32 results about "Polymeric prodrug" patented technology

Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound is

Methods of making and using the compounds and conjugates described herein are also provided.

A cascade carrier linked prodrug is described which comprises a biologically active moiety and a masking group having at least one nucleophile and being distinct from the carrier.

The invention relates to a reduced response camptothecin prodrug monomer as shown in a formula I, reduced response camptothecin polymeric prodrug amphipathic molecules of the reduced response camptothecin prodrug monomer, and a preparation method and application of the reduced response camptothecin prodrug monomer and the reduced response camptothecin polymeric prodrug amphipathic molecules. In the formula I, each i is 2 or 3 independently, each X is O or NH independently, and R is H, CH3 or CH2CH3. According to the preparation method, raw materials including camptothecin, triphosgene and the like are used for modifying 20 bits of hydroxyls of camptothecin to prepare a camptothecin prodrug monomer containing disulfide bonds, then the camptothecin prodrug monomer is subjected to high-conversion-rate polymerization by using active free radical polymerization method to obtain an amphiphilic polymer which contains a camptothecin drug repetitive unit and has an extremely high drug loading capacity (more than 50wt%), and in a tumor cell reducing environment, a side chain disulfide bond is broken to perform molecular rearrangement and release camptothecin prodrug molecules, so that the amphiphilic polymer has characteristics of a reduced response controlled-release raw drug. The polymeric prodrug amphipathic molecules improve the water solubility and stability of the drug and have a controlled release characteristic.

The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

The invention discloses a guanidine hypoglycemic drug-polysaccharide conjugate, as well as a preparation method and application thereof. The conjugate is formed by connecting primary amine on a guanidine drug and the aldehyde group on oxidative polysaccharide through a schiff base bond. Compared with an existing guandine hypoglycemic drug, on the one hand, the conjugate can be used as a polymeric prodrug for reducing blood glucose, so that the pharmacologic action is strengthened, few adverse responses exist, and the safety is higher; on the other hand, the conjugate can be combined with therapeutic genes for treating diabetes mellitus, in particular obese diabetic, and the curative effect of the conjugate on cellular level and animal pattern are better than those of active compounds and therapeutic gene. The results prove that the guanidine hypoglycemic drug-polysaccharide conjugate has tremendous potential in the aspect of drug combined gene therapy of diabetes mellitus due to the excellent biocompatibility and effective gene transfer efficiency; the synthesizing and preparing method is simple, the process is mature, and the yield is high.

The present invention relates to methods of treatment of neuroblastoma. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to patients in need thereof.

The invention relates to the fields of chemical synthesis and biological representation, and more particularly, provides a preparation method and an application of a pH-responsive amphiphilic rod-likepolymer prodrug, which is represented as the drawing in the specification. The preparation method of the amphiphilic rod-like polymer material includes the following steps: 1) synthesizing a rod-likeATRP initiator on the basis of glucan; 2) introducing a pH-responsive hydrophobic block on the basis of ATRP reaction; 3) introducing a hydrophilic block on the basis of ATRP reaction to obtain an amphiphilic polymer material; 4) substituting an ester group on the terminal of MGMA by means of hydrazine hydrate, thus producing a pH-responsive precursor; 5) forming a hydrazone bond by means of a carbonyl group on adriamycin and an amino group on the polymer material, thus producing the pH-responsive polymer prodrug. By means of weak acidity of interior of cancer cells, the amphiphilic rod-likepolymer prodrug can selectively release a drug by means of pH-stimulating response. The polymer prodrug is high in micelle stability, is high in drug carrying capacity and enables drug release to be under stimulating response control.

The invention discloses a preparation method of linear diblock polymeric prodrugs with pH simulative responsibility and in-vitro activity of the prodrugs with pH simulative responsibility. The preparation method is characterized in that with an RAFT (reversible addition and fragmentation chain transfer) polymerization reaction as a main reaction, different polymeric prodrugs are synthesized by changing the proportion of a hydrophilic block and a hydrophobic block, and folic acid is further used to partially modify and synthesize a drug delivery system with pH simulative responsibility and targeting performance. An experiment proves that the system has high drug load capacity, good water solubility and low toxic and side effects and has accurate and efficient cancer treatment potential, and the utilization rate of the drugs is effectively increased.

The present invention relates to methods of inhibiting angiogenesis in mammals. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to the mammals in need thereof. The present invention also relates to methods of treating a disease associated with angiogenesis in mammals by administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to the mammals in need thereof.

Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is:

where S-MP is 6-mercaptopurine.

The invention discloses a chitosan-based multi-environment-responsive type polymeric prodrug micelle and a preparation method thereof. The preparation method of the chitosan-based multi-environment-responsive type polymeric prodrug micelle comprises the steps that, a folic acid-chitosan conjugate and amino-terminated poly(N-isopropylacrylamide) are used to prepare folic acid-chitosan-poly(N-isopropylacrylamide); a grafted polymer of gambogic acid and the folic acid-chitosan-poly(N-isopropylacrylamide) is prepared; and the grafted polymer is dissolved in dimethyl sulfoxide and slowly dripped into water, and the solution is subjected to dialysis and freeze-drying to obtain the micelle. Chitosan is the main component, respectively links with folic acid and the poly(N-isopropylacrylamide) which is a thermosensitive polymer material via chemical bonding, and links with the gambogic acid which is an antitumor medicine via an ester bond. A formed polymeric prodrug is multi-environment-responsive to pH, temperature and esterase.

The invention relates to new prodrugs of active molecules. These prodrugs allow, in particular, the subcutaneous or intramuscular administration of active molecules of which the subcutaneous or intramuscular administration is problematic or impossible, in particular because of the toxicity at the injection site. The prodrugs according to the invention comprise an active ingredient, covalently linked with a polymer chain, preferably a hydrophilic and/or thermosensitive polymer chain. The invention relates, in particular, to polymeric prodrugs comprising a polymer chain formed at least in part by acrylamide monomer or one of its derivatives, the polymer comprising a proximal part and a terminal part; a first pharmaceutically active molecule covalently coupled to the proximal part of the polymer; possibly a second pharmaceutically active molecule covalently coupled to the terminal part of the polymer.