Abstract: A type of composite material where the matrix material and additive are held together by covalently or non-covalently bound ligands is described. A particularly useful composite material covered by the present invention is a carbon nanotube-reinforced composite material where the matrix consists of a polymer, covalently attached to a linker, where said linker is non-covalently attached to the carbon nanotube. Methods for the preparation of such composite materials are provided.

Abstract: A curable film-forming composition is provided, comprising: (a) a polymeric polyester binder comprising a plurality of carbamate groups; (b) a curing agent reactive with the carbamate functional groups of (a); and (c) a reaction product of: (1) a hydroxyl functional polymer comprising the reaction product of: (i) a monomer comprising at least two ethylenically unsaturated double bonds; (ii) a monomer comprising a carbon atom that is bonded to four moieties wherein one of the moieties is a hydrogen atom and the remainder of the moieties comprises an alkyl group, wherein at least one of the alkyl group-containing moieties comprises an ethylenically unsaturated double bond; and (iii) at least one monomer that is polymerizable with (i) and (ii); and (2) a lactone or lactam. Also provided are a multi-component composite coating composition that includes the curable film-forming composition described above and methods for forming a composite coating on a substrate.

Abstract: The invention relates to tungsten (VI) salts for use thereof in the treatment of infertility in a non-diabetic female mammal, for favoring normal reproduction and fertility in a non-diabetic female mammal, or for increasing the efficacy of an assisted reproductive technique applied to a mammal, as well as compositions containing same and methods for treatment using same.

Abstract: The present invention comprises the use of a therapeutically effective amount of a tungsten (VI) salt with a pharmaceutically or veterinarily acceptable cationic group, or a solvate of said salt, for the preparation of a medicinal product for the treatment of female infertility in non-diabetic mammals.

Abstract: The present disclosure provides novel crystalline forms of a compound that acts as a ?-arrestin effector, processes for preparing novel crystalline and amorphous forms of a compound that acts as a ?-arrestin effector and uses thereof.

Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

Abstract: The invention provides heteropolymer compositions and peptide compositions, and methods of making and using therapeutic compositions comprising amino acid heteropolymers for treatment of a subject for an autoimmune or an inflammatory disease, the heteropolymer compositions made by solid state synthesis. The invention also provides kits for assaying binding of a composition to a water-soluble MHC protein.

Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.

Abstract: The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.

Abstract: The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.

Abstract: There is provided a novel process for preparing polyamides (in particular cyclic and hairpin polyamides) comprising the step of coupling an amine with a Boc-protected amino acid monomer in the presence of diphosgene and/or triphosgene. Such a process may be performed on a solid or solution phase.

Abstract: The present invention provides a block copolymer for a drug conjugate which comprises a water-soluble polymer region consisting of polyethylene glycol and a polyamino acid region having a hydrazide group and a hydrophobic group in the side chain.

Abstract: The invention relates to a binder for producing materials based on wood chips and/or wood fibers. The aim of the invention is to design a binder which is used for producing and gluing materials based on wood chips and/or wood fibers, contains natural protein components, significantly reduces or even eliminates the drawbacks of the prior art, and can be economically produced and used. Said aim is achieved by a binder which is used for materials based on wood chips and/or wood fibers, comprises an aldehyde-based condensation resin and other additives, and is characterized in that the binder comprises a water-soluble reactive additive containing a peptide/amino acid mixture without moieties of water-insoluble and high-viscosity proteins. The invention also relates to a method for producing said binder as well as a molded article.

Abstract: A biocompatible, biodegradable, macromolecular water-absorbent hybrid material (WAHM), having a three-dimensional configuration with intermolecular covalent bonds and containing free functional groups, said polymer being formed by polymer-polymer intercoupling reaction between a natural water-soluble polymer A or its derivatives having a molecular weight between 20,000 and 300,000 Da, and a synthetic polymer B in an adequate ratio wherein the natural polymer A is selected from amphoteric reactants, partially denatured or chemically modified natural polymer, that dissociates in water to form both anions and cations, and which can undergo polymer-polymer intercoupling reactions, and wherein synthetic polymer B s a linear or branched reactive synthetic copolymer having a molecular weight of 50,000-500,000 Da derived from a vinyl monomer and an ethylenically unsaturated monomer, having a backbone with polymeric subunits covalently bonded to the polymer backbone, the subunits comprising ones with non-reactive and

Abstract: The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through ether linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.

Abstract: The present invention is directed to methods of producing conjugates of A? peptide immunogens with protein/polypeptide carrier molecules, which are useful as immunogens, wherein peptide immunogens are conjugated to protein carriers via activated functional groups on amino acid residues of the carrier or of the optionally attached linker molecule, and wherein any unconjugated reactive functional groups on amino acid residues are inactivated via capping, thus retaining the immunological functionality of the carrier molecule, but reducing the propensity for undesirable reactions that could render the conjugate less safe or effective. Furthermore, the invention also relates to such immunogenic products and immunogenic compositions containing such immunogenic products made by such methods.

Abstract: A solid phase peptide synthesis method is disclosed. The method includes the steps of deprotecting an amino group in its protected form that is protected with a protecting group that includes an ?,?-unsaturated sulfone; washing the deprotected acid in a solvent selected from the group consisting of water, alcohol, and mixtures of water and alcohol; coupling the deprotected acid to a resin-based peptide or a resin-based amino acid; and washing the coupled composition in a solvent selected from the group consisting of water, alcohol, and mixtures of water and alcohol.

Abstract: There is provided a novel process for preparing polyamides (in particular cyclic and hairpin polyamides) comprising the step of coupling an amine with a Boc-protected amino acid monomer in the presence of diphosgene and/or triphosgene. Such a process may be performed on a solid or solution phase.

Abstract: A method for providing high-density polymer surface for attaching proteins or peptides, and binding proteins, peptides, DNAs, cells, small molecules, and other chemical or biological molecules that are of interests in the areas of proteomic, genomic, pharmaceutical, drug discovery, and diagnostic studies.

Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.

Abstract: The present invention provides for an efficient process for making pramlinitide, as well as novel intermediates for the making of the same.

Abstract: ?-peptide regions of polypeptides can serve as structural mimics of ?-helices in wild type proteins. Because ?-helices of one protein often bind to a target protein in a biological pathway, a polypeptide that contains a helical ?-peptide region can be used to disrupt this type of protein-protein binding. As a result, polypeptides that contain a helical ?-peptide region can be used to treat conditions involving this type of protein-protein binding, such as viral infections and cell proliferation.

Abstract: An RGD polypeptide grafted poly (glycolic acid-L-lysine-L-lactic acid)/?-tricalcium phosphate composite material is composed of ?-tricalcium phosphate particles and RGD polypeptide grafted poly (glycolic acid-L-lysine-L-lactic acid) with mass ratio of 1:10-1:100, in which the ?-tricalcium phosphate particles are uniformly dispersed in the RGD polypeptide grafted poly (glycolic acid-L-lysine-L-lactic acid) matrix. The preparation method includes that poly (glycolic acid-L-lysine-L-lactic acid) is polymerized with GRGDY short peptide (glycin-arginine-glycin-aspartic acid-tyrosine sequence) to obtain RGD polypeptide grafted poly (glycolic acid-L-lysine-L-lactic acid), and then RGD polypeptide grafted poly (glycolic acid-L-lysine-L-lactic acid) is compounded with ?-tricalcium phosphate particles.

Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.

Abstract: A method of concentrating proteins from whole blood comprising exposing whole blood to covalently crosslinked hydrogel to remove water from the blood into the hydrogel to thereby concentrate the proteins in the whole blood. The hydrogel may absorb, for example, 50% or 90% of the water from the blood while excluding proteins with a weight of more than about 15,000 Daltons. In some embodiment, the hydrogels are dry, sterile, and spherical.

Abstract: The present invention relates to a thermosensitive and biocompatible poly(organophosphazenes) represented by Formula 1, and a preparation method thereof: wherein R is a methyl or ethyl group; R? is selected from the group consisting of COOR, CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R? is selected from the group consisting of CH2COOR, CH2CH2COOR, CH2CH(CH3)2, CH2C6H5, CH(CH3)CH2CH3 and CH3; R?? is a group selected from the group consisting of CH2COOR, CH2CH2COOR and H, wherein R is the same as defined above; n is a number between from 30 to 100; x is a number selected from the integers of 3, 4, 7, 12 and 16; y is a number between from 0.5 to 1.5; a equals to 1; and b and c equal to 0 or 1.

Abstract: Biocompatible crosslinked polymers, and methods for their preparation and use, are disclosed in which the biocompatible crosslinked polymers are formed from water soluble precursors having electrophilic and nucleophilic functional groups capable of reacting and crosslinking in situ. Methods for making the resulting biocompatible crosslinked polymers biodegradable or not are provided, as are methods for controlling the rate of degradation. The crosslinking reactions may be carried out in situ on organs or tissues or outside the body. Applications for such biocompatible crosslinked polymers and their precursors include controlled delivery of drugs, prevention of post-operative adhesions, coating of medical devices such as vascular grafts, wound dressings and surgical sealants. Visualization agents may be included with the crosslinked polymers.

Abstract: The present disclosure relates to processes for preparing metal-free, mono-dispersed polymers of amino acids. The polymers include homopolymers, random copolypeptides, block copolypeptides, block copolymers with at least one peptidyl block, grafted copolypeptides, and polypetidyl dendrimers. The disclosed process does not make use of a heavy metal catalyst, inter alia, copper or nickel containing reagents. The disclosed process encompasses a “living polymerization” such that the growth of each polymer chain is not truncated or otherwise halted by undesirable side reactions or limitations due to the length or size of the growing polymer chain, provides amino acid comprising polymers having a narrow polydispersity, is conducted at lower temperatures, and avoids the premature secondary folding that inhibits the formation of polymers having a low polydispersity index.

Abstract: A process for preparing a peptide by solid phase synthesis in the N to C direction comprising a capping step after an amide bond formation step to prevent or reduce deletion artefacts.

Abstract: The invention discloses a coordination compound comprising (1,2-diaminocyclohexane)platinum (II) moiety and poly(ethylene glycol)-block-poly(glutamic acid) copolymer moiety; and its use as an anti-cancer agent. The characteristic feature lies in the use of a copolymer whose poly(glutamic acid) segment has a chain length consisting of, on an average, less than 35 repeating units.

Abstract: Biocompatible crosslinked polymers, and methods for their preparation and use, are disclosed in which the biocompatible crosslinked polymers are formed from water soluble precursors having electrophilic and nucleophilic functional groups capable of reacting and crosslinking in situ. Methods for making the resulting biocompatible crosslinked polymers biodegradable or not are provided, as are methods for controlling the rate of degradation. The crosslinking reactions may be carried out in situ on organs or tissues or outside the body. Applications for such biocompatible crosslinked polymers and their precursors include controlled delivery of drugs, prevention of post-operative adhesions, coating of medical devices such as vascular grafts, wound dressings and surgical sealants. Visualization agents may be included with the crosslinked polymers.

Abstract: Proteinaceous gels having visualization agents and methods of use thereof are disclosed herein. Further, polymeric crosslinking agents are disclosed that have an inert water soluble polymeric component, biodegradable components, functional components reactive with chemical groups on a protein, for example, amine or thiol groups. The inert polymeric component may be flanked at each end with a biodegradable component which is flanked at each end with a protein reactive functional component. A polymeric crosslinking agent is disclosed having a biodegradable component, polyalkylene oxide, and at least three reactive functional groups that are each capable of forming a covalent bond in water with at least one functional group such as an amine, thiol, or carboxylic acid.

Abstract: A bio-liquid crystal polymer is made from a tissue-derived compound or the derivatives. The bio-liquid crystal polymer has a characteristic of liquid crystal under predetermined conditions and is biocompatible.

Abstract: Dendrimers comprising a dentritic polypeptide with one dendron having terminal cationic groups and a lipidic anchor, preferably comprising C6-24-alkyl group containing ?-amino acyl groups, preferably joined to the focal group, are used to assist transfection of cells in vitro and in vivo by DNA. The complex of dendrimer and DNA may be used in gene therapy, for instance to delivery clotting factor genes to cells.

Abstract: Materials, methods, and compositions for making crosslinked albumin hydrogels are included in the application. Embodiments include a biocompatible material of albumin crosslinked with an n-functional crosslinking agent wherein n is at least 3. Other embodiments include a cross-linking agent having a polyalkylene oxide member. Other embodiments include a system for administering an albumin material, the system having albumin and a crosslinking agent that reacts with the albumin to form a crosslinked material made of crosslinked albumin. Another embodiment is a method of making a biocompatible material that includes a step of mixing albumin with an n-functional crosslinking agent wherein n is at least 3.

Abstract: Carboxylic acid-substituted polyalkylene polyamines in which amine nitrogen atoms on the polyamine backbone structure are replaced by guanidine groups provide a pH range extending into high pH values. These substances are useful as carrier ampholytes in isoelectric focusing.

Abstract: Biocompatible crosslinked polymers, and methods for their preparation and use, are disclosed in which the biocompatible crosslinked polymers are formed from water soluble precursors having electrophilic and nucleophilic functional groups capable of reacting and crosslinking in situ. Methods for making the resulting biocompatible crosslinked polymers biodegradable or not are provided, as are methods for controlling the rate of degradation. The crosslinking reactions may be carried out in situ on organs or tissues or outside the body. Applications for such biocompatible crosslinked polymers and their precursors include controlled delivery of drugs, prevention of post-operative adhesions, coating of medical devices such as vascular grafts, wound dressings and surgical sealants. Visualization agents may be included with the crosslinked polymers.

Abstract: Polymeric crosslinking agents are disclosed that have an inert water soluble polymeric component, biodegradable components, functional components reactive with chemical groups on a protein, for example, amine or thiol groups. The inert polymeric component may be flanked at each end with a biodegradable component which is flanked at each end with a protein reactive functional component. A polymeric crosslinking agent is disclosed having a biodegradable component, polyalkylene oxide, and at least three reactive functional groups that are each capable of forming a covalent bond in water with at least one functional group such as an amine, thiol, or carboxylic acid.

Abstract: A bio-compatible, biodegradable macromolecular water-absorbent polymeric material having a three-dimensional configuration with intermolecular covalent bonds and containing free functional groups selected from OH, SH, NH2, and COOH. The polymer is formed by polymer-polymer inter-coupling interaction between a natural water-soluble polymer A or its derivatives having a molecular weight between 20,000 and 500,000 Da, and a synthetic polymer B in a ratio of A:B of 15:85 to 85:15.

Abstract: A method for preparing a solid support material for carrying out a chemical reaction, said method comprising the following steps: (i) reacting an amino functionalised solid material with a carboxylic acid having at least two similarly protected amino groups to form amide bonds between them, (ii) removing protecting groups in a single step, (iii) optionally repeating steps (i) and (ii) one or more times using the product of the preceding step as the amino functionalised solid material, and (iv) connecting a linkage agent to at least some of the free NH2 groups of the product. The method increases the loading capacity of the solid support material. It is particularly useful in connection with peptide synthesis.

Abstract: Process for the preparation of copolymeric polypeptides, which comprises, in a first stage, reacting glutamic acid and/or derivatives thereof with amines in the absence of solvents and catalysts, under condensation conditions and, in a second stage, adding one or more further amino acids and/or derivatives thereof and/or one or more identical and/or further amines simultaneously or in any desired order, and reacting them with the reaction product of the first stage in the absence of solvents and catalysts.

Abstract: This invention provides compositions and methods for enhancing delivery of glucocorticoids and ascomycins such as hydrocortisone, cyclosporin and FK506 across into and across one or more layers of the skin for the treatment of psoriasis and other inflammatory diseases of the skin.

Abstract: A crosslinked polymer bead which, when: (i) functionalized with a 2-chlorotrityl chloride group; (ii) coupled with Leu to 0.65 mmol/g; and (iii) coupled with Glu(t-Bu); allows coupling of FMOC-Lys(BOC)-OH at an amount of 1.5 equivalents in the presence of 1.5 equivalents of HOBT, 1.5 equivalents of DIEA and 1.5 equivalents of HBTU, to be completed, as determined by the Kaiser test, in no more than 35 minutes.

Abstract: The present invention relates to novel templates useful for generating novel compounds and to compounds produced utilizing the templates. The templates comprise quaternary amino acids that may be linked to solid supports. These templates make possible the production of novel classes of chemical compounds through a plurality of chemical reactions. The templates are advantageous for use in drug discovery regimes.

Abstract: The present invention relates to a process for the preparation of thermoprecipitating affinity polymers useful in the enhanced recovery of enzymes. The process comprises polymerising a monomer comprising a spacer and a co-monomer with a polymerisation initiator and a polymerisation accelerator at ambient temperature and pressure for a period ranging between 2 to 24 hours to obtain a polymer and then linking an inhibitor to pendant carboxyl groups of the spacers in the polymer to obtain an affinity polymer.

Abstract: Template-textured materials in the form of template-textured polymers (TGP) on various surfaces including membranes (i.e, template-textured membranes). Such materials are created by modifying the surface of solid carriers, which, by cross-linking polymerization of functional monomers initiated on the surface of said solid carriers in the presence of a template, leads to stable template prints that subsequently bind template molecules or template derivatives in a specific manner. The invention also relates to methods for the production of TGPs and to the use thereof for substance-specific separation of materials.

Abstract: The present invention relates to a novel solid support template of Formula (I) and methods for producing novel highly functionalized imidazoles, pyrazinones and benzodiazepinones through a plurality of chemical reactions utilizing the solid support template

Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the &agr;-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the &agr;-amine of a polypeptide having a cysteine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.

Abstract: The invention features a new solid supports having at least one amino functionality and a linker bound to the solid support through at least a portion of the amino functional groups. The invention also features solid support bound substrates suitable for use in the formation of macrocycles by a TE domain catalyzed macrocyclization reaction. The invention features methods of making the solid supports and solid support bound substrates of the invention and methods of effecting macrocyclizations of solid support bound substrates. The invention further provides new macrocyclic molecules having one or more peptide domains and one or more polyketide domains in the macrocyclic ring. In another embodiment of the invention, libraries of macrocycles are provided as well as methods of forming libraries of macrocycles from libraries of solid support bound substrates are provided.