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    NOVEL ASYMMETRICALLY BICIPITAL LIPID AND TUBULAR AGGREGATE FORMED BY USING THE SAME
    111.
    发明公开
    NOVEL ASYMMETRICALLY BICIPITAL LIPID AND TUBULAR AGGREGATE FORMED BY USING THE SAME 有权
    不相容，ZWEIKÖPFIGESLIPID UND MIT DIESEM GEBILDETESRÖHRENFÖRMIGESAGGREGAT

    公开(公告)号：EP1396496A1

    公开(公告)日：2004-03-10

    申请号：EP02711287.9

    申请日：2002-02-01

    申请人： Japan Science and Technology Agency ,  National Institute of Advanced Industrial Science and Technology

    发明人： MASUDA, M., Tsukuba Cntr ,  SHIMIZU, T. Tsukuba Cntr

    IPC分类号： C07H5/04

    CPC分类号： C07H5/04

    摘要： The present invention offers a novel asymmetric double-headed lipid capable of forming a stable, nanometer scale micro-tubular aggregated material of containing a sugar and a carboxylic acid at each end.
    The present invention is an asymmetric double-headed lipid represented by the general formula

            R-NHCO- (CH 2 ) n -COOH     (I)

    (in the formula, R represents an aldopyranose radical from which the terminal reducing hydroxyl group is excluded and n is from six to twenty) and a hollow micro-tubular aggregated material formed from the asymmetric double-headed lipid. The external diameter of the micro-tubular aggregated material is 10-300 nm, and the length is 0.3-10 µm. The micro-tubular aggregated material can be manufactured by dispersing the asymmetric double-headed lipid described above in water at pH of two to eight, next heating to 80-100°C to dissolve it and then gradually cooling the aqueous solution obtained.

    摘要翻译： 本发明提供了一种新型的不对称双头脂质，其能够在每一端形成含有糖和羧酸的稳定的纳米级微管聚集物。 本发明是由通式R-NHCO-（CH2）n-COOH表示的不对称双头脂质（在该式中，R表示不包括末端还原羟基的醛吡喃基，n 为6至20个）和由不对称双头脂质形成的中空微管聚集物。 微管状聚集体的外径为10〜300nm，长度为0.3〜10μm。 微管状聚集体可以通过将上述不对称双头脂质分散在pH为2〜8的水中，接着加热至80-100℃，使其溶解，然后逐渐冷却所得水溶液。

    CRYSTALLINE GLUCOSAMINE SULPHATE METAL SALTS AND PROCESSES FOR PREPARING THE SAME
    113.
    发明公开
    CRYSTALLINE GLUCOSAMINE SULPHATE METAL SALTS AND PROCESSES FOR PREPARING THE SAME 有权
    结晶葡萄糖胺硫酸盐金属盐及其制备方法

    公开(公告)号：EP1347986A2

    公开(公告)日：2003-10-01

    申请号：EP01998306.3

    申请日：2001-12-03

    申请人： Nicholas Piramal India Limited

    发明人： MUKHOPADHYAY, Triptikumar ,  BHAT, Ravi Gajanan ,  SREEKUMAR, E. S.

    IPC分类号： C07H5/04 ,  C07H5/06 ,  C08B37/00 ,  A01N43/04 ,  A61K31/20

    CPC分类号： C07H5/06

    摘要： The present invention relates to novel crystalline glucosamine sulphate metal salts for use in the treatment of acute and chronic forms of rheumatic and arthritic diseases and of all the pathological conditions originating from metabolic disorders of the osteo-articular tissues. More particularly, the present invention relates to novel crystalline glucosamine sulphate metal salts having low metal content wherein the metal may be either sodium or potassium. The present invention further relates to a solution-based and a solvent-free process for the preparation of the novel crystalline glucosamine sulphate metal salts having low metal content and to pharmaceutical compositions comprising the novel crystalline glucosamine sulphate metal salts having low metal content.

    摘要翻译： 本发明涉及新的结晶葡糖胺硫酸盐金属盐，用于治疗急性和慢性形式的风湿病和关节炎疾病以及所有源自骨关节组织代谢紊乱的病理状态。 更具体地说，本发明涉及具有低金属含量的新型结晶葡糖胺硫酸盐金属盐，其中金属可以是钠或钾。 本发明进一步涉及用于制备具有低金属含量的新型结晶葡糖胺硫酸盐金属盐的基于溶液的和无溶剂的方法，并涉及包含具有低金属含量的新型结晶葡糖胺硫酸盐金属盐的药物组合物。

    METHODS FOR SYNTHESIS OF ALPHA-D-GAL (1- 3) GAL-CONTAINING OLIGOSACCHARIDES
    114.
    发明公开
    METHODS FOR SYNTHESIS OF ALPHA-D-GAL (1- 3) GAL-CONTAINING OLIGOSACCHARIDES 审中-公开
    合成α-D-GAL（1-3）含GAL的寡糖的方法

    公开(公告)号：EP1257558A1

    公开(公告)日：2002-11-20

    申请号：EP01901031.3

    申请日：2001-01-12

    申请人： Alchemia Pty Ltd

    发明人： BORNAGHI, Laurent ,  DEKANY, Gyula ,  DRINNAN, Nicholas, Barry ,  PAPAGEORGIOU, John ,  WEST, Michael, Leo

    IPC分类号： C07H15/18 ,  C07H17/04 ,  C07H15/26 ,  C07H15/08 ,  C07H23/00 ,  C07H15/12 ,  C07H1/00 ,  C07H5/04 ,  C07H3/04 ,  C07D493/04 ,  A61K31/702 ,  A61K31/7016

    CPC分类号： C07D493/04 ,  C07B2200/11 ,  C07H13/12 ,  C07H15/08 ,  C07H15/14 ,  C07H15/18

    摘要： This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R3 is methoxy or methyl; R1 is H, benzoyl, pivaloyl, , 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.

    摘要翻译： 本发明涉及用于合成包含α-D-Gal（1→3）-D-Gal的生物活性二糖和三糖的试剂和方法。 特别地，本发明提供用于溶液或固相合成α-D-吡喃半乳糖基 - （1→3）-D-半乳糖及其衍生物的新试剂，中间体和方法。 在一个优选实施方案中，本发明提供了通式（II）的受保护的单糖结构单元：其中R 3是甲氧基或甲基; 乙酰基，氯乙酰基，乙酰丙酰基，4-甲基苯甲酰基，苄基，3,4-亚甲二氧基苄基，4-甲氧基苄基，4-氯苄基，4-乙酰氨基苄基或4-叠氮基苄基; 乙酰基，氯乙酰基，乙酰丙酰基，4-甲基苯甲酰基，苄基，3,4-亚甲二氧基苄基，4-甲氧基苄基，4-氯苄基，4-乙酰氨基苄基或4-叠氮基苄基。

    Process for the preparation of organic azides
    117.
    发明公开
    Process for the preparation of organic azides 有权
    Verfahren zur Herstellung von organischen Aziden

    公开(公告)号：EP1029867A2

    公开(公告)日：2000-08-23

    申请号：EP00200466.1

    申请日：2000-02-14

    申请人： Akzo Nobel N.V. ,  Sanofi-Synthélabo

    发明人： Claassen, Henricus Cornelis Jozephus

    IPC分类号： C07H15/04 ,  C07H5/04

    CPC分类号： C07H5/04

    摘要： A process for the addition of an azide function to an organic compound in which process a mixture is prepared by adding an epoxide-derivative of the organic compound and an alkali metal azide salt to a solvent is described. The mixture is heated to a reaction temperature at which the epoxide-derivative and the azide can react to form an azide derivative of the organic compound. An amount, near equimolar to the epoxide derivative, of a (1-6C)alkyl-(2-4C)carboxylic acid ester having a boiling point above the reaction temperature is added to the mixture before and/or during the reaction.

    摘要翻译： 描述了向有机化合物中加入叠氮化物功能的方法，其中通过将有机化合物的环氧化物衍生物和碱金属叠氮化物盐加入到溶剂中制备混合物的方法。 将混合物加热到环氧化物衍生物和叠氮化物可以反应的反应温度，形成有机化合物的叠氮化物衍生物。 将具有高于反应温度的沸点的（1-6C）烷基 - （2-4C）羧酸酯与环氧化物衍生物接近等摩尔的量在反应之前和/或反应期间加到混合物中。