摘要:
The present invention relates to glycosyl-etoposide prodrugs, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates for treating cancers.
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:
The invention relates to carbohydrate mimetics, which inhibit the binding of selectin to carbohydrate ligands, of the formula I ##STR1## excluding the compounds sialyl-Lewis-X and -A and their derivatives which, instead of an N-acetyl group, carry the substituents N.sub.3, NH.sub.2 or OH or which, instead of fucose, carry glycerol,and pharmaceutical compositions and diagnostic agents containing these derivatives, and methods for using these pharmaceutical compositions and diagnostic agents.
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:
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:
.alpha.-Glycosyl-L-ascorbic acid exhibiting no direct reducing activity is formed in a solution containing L-ascorbic acid and an .alpha.-glucosyl saccharide when subjected to the action of a saccharide-transferring enzyme. .alpha.-Glycosyl-L-ascorbic acid is superiorly stable, and readily hydrolyzable in vivo to exhibit the activities inherent to L-ascorbic acid. Thus, .alpha.-glycosyl-L-ascorbic acid is favorably useful as a stabilizer, quality-improving agent, antioxidant, physiologically active agent and uv-absorbent in food pharmaceutical and cosmetic industries.
摘要:
Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.