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32 results about "Polymeric prodrug" patented technology

Hydrogel formulations

A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
Owner:ASCENDIS PHARM AS

Hydrogel formulations

A polymeric prodrug composition including a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on its surface. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
Owner:ASCENDIS PHARM AS

Heterobifunctional polymeric bioconjugates

Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound isMethods of making and using the compounds and conjugates described herein are also provided.
Owner:BELROSE PHARMA

Polymeric prodrug with a self-immolative linker

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.
Owner:ASCENDIS PHARM GMBH

Prodrugs of anticancer agents employing substituted aromatic acids

InactiveUS6936597B2Modulate the rate of hydrolysisBiocideAntimycoticsLeaving groupPolymeric prodrug
Polymeric prodrugs of the formula: whereinB is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties;Y1 is selected from the group consisting of O, S, and NR5;M is NR3, O or S;Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group;(m) is zero or a positive integer;R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; andR4 is a polymeric residue;as well as methods of making and using the same are disclosed.
Owner:RESENIUS USA +1

Camptothecin prodrug monomer and polymeric prodrug amphipathic molecules thereof as well as preparation method and application of camptothecin prodrug monomer and polymeric prodrug amphipathic molecules

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.
Owner:UNIV OF SCI & TECH OF CHINA

Targeted polymeric prodrugs containing multifunctional linkers

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.
Owner:ENZON PHARM INC

Guanidine hypoglycemic drug-polysaccharide conjugate, as well as preparation method and application thereof

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.
Owner:CHINA PHARM UNIV

Treatment of neuroblastoma with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin

InactiveUS20100098654A1Difficulty of therapyEliminate and significantly reduce immune responseNervous disorderPharmaceutical non-active ingredientsPolymeric prodrugMedicine
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.
Owner:ENZON PHARM INC

Polymeric thiol-linked prodrugs

Thiol-linked polymeric prodrugs and methods of making and using the same are disclosed. The use of a sulfhydryl bond as the basic link for linking the polymer to the drug allows a prodrug to be formed which takes advantage of plasma enzymes in vivo. A preferred conjugate is Methods of preparing and treatment are also disclosed.
Owner:BELROSE PHARMA

Preparation method of pH-responsive amphiphilic rod-like adriamycin polymer prodrug

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.
Owner:SOUTHWEST UNIVERSITY

Preparation method of linear diblock polymeric prodrugs with pH simulative responsibility

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.
Owner:SOUTHWEST UNIVERSITY

Methods for inhibiting angiogenesis with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin

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.
Owner:BELROSE PHARMA

Camptothecin prodrug monomer and polymeric prodrug amphipathic molecules thereof as well as preparation method and application of camptothecin prodrug monomer and polymeric prodrug amphipathic molecules

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.
Owner:UNIV OF SCI & TECH OF CHINA

Heterobifunctional Polymeric Bioconjugates

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.
Owner:BELROSE PHARMA

Polymeric thiol-linked prodrugs employing benzyl elimination systems

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.
Owner:BELROSE PHARMA

Multi-branched polymeric prodrugs and their applications

The present invention relates to multi-branched polymeric prodrugs and applications thereof. Specifically, the present invention relates to a multi-branched polymeric prodrug having a structure of formula (I) or a pharmaceutically acceptable salt thereof, which is effective for topoisomerase I-related diseases in mammalian subjects, In particular, solid tumors in mammalian subjects have very good therapeutic effects. In the case of the same in vitro activity as inhibiting the proliferation of cancer cells, it has a more reasonable half-life and residence time of the drug in the body, greatly reduces the clearance rate, is more conducive to determining the way of drug administration, and reduces the number of administrations. It is expected to be developed into a new drug. A generation of antineoplastic drugs.
Owner:JIANGSU HANSOH PHARMA CO LTD +1

Chitosan-based multi-environment-responsive type polymeric prodrug micelle and preparation method thereof

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.
Owner:XUZHOU MEDICAL UNIV

Polymeric prodrugs and subcutaneous and/or intramuscular administration thereof

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.
Owner:CENT NAT DE LA RECHERCHE SCI +1

A redox-responsive hyperbranched polyprodrug nanomicelle and its preparation method and application

The invention provides a redox-responsive hyperbranched polyprodrug nano-micelle and its preparation method and application. In the invention, the hydrophobic drug is connected with the disulfide bond that can be cut by high GSH, and then the redox-responsive amphiphilic hyperbranched polyprodrug nano-micelle is synthesized through two-step RAFT polymerization. The redox-responsive hyperbranched polyprodrug nano-micelle of the present invention has the advantages of simple preparation process, good stability, prolonged blood circulation time, improved bioavailability of drugs, and the like. Moreover, the nano-micelle can break under the reducing environment of high GSH concentration in tumor cells, release hydrophobic drugs rapidly, and inhibit the proliferation of tumor cells. The redox-responsive hyperbranched polyprodrug nanomicelles of the present invention provide a new option for tumor therapy.
Owner:FUZHOU UNIV

Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug

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.
Owner:SOUTHWEST UNIV

Method for preparing nano particles of camptothecin polymeric prodrug amphipathic molecules as well as product and application of nano particles

The invention relates to a preparation method for different nano particles of reducing response camptothecin polymeric prodrug amphipathic molecules represented in a formula I as well as a product and an application of the nano particles, wherein morphology of a polymeric prodrug amphipathic molecule final assembly can be controlled just by regulating the kind of a solvent and through a way of adding water and regulating a water adding speed, so as to obtain four typical nano structures: spherical structure, disc-shaped structure, flower-shaped compound vesicle and staggered accumulated lamellar nano particles. The nano structures have high drug loading rate (more than 50wt%); compared with the most studied spherical nano particle at present, an assembly of the staggered accumulated lamellar structure is the longest in blood circulation time, followed by the disc-shaped nano particles. In addition, non-spherical particle is greater in tumor cytotoxicity compared with the spherical nano particles. In the formula I, various is independently represent 2 or 3; various Xes independently represent O or NH; R is H, CH3 or CH2CH3; m ranges from 4 to 400; and n ranges from 2 to 300; and number-average molecular weight of the reducing response camptothecin polymeric prodrug amphipathic molecule is 1200-220000.
Owner:UNIV OF SCI & TECH OF CHINA
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