Process for producing high 2-O-alpha-D-glucopyranosyl-L-ascorbic acid
    43.
    发明申请
    Process for producing high 2-O-alpha-D-glucopyranosyl-L-ascorbic acid 有权
    生产高2-O-α-D-吡喃葡萄糖基-L-抗坏血酸的方法

    公开(公告)号:US20010051711A1

    公开(公告)日:2001-12-13

    申请号:US09875963

    申请日:2001-06-08

    IPC分类号: C07H017/00

    CPC分类号: C07H17/04

    摘要: Disclosed is a process for producing a high nullG-AA content product, which comprises the steps of: contacting a solution as a material solution, containing nullG-AA, L-ascorbic acid, and a saccharides), with an anion exchange resin packed in a column to adsorb the nullG-AA and L-ascorbic acid on the anion exchanger; washing the anion exchanger with water to remove the saccharide(s) therefrom; feeding to the column an aqueous solution, as an eluent, of an acid and/or a salt with a concentration of less than 0.5 N to fractionate a fraction rich in 2-O-null-D-glucopyranosyl-L-ascorbic acid and a fraction rich in L-ascorbic acid; and collecting the former fraction.

    摘要翻译: 公开了一种制备高αG-AA含量产物的方法,其包括以下步骤:将含有αG-AA,L-抗坏血酸和糖的物质溶液的溶液与包含在其中的阴离子交换树脂接触) 用于吸附阴离子交换器上的αG-AA和L-抗坏血酸的柱; 用水洗涤阴离子交换剂以除去其中的糖类; 向柱中加入浓度小于0.5N的酸和/或盐的水溶液作为洗脱液,以分离富含2-O-α-D-吡喃葡萄糖基-L-抗坏血酸的级分和 级分富含L-抗坏血酸; 并收集前一部分。

    Synthetic insulin mimetic substances
    46.
    发明授权
    Synthetic insulin mimetic substances 失效
    合成胰岛素模拟物质

    公开(公告)号:US6093697A

    公开(公告)日:2000-07-25

    申请号:US902338

    申请日:1997-07-29

    摘要: Compounds are disclosed which have the formula (I) ##STR1## wherein R.sub.1 -R.sub.2 are each independently selected from the group consisting of: (a) a hydrogen atom; and (b) a lower alkyl group, straight or branched chain, having 1 to 8 carbon atoms; or R.sub.1 -R.sub.2 and the nitrogen atom to which they are bonded may together form a heterocyclic group; R.sub.3 -R.sub.10 are each independently selected from the group consisting of: (a) a hydrogen atom; (b) an alkyl group, straight or branched chain, having 1 to 24 carbon atoms; (c) a cycloalkyl group having 3 to 10 carbon atoms; (d) an alkenyl group, straight or branched chain, having 2 to 24 carbon atoms; (e) a cycloalkenyl group having 4 to 10 carbon atoms and one or more non-adjacent double bonds; (f) an aryl group having 6 to 10 carbon atoms; (g) an aralkyl group having 7 to 34 carbons atoms; (h) a heteroaryl group having 4 to 9 carbon atoms and at least one heteroatom selected from the group consisting of oxygen, nitrogen and sulfur; (i) a carboxyalkyl group, straight or branched chain, having 2 to 24 carbon atoms; (j) a carboxyaryl group having 7 to 34 carbon atoms; and (k) a heterocyclic group having 2 to 9 carbon atoms and at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen; or any adjacent two of R.sub.3 -R.sub.10 may together form a cycloalkyl group or heterocyclic group; and X.sub.1 and X.sub.2 are each independently selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom. Pharmaceutical compositions containing these compounds and the use thereof for the treatment of disorders of glucose metabolism are also disclosed.

    摘要翻译: 公开了具有式(I)的化合物,其中R 1 -R 2各自独立地选自:(a)氢原子; 和(b)具有1至8个碳原子的直链或支链的低级烷基; 或R 1 -R 2和它们所键合的氮原子可以一起形成杂环基; R3-R10各自独立地选自:(a)氢原子; (b)具有1至24个碳原子的直链或支链烷基; (c)碳原子数3〜10的环烷基; (d)具有2至24个碳原子的直链或支链烯基; (e)具有4-10个碳原子和一个或多个不相邻双键的环烯基; (f)具有6〜10个碳原子的芳基; (g)碳原子数为7〜34的芳烷基; (h)具有4至9个碳原子的杂芳基和至少一个选自氧,氮和硫的杂原子; (i)具有2至24个碳原子的直链或支链的羧基烷基; (j)具有7至34个碳原子的羧基芳基; 和(k)具有2至9个碳原子的杂环基和至少一个选自氧,硫和氮的杂原子; 或R 3 -R 10任意相邻的两个可以一起形成环烷基或杂环基; X 1和X 2各自独立地选自氧原子,硫原子和氮原子。 还公开了含有这些化合物的药物组合物及其用于治疗葡萄糖代谢紊乱的用途。

    Solution and solid-phase formation of glycosidic linkages
    48.
    发明授权
    Solution and solid-phase formation of glycosidic linkages 失效
    糖苷键的溶液和固相形成

    公开(公告)号:US5861492A

    公开(公告)日:1999-01-19

    申请号:US780914

    申请日:1997-01-09

    申请人: Daniel Evan Kahne

    发明人: Daniel Evan Kahne

    摘要: The invention relates to methods that permit the rapid construction of oligosaccharides and other glycoconjugates. Methods for forming multiple glycosidic linkages in solution in a single step are disclosed. The invention takes advantage of the discovery that the relative reactivity of glycoside residues containing anomeric sulfoxides and nucleophilic functional groups can be controlled. In another aspect of the invention, the reactivity of activated anomeric sugar sulfoxides is utilized in a solid phase method for the formation of glycosidic linkages. The methods disclosed may be applied to the preparation of specific oligosaccharides and other glycoconjugates, as well as to the preparation of glycosidic libraries comprising mixtures of various oligosaccharides, including glycoconjugates, which can be screened for biological activity.

    摘要翻译: 本发明涉及允许快速构建寡糖和其它糖缀合物的方法。 公开了在单一步骤中在溶液中形成多个糖苷键的方法。 本发明利用了可以控制含有异聚亚砜和亲核官能团的糖苷残基的相对反应性的发现。 在本发明的另一方面,活化的端基异构糖亚砜的反应性用于形成糖苷键的固相方法。 所公开的方法可以应用于制备特异性寡糖和其它糖缀合物,以及制备包含可以筛选生物活性的各种寡糖(包括糖缀合物)的混合物的糖苷文库。