07D519/00
    • The present invention relates to novel cephalosporin derivatives, processes for preparing thereof, compositions for preventing and/or treating infectious diseases which comprise the novel cephalosporin derivatives as active components, and the intermediate compounds in the synthesis of cephalosporin derivatives and processes for producing thereof.The present invention is based on the selection of groups containing a condensed heterocyclic ring, particularly a triazolopyrimidine ring or a thiadiazolopyrimidine ring, as substituents at the 3-position of the cephem skeleton, and of groups containing a catechol moiety, particularly a catechol carboxymethyloxyimino moiety or a catechol carboxyimino moiety, as substituents at the 7-position of the cephem skeleton.The compounds of the present invention containing the aforementioned substituents have a strong antibacterial activity against Gram-negative bacteria and also against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus. These compounds are extremely useful for the treatment of infectious diseases.
    • 本发明涉及新型头孢菌素衍生物,其制备方法,用于预防和/或治疗包含新型头孢菌素衍生物作为活性成分的感染性疾病的组合物,以及头孢菌素衍生物的合成中的中间体化合物及其制备方法。 本发明基于选择含有缩合杂环,特别是三唑并嘧啶环或噻二唑并嘧啶环作为头孢烯骨架3位上的取代基的基团,以及含有儿茶酚部分,特别是儿茶酚羧甲氧基亚氨基部分的基团 或邻苯二酚羧基亚氨基部分作为头孢烯骨架的7-位上的取代基。 含有上述取代基的本发明化合物对革兰氏阴性菌具有很强的抗菌活性,对抗耐甲氧西林金黄色葡萄球菌的革兰氏阳性菌具有很强的抗菌活性。 这些化合物对治疗感染性疾病非常有用。