Abstract: The invention relates to a process for synthesis, by inverse bead polymerization of a monomer phase, of a bead-like, cross-linked, hydrophilic copolymer which has binding activity toward ligands containing nucleophilic groups. The invention relates to support polymer materials with high binding capacity for penicillin acylase and low swelling factor, as well as to use of the same.

Abstract: The present invention provides cationic-polymer-lipid conjugates (CPLs) such as distal cationic-poly(ethylene glycol)-lipid conjugates which can be incorporated into conventional and stealth liposomes or other lipid-based formulation for enhancing cellular uptake. The CPLs of the present invention comprise a lipid moiety; a hydrophilic polymer; and a polycationic moiety. Method of increasing intracellular delivery of nucleic acids are also provided.

Abstract: The invention relates to a heat-sensitive compound having the property of being soluble in water below a critical temperature Tc and insoluble in water above this temperature Tc, this property being thermally reversible, characterized in that it comprises a first amphiphilic and thermally reversible part corresponding to one of the following formulae (I) and (II): 1

Abstract: The present invention includes polymeric transport systems corresponding to the formula: wherein: R31 is a linear or branched polymer residue; Y10 and Y11 are independently O, S, or NR40; X2 is O, S or NR41; R32-35, R37-41, R50 and R51 are independently selected among 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 and substituted C1-6 heteroalkyls; a, b and e are each independently selected positive integers; L is an amino acid residue or a bifunctional linker; X3 is wherein Y12 and Y13 are independently O, S, or NR41; Z is a bond, a moiety that is actively transported into a target cell, a hydrophobic moiety or combinations thereof; D1 and D2 are OH, a residue of a hydroxyl, a residue of an amine-containing moiety or a leaving group; and y1 and y2 are independently selected positive integers.

Abstract: Conjugates of a Factor VIII moiety and one or more water-soluble polymers are provided. Typically, the water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising the conjugates, methods of making the conjugates, and methods of administering compositions comprising the conjugates to a patient.

Abstract: The invention relates to methods of treating mixtures containing polymeric materials, e.g., collagen, to form a polymer that intercalates into the polymeric material. The treatment provides greater tensile strength to the mixture, among other advantages. The polymer is formed of a monomeric unit having at least one catechol group that is oxidized to a quinone upon polymerization.

Abstract: The present invention provides &egr;-polylysine represented by formula (1), having a polyorganosiloxane group introduced into the molecule, and a process for production of the &egr;-polylysine, in which the formula (1) is defined in the specification. The invention further provides an antimicrobial agent comprising an amino group-containing antimicrobial polymer having a polyorganosiloxane group introduced into the molecule, and an antimicrobial resin composition comprising an antimicrobial agent above and a resin.

Abstract: The invention relates to the use of increased-molecular-weight hirudin for the manufacture of an anticoagulant for extracorporeal renal replacement therapy which does not induce an autoimmune disease and which does not cross react with autoimmune antibodies. In particular, the use according to the invention does not induce type II thrombocytopenia (HIT II), and no cross reactivity occurs with antibodies to platelet-factor-4-heparin complexes.

Abstract: A makeup cosmetic and a skin cosmetic, which is produced by the following process and has viscosity in a specific range,

Abstract: The invention is concerned with positional isomers of monopegylated interferon alpha 2a, with a method for their isolation and for their use in the manufacture of medicaments for the treatment of illnesses, especially for the treatment of viral diseases.

Abstract: Methods, compositions and articles of manufacture for assaying a sample for a target polynucleotide are provided. A sample suspected of containing the target polynucleotide is contacted with a polycationic multichromophore and a sensor PNA complementary to the target polynucleotide. The sensor PNA comprises a signaling chromophore to absorb energy from the excited multichromophore and emit light in the presence of the target polynucleotide. The methods can be used in multiplex form. Kits comprising reagents for performing such methods are also provided.

Abstract: The present invention relates to a process for immobilization of nucleic acid molecules on a substrate, wherein the substrate is treated with atomic oxygen plasma prior to immobilizing the nucleic acid molecules thereon. The invention is further related to immobilized nucleic acid molecules and uses thereof.

Abstract: Dried hemoactive materials comprise both a cross-linked biologically compatible polymer and a non-cross-linked biologically compatible polymer. The cross-linked polymer is selected to form a hydrogel when exposed to blood. The non-cross-linked polymer is chosen to solubilize relatively rapidly when exposed to blood. The non-cross-linked polymer serves as a binder for holding the materials in desired geometries, such as sheets, pellets, plugs, or the like. Usually, the cross-linked polymer will be present in a particulate or fragmented form. The materials are particularly suitable for hemostasis and drug delivery.

Abstract: The present invention provides a method of detecting a biological agent including contacting a sample with a sensor including a polymer system capable of having an alterable measurable property from the group of luminescence, anisotropy, redox potential and uv/vis absorption, the polymer system including an ionic conjugated polymer and an electronically inert polyelectrolyte having a biological agent recognition element bound thereto, the electronically inert polyelectrolyte adapted for undergoing a conformational structural change upon exposure to a biological agent having affinity for binding to the recognition element bound to the electronically inert polyelectrolyte, and, detecting the detectable change in the alterable measurable property. A chemical moiety being the reaction product of (i) a polyelectrolyte monomer and (ii) a biological agent recognition element-substituted polyelectrolyte monomer is also provided.

Abstract: A conjugate comprised of a hydrophilic polymer covalently yet reversibly linked to a amine-, hydroxy- or carboxyl-containing ligand is described. The resulting conjugate is capable of releasing the parent amine, hydroxy, or carboxyl-containing compound via thiol-mediated cleavage. The system allows for delivery of various amino-, hydroxy-, or carboxy-containing drugs in the form of their thiolytically cleavable macromolecular conjugates.

Abstract: The invention concerns an electroactive complex, consisting of an electroactive homopolymer or copolymer polymer of at least two monomers, and anti-ligand and a ligand having specifically interacted with said antiligand, and further at least an electron donor group, and an electroactive probe, consisting of said polymer said antiligand capable of interacting specifically with said ligand and at least an electron donor group.

Abstract: The present invention relates to an improved process for making commercial quantities of a polypeptide or fragment thereof, e.g. a T-20 or a T-1249 composition, or a fragment of a T-20 or a T-1249 composition. One variant of a T-20 composition is known as Fuzeon™ enfuvirtide. The improvement includes using a low void space resin, a resin made from a copolymer having less than 5% organic extractables, a resin made using a chloride corrosion resistant filter, resin beads functionalized using a nitro-compound, resins made using jetting techniques, and resins made using seed expansion techniques. In yet other variants, the invention provides a composition made using the processes described herein.

Abstract: The present invention provides a chemically-modified protein prepared by binding polyethylene glycol to a polypeptide characterized by being the product of expression by a host cell of an exogenous DNA sequence and substantially having the following amino acid sequence: 1 (Met) n Thr Pro Leu Gly Pro Ala Ser Ser Leu Pro Gln Ser Phe Leu Leu Cys Cys Leu Glu Gln Val Arg Lys Ile Gln Gly Asp Gly Ala Ala Leu Gln Glu Lys Leu Cys Ala Thr Tyr Lys Leu Cys His Pro Glu Glu Leu Val Leu Leu Gly His Ser Leu Gly Ile Pro Trp Ala Pro Leu Ser Ser Cys Pro Ser Gln Ala Leu Gln Leu Ala Gly Cys Leu Ser Gln Leu His Ser Gly Leu Phe Leu lyr Gln Gly Leu Leu Gln Ala Leu Glu Gly Ile Ser Pro Glu Leu Gly Pro Thr Leu Asp Thr Leu Gln Leu Asp Val Ala Asp Phe Ala Thr Thr Ile Trp Gln Gln Met Glu Glu Leu Gly Met Ala Pro Ala Leu Gln Pro Thr Gln Gly Ala Met Pro Ala Phe Ala Ser Ala Phe Gln Arg Arg Ala Gly Gly Val Leu Val Ala Ser His L

Abstract: A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.

Abstract: Provided are crosslinked polymer compositions that include a first synthetic polymer containing multiple nucleophilic groups covalently bound to a second synthetic polymer containing multiple electrophilic groups. The first synthetic polymer is preferably a synthetic polypeptide or a polyethylene glycol that has been modified to contain multiple nucleophilic groups, such as primary amino (—NH2) or thiol (—SH) groups. The second synthetic polymer may be a hydrophilic or hydrophobic synthetic polymer, which contains or has been derivatized to contain, two or more electrophilic groups, such as succinimidyl groups. The compositions may further include other components, such as naturally occurring polysaccharides or proteins (such as glycosaminoglycans or collagen) and/or biologically active agents.

Abstract: Provided are crosslinked polymer compositions that include a first synthetic polymer containing multiple nucleophilic groups covalently bound to a second synthetic polymer containing multiple electrophilic groups. The first synthetic polymer is preferably a synthetic polypeptide or a polyethylene glycol that has been modified to contain multiple nucleophilic groups, such as primary amino (—NH2) or thiol (—SH) groups. The second synthetic polymer may be a hydrophilic or hydrophobic synthetic polymer, which contains or has been derivatized to contain, two or more electrophilic groups, such as succinimidyl groups. The compositions may further include other components, such as naturally occurring polysaccharides or proteins (such as glycosaminoglycans or collagen) and/or biologically active agents.

Abstract: Facially amphiphilic polymers and articles made therefrom having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a method to identify and optimize the facial amphiphilicity of polyamide, polyester, polyurea, polyurethane, polycarbonate and polyphenylene polymers. Utility as a contact disinfectant is disclosed.

Abstract: The aim of the invention is to provide a modified collagen peptide for preventing post-operative adhesions that is non-toxic, economic, in addition to being easy to obtain, sterilize, manipulate and implement, having controlled biodegradability and presenting a sufficiently strong initial mechanical resistance in situ (cohesion). This is achieved in the case of the modified collagen peptide for preventing post-operative adhesions according to the invention which is characterized in that it comprises at least one collagen peptide that is modified by grafting thiol functions that are free or substituted, cross-linkable and/or at least partly cross-linked, whereby the thiol functions are provided by mercaptoamine radicals that are exclusively grafted on the aspartic and glutamic acids of the collagen chains by means of amide bonds. The modified collagen peptide can exist in the form of a homogeneous or composite film, as a gel or in as a liquid which can be applied and cross-linked per se as on in vivo tissue.

Abstract: The present invention provides methods of discovering and mapping secondary binding sites on biological molecules (e.g., proteins), the effects, if any, of site occupancy on the primary function of the molecule, and the screening of small molecules against the secondary binding sites. The invention further provides novel complexes for modification of secondary binding sites and the resulting modified biological molecules.

Abstract: The present invention provides polysubstituted polycarboxylic phosphoamide biopolymers (PPPBs) comprising polysaccharides and glycopolypeptides attached to a phospho-citrate backbone. Phosphorylation of the biopolymers yields phosphorylated polysubstituted polycarboxylic phosphoamide biopolymers (pPPPBs) which can be used as inflammatory response modulators, immunomodulators and/or biological response modifiers. Methods for producing the PPPBs in yeast subjected to multiple chemical stressors, and uses of compositions derived therefrom, are provided.

Abstract: A method of bonding a substance to be incorporated into a free terminal of a water-soluble polymer compound chain, characterized by reacting a reactive functional group present at the free terminal of the water-soluble polymer compound chain which is bonded at a binding terminal thereof in the manner of bristles of a brush onto a surface of a base material; with the substance to be incorporated capable of reacting with the reactive functional group; in the presence of a water-soluble polymer compound which promotes the bonding, is disclosed.

Abstract: This invention relates to novel solid support based on selenium and a method for the preparation thereof. The solid support is useful in solid phase synthesis of organic compounds including combinatorial libraries of compounds.

Abstract: A phototriggerable composition and method for use in crosslinking protein such as collagen comprising application of a tethered diazopyruvate composition followed by irradiation, whereby the composition results in the sutureless wound closure of, for example, a tendon or cornea.

Abstract: A polymer comprising recurring units represented by formula (I): 1

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

Abstract: The present invention relates to the preparation of polyethylene glycol carbonate active esters useful for the PEGylation of biological active and pharmaceutically useful peptides and proteins. The invention involves the use of activated carbonate and oxalate esters in the formation of polyethylene glycol mixed carbonate active esters that then react with a linker or directly with a target peptide or protein.

Abstract: Methods and compositions for improving the angiogenesis-inhibitory effect of an anti-angiogenic serpin, or anti-angiogenic fragment thereof, by covalently linking a polymer moiety to the serpin such that the biological half-life of the serpin is extended for inhibition of diseases having a pathological angiogenic component including diabetic retinopathy, age-related macular degeneration, rheumatoid arthritis, endometriosis, psoriasis, juvenile hemangioma, and cancer.

Abstract: An object of the present invention is to provide an immunoassay of PSA using an agglutination accelerator, which has an agglutination accelerating effect equal to or stronger than the known agglutination accelerator; hardly generates non-specific turbidity; and hardly generates salting out even in a solution with a high salt concentration.

Abstract: High molecular weight derivatives of activated poly(ethylene glycol) and the like polymers are prepared in high purity by conjugating a large PEG molecule to a small PEG molecule. Most of the reaction steps can be accomplished on the more readily purified small molecule to avoid laborious purification of the high molecular weight derivatives.

Abstract: A process for purification which permits satisfactory removal of impurities from a block copolymer consisting essentially of polyethylene glycols and poly(acidic amino acid) and is suitable for the production of a polymeric carrier having a pharmaceutically acceptable purity; a process for producing such a polymeric carrier; a block copolymer reduced in impurity content; a polymeric carrier as described above; pharmaceutical preparations in polymeric form, produced by the use of the carrier; and a method of subjecting polyethylene glycols and poly(acidic amino acids)—which are impurities contained in the block copolymer—to treatment with either an ion-exchange resin or a partition/absorption resin and then determining the quantities of them with a gel filtration column.

Abstract: We describe a class of polymaleic anhydride polymers capable of disrupting cell membranes. Co-delivery of these polymers with biologically active compounds increases cellular cytoplasmic delivery of the compounds.

Abstract: A dihydroxyphenyl cross-linked macromolecular network is provided that is useful in artificial tissue and tissue engineering applications, such as artificial or synthetic cartilage. The network is made by first providing a polyamine or polycarboxylate macromolecule (having a plurality of amine or carboxylic acid groups respectively attached along the length of the molecule), reacting this macromolecule with a hydroxyphenyl compound having a free carboxylic acid group in the case of a polyamine or a free primary amine group in the case of a polycarboxylate, and substituting the hydroxyphenyl compound onto the macromolecule via a carbodiimide-mediated reaction pathway to provide a hydroxyphenyl-substituted macromolecule. This macromolecule is then linked to other such macromolecules via an enzyme catalyzed dimerization reaction between two hydroxyphenyl groups attached respectively to different macromolecules under metabolic conditions of temperature and pH.

Abstract: Disclosed are a gel in which two or more ligands which are biomacromolecules are grafted, a process for producing the gel, a method for measuring a specific molecule in a sample using the gel, an apparatus, a measurement kit and a pharmaceutical composition comprising the gel, and a diagnostic method for various diseases using the measurement kit.

Abstract: The present invention relates to a recycling process for the preparation of solid phase bonded 2-chlorotrityl chloride (2-CTC resin) useful for solid phase peptide synthesis, wherein active chloride CTC resin is regenerated by reacting the spent resin with a chlorinating agent in organic solvent.

Abstract: One aspect of the present invention relates to methods and compositions for attenuating xenograft rejection by administering, to an animal receiving the xenograft, an amount of a polymer-derivatized xenoantigen (hereinafter “xenopolymer”) effective for inhibiting or lessening the severity of hyperacute rejection response (HAR), or other immunological response to the graft, that is dependent on the presence of the xenoantigen on the grafted tissues or cells. In certain embodiments, the xenopolymer is administered in an amount sufficient to neutralize host antibodies (“xenoreactive antibodies” or “XNA”) immunoreactive with the xenoantigen. The xenopolymer may additionally, or alternatively, be used as a tolerogen (or anergen) for the xenoantigen, e.g., able to suppress, to some degree, the production/secretion of XNAs by the immune system of the host.

Abstract: A biodegradable cationic lipopolymer comprising a polyethylenimine (PEI), a lipid, and a biocompatible hydrophilic polymer, wherein 1) the lipid and the biocompatible hydrophilic polymer are directly linked to the PEI backbone or 2) the lipid is linked to the PEI backbone through the biocompatible hydrophilic polymer. The cationic lipopolymers of the present invention can be used for delivery of a nucleic acid or any anionic bioactive agent to various organs and tissues after local or systemic administration.

Abstract: This invention pertains to the field of PNA dimer and PNA oligomer synthesis.

Abstract: The invention relates to crosslinked elastin, a water-soluble crosslinking agent to be used for crosslinking, molded elastin articles, medical instruments and regeneration tissues using the crosslinked elastin, and a surgical therapy method and regeneration treatment wherein the medical instruments are employed. There is provided a biocompatible functional material having elasticity suitable for transplantation into the body without causing detachment of cell adhesion proteins.

Abstract: Methods are provided for the synthesis of polymer conjugates of cytokines, chemokines, growth factors, polypeptide hormones and receptor-binding antagonists thereof, which conjugates retain unusually high receptor-binding activity. Preparation of polymer conjugates according to the methods of the present invention diminishes or avoids steric inhibition of receptor-ligand interactions that commonly results from the attachment of polymers to receptor-binding regions of cytokines, chemokines, growth factors and polypeptide hormones, as well as to agonistic and antagonistic analogs thereof. The invention also provides conjugates and compositions produced by such methods. The conjugates of the present invention retain a higher level of receptor-binding activity than those produced by traditional polymer coupling methods that are not targeted to avoid receptor-binding domains of cytokines, chemokines, growth factors and polypeptide hormones.

Abstract: The present invention relates to site-specific conjugation of synthetic particles to proteins.

Abstract: Polyphosphazenes suitable for use as immunostimulants alone or in combination with an antigen are disclosed.

Abstract: Colorimetric sensors comprising a receptor incorporated within polydiacetylene assemblies to form a transducer capable of indicating a color change when contacted with an analyte are disclosed. Methods of using the colorimetric sensor and a kit for the colorimetric detection of an analyte are also disclosed.

Abstract: The present invention includes a bifunctional specificity structure that includes a peptide linker having a first and a second binding domain, wherein the first binding domain is selective for a first biomaterial and the second binding domain is selective for a second biomaterial. The present invention also includes a method of making and identifying the bifunctional structure of the present invention and methods of using the same.

Abstract: The present invention relates to novel compositions and methods for delivering substances to target tissues and cells by contacting the targets with delivery systems associated with membranes (e.g., biocompatible or bioerodable membranes). More particularly, the present invention is directed to dendrimer-based methods and compositions for use in disease therapies, wound healing, and generally, improved gene transfection and compound delivery to target cells and tissues in vitro and in vivo.

Abstract: The present invention discloses novel crosslinked biomaterial compositions which are prepared using hydrophobic polymers as a crosslinking agent. Preferred hydrophobic polymers are those that contain two or more reactive succinimidyl groups, including disuccinimidyl suberate, bis(sulfosuccinimidyl)suberate, and dithiobis(succinimidyl)propionate. Crosslinked biomaterial compositions prepared using mixtures of hydrophobic and hydrophilic crosslinking agents are also disclosed. The compositions of the present invention can be used to prepare formed implants for use in a variety of medical applications.