Abstract: The present invention provides a composition of nanoparticles comprising a biological mimetic base component that forms the structure of the nanoparticle. By interacting with the functional groups of the base component, the half-life of a bioactive molecule is extended.

Abstract: The invention relates to a capped cyclodextrin-hydrophobic moiety conjugate, to a supramolecular polymer formed of capped cyclodextrin-hydrophobic moiety conjugates according to the invention and to a siRNA-cyclodextrin complex comprising a supramolecular polymer according to the invention. The invention also relates to a method for manufacturing the capped cyclodextrin-hydrophobic moiety conjugate, the supramolecular polymer, the siRNA-cyclodextrin complex according to the invention. The capped cyclodextrin-hydrophobic moiety conjugate of the invention comprises a capped cyclodextrin group and at least one hydrophobic moiety bound by a first linker to one of the carbon atoms of the cap. The invention can be used for various applications in particular in the pharmaceutical field.

Abstract: The present invention provides methods for selecting a suitable anticancer therapy, and for identifying and predicting response for the treatment of a gastric cancer.

Abstract: To provide a novel substance having an excellent water-dispersibility capable of forming an emulsion which spreads rapidly onto the skin, does not undergo aggregation or segregation due to a salt, and is excellent in a low temperature stability. The aforementioned problems were found to be solved by means of a certain polysaccharide and the invention was established.

Abstract: The present invention relates to a method for transducing a target cell, the method comprising the step of contacting a target cell with a retroviral vector and a poloxamer having a molecular weight of 12.8 kDa to about 15 kDa. Further, the invention relates to the use of a poloxamer as defined herein, optionally in combination with a polycationic substance as defined herein, for transducing a target cell with a retroviral vector and a kit comprising a retroviral vector, a poloxamer as defined herein and, optionally, instructions for use.

Abstract: The present invention provides a Ge adsorbent for a 68Ge—68Ga generator, which is a polysaccharide polymer having a glucamine group represented by the formula (1) or the formula (2), wherein R1 is a hydrogen atom or an alkyl group, and * is a bonding position.

Abstract: A hydrogel is provided which is obtained by reacting an azide group and a cyclooctyne group in the absence of a catalyst, especially in the absence of a copper catalyst. The hydrogel has: (a) a first polymer moiety composed of hyaluronic acid, carboxymethyl dextran or the like; (b) a second polymer moiety composed of hyaluronic acid, carboxymethyl dextran or the like, said second polymer moiety being of a kind that is same as or different from the kind of the moiety (a) and is composed of a molecule different from the moiety (a); and (c) a triazole ring group or a derivative group thereof.

Abstract: In certain embodiments, a nano-sized vehicle (e.g., a nanogel comprising nanoparticles) is provided herein for drug delivery with tunable biodistribution, low toxicity, and degradability, and with demonstrated targeting to bone. The composition is useful, for example, in the treatment of bone disease, particularly bone metastases from cancers such as breast, prostate, or lung cancer.

Abstract: Cationic dextran polymer derivatives including an ester-linked amine-containing substituent and an alkyl ester substituent and methods for making such dextran polymer derivatives are disclosed.

Abstract: The present invention relates to an amphiphilic polymer whose property and structure can change under hypoxic conditions, and to nanoparticles formed by self-assembly of the amphiphilic polymer. The hypoxia-responsive nanoparticles according to the present invention release a drug selectively under hypoxic conditions. Thus, the nanoparticles can be used for the selective diagnosis and treatment for diseases that are accompanied by hypoxia. Particularly, the nanoparticles can release a drug only to a targeted tumor in cancer therapy, and thus have minimized side effects and maximized therapeutic effects.

Abstract: Hydroxamate substituted azaindoline cyanine dyes, conjugates thereof and methods of using the same are provided. The subject cyanine dyes include an azaindoline ring having a hydroxamate substituent. The dyes may further include a reactive group moieties (RGM) and/or a water soluble group. Also provided are conjugates of the subject dyes. Also provided are tandem conjugates including a fluorescent protein capable of energy transfer to the dye. Methods of detecting an analyte in a sample by contacting the sample with a detection reagent are provided. The detection agent may be a dye-conjugate that specifically binds the analyte, or may be a reactive dye which conjugates to the analyte. Also provided are compositions, e.g., kits, etc., incorporating such dyes which facilitate use in such methods.

Abstract: Provided herein are water-soluble carbohydrate polymers which are monoderivatized at their reducing terminus, such that the carbohydrate polymers can be selectively conjugated at a single location. Also provided are methods of preparation and conjugation of the monoderivatized carbohydrate polymers.

Abstract: Methods and materials are disclosed relating to an improved method for amplifying a signal in a diagnostic assay for a nucleic acid, comprising the steps of providing an amplification polymer bound to a nucleic acid analyte, wherein the amplification polymer comprises a plurality of amine groups; binding amine groups on the amplification polymer with a detectable label complex; and reacting under high salt conditions an acetylating compound with amine groups not bound with a detectable label complex.

Abstract: Provided are polymer particles which can be used at a high flow rate when used as a filler for chromatography, that is, has excellent resistance flow rate appropriate for processing in large quantities, and also has a high binding capacity for target molecules such as proteins when an appropriate ligand is contained in the particles, and a method for producing the polymer particles; specifically, crosslinked polymer particles and a method for producing the crosslinked polymer particles, polysaccharide composite particles and a method for producing the polysaccharide composite particles, a filler for chromatography using the polymer particles, and an adsorbent for antibody purification. Disclosed are: A.

Abstract: This invention relates to a method of conveniently functionalizing the reducing end of a carbohydrate polymer. The method also allows for the length of the polymer to be differentially functionalized. The invention provides a method for preparing polymers with a different functional groups or functionality on the sides than on the reducing end. An advantage of the method of the invention is that the procedures are simpler, preferably requiring less time, fewer steps, reduced temperatures and less harsh chemical components than conventional procedures for differential modification, with the further advantage that the reactions can be carried out in aqueous media.

Abstract: A method for making functionalized porous crosslinked polysaccharide gel coated structures used as liquid chromatography media is provided. The method includes impregnating a porous substrate with a room temperature stable aqueous polysaccharide solution containing water, 0.1% to 20% of a polysaccharide, 18% to 54% of a gel-inhibiting agent to prevent the gel from re-gelling, and 0.001% to 10% of an anionic fluorosurfactant for optimum solution coatability onto the substrate, each concentration is by total weight of the aqueous solution. Next water is evaporated from the coating, followed by exposing the dehydrated coating to a gelling agent thereby forming a porous polysaccharide gel coated substrate. Next the gel coated substrate is exposed to a crosslinking agent forming a porous crosslinked polysaccharide gel coated substrate.

Abstract: A polysaccharide comprising carboxyl functional groups, at least one of which is substituted with at least one hydrophobic radical: the hydrophobic radical being a residue of a hydrophobic alcohol having a linear, branched or cyclic alkyl chain containing at least 6 carbon atoms, the hydrophobic radical being bonded to a linker arm R by a function G, the linker arm R being bonded to a carboxyl function of the polysaccharide by a bond F, R being an at least divalent radical of a chain including between 1 and 15 carbons, which is optionally branched and/or unsaturated, optionally including one or more heteroatoms, chosen amongst O, N and/or S, F being an amide function, G being a carbamate function, the unsubstituted carboxyl functions of the polysaccharide being in the form of a cation carboxylate, said cation being chosen amongst alkali metal cation.

Abstract: The present invention provides antimicrobial nanoparticle conjugates and an efficient method of preparing same. In particular, the invention relates to the preparation of antifungal nanoparticle conjugates comprising amphotericin B covalently immobilized to nanoparticles. The conjugates, and suspensions thereof, can be used to form antifungal coatings with particular application to medical devices and materials.

Abstract: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.

Abstract: The invention discloses a method for producing a hemostatic composition comprising mixing a biocompatible polymer suitable for use in hemostasis and a genipin-type crosslinker, crosslinking said polymer by said genipin-type crosslinker to obtain a crosslinked biocompatible polymer, and finishing said crosslinks polymer to a pharmaceutically acceptable hemostatic composition, new hemostatic compositions and methods for using such compositions.

Abstract: The present invention relates to polyamine-containing polymers and methods of their synthesis and use. The polymer may be hydroxyethylcellulose, dextran, poly(vinyl alcohol) or poly(methyl acrylate).

Abstract: An inhibiting heart failure disease pharmaceutical composition is provided. The pharmaceutical composition includes: an effective amount of a KMUP-3 amine salt of formula (I); wherein RX contains a carboxylic group donated from one selected from a group consisting of a sodium carboxyl methylcellulose (sodium CMC), a ?-polyglutamic acid derivative, and co-polymer salt; RX? is an anion form of the carboxylic group; and a pharmaceutically accepted carrier.

Abstract: The invention relates to an oligodextran, chosen from dextrans whose average degree of polymerization is less than 10, modified by at least one substituent of general formula I: —R1-[[AA]-[R2]n]m??formula I It also relates to a pharmaceutical composition characterized in that it comprises an oligosaccharide according to the invention and an active ingredient is chosen from the group consisting of proteins, glycoproteins, peptides and non-peptide therapeutic molecules.

Abstract: The invention provides a copolymer of hyaluronic acid (HA) grafted with a dextran-tyramine (Dex-TA) conjugate.

Abstract: An anionic polysaccharide comprising carboxylic acid functional groups of formula I: in which: the polysaccharide may be either, synthetic or modified, i represents the degree of functionalization of the hydroxyls, j represents the degree of functionalization of the hydroxyls, L and Q represent an optionally branched and/or unsaturated chain comprising from 1 to 15 carbons, F is a functional group chosen from the group consisting of the carbamate functional group, the carbonyl being bonded to the Q radical, the ester functional group, the carbonyl being bonded to the Q radical, the amide functional group, the carbonyl being bonded to the Q radical, and the carboxylate functional group, and Grp is chosen from the group consisting of a mono- or divalent cation and of a chain comprising from 4 to 50 carbons.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: Cationic dextran polymer derivatives including an ester-linked amine-containing substituent and an alkyl ester substituent and methods for making such dextran polymer derivatives are disclosed.

Abstract: The synthesized piperazium salt of KMUPs disclosed in the present invention is characterized by presented pharmaceutics having functions to improve 5-HT function and eNOS expression of KMUPS in lung diseases, such as proliferation, obliteration, pulmonary artery hypertension. The pharmaceutical composition for inhibiting monocrotaline (MCT)-induced proliferation of pulmonary artery includes an effective amount of a complex salt of formula (I): wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; RX contains a carboxylic group donated from one selected from a group consisting of a Statin, a Co-polymer, a poly-?-polyglutamic acid (?-PGA) derivative and sodium CMC; and ?RX substituent is an anion of the carboxylic group carrying a negative charge; and a pharmaceutically accepted carrier.

Abstract: We describe methods that allow either carbodiimides or other carboxyl-reactive substances to be mixed with solutions of carboxylic acids or phosphates or amines or combinations thereof, so as to form a homogeneous mixture which is then dried, preferably in a freeze drying process. The mixture is then contacted with an entity, which preferably involves the dissolution of the mixture with a buffered solution of the entity, so as to initiate a conjugation reaction between the entity and a component in the mixture.

Abstract: Methods and reagents are disclosed for reducing an amount of non-covalently bound polysaccharide on a support. The method comprises contacting a support comprising both covalently bound polysaccharide and non-covalently bound polysaccharide with an aqueous solution comprising an amount of a chaotropic agent effective to remove non-covalently bound polysaccharide from the support.

Abstract: Acid polysaccharides characterized by the concomitant presence of partial esters with non-polysaccharide carboxylic acids and esters between the acid groups of the initial polysaccharide and the alcohol groups of the repetitive units, with the formation of crosslinking among the polysaccharide chains.

Abstract: Compounds and methods are disclosed in which a prodrug can be delivered in an elevated oxidative state to cells by means of graphitic nanoparticles to which the prodrug is attached by a hydrophilic polymer and which have been made soluble by a hydrophilic polymer, such as PEG. The graphitic nanoparticle may be a single walled carbon nanotube (SWNT). The prodrug may be a DNA-binding metal-based drug. Exemplified is a platinum(IV) complex c,c,t-[Pt(NH3)2Cl2(OEt)(O2CCH2CH2CO2H)], which is nearly nontoxic to testicular cancer cells, but displays a significantly enhanced cytotoxicity profile when attached to the surface of amine-functionalized soluble SWNTs. An amine functionality on the hydrophilic polymer may be used to link the prodrug.

Abstract: The present invention provides reagents containing binding moieties conjugated to dextran moieties, methods of making such reagents, and use of such reagents in a variety of molecular and cellular assays.

Abstract: Dextran of the following general formula I: is described, wherein R represents a chain containing from 1 to 15 carbon atoms and having at least one acid functional group prior to attachment to AA, the chain optionally being branched and/or unsaturated and containing one or more heteroatoms, such as O, N or/and S, F represents an ester, a carbamate or an ether, AA represents a hydrophobic amino acid radical, L or D, derived from a coupling between an amine of an amino acid and at least one acid functional group of R; the amino acid, prior to attachment to R, being selected from the group consisting of tryptophan, phenylalanine, leucine, isoleucine, alanine and valine, and alcohol, amide or decarboxylated derivatives thereof, and alkaline cation salts thereof, i represents the molar fraction of substituent F—R-[AA]n per glycosidic unit and is from 0.1 to 2, n represents the molar fraction of R groups substituted by AA and is from 0.

Abstract: The invention provides a novel class of fluorescent compounds. Also provided are conjugates of the fluorescent compounds, methods of using the fluorescent compounds and their conjugates as well as kits including the fluorescent compounds and their conjugates.

Abstract: Modified polysaccharides and crosslinked modified polysaccharide compositions are described. Methods of using the crosslinked modified polysaccharide compositions to deliver proteins, oligonucleotides, or pharmaceutical agents are also disclosed.

Abstract: The present invention provides methods for making porous crosslinked polysaccharide hydrogel coated structures. The methods include impregnating a porous substrate with a room temperature stable aqueous polysaccharide solution containing, water, a polysaccharide having a concentration in the aqueous solution from about 0.1% to about 20%, a gel-inhibiting agent having a concentration in the aqueous solution from about 18 to about 54%, and an anionic fluorosurfactant having a concentration in the aqueous solution from about 0.001% to about 10% by total weight of the aqueous solution. Followed by evaporating the water from the polysaccharide coating; and exposing the dehydrated polysaccharide coating to a gelling agent form a porous polysaccharide hydrogel coated substrate. The hydrogel coated substrate is exposed to a crosslinking agent to form a porous crosslinked polysaccharide hydrogel coated substrate.

Abstract: Anionic polysaccharide derivatives partially functionalized by at least two vicinal hydrophobic groups, the hydrophobic groups, which are identical or different, being carried by an at least trivalent radical or spacer, a method of synthesis of the functionalized polysaccharides, and pharmaceutical compositions having one of the polysaccharides and at least one active principle are provided.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: The present invention is related to a modified hydroxypolymer conjugate, preferably a dextran-guanidine-biphosphonate conjugate for treating not only skeletal tumors i.e. bone metastasis, particularly bone metastasis related to hormone refractory prostate cancer HRPC and breast cancer, but also osteoporosis. A method for producing and using said hydroxypolymer conjugate is also disclosed.

Abstract: A mineral absorption accelerator, and an anemia improving agent, food and drink or food and drink material containing the mineral absorption accelerator are provided, the mineral absorption accelerator including: an ?-glucosidase inhibitory component.

Abstract: Methods and compositions are provided for the reduction of fouling of objects present in marine environments. The methods and compositions include anticoagulants, such as, for example, glycosaminoglycans, coumarin-type molecules, metal chelators, plasminogen activators and platelet inhibitors. The methods include reducing marine fouling, comprising incorporating an anticoagulant compound into a marine coating. In addition, the methods include identifying compounds useful for reducing marine fouling, comprising measuring either blood coagulation or barnacle cement polymerization in the presence and absence of the compound, wherein a reduction in the blood coagulation or the barnacle cement polymerization in the presence of the compound identifies the compound as useful for reducing marine fouling. The coagulation or the polymerization can be measured by a serine protease activity or a transglutaminase activity.

Abstract: The near-infrared wavelengths (700 nm-900 nm) are a suitable optical window for light penetration and deep tissue imaging. The present invention provides a near-infrared fluorescent blood pool contrast agent. The agent is of use to detect and quantify pathological capillary leak in live animals, e.g., serially imaging of traumatized tissue (muscle) as well as tumors.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: The present disclosure provides compositions for enhanced delivery of therapeutic agents. Drug delivery vehicle compositions may include a modified polysaccharide (e.g. chitosan) having at least one secondary amine or at least one tertiary amine and a therapeutic agent such as a therapeutic nucleic acid and/or a therapeutic anionic agent. Various additional modifications of a modified polysaccharide of the disclosure are also described. Exemplary therapeutic agents may include but are not limited to nucleic acids, polynucleotides, siRNA and/or pDNA. Compositions of the disclosure may be formulated as nanoparticles and may provide one or more advantages including efficient transfection, bio-delivery, availability, buffering ability, serum stability. Methods for synthesizing the drug delivery compositions are also set forth. The disclosure also provides methods for delivering/administering therapeutic agents using the drug delivery compositions of the disclosure to a patient in need thereof.

Abstract: The present disclosure provides polymer compounds binding with lipoamide produced by the reaction of the primary amine group of lipoamide with the carboxy group of polysaccharide compounds such as chondroitin sulfates, carboxymethyl celluloses, or hyaluronic acids; functional compounds such as peptides, proteins, growth factors; or drugs; or biocompatible polymers such as poly(ethylene oxide), poly(vinyl alcohol), or poly(vinyl pyrrolidone). The present disclosure also provides their synthesis methods, products of hydrogels and films using the same as and methods for manufacturing the products.

Abstract: A process for forming polysaccharide structures such as beads, gel films and porous coatings on porous substrates by forming a room temperature gel-inhibited solution of a polysaccharide, one or more gel-inhibiting agent(s) and a solvent such as water, heating the mixture until all the components are dissolved, cooling the mixture as a solution to about room temperature, forming a three dimensional structure with the solution and adding the structure to a gelling agent to form a polysaccharide gel. Optionally, the solution can be added to a porous structure such as a non-woven fabric or a porous membrane and the solution is allowed to dry before being subjected to the gelling agent. Porous structures having a polysaccharide coating and being capable of convective flow through the pores of the structure and diffusive flow through the coating can be formed.

Abstract: Designed herein are multivalent heterobifunctional polymers for binding to a biological target exhibiting biological activity and to an effector template which can affect the biological activity of the biological target or detect the presence of the biological target. The polymers comprise a plurality of pre-arranged heterobifunctional ligands connected thereto, and each heterobifunctional ligand comprises a first functionality capable of binding to the biological target, and a second functionality capable of binding to the effector template. The heterobifunctional ligands are pre-arranged on the polymer so as to form a ternary complex between the polymer, the biological target and the effector template. The polymers, methods and compositions described herein provide an approach for the design and production of new therapeutic agents as well as agents useful in a variety of non-therapeutic applications.

Abstract: Room temperature stable, non-gelling polysaccharide solutions such as agaroses, dextrans and cyclodextrans are made by the present invention. It has been found that by incorporating certain gel-inhibiting additives into an aqueous polysaccharide solution, the gel point is reduced or eliminated and the solution remains liquid at room temperature indefinitely. Additives that have been found to work include salts, such as lithium chloride and zinc chloride and bases, such as sodium hydroxide and lithium hydroxide. Mixtures of said salts and said bases can also be used with the same desired results. The composition of these solutions of the present idea can be further modified to include other additives, such as organic co-solvents or non-solvents, pH modifiers, surfactants or other polymers to customize the properties of the solution to improve the processability for the desired application and to form structures such as films, beads and coated porous substrates.

Abstract: The present invention provides hydrogels and compositions thereof for vocal cord repair or augmentation, as well as other soft tissue repair or augmentation (e.g., bladder neck augmentation, dermal fillers, breast implants, intervertebral disks, muscle-mass). The hydrogels or compositions thereof are injected into the superficial lamina propria or phonatory epithelium to restore the phonatory mucosa of the vocal cords, thereby restoring a patient's voice. In particular, it has been discovered that hydrogels with an elastic shear modulus of approximately 25 Pa are useful in restoring the pliability of the phonatory mucosa. The invention also provides methods of preparing and using the inventive hydrogels.