Synthetic polymers with glycoside side chains
    12.
    发明授权
    Synthetic polymers with glycoside side chains 失效
    具有糖苷侧链的合成聚合物

    公开(公告)号:US4673707A

    公开(公告)日:1987-06-16

    申请号:US814131

    申请日:1985-12-27

    CPC分类号: C08F8/00 C07H15/26 C08H1/00

    摘要: Derivatized polymers containing glycoside side chains linked to the polymer by ether, sulfide, or amine linkages are prepared by reacting a polymer containing alcohol, thiol, and/or amine groups with a glycidyl glycoside having the formula ##STR1## where (SAC).sub.n represents a saccharide residue with n being 1-20. Typical polymers include poly(vinyl) alcohol, poly(ethyleneimine), poly(dimethylaminopropyl methacrylamide), and proteins such as caseinate or gluten. Typical glycosides are glycoside of glucose and maltodextrin-10.

    摘要翻译: 通过使含有醇,硫醇和/或胺基团的聚合物与具有式(IMAGE)的缩水甘油基糖苷反应,其中(SAC)n表示(SAC)n表示,含有通过醚,硫醚或胺键与聚合物连接的糖苷侧链的衍生化聚合物 n为1-20的糖残基。 典型的聚合物包括聚(乙烯基)醇,聚(乙烯亚胺),聚(二甲基氨基丙基甲基丙烯酰胺)和蛋白质如酪蛋白酸盐或面筋。 典型的糖苷是葡萄糖和麦芽糖糊精-10的糖苷。

    Novel nitrosourea compounds and process for preparing the same
    13.
    发明授权
    Novel nitrosourea compounds and process for preparing the same 失效
    新型亚硝基脲类化合物及其制备方法

    公开(公告)号:US4182757A

    公开(公告)日:1980-01-08

    申请号:US922811

    申请日:1978-07-10

    CPC分类号: C07H13/12 C07C275/68

    摘要: A nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is alkyl of one to six carbon atoms, hydroxyalkyl of one to six carbon atoms, alkenyl of three to five carbon atoms or alkynyl of three to five carbon atoms, R.sup.2 is aldopentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl, O-aldo-hexopyranosyl-(1.fwdarw.4)-aldo-hexopyranosyl or a group of the formula: --CH.sub.2 (CHOH).sub.n CH.sub.2 OH, and wherein n is zero or an integer of one to four. A method of preparation is disclosed whereby said nitrosourea compound is prepared by the nitrosation of a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are the same as above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent.

    摘要翻译: 一种下式的亚硝基脲化合物:其中R1是1-6个碳原子的烷基,1-6个碳原子的羟基烷基,3-5个碳原子的链烯基或3-5个碳原子的炔基,R2是醛戊二醛,醛 - 吡喃葡萄糖基,醛 - 六吡喃糖基,O-羟基 - 六吡喃糖基 - (1-> 4) - 羟基 - 六吡喃糖基或式-CH 2(CHOH)n CH 2 OH的基团,其中n为0或1〜4的整数。 公开了一种制备方法,其中所述亚硝基脲化合物是通过亚化下式化合物制备的:其中R1和R2与上述相同。 所述的亚硝基脲化合物可用作抗肿瘤或抗白血病药。

    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS
    18.
    发明申请
    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS 有权
    新型肝脏靶向药物及其合成

    公开(公告)号:US20110077386A1

    公开(公告)日:2011-03-31

    申请号:US12891004

    申请日:2010-09-27

    IPC分类号: C07H15/02 C07C229/02

    CPC分类号: C07H15/04

    摘要: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

    摘要翻译: 本发明提供新型肝靶向剂及其合成方法。 公开了以赖氨酸为基础的三乙酸结构作为骨架的肝靶向剂,其以糖基取代多价,与半乳糖胺链或乳糖链结合。 特别地,仅涉及一个氨基酸L-赖氨酸以提供三价值。 N,N-苄氧羰基-Nα-二羧甲基-L-赖氨酸中的所有羧基可以在一个步骤中与αGalNAc或ahLac的三种糖苷缀合。 本发明还提供了六乳糖苷。 特别地,TFA-AHA-Asp用于缀合2摩尔NTA(ahLac)3。 本发明还提供了一种在NTA和DTPA之间添加间隔物的方法。 延长的肝细胞特异性糖配体比未延长的肝细胞特异性糖配体具有更高的111In-放射性标记产率。

    LONG-CHAIN CHONDROITIN SUGAR CHAIN AND METHOD FOR PRODUCING THE SAME AND METHOD FOR PROMOTING SYNTHESIS OF CHONDROITIN
    19.
    发明申请
    LONG-CHAIN CHONDROITIN SUGAR CHAIN AND METHOD FOR PRODUCING THE SAME AND METHOD FOR PROMOTING SYNTHESIS OF CHONDROITIN 有权
    长链佐酮糖链及其生产方法及促进合成辛伐他汀的方法

    公开(公告)号:US20090263867A1

    公开(公告)日:2009-10-22

    申请号:US12097725

    申请日:2006-12-14

    IPC分类号: C12P19/44 C07H15/02

    CPC分类号: C12P19/26 C08B37/0069

    摘要: A method for producing a chondroitin sugar chain comprises at least the following step: a step of allowing “a glucuronic acid donor”, “an N-acetyl galactosamine donor”, “a sugar receptor” and “a bacterial cell enzyme which synthesizes chondroitin” to coexist in a reaction system in the presence of a surfactant. Here, the surfactant is preferably selected from n-nonyl-β-D-thiomaltopyranoside, sucrose monocaproate and sucrose monolaurate. The chondroitin sugar chain has all the following properties 1) to 3): 1) a weight average molecular weight: 50,000 or more when it is measured by gel filtration chromatography, 2) it is completely degraded to disaccharides with chondroitinase ABC, 3) when the sugar chain is decomposed with chondroitinase ABC and the decomposed products are subjected to a disaccharide analysis, substantially all of them correspond to an unsaturated disaccharide unit of chondroitin.

    摘要翻译: 生产软骨素糖链的方法至少包括以下步骤:允许“葡糖醛酸供体”,“N-乙酰半乳糖胺供体”,“糖受体”和“合成软骨素的细菌细胞酶”的步骤 在表面活性剂存在下在反应体系中共存。 这里,表面活性剂优选选自正壬基-β-D-硫代木糖淀粉糖苷,蔗糖单己酸酯和蔗糖单月桂酸酯。 软骨素糖链具有以下特性1)〜3):1)通过凝胶过滤色谱法测定的重均分子量为50,000以上,2)软骨素酶ABC完全降解为二糖,3)当 糖链用软骨素酶ABC分解,分解产物进行二糖分析,基本上都与软骨素的不饱和二糖单元相对应。