Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.

Abstract: A drug delivery composition for nasal administration is provided which comprises the antiviral agent ICAM-1 and a bioadhesive material. The bioadhesive material may be a chitosan solution, a liquid formulation comprising a polymeric material or a plurality of bioadhesive microspheres. The polymeric material is preferably gellan gum or alginate. The microspheres may comprise starch, chitosan, hyaluronic acid, or gelatin.

Abstract: Glycosylated polyamines comprising of mono- or oligo-saccharides that are glycosidically linked to an aliphatic polyamine, and pharmaceutically acceptable salts, prodrugs and derivatives thereof are provided. An exemplary glycosylated polyamine has the following structure: Glycosylated polyamines, their pharmaceutically acceptable salts, prodrugs and derivatives are useful, for example, as anticancer compounds for the treatment of a variety of cancers. Methods for synthesis of glycosylated polyamines are disclosed. In addition, metal complexes of glycosylated polyamines, the preparation of such metal complexes, analytical methods using the metal complexes are provided. Methods for detecting equatorial and axial conformation of a group other than hydrogen at the C2 position of a saccharide molecule are also provided.

Abstract: A method for producing a S-nitrosylated species is provided. The method comprises: (a) providing a deoxygenated, alkaline aqueous solution comprising a thiol and a nitrite-bearing species; (b) acidifying the solution by adding acid to the solution while concurrently mixing the solution (e.g., by vigorously stirring the solution) to produce the S-nitrosylated species; and (c) isolating the S-nitrosylated species. The nitrite-bearing species can be, for example, an inorganic nitrite, such as an alkali metal nitrite, or an organic nitrite, such as an alkyl nitrite (e.g., ethyl nitrite, amyl nitrite, isobutyl nitrite or t-butyl nitrite). The thiol is preferably a thiol-containing polysaccharide, a thiol-containing lipoprotein, a thiol-containing amino acid or a thiol-containing protein, and more preferably a thiol-containing polysaccharide such as thiolated cyclodextrin. In many preferred embodiments, the S-nitrosylated species is insoluble in the acidified solution, precipitating upon formation.

Abstract: The invention provides a process for the sterilization of a powdered form of a glucocorticosteroid, sterile glucocorticosteroids, sterile formulations containing glucocorticosteroids and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or lungs.

Abstract: The present invention provides an anti-thrombogenic and cellular-adhesion coating composition for blood-contacting surfaces. The coating comprises a covalent complex of from 1 to 30 hydrophobic silyl moieties of Formula I: wherein R1 is an C1-18 alkyl or C6-32 aryl group, each R2 is independently selected from the group consisting of C1-18 alkyl and C6-32 aryl, R3 is N or O, n is a number from 1 to 10, directly bound to a heparin molecule via covalent bonding, with an adhesive molecule directly bound to the heparin molecule. In one embodiment, the coating comprises benzyl-(1,2 dimethyl)disilyl heparin, wherein an adhesive molecule, such as fibronectin, is bound to the heparin.

Abstract: The invention relates to certain stable microsphere compositions containing a fat, a wax or a mixture thereof; an active ingredient selected from LL-F28249&agr;-&lgr; compounds, 23-oxo or 23-imino derivatives of LL-F28249&agr;-&lgr; compounds, milbemycin compounds and avermectin compounds; an antioxidant and, optionally, an oil, a semi-soft fat, a fatty acid derivative or mixture thereof. The invention also relates to a method for introducing and maintaining levels of the active compound in the blood of warm-blooded animals for extended periods of time and for the prevention or treatment of infections and infestations caused by helminths, nematodes, acarids and endo- and ectoparasitic arthropods in warm-blooded animals by the parenteral administration of compositions of the invention.

Abstract: A process is disclosed for the production of an anticoagulant composition which allows for the accurate analysis of blood electrolyte concentrations. Also disclosed is the anticoagulant composition produced in accordance with the disclosed method and an apparatus containing said composition useful in the selection and sampling of blood.

Abstract: The invention relates to leukotriene B4 derivatives of general formula (I) in which R1 stands for CH2OH, CH3, CF3, COOR4, CONR5R6; R2 stands for H or an organic acid radical with 1-15 C atoms; R3 stands for H; R4 is hydrogen, C1-C10-alkyl, C3-C10-cycloalkyl, a C6-C10-aryl radical optionally substituted by 1-3 halogen, phenyl, C1-C4-alkyl, C1-C4-alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy, or CH2—CO—(C6-C10) aryl, or a 5-6 link ring with at least 1 heteroatom; A is a trans-, trans-CH═CH—CH═CH, a —CH2CH2—CH═CH— or a tetramethylene group; B is a C1-C10 linear or branched-chain aklylene group or the group (a) or (b); D is a direct bonding, oxygen, sulphur, —C≡C—, —CH═CR7, or a direct bonding with B. The invention also relates to salts thereof, having physiologically compatible bases and their cyclodextrin clathrates.

Abstract: A therapeutic food composition for treatment of diabetic patients to diminish fluctuations in blood sugar levels and prevent hypoglycemic episodes, comprising per unit about 20-50 grams of nutrients including slowly absorbed or digested complex carbohydrate, preferably uncooked cornstarch; more rapidly absorbed complex carbohydrate; protein; fat; and at least one sweetening agent, but less than about 3 grams of any simple sugar other than fructose. Fructose may be present in the composition in quantities greater than 3 grams per unit. Diabetic patients may be treated to diminish blood sugar fluctuations and prevent hypoglycemia via the administration of the novel food composition as an evening or pre-bedtime snack-or during the daytime hours to patients receiving insulin therapy or engaging in activities that might provoke hypoglycemia.

Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.

Abstract: The invention provides a composition of matter comprising two &bgr;-cyclodextrin molecules and a cleavable linker attached to and joining each such &bgr;-cyclodextrin. This invention further provides a composition which comprises a hydrophilic matrix comprising the above-described composition of matter and a photosensitizer encapsulated within the matrix, wherein the cleavable linker is cleaved upon exposure to light of a wavelength appropriate for the light to be absorbed by the photosensltlzer. This invention also provides a method of killing a tumor cell which comprises bringing into proximity with the tumor cell the above-described composition and exposing the composition to light so as to cleave the cleavable linker and release the photosensitizer.

Abstract: The present application relates to a group of novel substituted pentose and hexose monosaccharide derivatives, not previously disclosed, which exhibit potent anti-cell adhesion and anti-inflammatory activities. Methods of preparation, pharmaceutical compositions containing the compounds and methods of treatment, suppression and prevention of cell adhesion mediated chronic inflammatory disorders are also described.

Abstract: A method for suppressing immune responses in animals by administering gangliosides to the animal. Gangliosides having terminal sialic acid groups are disclosed as being especially effective as immunosuppressive agents. The especially effective immunosuppressive gangliosides include GM4 and GM5. Ganglioside compositions for use in suppressing immune responses are also disclosed.

Abstract: The invention relates to new heparin derivatives from bovine or porcine heparin which have a molecular weight equal to or larger than the standard heparin, show a sulfur content which is equal to or higher than that of the starting heparin or at least 13% w/w, have an anticoagulant activity in the anti-FXa assay of less than 10% of the standard heparin it was made from, show a ratio of APTT activity over anti-FXa activity of 3-35, show a reduced prolongation of bleeding time compared to the standard heparin it was made from as measured in the rat tail after i.v. administration and show enhancement of the rate of development of coronary collaterals in dogs equal to or better than clinically used heparin. The invention also relates to processes for preparation of the new bovine and porcine heparin derivatives.

Abstract: The invention is novel liquid chitosan-containing compositions, their methods of preparation, and their methods of use. In particular, the invention is a novel chitosan-containing liquid suspension composition which remains stable and is usable as an additive, for instance, in water or aqueous solution (i.e., water-based liquids).

Abstract: A process for preparing liquid iodophores with poly-N-vinyllactams and dextrins as carrier materials, which comprises heating a mixture of the carrier materials, iodine and iodide ions or, in place of the iodide ions, a reducing agent in aqueous medium in the presence of a monohydric or polyhydric alcohol having 1 to 6 carbon atoms at from 40 to 100° C.

Abstract: The present invention relates to derivatives of phosphorylated carbohydrates and pharmaceutical compositions comprising as a pharmaceutically active ingredient at least one of these compounds.

Abstract: The invention relates to a process for the selective oxidation of primary alcohols of oligosaccharides to form the corresponding carboxylic acid derivatives of the alcohols using catalytic amounts of a di-tertiary-alkyl nitroxyl free radical, characterized in that 1,3-dibromo-5,5-dimethylhydantoin or 1,3-dichoro-5,5-dimethylbydantoin is used as oxidant and the reaction is performed in neutral to basic conditions at a pH<10. The process of the invention is useful for the production of (partially protected) oligosaccharides comprising carboxylate groups, both intermediates and end products.

Abstract: A carrier and a method for preparing it are provided for use in the delivery of therapeutic agents. A polysaccharide is reacted with an oxidizing agent to open sugar rings on the polysaccharide to form aldehyde groups. The aldehyde groups are reacted to form covalent oxime linkages with a second polysaccharide and each of the first and second polysaccharide is selected from the group consisting of hyaluronic acid, dextran, dextran sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, heparan, heparan sulfate and alginate.