Abstract: The invention relates generally to colloidal particle having a core material and a gelatin/aminodextran coating with pendent functional groups attached thereto. Biological substances or molecules, especially monoclonal antibodies, may be attached to said particles. The monoclonal antibody containing particles are useful in a variety of positive and negative biological assays.

Abstract: Compositions useful for regenerating cells and tissues comprise at least one functionalized dextran which has been substituted with carboxymethyl, benzylamide, or benzylamide sulfonate. These dextrans can be used alone or in combination with acid or basic fibroblast growth factors to enhance tissue or cell regeneration. Additionally, these dextrans enhance the stability of acid or basic fibroblast growth factors.

Abstract: A novel polysaccharide derivative, a drug carrier comprising a novel polysaccharide derivative, and a drug complex are disclosed. The polysaccharide derivative according to the present invention comprises a polysaccharide having a carboxyl group in which a peptide chain is introduced at a part or all of the carboxyl groups of the polysaccharide. The peptide chain comprises 1-8 amino acids which may be the same or different. A part or all of the amino groups in the peptide chain which are not involved in the linkages with the carboxyl groups of the polysaccharide or the carboxyl groups in the peptide chain may form an acid amide linkage or an ester linkage with a carboxyl group, an amino group or a hydroxyl group of a third compound such as drugs. The polysaccharide derivative has a property of accumulating in a high amount at a tumor, and thus can deliver efficiently a drug which has a side-effect or a limited sustainment of the drug efficacy to the tumor.

Abstract: The invention relates to polysaccharides which are crosslinked with bifunctional crosslinkers and are no longer water-soluble but are still biodegradable, have a swelling of from 100 to 1000%, where the swelling, which means the percentage gain in weight, is determined by the following equation: ##EQU1## in which A is the percentage gain in weight, W.sub.o is the weight of the dry polymer and W.sub.t is the weight of the swollen polymer saturated with water. It likewise relates to a process for preparing the crosslinked polysaccharides and to the use of the crosslinked polysaccharides for coating and/or embedding medicinal active substances or drug compositions. The invention furthermore relates to a drug which contains an active substance which acts in the large intestine or an active substance which is broken down on passing through the stomach or small intestine, coated with or embedded in one of the crosslinked polysaccharides.

Abstract: An improved, water-soluble polydextrose containing 0.3 mol % or less of bound citric acid, a process therefor, and foods containing same.

Abstract: Grafted polysaccharide compositions comprising polysaccharides grafted with antioxidants on at least one hydroxyl group of the polysaccharide. The use of antioxidant grafted polysaccharides or antioxidant grafted crosslinked polysaccharides as a treatment for arthritis, as a drug delivery vehicle, to reduce the incidence of post-operative adhesion formation, to promote the healing of chronic wounds and ulcers, and as a component of cosmetic formulations.

Abstract: A polydextrose having improved color, flavor and decreased reactivity toward food ingredients having amine functionality. The polydextrose comprises a water-soluble highly branched polydextrose having been prepared by a process which comprises melting dextrose in the presence of a food-acceptable acid catalyst. The improved polydextrose of this invention has substantially no reducing glucose groups. Another aspect of this invention is directed to a method of making the above-described improved polydextrose which comprises exposing unimproved polydextrose to an environment capable of chemically transforming the reducing glucose groups contained in the unimproved polydextrose, thereby substantially eliminating their reducing properties. An improved polymaltose prepared by heating maltose in the presence of a food-acceptable acid catalyst and chemically transforming the reducing glucose groups contained in the polymaltose, thereby eliminating their reducing properties, is also described.

Abstract: Disclosed herein are surface activated, organic polymers useful for biopolymer synthesis. Most preferably, aminated polypropylene is used for the synthesis of oligonucleotides thereto, and these devices are most preferably utilized for genetic analysis of patient samples.

Abstract: The present invention pertains to a process for the production of polyol fatty acid polyesters by reacting a reactant mixture of polyol, a fatty acid lower alkyl ester, a transesterification catalyst and an alkali metal soap emulsifier. The process comprises removing non-dissolved alkali metal soap from the reaction mixture at a degree of transesterification of more than 60%, preferably 65-90%, and recycling the alkali metal soap that is removed during the transesterification to the starting reactant mixture. The invention is applicable both to a batch-wise polyol polyester synthesis and to a continuous synthesis.

Abstract: Sulphonated derivatives of cyclomalto-oligosaccharides, their preparation process and support for active substances containing said derivatives.These derivatives are in accordance with the following formula (I) ##STR1## in which n is an integer from 2 to 50 and R represents --SO.sub.3.sup.- Na.sup.+ or --OH, in which R can differ from one cycle to the other. They can be used for transporting injectable or ingestable medicaments.

Abstract: A pharmaceutical composition comprising dermatan sulphate, together with a low molecular weight heparin, free or fixed combination, is useful as a antithrombolytic agent with a low risk of bleeding complications.

Abstract: A method for producing a substantially stable water-soluble polysaccharide conjugate of a polyene antibiotic is described. The method comprises the following steps: (a) activating the polysaccharide to a dialdehyde by periodate oxidation; (b) purifying the dialdehyde from interfering anions and by-products; (c) coupling the polyene to the purified dialdehyde by Schiff base formation to form the conjugate; and (d) purifying the conjugate. In a preferred embodiment, the conjugate of step (c) is reduced to an amine conjugate by a reducing agent prior to purification. Also described are imine and amine polysaccaride conjugates of the polyene Nystatin.

Abstract: Sapphyrins are provided having appended functional groups that render the sapphyrin water-soluble. Such water-soluble sapphyrins are useful for photodynamic therapy, for example.

Abstract: A material compatible with blood obtained by heparinizing a polymer having quarternary ammonium groups with an alkali metal salt or an alkaline earth metal salt of heparin or the analog by ion exchange is provided. The equivalent ratio (M/S) of alkali metal atoms or alkaline earth metal atoms (M) in the heparin or the analog bonded to the polymer to sulfur atoms (S) in heparin or the analog bonded to the polymer is 0.4 or less.

Abstract: Polysaccharides (e.g., dextran) of different molecular weights were substituted at the anomeric carbon with polyalkylene oxides of different molecular weights to give novel diblock copolymers. The copolymers inhibit bacterial aggregation. The copolymers are useful as antiplaque agents, as agents to prevent bacterial aggregation in an aqueous system or in a fermentation system.

Abstract: A method is provided for preparing an antitumor dextran by contacting a culture broth containing sucrose with an antitumor dextran obtained from Lactobacillus confusus and collecting the antitumor dextran from the culture broth. The enzyme can be used as a crude enzyme solution or may be further purified by conventional means. The Lactobacillus confusus is preferably one of the following: 40-1 strain (FERM BP-2865) , 40-3 strain (FERM BP-2866) , 77-1 strain (FERM BP-2867), 78-1 strain (FERM BP-2868) or 80-1 strain (FERM BP-2869).

Abstract: This invention encompasses a method and compositions which inhibit pancreatic cholesterol esterase and triglyceride lipase and hence, lower cholesterol and triglycerides in the blood stream.

Abstract: A method for the production of oxyacids from carbohydrates by catalytic oxidation with an oxygen containing gas in an alkaline medium, wherein the oxidation is carried out by homogeneous catalysis in the presence of a catalytic amount of an ion of a transition metal selected from the group consisting of Cu, Cr, Co, Ni, Fe, V, Ti, Mn and mixtures thereof.

Abstract: A substantially purified arabinogalactan, its degradative products and selected modifications thereof have been found to act as carriers for delivering therapeutic agent to cell receptors capable of receptor mediated endocytosis (RME). The arabinogalactan and its degrative products once derivatived are capable of forming a complex between the therapeutic agent and the polysaccharide such that the complex retains the ability to recognize and bind to the RME receptor.

Abstract: Covalent conjugates of water soluble dextrans and adenosine agonists or antagonists wherein the dextran is coupled through the C6 or C8 positions of the purine ring. These compounds activate or block adenosine A.sub.1 or A.sub.2 receptors are useful in treating hypertension.

Abstract: Lactobacillus confusus strains capable of producing a dextran which has biological activities such as an excellent antitumor activity, etc. are disclosed. Also disclosed is a method for producing said dextran using said microorganism or dextran synthetase prepared by said microorganism.

Abstract: The invention relates to a method of preparing N.sup.6 -substituted NAD, NADP or FAD by Dimroth rearrangement, wherein the rearrangement is carried out without preceding reduction and subsequent reoxidation.

Abstract: A novel composition of matter comprising a ligand-carbohydrate-cytotoxic drug conjugate is produced by the steps of (1) reacting a carbohydrate with a ligand, (2) reacting the product of step (1) with a cytotoxic drug, and (3) stabilizing the product of step (2) by reduction. The composition is used for treating a neoplastic disease by a process of administering a non-toxic, effective amount of a ligand-carbohydrate-cytotoxic drug conjugate to a human being or animal in need of such a treatment.

Abstract: Disclosed is a polysulfate of a .beta.-cyclodextrin in which at least one of 7 D-glucose units constituting the .beta.-cyclodextrin is a unit represented by the formula (I-a): ##STR1## wherein R.sup.1 is an alkyl group having 1 to 8 carbon atoms, a lower alkyl group having a substituent(s) or a lower alkenyl group, or a salt thereof, which has excellent antiretrovirus activity and is useful as an antiretrovirus agent.

Abstract: The present invention relates to a novel cycloisomaltooligosaccharide selected from the group consisting of novel cycloisomaltoheptaose having a cyclic structure composed of 7 glucose residues in .alpha.-1,6 linkage, novel cycloisomaltooctaose having a cyclic structure composed of 8 glucose residues in .alpha.-1,6 linkage and novel cycloisomaltononaose having a cyclic structure composed of 9 glucose residues in .alpha.-1,6 linkage, novel cycloisomaltooligosaccharide synthase forming said oligosaccharides from dextran, and a process for producing said oligosaccharides by use of said enzyme or a microorganism capable of producing said enzyme.

Abstract: A composition for use in surgical operations to prevent adhesions between tissue surfaces, comprising an aqueous solution containing dextran in an amount of 7 to 20% and hyaluronic acid in an amount of 0.5 to 6%, the dextran having a weight average molecular weight within the range of 30,000 to 75,000 and the hyaluronic acid having a weight average molecular weight within the range 500,000 to 6,000,000.

Abstract: A particulate aromatic or araliphatic carbamate of a polysaccharide having a mean particle diameter of 1 to 200 .mu.m and a specific surface area of 0.5 to 300 m.sub.2 /g is prepared by first dissolving an aromatic or araliphatic carbamate of a polysaccharlde in an organic solvent, adding a hydrocarbon having 4 to 22 carbon atoms in an amount of 0 to 0.5 time by volume of that of the organic solvent, gradually adding the resultant solution to a sufficiently agitating aqueous surfactant solution, removing the organic solvent while continuing the agitation, isolating solid particles, and washing and drying the solid particles. The particulate aromatic or araliphatic carbamate of a polysaccharide has an excellent capability of resolution and, as such, can be used as a stationary phase of preparative liquid chromatography without being supported on a support.

Abstract: The present invention includes an image-enhancing agent comprising a biodegradable, water-soluble polymer, synthetic or naturally derived and having repeating hydrophilic monomeric units with amino or hydroxyl groups. This agent also includes chelating agents comprising functional groups bound to an amino or hydroxyl group of the monomeric units. These chelating agents have a formation constant for divalent or trivalent metal cations of at least about 10.sup.8 at physiological temperature and pH. This image-enhancing agent is biodegradable to intermediary metabolites, excretable chelates, oligomers, monomers or combinations thereof of low toxicity. These image-enhancing agents may further comprise a paramagnetic metal ion for enhancement of the image arising from induced magnetic resonance signals. Images resulting from scanning of gamma particle emissions may be enhanced when the image-enhancing agent of the present invention comprises radioisotopic metal ions emitting gamma particles.

Abstract: An organ preservative solution containing a low molecular weight dextran in a pharmacologically acceptable storage solution is suitable for storage and preservative of organs for transplantation.

Abstract: Improved compositions and methods for selective access to tumor regions (or other regions of abnormal endothelial properties). This capability provides powerful contrast-enhancement agents for nuclear magnetic resonance imaging. A polyatomic complex which includes intramolecular ferromagnetic coupling between metal atoms is associated with a polymer or microsphere carrier matrix which will bind to endothelial determinants. A solution containing this carrier complex is injected into a human (or other) body to be imaged. The carrier complex will preferentially extravasate at locations where the blood vessel walls have increased porosity or microvascular surface changes, and especially at tumor sites. Thus, the changes in relaxation time induced by the presence of the carrier complex will provide a high-gain marker for magnetic resonance imaging.

Abstract: A method of producing an absorbent composition. A polymeric material characterized as having surface anionic reactive sites is mixed with a source of multivalent metal ions to render the polymeric material sorbent of aqueous liquids. A dispersant is then added to form a wet slurry which is subsequently dried to a granular consistency.

Abstract: A polysulfate of a cyclodextrin in which at least one of 6 to 8 D-glucose units constituting the cyclodextrin has been replaced by a unit represented by Formula(1): ##STR1## wherein R is a group represented by the formula: ##STR2## where R.sup.1 to R.sup.7 are defined in the specification, which have an excellent antiretrovirus activity, particularly an excellent proliferation-inhibiting activity against HIV.

Abstract: A polysaccharide chemically joined to a nitroxyl spin label (NSL) compound has use for the preparation of an NMR diagnostic composition. An agent for modifying H.sub.2 O relaxation times in NMR diagnosis may comprise a polysaccharide to which is chemically linked both an NSL compound and an organic complexing agent to which is complexed a paramagnetic metal ion, such as Gd(III) or Cu(II). Polysaccharides include dextran, starch and cellulose. The preferred NSL compound is 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl.

Abstract: A polysulfate of a cyclodextrin in which at least one of 6 to 8,D-glucose units constituting the cyclodextrin has been replaced by a unit represented by Formula (1): ##STR1## wherein R is a group represented by the formula: ##STR2## where R.sup.1 to R.sup.7 are defined in the specification, which have an excellent antiretrovirus activity, particularly an excellent proliferation-inhibiting activity against HIV.

Abstract: The invention related generally to the preparation of colloidal metal(O) particles having a crosslinked aminodextran coating with pendent amine groups attached thereto. The aminodextran acts as both a reductant for reducing metal ions to metal(O) particles and as the protective agent which coats the metal(O) particles thus formed. After stabilizing the aminodextran coating by use of a crosslinking agent, the coated particles can be used to covalently bind proteins. The resulting protein containing colloidal particles can be used as markers in optical and electron microscopy, in immunological and biological assays, and possibly as therapeutic agents.

Abstract: Disclosed is a method for producing a water-swellable, generally water-insoluble, carboxyalkyl polysaccharide having improved absorption properties. The method involves forming a solution of carboxyalkyl polysaccharide and water, recovering the carboxyalkyl polysaccharide from the solution and heat-treating said recovered carboxyalkyl polysaccharide. Also, described is a carboxyalkyl polysaccharide having improved absorption properties.

Abstract: .sup.19 F labelled compounds are disclosed which are useful in methods of NMR imaging and spectroscopy. The compounds comprise a .sup.19 F-containing sensor moiety, and a transport polymer or substrate, and can optionally also comprise a spacer moiety to separate the sensor moiety and the transport polymer.

Abstract: To localize targets within the body (i.e., fixed intravascular antigens on emboli, neovascular endothelium, endothelium altered by regional inflammation) antibodies are linked via dextran spacer arms to rapidly cleared, Tc-99m labeled, microspheres. A micron-sized, albumin microsphere has been synthesized that is designed to enhance target surface interaction and to have a high antibody loading capacity. Stable, hydrophilic microspheres are produced from a pH dependent refolding of albumin followed by heat annealing. To couple dextran, the microspheres are derivatized with succinic anhydride and then linked via carbodiimide to succinic dihydrazide. After periodate oxidized dextran forms hydrazone linkages to the microspheres, additional dihydrazide coupled to the dextran spacer arm is used to link periodate oxidized IgG via its Fc domain carbohydrate. A milligram of the resulting 0.5-1.0 micron microspheres contains 50 to 350 ug of dextran and up to 10.sup.5 covalently bound IgG molecules per microsphere.

Abstract: There are provided paramagnetic compounds comprising a paramagnetic metal species chelated by a chelating moiety bound by an amide group to a linker group itself bound by an ester group to a macromolecule, wherein said linker group provides a carbon chain of at least 2 atoms between said amide group and said ester group. The novel compounds are particularly suitable as contrast agents, e.g. in magnetic resonance imaging.

Abstract: A composition for the prevention of adhesions between body tissues after a surgical operation, containing dextran and hyaluronic acid. The composition further claims the use of said components for the preparation of such a composition as well as its use as an agent for the prevention of adhesions.

Abstract: Adriamycin derivatives represented by formula (I) ##STR1## wherein R denotes a divalent hydrocarbon group,CD denotes a cyclodextrin residue,m is 1 to 8, andn is 0 to 8.The compounds exhibit excellent anti-cancer activity over a wide administration range, have low toxicity and sustained release, and maintain activity for a long period of time; thus, they are quite useful as an anti-cancer agent.

Abstract: Polycyclic mutagens are removed from aqueous or organic solutions by contacting the solution with a grafted dextranomer adsorbent which contains hydroxypropyl groups covalently linked to a reactive phthalocyanine dye.

Abstract: Methods are provided for the purification of interleukin-2 (IL-2) from a wide variety of sources, including synthetic mixtures, culture medium conditioned by natural IL-2 producing cells, and mammalian and bacterial recombinant IL-2 expression systems. The methods of the invention employ IL-2 receptor-affinity adsorbents in which soluble IL-2 receptors have been immobilized on solid supports. Through the use of these affinity adsorbents, highly purified IL-2 can be produced in a single step from bacterial extracts or conditioned medium. The IL-2 thus purified is largely free of aggregated forms, which are often present when other purification methods are used.

Abstract: The present invention includes an image-enhancing agent comprising a biodegradable, water-soluble polymer, synthetic or naturally derived and having repeating hydrophilic monomeric units with amino or hydroxyl groups. This agent also includes chelating agents comprising functional groups bound to an amino or bydroxyl group of the monomeric units. These chelating agents have a formation constant for divalent or trivalent metal cations of at least about 10.sup.8 at physiological temperature and pH. This image-enhancing agent is biodegradable to intermediary metabolites, excretable chelates, oligomers, monomers or combinations thereof of low toxicity.These image-enhancing agents may further comprise a paramagnetic metal ion for enhancement of the image arising from induced magnetic resonance signals.Images resulting from scanning of gamma particle emissions may be enhanced when the image-enhancing agent of the present invention comprise radioisotopic metal ions emitting gamma particles.

Abstract: The subject matter of the invention is the use of organic polymers which contain inorganic anionic groups for prophylaxis and therapy of retrovirus infections in mammals.

Abstract: Methods are provided for the purification of interleukin-2 (IL-2) and chimeric proteins containing an IL-2 moiety from a wide variety of sources, including synthetic mixtures, cell culture conditioned medium and mammalian and bacterial recombinant expression systems. The methods of the invention employ IL-2 receptor-affinity adsorbents in which soluble IL-2 receptors have been immobilized on solid supports. Through the use of these affinity adsorbents, highly purified IL-2 and chimeric proteins containing an IL-2 moiety can be produced in a single step from bacterial extracts or conditioned medium. The proteins thus purified are largely free of aggregated forms, which are often present when other purification methods are used.

Abstract: The invention concerns a polymer product for immobilizing of metal ions, adsorption, and the like, with the structureP--X--A--Qwherein P is a hydrophilic polymer with a molecular weight of more than 3 000 Daltons. X is a heteroatom, O, S or N, A is an atom sequence with at least 3 carbon atoms, and Q is a group with at least two branches with terminal, metal, metal chelate forming substituents, each having at least two hetero atoms, N, O or S, separated by two or at most three carbon atoms in a sequence or Q is a macrocyclic ring with at least 8 and not more than 30 atoms, at least 3 of which are nitrogen atoms, in sequence in the ring, and the preparation thereof which is done by activating a hydrophilic polymer with epoxi or vinylsulfone or inserting of aldehyde groups, couupling with tris-(2-aminoethyl)-amin and treating with reagents chosen from .alpha.-haloalkanoate, .alpha.

Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.

Abstract: Dextran sulfate, .beta.-1,3-glucan sulfate, and the salts thereof are angiostatic and useful for treatment and prevention of various diseases caused by abnormally accelerated angiogenesis. Combination of such a compound with a steroidal or non-steroidal substance increases the angiostatic activity of each compound to induce the combined effect.

Abstract: A channel protein having a Na.sup.+ /K.sup.+ selectivity of approximately 100 and capable of affecting Na.sup.+ membrane transport is disclosed. Amiloride derivatives, and amiloride gel materials incorporating such derivatives, useful in treating membrane transport, cellular volume and cellular pressure disorders and in isolating the channel protein are also disclosed. Use of the channel protein in diagnostic assays and screening assays is described.