Abstract: The invention provides a bio-related substance bonded to a high-molecular-weight polyethylene glycol derivative that does not cause vacuolation of cells. The bio-related substance bonded to a degradable polyethylene glycol derivative is represented by the formula (A): wherein m is 1-7, n1 and n2 are each independently 45-682, p is 1-4, R is an alkyl group having 1-4 carbon atoms, Z is an oligopeptide with 2-8 residues composed of neutral amino acids excluding cysteine, Q is a residue of a compound having 2-5 active hydrogens, D is the bio-related substance, L1, L2, L3, L4 and L5 are each independently a single bond or a divalent spacer, and y is 1-40.

Abstract: A peptide-polymer conjugate is provided for use in treating malaria infections, and in particular terminal or drug resistant malaria infections. The conjugate is formed from a polymer to which a peptide having activity against a malaria parasite is co-valently attached. The peptide is a cyclic decapeptide from the closely-related group of tyrocidines, tryptocidines, phenycidines and gramicidin S, and the polymer is a hydrophilic and biocompatible polymer with a terminal thiol, such as poly(N-vinylpyrrolidone) (PVP). The polymer chains can be decorated with a hydrophilic targeting ligand that specifically targets an epitope on red blood cells, and in particular red blood cells infected with a plasmodial parasite. A method for synthesising the peptide-polymer conjugate is also provided.

Abstract: A polyrotaxane containing an affinity binding group has been designed and prepared. The polyrotaxane of the invention can be used for characterization and determination of the three-dimensional structures of biological molecules, such as proteins.

Abstract: The present invention relates to a new class of cationic polymers that self-assemble with a pH-sensitive dissolution switch, and their uses to deliver molecules of interest to a cell. The present invention also relates to compositions comprising said cationic polymers non-covalently associated with a molecule of interest, in particular with a siRNA.

Abstract: Provided is a cell adhesion inhibitor which exhibits low cytotoxicity and an excellent cell adhesion prevention effect; a tool and an apparatus each having a surface modified through application of the cell adhesion inhibitor thereto; a method for producing each of the surface-modified tool and apparatus; a biomedical structure and a production method therefor; and a microchannel device and a production method therefor. The invention provides a cell adhesion inhibitor comprising, as an active ingredient, a polymer comprising a repeating unit having a sulfinyl group in a side chain thereof.

Abstract: The invention relates to a supramolecular polymer obtained from the reaction of (i) an amine bearing a nitrogen-containing heterocyclic group: imidazolidone, trimethyleneurea or triazine, which is capable of associating by means of hydrogen bonds and (ii) at least one fatty acid monomer comprising at least one reactive function, a dimer of identical or different fatty acids and/or a trimer of identical or different fatty acids, or a derivative of said fatty acid(s) which is selected from a fatty acid ester, and a fatty acid chloride.

Abstract: The invention relates to a biocidal composition comprising a carboxyl functional polymer and biocidal quaternary ammonium ions. The polymer is a copolymer comprising maleic acid monomer units and/or anions thereof and vinyl ether comonomer units. The composition may be in the form of a film on a surface or in the form of a solution.

Abstract: The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance.

Abstract: A rotaxane consisting of a cucurbituril and an uncharged guest molecule, having low or null affinity therebetween is provided as well as processes for providing the same. Various uses as energy converters (“frictionless” molecular motors), biochips and biosensors using the same are also provided.

Abstract: A novel class of Cylic Acetal biomaterials (CABs) based on a cyclic acetal unit is disclosed and claimed by Applicants. Two novel biomaterials suitable for use in a variety of biological applications including in the orthopedic field for joint and cartilage replacement and/or repair, and bone cement. The biomaterials are comprised of either a network of monomers of 5-ethyl-5-(hydroxymethyl)-?,?-dimethyl-1,3-dioxane-2-ethanol diacrylate (EHD) and a hydrogel comprised of EHD and poly(ethylene glycol) diacrylate (PEG-EHD).

Abstract: A polymer includes at least one monomeric unit represented by Formula I, II, or III: where X is CH2 or O; R1 is H, COOR2, COCH3, CONHR2, OR2 or SR2; L is a bond or a linker group; AA is a group derived from an active agent; each R2 is independently H, a cation, an alkyl, an alkenyl, an alkynyl, COCH3, CH2CH2OH, CH2CH2OR3, an amino acid, a small peptide, a large peptide, enzyme, protein, growth factor, cytokine, antibody, single chain antibody, antibody fragment, COCCH3?CH2, COCH?CH2, CH2CO2H, CH2CH2CO2H, CH2CH2SH, CH2CH2SR3 or (CH2CH2O)n?R4; n? is an integer from 1 to 2000; each R3 is independently trityl, 4-methyltrityl or 2 pyridyl; each R4 is independently H, an alkyl, an alkenyl, an alkynyl, COCCH3?CH2, COCH?CH2, CH2CHO, CH2CH2CHO, CO2H, CO2R5, CH2CO2H, CH2CH2CO2H, CH2NH2, CH2NHR5, CH2N(R5)2, CH2CH2NH2, CH2CH2NHR, CH2CH2N(R5)2, SH, CH2CO2R5, or CH2CH2CO2R5; and each R5 is independently maleimide, a cation, an amino acid, a small peptide, a large peptide, protein, enzyme, growth factor, cytokine, antibody,

Abstract: The present invention relates to a polymer obtained from the polymerization of: (i) at least one monomer of formula (I) (CH2?CR1)CO—K (1) wherein: K represents O—Z or NH—Z, Z representing (CR2R3)m-CH3, (CH2—CH2—O)m-H, (CH2—CH2—O)m-CH3, (CH2)m-NR4R5 with m representing an integer from 1 to 30; R1, R2, R3, R4 and R5 independently represent H or a C1-C6 alkyl; (ii) at least between 0.1 and 50% mol, advantageously between 1 and 30% mol, more advantageously between 1 and 20 mol % of a cyclic monomer having a exomethylene group of formula (II) wherein: R6, R7, R8 and R9 represent independently H or a C5-C7 aryl group or R6 and R9 are absent and R7 and R8 form together with the carbon atom on which they are bonded a C5-C7 aryl group; i and j represent independently an integer chosen between 0 and 2; X represents either O or X is not present and in this latter case, CR6R7 and CR8R9 are linked via a single bond C—C and (iii) at least one bio-resorbable block copolymer cross-linker.

Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: [Problems] To provide a novel taxane derivative which can release the medicinal substance in a bioenzyme-independent manner, is expected to have an effective therapeutic efficacy, and has a water-solubility. [Means for Solving Problems] Disclosed is a polymer conjugate of a taxane, which comprises a polymer having a polyethylene glycol moiety and two or more succinic acid monoamide moieties and a taxane, wherein a carboxylate group in the polymer and an alcoholic hydroxyl group in the taxane are bound to each other via an ester bonding.

Abstract: Biocompatible polymers having polymer backbones with at least one secondary amine suitable for diazeniumdiolation are disclosed. Specifically, methods for providing secondary amines-containing polymers using epoxide-opening reactions are provided. More specifically, nitric oxide-releasing medical devices made using these polymers are disclosed.

Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.

Abstract: An alternating copolymer comprising a backbone of residues of a maleic anhydride derivative and those of a compound containing vinylic unsaturation, which also comprises residues of an active compound containing a nucleophilic group, bound to the backbone by a residue of the nucleophilic group, including such a copolymer comprising residues of an active compound containing an alcohol, thiol or amine group. The chemical and biological properties of actives, such as protease inhibitors, neurotransmitter drugs, and other small molecule active drugs, are enhanced, and new applications enabled. Also, artefacts, including a solid medical implant device, dressing or scaffold or a fluid adhesive or medicinal composition comprising such a polymer, and a method of use of such a polymer, including a method for the treatment or prophylaxis of wounds.

Abstract: Compositions and methods for tissue repair are provided including cell binding peptides and growth factor binding peptides. The cell binding peptides bind to one or more of stem cells, fibroblasts, or endothelial cells. The growth factor binding peptides include platelet derived growth factor (PDGF) binding peptides and growth differentiation factor (GDF) binding peptides. The tissue for repair includes tendon, muscle, connective tissue, ligament, cardiac tissue, vascular tissue, or dermis. Implantable devices for tissue repair are provided to which the cell and growth factor binding peptides are attached, such as acellular extracellular matrix having attached binding peptide.

Abstract: The present invention provides an immunogen composition and methods for using the same for the development of immunity, and particularly at mucosal sites in a mammal, thereby providing immunity at the site of entry for many major pathogenic organisms and also systemic immunity. The immunogen composition includes an antigen, a biocompatible polymer, and a liquid vehicle, with the biocompatible polymer and liquid vehicle being present in such proportions and interacting in such a way that the immunogen composition exhibits reverse-thermal viscosity behaviour. A delivery vehicle composition including a drug other than an antigen is also provided. Methods are provided for delivering the compositions of the invention to a host.

Abstract: Described herein are MetAP-2 inhibitors and compositions and formulations thereof, and more particularly compositions and formulations of MetAP-2 inhibitors wherein the MetAP-2 inhibitor is associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety. The present invention also relates to compositions and formulations comprising MetAP-2 inhibitors for oral administration or administration via routes such as topical or ocular administration. The present invention also provides methods to treat conditions associated with or related to the over-expression or over-activity of MetAP-2 by administering the compositions and formulations comprising MetAP-2 inhibitors as disclosed herein.

Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate, followed by hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that demonstrate reduced activity when permanently coupled to PEG maintain a therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG derivatives of the invention can be used to impart improved water solubility, increased size, a slower rate of kidney clearance, and reduced immunogenicity to a conjugate formed by attachment thereto. Controlled hydrolytic release of the bound molecule into an aqueous environment can then enhance the drug's delivery profile by providing a delivery system which employs such polymers and utilizes the teachings provided herein.

Abstract: The invention provides methods for suppressing the degradation of wood, wood products, and wooden structures due to infestation by wood-boring organisms, by use of a polyurea composition. The invention also provides for wood, wood products, and wood structures that are resistant to degradation due to borer infestation by use of a polyurea composition.

Abstract: Activated polymeric bicine derivatives such as, as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.

Abstract: The present invention is to provide a tissue-specific transporter inhibitor which is not absorbed through the digestive tract and can prevent deterioration in the QOL of a patient caused by diet therapy, and a therapeutic drug for tissue dysfunction diseases and a therapeutic drug for suppressing the progress of chronic renal failure containing the inhibitor as an active ingredient. A tissue-specific transporter inhibitor which is not absorbed through the digestive tract is constructed by introducing a dipeptide which is a ligand of an oligopeptide transporter 1 into a supramolecular structure polyrotaxane wherein its structurally modified active residue is expected to be excellent in the interaction with a transmembrane transporter.

Abstract: Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.

Abstract: Film-forming compositions, as well as methods of making and using, wherein the compositions include an optional active agent, water, a surfactant, and a water-soluble or water-dispersible vinyl polymer comprising amine group-containing side-chains and a copolymerized hydrophobic monomer; wherein the amine equivalent weight of the polymer is at least about 300 grams polymer per equivalent of amine group.

Abstract: A composition, comprising, in a physiologically acceptable medium, an aqueous phase dispersed in an oily phase by means of an emulsifier of at least one oligomer or one polymer derived from a polyolefin, comprising a polyolefinic apolar component comprising at least 40 carbon atoms and at least one polar component.

Abstract: Use of a non-fermented osmotic laxative as an active agent for preparation of a medicinal product for treating and/or preventing colon and/or rectum cancers. A method of treating or preventing colon or rectum cancer comprising administering to a mammal a therapeutically effective amount of a non-fermented osmotic laxative.

Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate and then for hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that previously had reduced activity when permanently coupled to PEG can have therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG of the invention can be used to impart water solubility, size, slow rate of kidney clearance, and reduced immunogenicity to the conjugate. Controlled hydrolytic release of the bound molecule in the aqueous environment can then enhance the drug delivery system.

Abstract: Film-forming compositions, as well as methods of making and using, wherein the compositions include an optional active agent, water, a surfactant, and a water-soluble or water-dispersible vinyl polymer comprising amine group-containing side-chains and a copolymerized hydrophobic monomer; wherein the amine equivalent weight of the polymer is at least about 300 grams polymer per equivalent of amine group.

Abstract: Biocompatible biodegradable polymer or copolymer is capped at one end and has free hydroxyl at the other end. The free hydroxyl can be reacted to link a plurality of functional groups some or each of which can be reacted to attach directly or via a spacer molecule a moiety containing an aminoxyl-containing radical or to a moiety comprising other drug molecule residue or a moiety comprising other biologically active agent residue.

Abstract: A polymer comprising: a polymeric backbone comprising at least one unit having the structure (I), wherein R-R4 comprise groups selected from the group consisting of H, C1-C12 alkyl, C6-C18 aryl, C7-C18 aralkyl, C6-C18 cycloalkyl or any of the group consisting of C1-C12 alkyl, C6-C18 aryl, C7-C18 aralkyl, C6-C18 cycloalkyl substituted, within the carbon chain or appended thereto, with one or more heteroatoms; R and R2 or R and R4 or R and R1 or R2 and R3 may be joined so that with the carbon atom(s) to which they are attached they together form a saturated, partially unsaturated or unsaturated ring system respectively, may have a pendent group which may incorporate a linker unit, (for example a peptide linkage) or a unit having the structure (I); A comprises a proton donating moiety selected from the group consisting of formula (1).

Abstract: This invention relates to soluble derivatives of wortmannin that utilizes water-soluble polymers as carriers for a drug and includes compounds having the structures as described within the specification.

Abstract: A method and device are disclosed which prevent the intrusion of insects onto wood structures by using a barrier capable of retaining pesticide. In the disclosed method, the barrier maintains a minimal effective level of insecticide for a predetermined period of time.

Abstract: The present invention is to provide a tissue-specific transporter inhibitor which is not absorbed through the digestive tract and can prevent deterioration in the QOL of a patient caused by diet therapy, and a therapeutic drug for tissue dysfunction diseases and a therapeutic drug for suppressing the progress of chronic renal failure containing the inhibitor as an active ingredient. A tissue-specific transporter inhibitor which is not absorbed through the digestive tract is constructed by introducing a dipeptide which is a ligand of an oligopeptide transporter 1 into a supramolecular structure polyrotaxane wherein its structurally modified active residue is expected to be excellent in the interaction with a transmembrane transporter.

Abstract: Cationic starch graft copolymer composed of the monomers a) to d)

Abstract: The invention provides a multi-arm block copolymer for use in delivering a variety of bioactive agents. The copolymer of the invention contains a central core from which extend multiple (3 or more) copolymer arms. Each copolymer arm possesses an inner polypeptide segment and an outer hydrophilic polymer segment. Thus, the overall structure of the copolymer comprises an inner core region that includes the central core and the inner polypeptide segment, while the outer core region is hydrophilic in nature. The multi-arm copolymer of the invention is particularly useful for delivery of biologically active agents that can be entrapped within the inner core region.

Abstract: There are disclosed a method for producing a cross-coupling compound of formula (3):

Abstract: The invention concerns a biocompatible polymer having a mole weight more than 50000 g/mole, preferably 90000 g/mole for fixing biological ligands comprising at least a first linear segment consisting of a hydrophobic homopolymer derived from polymerisation of a hydrophobic monomer A; a second linear segment consisting of a hydrophilic polymer derived from copolymerisation of a monomer B bearing a reactive function X and a hydrophilic monomer C not bearing any reactive function, said second segment being covalently bound to one end of the first segment. The invention also concerns a biological polymer-ligand-conjugate, a device for capturing a target molecule comprising a solid support whereon is immobilised a biological polymer-ligand conjugate and methods for preparing said polymer. The invention is mainly applicable in the field of diagnosis.

Abstract: Nanocapsules useful for encapsulating bioactive molecules such as proteins are disclosed. These nanocapsules are comprised of branched or hyperbranched polymers and copolymers and have a core-shell structure forming a pocket volume appropriate for complexing and retaining enzymes and other bioactive molecules. The nanoencapsulated bioactive molecule is stable in extreme temperatures and pH, soluble in aqueous or organic solvents, and can be lyophilized to a dry powder for long-term storage without loss of enzyme activity.

Abstract: A polymer which comprises one or more units of formula (II) in the backbone: —R2—A—L—A—R3—A—L—A—  (II) wherein R2 and R3 are each independently a group that will yield a biologically active compound upon hydrolysis of the polymer; each A is independently an amide or ester linkage; and each L is independently a linking group. Methods of producing these polymer, intermediates useful for preparing these polymers, and methods of using these polymers to deliver biologically active compounds to a host are also provided.

Abstract: A prion-physiological structure and associated method of formation. A provided abnormal prion has a transforming power over a normal prion to convert the abnornal prion into defective prion that mimics the abnormal prion. A linker molecule is then bonded to the abnormal prion, wherein a polymer that is covalently attached to the linker molecule facilitates formation of a polymerized abnormal prion that does not have the transforming power over the normal prion.

Abstract: PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate and then for hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that previously had reduced activity when permanently coupled to PEG can have therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG of the invention can be used to impart water solubility, size, slow rate of kidney clearance, and reduced immunogenicity to the conjugate. Controlled hydrolytic release of the bound molecule in the aqueous environment can then enhance the drug delivery system.

Abstract: The invention relates to an adduct of polyalk(en)yl succinic anhydride and a compound of formula (I): wherein R1 is hydrogen, hydroxyl, hydrocarbyl, hydroxyhydrocarbyl, carbamyl, 1-acetyl, amino, or nitro; R2 is hydrogen, hydroxyl, hydrocarbyl, hydroxyhydrocarbyl, carbamyl, 1-acetyl, amino, or nitro; R3 is hydrogen or hydrocarbyl; and X is O, S or NH; or a derivative of such an adduct. The invention also relates to an emulsifier comprising such an adduct or derivative, and the invention also relates to compositions including such an emulsifier.

Abstract: Polyanhydrides which degrade into biologically active salicylates and alpha-hydroxy acids and methods of using these polyanhydrides to deliver the salicylates and alpha-hydroxy acids to a host are provided.

Abstract: The present invention provides water-soluble polymer conjugates of the anti-malarial drug, artelinic acid, using water soluble and non-peptidic polymer backbones, such as poly(ethylene glycol). The invention includes conjugates made using mPEG, bifunctional PEG and multi-arm PEG. The invention further includes a method of forming such conjugates and a method of treating malaria using the conjugates.

Abstract: The present invention provides water-soluble polymer conjugates of the anti-malarial drug, artelinic acid, using water soluble and non-peptidic polymer backbones, such as poly(ethylene glycol). The invention includes conjugates made using mPEG, bifunctional PEG and multi-arm PEG. The invention further includes a method of forming such conjugates and a method of treating malaria using the conjugates.

Abstract: Crosslinkable polymer compositions are provided which can be in the form of a polymer powder which is redispersible in water or as an aqueous dispersion.

Abstract: The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a guanidinium moiety-containing polymer composition to a mammal, such as a human, whereby bile acids are sequestered. The polymers of the invention comprise guanidinium moieties and optionally, additional substituents such as a hydrophobic group, a quaternary ammonium-containing group or a combination thereof.