Abstract: A water insoluble polymeric composition which is a reaction product of a cyclodextrin monomer and a polyfunctional crosslinker from the group of polyisocyanates, dihalohydrocarbons, and dihaloacetylhydrocarbons is disclosed together with a process for removing a target organic compound from an aqueous composition including contacting the aqueous composition containing a target organic compound with a water insoluble cyclodextrin polymer which is the reaction product of a cyclodextrin monomer and a polyfunctional crosslinker from the group of polyisocyanates, dihalohydrocarbons, and dihaloacetylhydrocarbons for time sufficient to form a reaction product between the water insoluble cyclodextrin polymer and the target organic compound whereby the concentration of the target organic compound in the aqueous composition is reduced. Organic chromophores added to the water insoluble cyclodextrin polymers can provide organic nonlinear optical materals.

Abstract: A method of locating one or more salts of a compound, said salts having a solubility in a cyclodextrin equal to or greater than a desired target solubility, comprising obtaining a series of salts of said compound, measuring the equilibrium solubility of each salt in said series in said cyclodextrin, and comparing each measured solubility with said target solubility.

Abstract: This invention provides rotaxane type dyes. Specifically, the rotaxane type dye according to the invention has a rotaxane structure which binds dye molecules to both of the termini of a chain group penetrating a cyclodextrin ring, which possesses excellent water-solubility, and which is capable of having a plurality of different dyes.

Abstract: Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.

Abstract: Disclosed are novel polymers derivatized with at least one —SNO group per 1200 atomic mass unit of the polymer. In one embodiment, the S-nitrosylated polymer has stabilized —S-nitrosyl groups. In another embodiment the S-nitrosylated polymer prepared by polymerizing a compound represented by the following structural formula: R is an organic radical. Each X′ is an independently chosen aliphatic group or substituted aliphatic group. Preferably, each X′ is the same and is a C2-C6 alkylene group, more preferably —CH2—, —CH2CH2—, —CH2CH2CH2— or —CH2CH2CH2CH2—. p and m are independently a positive integer such that p+m is greater than two. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: Bacillus subtilis protease catalyzes the acylation of organic solvent-insoluble polysaccharides in isooctane solution containing vinyl esters of fatty acids as acyl donor. The reaction occurs only when the enzyme is solubilized via ion-pairing with the anionic surfactant dioctyl sulfosuccinate, sodium salt (AOT). Enzyme based acylation was demonstrated with amylose, cyclodextrins, cellulose, cellulose derivatives, and other polysaccharides such as chitosan, pullulan, and maltodextrose. These polysaccharides are reactive either as a cryogenically milled powder suspended in the organic solvent or as a thin film deposited onto ZnSe slides. For chitosan, &agr;-cyclodextrin, and hydroxyethyl cellulose (HEC), the enzymatic crosslinking reaction occurs using adipic acid divinyl ester (C6DVE). HEC forms a compound that gels in solvents such as ethyl alcohol and dimethyl sulfone oxide (DMSO).

Abstract: A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of the formula I wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2, or SO2NR5, R5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7-&bgr;-cyclodextrin or 2-hydroxypropyl-&bgr;-cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.

Abstract: A cyclodextrin derivative, wherein at least 60 percent of the free hydroxy groups of said cyclodextrin are acylated with acyl groups where at least one of said acyl groups comprise a free carboxylic group.

Abstract: Particles comprising an outer wall formed of one or more saccharide components selected from the group consisting of monosaccharides and oligosaccharides crosslinked by interfacial crosslinking in emulsion, preferably at room temperature, with a polyfunctional acylating crosslinking agent to produce ester linkages between the acylatable hydroxyl group(s) of the primary alcohol(s) of the saccharide component and the acyl groups of the polyfunctional acylating agent. These particles can be used for the manufacture of cosmetic, pharmaceutical and food compositions.

Abstract: Sulfoalkyl ether cyclodextrins are produced by a process of treating an unsubstituted cyclodextrin starting material with an alkyl sultone in the presence of a base. The base is added in a stepwise, pH controlled manner so that substantially the entire initial charge of cyclodextrin starting material is at least partially reacted. Additional base is then added to complete the reaction, and residual alkyl suftone is destroyed. The product advantageously contains low levels of both residual cyclodextrin and residual alkyl sultone.

Abstract: The present invention is drawn to pharmaceutical composition comprising cyclodextrin and a pharmaceutically active agent or prodrug, wherein the cyclodextrin is present at less than 75% equimolar amounts of the above agent or prodrug. The present invention is further drawn to a method of extending the shelf-life of a pharmaceutically active agent or prodrug by adding one or more cyclodextrins a less than 75% equimolar amounts to said pharmaceutically active agent or prodrug.

Abstract: The present invention relates in general to a method for the reduction of oxygenated compounds of rhenium and technetium and in particular to the reduction of perrhenate or pertechnetate ions.More particularly, the invention relates to reactions for the reduction of the said oxygenated compounds which are carried out in the course of the preparation of complexes of the radionuclides .sup.186 Re, .sup.188 Re and .sup.99m Tc; in these reactions, the radionuclide perrhenate or pertechnetate ion is reduced in the presence of a reducing agent and a ligand which can form a complex with the radionuclide in its reduced oxidation state.

Abstract: New glucose-based surfactants and methods of their synthesis are described. The surfactants are synthesized through the preparation of an intermediate glucose 4,6-cyclic sulfate. The surfactants are economical to prepare and have excellent surface-active properties.

Abstract: The invention relates to polyrotaxanes that contain metal complexes or iodine-containing benzene derivatives as imaging components for MRT diagnosis and x-ray diagnosis.

Abstract: Disclosed is a novel amylase which mainly forms maltohexaose and maltoheptaose when acts on starch, but does not substantially hydrolyze maltohexaose and a lower molecular oligosaccharide than maltohexaose. The amylase can be prepared from microorganisms of the genus Alcaligenes, and has a relatively-high optimum temperature and thermal stability, as well as a relatively-wide range of optimum pH and pH stability. By using the amylase, saccharide compositions rich in maltohexaose and/or maltoheptaose or those rich in maltohexaitol and/or maltoheptaitol can be readily prepared in an industrial scale, and the saccharide compositions thus obtained can be used in a variety of food products, cosmetics and pharmaceuticals.

Abstract: The present invention provides a metalloporphyrin catalyst represented by the structure: ##STR1##

Abstract: The invention relates to thioureido-cyclodextrins, usable in particular to solubilize anti-tumor and antiparasitic agents and their preparation processes.These thioureido-cyclodextrins correspond to the formula: ##STR1## with m=6, 7 or 8, R.sup.1 represents OH or NH--CS--NHR.sup.2, at least one of the R.sup.1 being NH--CS--NHR.sup.2,R.sup.2 represents an alkyl, monosaccharide, oligosaccharide glycosyl-amino acid or glycopeptide group.These cyclodextrins are usable for solubilizing anti-tumor or antiparasitic agents of the Taxol family.

Abstract: The invention relates to new metal complex-containing or iodine-containing benzene derivatives that contain pseudopolyrotaxanes. They are valuable compounds for diagnosis. The pseudopolyrotaxane complexes have general formula (I), in which n represents the numbers 6, 7 or 8; m represents the numbers 2 to 50; X represents a direct bond or the radical --O--CO--CH(CH.sub.3)--; R.sub.1 and Y have the meaning that is indicated in the description and represent R.sub.3 --Y--R.sub.4 polyalkylene glycols.

Abstract: Sulfoalkyl ether cyclodextrin (SAE-CD) based controlled release pharmaceutical formulations are provided by the present invention. The present solid pharmaceutical formulations consist of a core comprising a physical mixture of one or more SAE-CD derivatives, an optional release rate modifier, a therapeutic agent, a major portion of which is not complexed to the SAE-CD, and an optional release rate modifying coating surrounding the core. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative is used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents. Multi-layered, osmotic pump, coated, and uncoated tablet, minitablet, pellet, micropellet, particle, powder, and granule dosage forms are disclosed herein.

Abstract: The invention relates to novel cyclodextrin derivatives of formula (I)CD(OH).sub.l (OR.sub.1).sub.m (OR.sub.2).sub.n (I)in which:OR.sub.1 represents a screening or antioxidant group or a mixture thereof,OR.sub.2 represents an alkyl or hydroxyalkyl radical, l, m and n are statistical values.The invention also relates to a process for the preparation of these compounds and to the use of these compounds in cosmetics.

Abstract: The present invention discloses that retrograded starch having more than 55% resistant starch with >50% chains of DP 10-35 gives rise to a significantly higher amount of n-butyrate production under conditions simulating the human colon. It is expected that such an increased n-butyrate production will diminish the development of colon diseases notably of colon cancer.

Abstract: Mono- and di-derivatives of cyclodextrins are completely defined, also a method for their synthesis and purification, functionalised cyclodextrins obtained from these derivatives, and the synthesis of supports comprising these cyclodextrin derivatives. Use of the supports for the preparation of separation of enantiomers, for asymmetric synthesis, for catalysis, for the preparation or separation of geometrical isomers or positional isomers, or for the preparation or separation of organic molecules with a hydrophobic nature is also described.

Abstract: Novel contrast media for use in ultrasonic imaging are described. Such contrast media may be comprised of an aqueous solution of one or more biocompatible polymers, wherein said biocompatible polymers are coated with and/or in admixture with at least one silicon containing compound. Alternatively, the contrast media may be comprised of an aqueous solution of one or more biocompatible synthetic polymers, or an aqueous solution of cellulose. The contrast media may be employed, if desired, with anti-gas agents and/or suspending agents.

Abstract: Polymerizable saccharide monomers are made by the reaction of a saccharose and a (meth)acrylate. Hydrophilic, hydrophobic and thermoreversible gels and foams are formed upon polymerization of the saccharide monomers. Hydrophilic sucrose monomers are synthesized by reaction of sucrose with an epoxy acrylate. Hydrophobic sucrose monomers are synthesized by reaction of sucrose with methacrylol chloride followed by acetyl chloride. Thermoreversible sucrose monomers are obtained by modifying sucrose with polymerizable substituents prepared from methacryloyl chloride and aminocarboxylic acids. The modified sucrose monomers are copolymerized with hydrophobic poly(alkyleneoxide) (meth)acrylates to produce hydrogels exhibiting inverse thermoreversible properties. The thermosensitive hydrogels are biodegradable and can be used in the area of controlled drug delivery.

Abstract: The present invention generally relates to the regulation of plant physiology, in particular to methods for inhibiting the ethylene response in plants or plant products, and has three embodiments. The first embodiment relates to methods of minimizing impurities capable of reversibly binding to plant ethylene receptor sites during the synthesis of cyclopropene and its derivatives such as methylcyclopropene, thereby avoiding the negative effects these impurities have on plants treated with cyclopropene and its derivatives. The second embodiment relates to complexes formed from molecular encapsulation agents such as cyclodextrin, and cyclopropene and its derivatives such as methylcyclopropene, in addition to cyclopentadiene and diazocyclopentadiene and their derivatives, thereby providing a convenient means for storing and transporting these compounds capable of inhibiting the ethylene response in plants, which are reactive gases and highly unstable because of oxidation and other potential reactions.

Abstract: Novel and improved chiral stationary phases (CSP) materials comprising a support and completely regiodefined derivitized cyclodextrin chemically bonded via single or double urethane linkage(s) universally applicable in HPLC, LC, TLC, and CCE are obtained using a process based on the almost quantitative reaction of pre-synthesized regiodefined per-functionalized mono- or di- azidocyclodextrin with primary amines.

Abstract: This invention provides an agent against HIV-1 and related viruses, the agent being or including dextrin sulphate containing at most two sulphate groups per glucose unit. The invention also provides a composition containing such an agent, and the use of the agent or composition against HIV-1 and related viruses. By restricting the degree of substitution of the dextrin sulphate to a maximum of 2, the invention makes it possible to produce a dextrin sulphate having adequate anti-HIV activity whilst maintaining toxicity within acceptable limits.

Abstract: The preparation of compositions containing cyclodextrin moieties which are modified by fusing 1,4 dioxane rights to glucopyranosyl residues is described.

Abstract: Polymerizable cyclodextrin derivatives (PCDs) for use in dental applications are disclosed. Each PCD molecule contains covalently attached polymerizable groups, and may also contain other covalently attached functional ligand groups, and molecularly encapsulated comonomers, polymerization inhibitors (stabilizers), polymerization initiators, and other desirable molecules. The covalently attached groups are ether or ester substituents, or their derivatives, in statistically predetermined proportions. The molecular members of PCD libraries may have quasi-random molecular configurations in the numbers and locations of their various substituents. Appropriate formulations containing PCD libraries can yield unique structural adhesives and resins for use in health-care procedures.

Abstract: The present invention relates to polymerizable derivatives of carbohydrates comprising a carbohydrate radical and more than one radically polymerizable hydrocarbon group which is linked optionally via a spacer to the carbohydrate radical, to homopolymers, copolymers, block copolymers, graft copolymers and polymeric networks thereof, to capsules, fibers, films and coatings having water-binding and biocompatible properties, and to molded articles, for example contact lenses or biomedicinal articles, comprising the mentioned polymers, as well as to processes for the preparation of the mentioned polymers and articles.

Abstract: By controlling basicity of the reaction, is possible to alkylate preferentially the secondary hydroxyls of cyclodextrins. These hydroxyls surround the principal, wide, entry into the cyclodextrin cavity and, thus, their substitution by suitably chosen substituents can improve the formation of inclusion complexes. By methods of the invention, cyclodextrin derivatives substituted with fused 1,4-dioxane ring(s) can be obtained. If a reagent with one alkylating moiety is used, a mixture of ethers of cyclodextrin is formed. Using methods of this invention, up to 96% of the substitution can be directed to the secondary hydroxyls.

Abstract: A library of diverse molecular configurations containing many combinations and permutations of polymerizable cyclodextrin derivatives (PCDs) is disclosed for use in dental bonding formulations and other applications. Each PCD molecule in the library contains numerous (at least one or more) covalently attached polymerizable groups, and may also contain covalently attached ligand groups, such as free carboxyl groups, tertiary amino groups, or both, which substituents are attached in statistically predetermined proportions by ether or ester linkages. The PCDs may also contain molecularly encapsulated comonomers, polymerization inhibitors (stabilizers), polymerization initiators, and other desirable molecules. The molecular members of the PCD libraries may have quasi-random molecular configurations in the numbers and locations of their various substituents.

Abstract: A novel dextrin-type starch is suitable for supplying energy to human beings in preparation for or after a physical activity. The starch is characterized in that it has a molecular weight of from about 15,000 to about 10,000,000, and in that its molecules are heavily branched. The invention also relates to a composition and to a method for supplying energy preparatory to a physical activity, using a starch.

Abstract: The amount of cholesterol in low density lipoproteins in a sample can be measured by contacting the sample with one or more reagent solutions to carry out the reaction in the presence of a polyanion and an amphoteric surfactant, followed by optical measurement of the reaction product.

Abstract: A cyclodextrin derivative, wherein at least 60 percent of the free hydroxy groups of said cyclodextrin are acylated with acyl groups where at least one of said acyl groups comprise a free carboxylic group.

Abstract: A biocidal composition which comprises an inclusion complex of a halopropargyl compound and a cyclodextrin or a modified cyclodextrin, useful broadly in industrial systems and more particularly in aqueous compositions used in connection with paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, and the like.

Abstract: Reaction at the interface of an organic solution containing an acidic reactant and an aqueous alkaline solution containing nonreducing carbohydrates such as sucrose, sugar alcohols, cyclodextrins, and polysaccharides imparts a specificity to the reaction for one or more of the primary alcohol groups of the carbohydrate reactant. The resulting activated, nonreducing carbohydrate intermediate can then be converted to a series of substantially pure, low molecular weight reaction products, including a sucrose trimer and dianhydrosucrose, and to a series of substantially pure, higher molecular weight reaction products, including 6-O-sucro cyclodextrins and poly-6-O-sucro amylose.

Abstract: Method for the culture of microorganisms of the genera Helicobacter, Campylobacter and Arcobacter, wherein culture media are employed, which comprise, in place of blood or its derivative, cyclodextrins, methylcellulose or mixtures thereof.

Abstract: Starch containing amylopectin is hydrolyzed with an alpha-amylase, preferably derived from Bacillus stearothermophilus, under conditions which cause a non-random cleavage of the starch molecules to yield fragments (molecules) having similar size and branching characteristics and a molecular weight range from about 20,000 to about 50,000 daltons are made. All of the desired molecules have (.alpha.1,6) linkages. The hydrolysate is treated to enrich the concentration of the desired fragments and the enriched portion can be processed further to make a maltodextrin having a D.E. of less than about 8.

Abstract: Sulfoalkyl ether-cyclodextrin (SAE-CD) based pharmaceutical formulations are provided by the present invention. These formulations comprise SAE-CD derivatives and a therapeutic agent, a major portion of which is not complexed to the SAE-CD. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative can be used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents.

Abstract: Polyionic derivatives of cyclodextrins and methods for preparing these derivatives are provided in which a polyionic derivative of cyclodextrin is combined with a growth factor, preferably a heparin binding growth factor. These compositions are of low solubility and are applied directly to the location of a wound. By virtue of the low solubility, the compositions remain in place at the site of application and slowly release growth factor. In an alternative embodiment, the cyclodextrin derivatives are administered in the absence of growth factor and are used to absorb growth factor present in the body at the location of the wound in order to prevent overstimulation of the wound response.

Abstract: The present invention a polyhydroxycarboxylic acid composition derived from maltodextrins by oxidation with an oxygen containing oxidant. The invention also relates to a process for the production of oxyacids from carbohydrates by oxidation with an oxygen containing oxidant. More particularly the present invention relates to the oxidation of starch hydrolysates or maltodextrins having a DE of less than 20. The invention further relates to oxidation products and the use thereof.

Abstract: A water base erasable ink composition for use in marking pens which comprises:(a) water as a solvent;(b) a coloring agent;(c) an aqueous emulsion of at least one nonvolatile oily material which is liquid at room temperatures and is selected from the group consisting of aliphatic carboxylic acid esters, higher hydrocarbons and higher alcohols in a dry amount of 1-50% by weight;(d) a cyclodextrin or its derivative in an amount of 0.1-20% by weight; and(e) a resin which is film-forming at room temperatures.The ink composition has improved storability over a long period of time.

Abstract: The invention relates to cyclodextrin derivatives of formula (I)CD(OH).sub.I (OCOR).sub.m (OR.sub.2).sub.n (1)in which each R.sub.1 independently denotes a C.sub.6 -C.sub.24 alkyl radical or a C.sub.8 -C.sub.24 alkenyl radical, each R.sub.2 independently denotes a C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl radical, and I, m and n are statistical values. The invention also relates to a process for the preparation of the compounds of formula (I) and to the use of these compounds in cosmetics.

Abstract: Use of at least one polymer or one biopolymer, called HBGFPP, specifically protecting the growth factors of the FGF and beta TGF families from tryptic degradation in the manufacture of a drug for the treatment of muscular tissues.

Abstract: The present invention provides polyanionic, substituted CDs having cellular growth modulating-activity. The invention further provides CDs having anionic groups on one side of the CD molecule. Therapeutic methods for using, as well as methods of making the CD compounds of the invention, are also disclosed herein.

Abstract: Clathrate compounds comprising an isoflavone derivative and a cyclodextrin are disclosed. The clathrate compounds have improved water solubility and good taste properties, thereby making the compounds a useful ingredient in edible compositions.

Abstract: Inclusion Complexes of Racemic Ibuproxam and of Optically Active Ibuproxam with Cyclodextrin Derivatives, Process for the Preparation Thereof, Pharmaceutical Preparations Containing these Inclusion Complexes or Containing Optically Active S-(+)-Ibuproxam, and Use ThereofThere are disclosed novel inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone. Further a process for preparing S-(+)-ibuproxam and inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic derivatives of .beta.-cyclodextrin and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, is disclosed.Disclosed are also pharmaceutical compositions containing these inclusion complexes or optically active S-(+)-ibuproxam.

Abstract: An improved oral rehydration solution comprising a mixture of rice dextrin and required electrolytes is provided. The functionality of the rice dextrin in oral rehydration solutions is superior to glucose in infants with chronic diarrhea.Iadd., .Iaddend.resulting in lower stool output and enhanced water retention .Iadd.during the initial six hours of therapy.Iaddend.. Rice dextrin also has a polymer profile which provides more readily available glucose than corn dextrin or rice flour. There is also provided a process for clarifying solutions of rice dextrin which involves a first filtration at 35.degree. C. and 50.degree. C. and a second filtration at temperatures above 80.degree. C. using filter aid and activated carbon.

Abstract: Substituted cyclodextrins of the general formula ##STR1## in which R.sup.2 and R.sup.6 mean straight-chain or branched alkyl or alkenyl groups with 1 to 8 carbon atoms or cycloalkyl groups with 5 to 8 carbon atoms which can be the same or different, andR.sup.3 represents a straight-chain or branched alkyl or alkenyl group, which can be the same or different to the residues R.sup.2 and R.sup.6, with 1 to 8 carbon atoms or a cycloalkyl group with 5 to 8 carbon atoms, oran acyl group with an optionally substituted, saturated or olefinically unsaturated aliphatic or cycloaliphatic or with an aromatic hydrocarbon residue with 1 to 8 carbon atoms, andn=6 or 7,a process for their production, and a process for the separation of chiral organic compounds by chromatographic separation processes in which the substituted cyclodextri are used as stationary phase.