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    • 1. 发明授权
    • Dextran derivatives, preparation and medicinal applications
    • 葡聚糖衍生物,制剂和药物应用
    • US06646120B1
    • 2003-11-11
    • US09367111
    • 2000-09-26
    • Frederic ChaubetRemi HuynhLatifa DahriJose CorreiaMarcel JozefowiczJacqueline Jozefonvicz
    • Frederic ChaubetRemi HuynhLatifa DahriJose CorreiaMarcel JozefowiczJacqueline Jozefonvicz
    • C08B3702
    • C08B37/0021
    • The invention concerns dextran derivatives, their applications as medicines with specific biological action, and their preparation method. Said derivatives correspond to the general formula DMCaBbSUcSd, in which: D represents a polysaccharide chain, preferably consisting of sequences of glucoside units, MC represents methylcarboxylate groups, B represents carboxymethylbenzylamide groups, Su represents sulphate groups, S represents sulphonate groups, a, b, c and d represent the degree of substitution (ds), respectively in groups, MC, B, Su and S; a being equal to 0 or ≧0.3, b being equal to 0 or ≧0.1, c being equal to 0 or ≧0.1 and d being equal to 0 or ≧0.1 provided that when d=0, a and/or b are not equal to 0, said products having homogeneity of chain size distribution, illustrated by a gauss elution profile symmetrical in high performance steric exclusion chromatography, and homogeneity in the distribution of charged chemical groups, illustrated by an elution profile with a single symmetrical peak in low pressure ion-exchange chromatography.
    • 本发明涉及葡聚糖衍生物,它们作为具有特定生物作用的药物的应用及其制备方法。 所述衍生物对应于通式DMCaBbSUcSd,其中:D表示多糖链,优选由葡萄糖苷单元序列组成,MC表示甲基羧酸酯基,B表示羧甲基苄基酰胺基,Su表示硫酸基,S表示磺酸酯基,a,b, c和d分别代表组,MC,B,Su和S的取代度(ds); a等于0或> = 0.3,b等于0或> = 0.1,c等于0或> = 0.1,d等于0或> = 0.1,条件是当d = 0时,a和/或 b不等于0,所述产物具有链尺寸分布的均匀性,由高效空间排阻色谱中对称的高斯洗脱曲线所示,以及带电化学基团分布的均匀性,通过具有单个对称峰的洗脱曲线 在低压离子交换层析中。
    • 2. 发明授权
    • Article for tuesyl-activated dextran for solid-phase coupling
    • 用于固相偶联的甲酚激活葡聚糖的文章
    • US06262256B1
    • 2001-07-17
    • US09073646
    • 1998-05-06
    • Henrik ElsnerSøren Mouritsen
    • Henrik ElsnerSøren Mouritsen
    • C08B3702
    • C07K17/08C07K1/042C12N11/06G01N33/545G01N33/548
    • A method of modifying the binding properties on a surface of a solid phase on which there are nucleophilic groups, which is characterized in that the surface is treated with a solution of an activated polysaccharide; a method of immobilizing a chemical compound to a solid phase on which there are immobilized activated polysaccharides, whereby the chemical compound is contacted with the surface of the solid phase the binding properties of which are modified by the method according to the invention; an article which is characterized in that to the surface thereof an activated polysaccharide is fixated, such as activated dextran or activated agarose, and use of this article for use in solid phase reactions, in solid phase assay, solid phase peptide synthesis, solid phase nucleotide synthesis, solid phase enzyme processing, and joining of biological surfaces.
    • 一种修饰在其上具有亲核基团的固相表面上的结合性质的方法,其特征在于表面用活化多糖的溶液处理; 将化合物固定在其上固定有活化多糖的固相的方法,由此化学化合物与固相的表面接触,其结合性质通过本发明的方法进行改性; 其特征在于,其活性多糖被固定,例如活化的葡聚糖或活化的琼脂糖,并使用该制品用于固相反应,固相测定,固相肽合成,固相核苷酸 合成,固相酶加工和生物表面的接合。
    • 4. 发明授权
    • Water-soluble polymeric metal ion affinity compositions and methods for using the same
    • 水溶性聚合物金属离子亲和性组合物及其使用方法
    • US06703498B2
    • 2004-03-09
    • US10176955
    • 2002-06-20
    • Grigoriy S. Tchaga
    • Grigoriy S. Tchaga
    • C08B3702
    • C08B37/0021C07C229/76C07K1/22
    • Water-soluble metal ion affinity compounds and methods for using the same are provided. The subject compounds include an aspartate based metal chelating ligand bonded to a water-soluble polymeric substrate, where the ligand is complexed with a metal ion. In certain embodiments, the subject compounds further include a member of a signal producing system, e.g., a directly or an indirectly detectable label moiety. Also provided are water-insoluble supports having the subject compounds present on, e.g., immobilized on, at least one surface thereof. The subject compounds find use in a variety of different applications, including analyte detection and analyte purification applications.
    • 提供了水溶性金属离子亲和性化合物及其使用方法。 主题化合物包括与水溶性聚合物底物结合的天冬氨酸盐基金属螯合配体,其中配体与金属离子络合。 在某些实施方案中,本发明化合物还包括信号产生系统的成员,例如直接或间接可检测的标记部分。 还提供了具有例如固定在其至少一个表面上的主题化合物的水不溶性载体。 主题化合物可用于各种不同的应用,包括分析物检测和分析物纯化应用。
    • 5. 发明授权
    • Process for producing drug complexes
    • 生产药物复合物的方法
    • US06291671B1
    • 2001-09-18
    • US09147341
    • 1999-03-22
    • Kazuhiro InoueHiroshi SusakiMasahiro Ikeda
    • Kazuhiro InoueHiroshi SusakiMasahiro Ikeda
    • C08B3702
    • A61K47/61
    • A method for preparing a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids, or a drug complex in which a polysaccharide derivative having carboxyl groups and a residue of a drug compound are bound to each other without the spacer, characterized in that an organic amine salt of the polysaccharide derivative having carboxyl groups is reacted with the drug compound or the spacer bound to the drug compound in a non-aqueous system. The reaction between the polysaccharide derivative having carboxyl groups and the drug compound bound with the spacer or the like can be carried out in high yields, and when a drug compound having a lactone ring is subjected to the reaction, side reactions can be reduced.
    • 一种制备药物复合物的方法,其中具有羧基的多糖衍生物和药物化合物的残基通过包含氨基酸或包含肽键合的2-8个氨基酸的间隔子的间隔物彼此结合,或 其中具有羧基的多糖衍生物和药物化合物的残基在没有间隔基的情况下彼此结合的药物复合物,其特征在于,具有羧基的多糖衍生物的有机胺盐与药物化合物或间隔基 在非水系统中与药物化合物结合。 具有羧基的多糖衍生物与与间隔物等结合的药物化合物之间的反应可以高收率地进行,当使具有内酯环的药物化合物进行反应时,可以减少副反应。
    • 7. 发明授权
    • High yield S-nitrosylation process
    • 高产率的S-亚硝基化工艺
    • US06417347B1
    • 2002-07-09
    • US09645171
    • 2000-08-24
    • Robert A. HerrmannDavid Knapp
    • Robert A. HerrmannDavid Knapp
    • C08B3702
    • C07C381/00C08B37/00C08B37/0012
    • A method for producing a S-nitrosylated species is provided. The method comprises: (a) providing a deoxygenated, alkaline aqueous solution comprising a thiol and a nitrite-bearing species; (b) acidifying the solution by adding acid to the solution while concurrently mixing the solution (e.g., by vigorously stirring the solution) to produce the S-nitrosylated species; and (c) isolating the S-nitrosylated species. The nitrite-bearing species can be, for example, an inorganic nitrite, such as an alkali metal nitrite, or an organic nitrite, such as an alkyl nitrite (e.g., ethyl nitrite, amyl nitrite, isobutyl nitrite or t-butyl nitrite). The thiol is preferably a thiol-containing polysaccharide, a thiol-containing lipoprotein, a thiol-containing amino acid or a thiol-containing protein, and more preferably a thiol-containing polysaccharide such as thiolated cyclodextrin. In many preferred embodiments, the S-nitrosylated species is insoluble in the acidified solution, precipitating upon formation. The S-nitrosylated species can be isolated, for example, by a process in which the precipitate is removed from the solution (e.g., by centrifugation) and the aqueous solvent remaining in the precipitate is sublimated (e.g., by freezing the precipitate and subjecting it to a vacuum). The isolated S-nitrosylated product is preferably protected from heat, light, moisture and oxygen.
    • 提供了生产S-亚硝基化物质的方法。 该方法包括:(a)提供包含硫醇和含亚硝酸盐的物质的脱氧碱性水溶液; (b)通过向溶液中加入酸来酸化溶液,同时混合溶液(例如通过剧烈搅拌该溶液)以产生S-亚硝基化物质; 和(c)分离S-亚硝基化物质。 含有亚硝酸盐的物质可以是例如无机亚硝酸盐,例如碱金属亚硝酸盐或有机亚硝酸盐,例如亚硝酸烷基酯(例如亚硝酸亚乙酯,亚硝酸戊酯,亚硝酸异丁酯或亚硝酸叔丁酯)。 硫醇优选为含硫醇的多糖,含硫醇的脂蛋白,含巯基的氨基酸或含硫醇的蛋白质,更优选含硫醇的多糖如硫醇化环糊精。 在许多优选实施方案中,S-亚硝基化物质不溶于酸化溶液,在形成时沉淀。 S-亚硝基化物质可以例如通过其中从溶液中除去沉淀物(例如通过离心)并且残留在沉淀物中的水性溶剂升华的方法分离(例如,通过冷冻沉淀物并使其沉淀 到真空)。 分离的S-亚硝基化产物优选保护免受热,光,水分和氧气的影响。