Abstract: Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of autoimmune disease, inflammatory disease, or cancer. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.

Abstract: Methods and compositions relating to CDP-taxane conjugates are described herein.

Abstract: Methods and compositions relating to CDP-proteasome inhibitor conjugates are described herein.

Abstract: Described herein is a cyclodextrin containing polymer conjugate.

Abstract: There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex, and therapeutic uses of the complex.

Abstract: The present invention relates to the medical field. In a first aspect the present invention relates to novel water soluble cyclodextrin-curcumin complexes having a pharmacological activity, in particular an anti-tumour and/or anti-inflammatory activity, and improved physico-chemical properties. In a second aspect, the present invention relates to a method for preparation of said water soluble curcumin derivatives. The invention further relates in a third aspect to a pharmaceutical composition comprising an effective amount of said water soluble curcumin derivatives. In a fourth aspect, the present invention concerns the use of said water soluble cucumin derivatives as a medicament and the use of said water soluble curcumin derivatives for the preparation of a medicament for the treatment of cancer and inflammatory diseases.

Abstract: The invention provides a composition containing particulate composite of a polymer and a therapeutic agent. The composition also contains a complexing agent. The polymer interacts with the complexing agent in a host-guest or a guest-host interaction to form an inclusion complex. A therapeutic composition of the invention may be used to deliver the therapeutic agent and to treat various disorders. Both the polymer of the particulate composite and the complexing agent may be used to introduce functionality into the therapeutic composition. The invention also relates to a method of preparing a composition. The method combines a therapeutic agent, a polymer having host or guest functionality, and a complexing agent having guest or host functionality to form the therapeutic composition. The complexing agent forms an inclusion complex with the polymer. The invention also relates to a method of delivering a therapeutic agent.

Abstract: The present invention relates to acenaphtho heterocyclic compounds, cyclodextrin inclusion compounds and complexes thereof, and their uses in manufacturing the inhibitors of BH3 analogue, Bcl-2 family proteins. The acenaphtho heterocyclic compounds are obtained by introducing oxo-, thio-, carbonyl, ester or acyl in the 3-, 4- and 6-position of 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile, or further substituting 9-cyano with carboxyl, ester or amide. The compounds can simulate BH3-only protein, competitively binding and antagonizing Bcl-2, Bel-XL and Mcl-1 proteins in vitro or intracellular, to induce cell apoptosis. The cyclodextrin inclusion compounds and complexes can improve the effects. Therefore, they all can be used in the manufactures of anticancer compounds.

Abstract: A printing ink or coating composition contains optionally colorant and one or more derivatives of starches or modified starches.

Abstract: Compositions and methods of making a modified polyhydroxylated polymer comprising a polyhydroxylated polymer having reversibly modified hydroxyl groups, whereby the hydroxyl groups are modified by an acid-catalyzed reaction between a polydroxylated polymer and a reagent such as acetals, aldehydes, vinyl ethers and ketones such that the modified polyhydroxylated polymers become insoluble in water but freely soluble in common organic solvents allowing for the facile preparation of acid-sensitive materials. Materials made from these polymers can be made to degrade in a pH-dependent manner. Both hydrophobic and hydrophilic cargoes were successfully loaded into particles made from the present polymers using single and double emulsion techniques, respectively. Due to its ease of preparation, processability, pH-sensitivity, and biocompatibility, of the present modified polyhydroxylated polymers should find use in numerous drug delivery applications.

Abstract: Methods and compositions relating to CDP-proteasome inhibitor conjugates are described herein.

Abstract: Methods and compositions relating to CDP-epothilone conjugates are described herein.

Abstract: Crosslinking systems suitable for use in a polymer melt composition wherein the polymer melt composition comprises a hydroxyl polymer; polymeric structures made from such polymer melt compositions; and processes/methods related thereto are provided.

Abstract: The present invention is directed to a macrocyclic derivative which is formed by modification of a macrocycle. The invention further relates to assemblies formed by the self-assembly of such macrocyclic derivatives in aqueous solvent, and includes bilayer vesicles, micelles, monolayers, nanoparticles, colloidal assemblies and surface-coated assemblies.

Abstract: Crosslinking systems suitable for use in a polymer melt composition wherein the polymer melt composition comprises a hydroxyl polymer; polymeric structures made from such polymer melt compositions; and processes/methods related thereto are provided.

Abstract: A branched dextrin insusceptible to digestion and having a low osmotic pressure, as well as a method for producing such a branched dextrin is provided. The branched dextrin characterized by having a structure wherein glucose or isomalto oligosaccharide is linked to a non-reducing terminal of a dextrin through an ?-1,6 glucosidic bond and having a DE of 10 to 52. A method characterized in that, in a method for producing a branched dextrin by allowing maltose-generating amylase and transglucosidase to act on an aqueous dextrin solution, the maltose-generating amylase and transglucosidase are adjusted so as to attain an enzyme unit ratio of 2:1 to 44:1 and allowed to act.

Abstract: The invention relates to new compounds of type hexakis(6-deoxy-6-NH(CH2)n—R1)?-cyclodextrin and heptakis(6-deoxy-6-NH(CH2)n—R1)-(?-cyclodextrin, and octakis(6-deoxy-6-NH(CH2)n—R1)-?-cyclodextrin, where n=2-6 when R1=NH2 and n=0 when R1=C(?NH)NH2 and n=2-6 when R1=NH—C(?NH)NH2 and their use in the compaction of DNA and in cell permeation. The invention also relates to methods of synthesis of the above compounds.

Abstract: A cell-sheet releasing agent of the present invention contains an aminated polyrotaxane. The polyrotaxane constituting the skeleton of the cell-releasing agent of the present invention has a structure in which cavities of a plurality of cyclic molecules are threaded onto a linear molecule and both terminals of the linear molecule have a bulky cap bonded thereto so that the cyclic molecules are not dethreaded from the linear molecule. Furthermore, the aminated polyrotaxane contained in the cell-releasing agent of the present invention is a compound in which at least some of hydroxy groups in the cyclodextrin structure contained in the polyrotaxane are each substituted with a substituent having an amino group. According to this cell-sheet releasing agent, cultured cells anchored to the surface of a container can be released without damaging the cells and without controlling the temperature.

Abstract: In one aspect, the present invention provides otoprotectant compositions useful for ameliorating hearing loss. In some embodiments, the otoprotective compositions comprise at least one glutathione peroxidase mimic. In some embodiments, the otoprotective compositions comprise at least one glutathione peroxidase mimic and at least one otoprotectant selected from the group consisting of a xanthine oxidase inhibitor and a glutathione or glutathione precursor. In some embodiments, the otoprotective compositions comprise at least one glutathione peroxidase mimic, at least one xanthine oxidase inhibitor, at least one glutathione or glutathione precursor. In another aspect, the present invention provides methods for ameliorating hearing loss by administering to a subject an amount of an otoprotective composition that is effective to ameliorate hearing loss.

Abstract: The invention relates to a process for the preparation of reactive cyclodextrins, in which process the cyclodextrins CD are reacted with a bifunctional alkyl compound X—(CH2)n—Y, wherein X is a group which reacts with CD, n is an integer from 2 to 20 and Y is a group which reacts with a group Z or is a group-Reactive which is capable of reaction with cellulosic or proteinic materials and, optionally, in a further step, insofar as Y is a group which reacts with a group Z, the resulting product is reacted with a reactive anchor compound Z-Reactive to form the reactive cyclodextrin, and also to reactive cyclodextrins prepared in accordance therewith, to materials dressed therewith and to the use thereof.

Abstract: A trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a water-soluble cyclodextrin derivative has improved solubility.

Abstract: The invention provides a new class of antibiotics to which pathogenic bacteria have not been exposed, and thus should not have developed resistance. This new class of antibiotics are derivatives of ?-cyclodextrin (?-CD), which is a cyclic molecule comprising seven D-glucose units.

Abstract: Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

Abstract: Disclosed are a method for the reduction of an oligosaccharide mixture and an oligosaccharide mixture prepared thereby. In accordance with the disclosed invention, a mixture of oligosaccharides having a given DP profile is reduced to a DE of essentially zero by catalytically hydrogenating the mixture under reaction conditions sufficient to preserve the DP profile of the mixture, which reaction conditions typically include a reaction temperature ranging from about 50° C. to about 150° C. and a reaction pressure ranging up to about 1500 psi. Surprisingly, when the mixture is a malto-oligosaccharide mixture, the reduced mixture will have a superior color-fastness and thermal stability as compared to a similar unreduced mixture of malto-oligosaccharides, and also low reactivity towards nitrogen-containing species.

Abstract: The present invention relates to water-soluble, non-covalent complexes of a group of prostaglandin derivatives including latanoprost and monosubstituted, charged ?-cyclodextrins, as well as uses of these complexes in therapeutic compositions that are administered topically for treating intraocular hypertension and glaucoma.

Abstract: Water soluble iron carbohydrate complex obtainable from an aqueous solution of iron(III) salt and an aqueous solution of the oxidation product of one or more maltodextrins using an aqueous hypochlorite solution at a pH-value within the alkaline range, where, when one maltodextrin is applied, its dextrose equivalent lies between 5 and 20, and when a mixture of several maltodextrins is applied, the dextrose equivalent of the mixture lies between 5 and 20 and the dextrose equivalent of each individual maltodextrin contained in the mixture lies between 2 and 40, process for its production and medicament for the treatment and prophylaxis of iron deficiency conditions.

Abstract: The present invention is directed to conjugates for biorecognition comprising (i) an carbohydrate backbone structure (PO) of 5 to 20 monosaccharide units, (ii) oligosaccharide biorecognition groups (Bio) of 1 to 10 monomer units, (iii) a bifunctional spacer groups of the formula -(y)p-(S)q-(z)r-, wherein S is a spacer group, p, q and r are each 0 or 1, whereby at least one of p and r is different from 0, and y and z are chemoselective ligation groups, which covalently link a said Bio group to said backbone structure, and the degree of conjugation, indicating the average number of covalently attached Bio biorecognition groups per monomer unit of the backbone, being from 0.2 to 1. The invention is also directed to processes for their preparation, intermediates for use in the process as well as use of said conjugates, especially for inhibiting pathogenic bacteria.

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 invention provides methods for making copolymers and multi-arm block copolymers useful as drug delivery vehicles. The multi-arm block copolymers comprise a central core molecule, such as a residue of a polyol, and at least three copolymer arms covalently attached to the central core molecule, each copolymer arm comprising an inner hydrophobic polymer segment covalently attached to the central core molecule and an outer hydrophilic polymer segment covalently attached to the hydrophobic polymer segment, wherein the central core molecule and the hydrophobic polymer segment define a hydrophobic core region. The solubility of hydrophobic biologically active agents can be improved by entrapment within the hydrophobic core region of the block copolymer. The invention further includes pharmaceutical compositions including such block copolymers, pharmaceutical compositions, and methods of using the block copolymers as drug delivery vehicles.

Abstract: The invention concerns a method for extemporaneous and reversible concentration of liposomes, the mixed liposome-cyclodextrin aggregates obtainable by the method, and uses thereof in the pharmaceutical, diagnostic and cosmetic field.

Abstract: The present invention relates to a compound having a cyclodextrin skeleton wherein a hydrogen atom at the C-6 position in at least one of the sugar moieties has been substituted with a cyano group thereby forming a cyanohydrin-type group. The compounds are found to be excellent catalysts, e.g. for the hydrolysis of aryl glycosides. Accordingly, the compounds of the invention are useful as medicaments, in particular for the treatment of poisoning and drug abuse. The compounds, optionally immobilized to a solid phase material, are useful to reduce the content of harmful substances, e.g. metabolites of fungi, insects, etc., from compositions such as foodstuff.

Abstract: The present invention provides a formulation characterised by the simultaneous presence in cyclodextrin based supramolecular complexes, of two components, one of which possesses insecticidal, acaricidal, fungicidal, snailcidal or vermicidal activity and the other possesses an activity synergistic with the first, enhancing its effectiveness. The biologically active substance is chosen from the following classes of chemical products: carbamates, organophosphates, thioureas, pentatomic or hexatomic heterocycles in which 1, 2 or 3 nitrogen atoms are present. The synergistic substance can be chosen from components containing at least one aromatic or non aromatic carbocyclic ring, such as piperonyl butoxide, sesamol, verbutin or MGK 264. For the same dose, the activity of the present formulations is greater than that of the mixture of the two active components alone or separately complexed with cyclodextrin.

Abstract: The invention relates to new compounds of type hexakis(6-deoxy-6-NH(CH2)n, —R1)?-cyclodextrin and heptakis(6-deoxy-6-NH(CH2)n—R1)-(?-cyclodextrin, and octakis(6-deoxy-6-NH(CH2)n—R1)-?-cyclodextrin, where n=2-6 when R1?NH2 and n=0 when R1?C(?NH)NH2 and n=2-6 when R1?NH—C(?NH)NH2 and their use in the compaction of DNA and in cell permeation. The invention also relates to methods of synthesis of the above compounds.

Abstract: The present invention is directed to pharmaceutical compositions containing crystalline methylated cyclodextrins, which enhance the solubility of the pharmaceutically active agent or agents of the formulation.

Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.

Abstract: The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with ?-cyclodextrin in an aqueous complexation medium comprising ?-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with ?-cyclodextrin and its inclusion complexes.

Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.

Abstract: Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: In a reaction system having at least two liquid-liquid interfaces between an organic phase of raw material containing a compound(s) to be separated and an aqueous phase of an aqueous solution of inclusion-complexing agent and between that aqueous phase and an organic phase(s) of extraction solvent(s), the compound(s) to be separated is entrapped into the aqueous phase through formation of an inclusion complex(es) of the inclusion-complexing agent with the compound(s), while the compound(s) is entrapped into the organic phase(s) of extraction solvent(s) through dissociation of said inclusion complex(es). The foregoing operation is performed using, for example, a squarish U-shaped tube or an H-shaped tube with bottom plates. Preferred examples of inclusion-complexing agent include highly water-soluble branched cyclodextrins.

Abstract: The present invention provides a functionalized polymer which can be used extensively in the field of medical drugs as well as medical devices and which is obtainable in an organic synthetic manner from glycosaminoglycan controlling adhesion, migration and proliferation of cells via linkage to various cellular growth factors or cytokines or direct interactions with the cells. The functionalized polymer of the present invention is characterized in that it comprises a carbohydrate corresponding to at least a part of the basic structure of glycosaminoglycan introduced into a vinyl-type polymer chain.

Abstract: The present invention relates to folic acid-polysaccharide complexs and method of preparation thereof, more particularly relates to folic acid-Dextran complexs, method of preparation thereof, pharmaceutical compositions having said complex as active component and uses of said composition in therapy of tumors. The folic acid-polysaccharide complexs of the present invention have general formula of: (X)n—Y, wherein X is identical or different, and is selected from folic acid, derivatives of folic acid and other substances that can enter into cell via the pathway of folic acid receptor; Y is polysaccharide; n?1.

Abstract: The present invention relates to an inclusion complex of Rifampicin and cyclodextrin (CD) that can be used as an anti-tubercular drug. The present invention also relates to a process for synthesizing inclusion complexes of the anti-tubercular drug, Rifampicin, with ?-CD (?-cyclodextrin) and HP-?-CD (2-hydroxy propyl cyclodextrin) and characterization of these inclusion complexes.

Abstract: The present invention is directed to novel aminooxy-cyclodextrin derivatives of the formula (1): CD—(X—Y—ONH2)n, wherein CD is mono- or polydeoxy ?-, ?-, or ?-cyclodextrin, carrying in its 6-, 3- and/or 2-position a group containing the aminooxy group, and optionally carrying substituents different from (X—Y—ONH2). Y is a linker group between the aminooxy group and the mono- or polydeoxy-CD group, X is a functional group or an atom necessary to connect the linker Y and the deoxy CD group, or Y is a direct bond when X is a direct bond, and n is ?1, but ?24, 21 and 18 for ?-, ?- or ?-cyclodextrin, respectively, the protected aminooxy derivatives thereof, as well the methods for their preparation and use.

Abstract: The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.

Abstract: The process entails increasing the concentration of cyclodextrin to 15% (w/w) and above to form complexes through a precipitation process in order to increase the yield of complexes, increase the amount of guest complexed, and decrease the particle size of the complex.

Abstract: A stable composition for removing unwanted molecules from a surface comprises low-degree of substitution cyclodextrin derivatives. The compositions are suitable for capturing unwanted molecules from inanimate surfaces, including fabrics, including carpets, and household surfaces such as countertops, dishes, floors, garbage cans, ceilings, walls, carpet padding, air filters, and the like, and from animate surfaces, including skin, hair, and the like. The compositions can further comprise cyclodextrin-compatible and -incompatible materials, and other optional ingredients.

Abstract: Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: The invention concerns more particularly dodecylthio-phenylacetanilide derivative complexes such as (S)-2?,3?,5?-trimethyl-4?-hydroxy-?-dodecylthio-phenylacetanilide or related derivatives thereof and cyclodextrins.

Abstract: The invention provides cyclodextrin derivatives that may be used to transport hydrophobic molecules for pharmaceutical or cosmetic applications, by forming organised systems in an aqueous medium, alone or with phospholipids. The cyclodextrin derivatives of the present invention have the formula: in which, R1 represents a steroid, R2 represents an alkyl or aryl group, substituted if applicable, R3 represents H or R2, all the R4 represent OR2, or one of the R4 represents —NHCO(CH2)mCONHR1, m is an integer ranging from 1 to 8, and n is equal to 5, 6 or 7.

Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.