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65 results about "Sugar derivative" patented technology

Series of quinazoline sugar derivatives used as protein tyrosine kinase inhibitor, preparation method and application thereof

InactiveCN101857618ASolve the problem of low activity of inhibiting tyrosine kinaseGood water solubilityOrganic active ingredientsSugar derivativesSolubilityProtein-Tyrosine Kinases
The invention provides a quinazoline sugar derivative and a preparation method and application thereof, which can solve the problem of low activity of inhibiting tyrosine kinase in the prior art. The prepared quinazoline sugar derivative has high water solubility and high activity of inhibiting human skin cancer cells A431, and can be used for preparing medicaments for preventing or treating tumors. The quinazoline sugar derivative provided by the invention is a kind of compounds which have novel structures and comprise abundant glycosyl group segments at a 6-bit side chain of a quinazoline parent ring, wherein the raw materials adopted in a method for performing glycosylation on quinazoline rings are readily available; the synthesis method is simple; the purification mode is simple and convenient and quick; and the quinazoline sugar derivative has high water solubility, high biological activity, particularly obvious activity of selectively inhibiting an EGFR, and obvious anti-tumor effect, so the kind of compounds has a wide application prospect in medicaments for preventing or curing tumors. The quinazoline sugar derivative comprises the following structural formula.
Owner:OCEAN UNIV OF CHINA

Amphiphilic polysaccharide derivative carrier for targeting tumor new blood vessels as well as preparation and application of pharmaceutical composition of amphiphilic polysaccharide derivative carrier

The invention relates to an amphiphilic polysaccharide derivative carrier for targeting tumor new blood vessels. According to the derivative, a polysaccharide skeleton is coupled with functional polypeptide targeting E-selectin by virtue of a disulfide bond to ensure that polysaccharide has amphipathy, and is assembled into nano particles for targeting the tumor new blood vessels after carrying an antitumor drug or a tumor new blood vessel inhibitor in an aqueous medium. The nano particles deliver medicines to the tumor new blood vessels in an active targeting manner by virtue of the high affinity between the functional polypeptide targeting the E-selectin and the E-selectin on the surface of the tumor new blood vessels, then a disulfide bond connecting arm can be specifically degraded by a strong reducing environment in endothelial cells of the tumor new blood vessels to cause that the functional polypeptide targeting the E-selectin is separated from polysaccharide, and the medicines are quickly released to treatment target points, so that the concentration of free medicines at tumor new blood vessel parts can be significantly improved and the antitumor curative effect is enhanced. An auxiliary material can be used as a carrier for water-insoluble, indissolvable or amphiphilic antitumor drugs and the tumor new blood vessel inhibitor, and is administrated by injecting into blood vessels or muscles, or is administrated orally or externally. The amphiphilic polysaccharide derivative carrier provided by the invention is simple in preparation method, mature in process and suitable for large-scale production.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES

Antibody-conjugates with improved therapeutic index for targeting cd30 tumours and method for improving therapeutic index of antibody-conjugates

The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1-4 core N-acetylglucosamine moieties with a compound of the formula S(F1)x-P in the presence of a catalyst, wherein S(F1)x is a sugar derivative comprising x functional groups F1 capable of reacting with a functional group Q1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F1)x moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q1 capable of reacting with functional group F1 and a target molecule D connected to Q1 via a linker L2 to obtain the antibody-conjugate wherein linker L comprises S—Z3-L2 and wherein Z3 is a connecting group resulting from the reaction between Q1 and F1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.
Owner:SYNAFFIX

Amphiphilic polysaccharide derivative containing cholesterol and phytolectin group as well as preparation method and application of amphiphilic polysaccharide derivative

The invention discloses an amphiphilic polysaccharide derivative containing cholesterol and phytolectin group as well as a preparation method and application of the amphiphilic polysaccharide derivative. According to the invention, firstly, an amphiphilic polysaccharide derivative containing cholesterol and a phytolectin group is synthesized; and further an insulin-loaded amphiphilic polysaccharide derivative nanoparticle with glucose responsiveness is synthesized. The capability of combining free glucose molecules in the surrounding environment of the phytolectin group in the nanoparticle ishigher than that of combining glucose groups on polysaccharide chains, so that the chain segments of the amphiphilic polysaccharide derivative become loose, the size of the nanoparticles is increased,insulin is released, and intelligent regulation and control are realized. The preparation conditions of the amphiphilic polysaccharide derivative and the nanoparticle are mild, the used raw materialsare safe, and the activity of specific binding of phytolectin to glucose molecules and the structural stability and biological activity of insulin are maintained. The amphiphilic nanoparticle for intelligently regulating and controlling insulin release prepared by the invention is expected to be used as an insulin delivery carrier, and can intelligently regulate and control insulin release according to the change of the blood glucose level in the body of a diabetes patient, so that the amphiphilic nanoparticle has a certain application prospect in the aspect of diabetes treatment.
Owner:SUN YAT SEN UNIV
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