Abstract: This invention provides compositions for inhibiting the binding between two cells, one expressing P- or L-selectin on the surface and the other expressing the corresponding ligand. A covalently crosslinked lipid composition is prepared having saccharides and acidic group on separate lipids. The composition is then interposed between the cells so as to inhibit binding. Inhibition can be achieved at an effective oligosaccharide concentration as low as 106 fold below that of the free saccharide. Since selectins are involved in recruiting cells to sites of injury, these composition scan be used to palliate certain inflammatory and immunological conditions.

Abstract: This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure wherein X is R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10, are each, independently, hydrogen, acyl of 2-7 carbon atoms, perfluoroacyl of 2-10 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, benzoyl, benzyl or —SO3M; M is hydrogen, lithium, sodium, potassium or ammonium; R11 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, halogen, nitrile, nitro, or alkoxy of 1-6 carbon atoms; R12 is hydrogen, nitro, amino, acylamino of 2-7 carbon atoms, perfluoroacylamino of 2-7 carbon atoms, alkylamino of 1-6 carbon atoms, perfluoroalkylamino of 1-6 carbon atoms, dialklylamino where each alkyl chain is independently 1-6 carbon atoms, perfluorodialklylamino where each alkyl chain is independently 1-6 carbon atoms alkylsulfonylamino of 1-6 carbon atoms, perfluoroalkylsulfonylamino of 1-6 carbon atoms, arylsulfonylamino of 6-10

Abstract: Process for the preparation of O-sulfated K4, K5 and K40 polysaccharides useful for the treatment of tumoral, HIV-1 and coagulation pathologies and in cosmetic preparations, wherein the K4, K5 or K40 polysaccharide in the form of sodium salt is suspended in an aprotic solvent and directly submitted to the reaction of O-sulfation with a pyridine-sulphur trioxide or trimetylamine-sulphur trioxide adduct or with chlorosulfonic acid.

Abstract: Sucrose ester and ether products, useful as food or beverage bulking agents, reduced calorie sweeteners, fat replacement agents, stabilizing agents, thickening agents and emulsifying agents; adhesives; biodegradable plastics and films; sizing agents for paper and textiles; ethical pharmaceuticals and new fibers are prepared by using a two-phase reaction system in which sucrose is dissolved in an alkaline, aqueous solution and an acidic reagent such as a bifunctional acid dichloride or epoxide is added to the sucrose in a water-immiscible organic solvent. Several types of products are produced: water-insoluble sucrose ester (ether) copolymers; water-soluble sucrose ester (ether) copolymers; sucrose ester (ether) dimers; and intramolecular, cyclic sucrose esters (ethers). These products can be further varied by using different kinds of acid dichlorides or epoxides that contain different kinds of functional groups.

Abstract: The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediated by a neural cell growth repulsion factor. The activator may comprise a direct or an indirect activator of the protein kinase; the repulsion factor typically comprises one or more natural, endogenous proteins mediating localized repulsion or inhibition of neural cell growth; and the target cells are generally vertebrate neurons, typically injured mammalian neurons. The subject compositions include mixtures comprising a neural cell, an activator of a cyclic nucleotide dependent protein kinase and a neural cell growth repulsion factor.

Abstract: The present invention relates to a purified, easily produced poly-.beta.-1.fwdarw.4-N-acetylglucosamine (p-GlcNAc) polysaccharide species useful in drug compositions. The p-GlcNAc of the invention is a polymer of high molecular weight whose constituent monosaccharide sugars are attached in a .beta.1.fwdarw.4 conformation, and which is free of proteins, and substantially free of single amino acids, and other organic and inorganic contaminants. In addition, derivatives and reformulations of p-GlcNAc are described. The present invention further relates to methods for the purification of the p-GlcNAc of the invention from microalgae, preferably diatom, starting sources. Still further, the invention relates to methods for the derivatization and reformulation of the p-GlcNAc. Additionally, the present invention relates to the uses of pure p-GlcNAc, its derivatives, and/or its reformulations.

Abstract: The present invention relates to a purified, easily produced poly-.beta.-1.fwdarw.4-N-acetylglucosamine (p-GlcNAc) polysaccharide species useful in collagen copolymers. The p-GlcNAc of the invention is a polymer of high molecular weight whose constituent monosaccharide sugars are attached in a .beta.-1.fwdarw.4 conformation, and which is free of proteins, and substantially free of single amino acids, and other organic and inorganic contaminants. In addition, derivatives and reformulations of p-GlcNAc are described. The present invention further relates to methods for the purification of the p-GlcNAc of the invention from microalgae, preferably diatom, starting sources. Still further, the invention relates to methods for the derivatization and reformulation of the p-GlcNAc. Additionally, the present invention relates to the uses of pure p-GlcNAc, its derivatives, and/or its reformulations.

Abstract: Compounds that exhibit selectin binding activity are described and have the following structural formula: ##STR1## where W is selected from a group including structures a-d below ##STR2## wherein p is an integer of from 0-2, q is an integer of from 0-3, and r is an integer of from 0-5;A is selected from the group consisting of .alpha. and .beta. forms of sialic acid, Kemp's acid, quinic acid, R and S forms of mandelic acid, R and S forms of glyceric acid, R and S forms of lactic acid, propionic and acetic acid, and esters and amides thereof, --SO.sub.3, sulfonate, --PO.sub.3, phosphonate, trifluoromethyl, diazine and triazine;B is selected from a group consisting of .alpha. and .beta. forms of fucose, arabinose and esters and substituted forms thereof wherein one or more of the OH groups is independently substituted with F, N.sub.3, NHAc, NHCOCF.sub.3. The remaining variable are described in the specification.

Abstract: Glyco-amino acids and glycopeptides having three-dimensionally stable configurations are described. These glyco-amino acids and glycopeptides have glycoside functional groups, such as fucose and analogues and derivatives thereof, covalently bound to an amino acid or peptide having a free carboxylic group or sulfate group in an orientation that facilitates the binding between these groups and selectin receptors. The present glyco-amino acids and glycopeptides may be used in the treatment of selectin-mediated disorders, such as inflammation, autoimmune disease and cancer.

Abstract: A synthetic insulin mimetic compound is disclosed. Small synthetic amines of disaccharides, such as 2-deoxy-2-amino-galactopyranosyl pinitol are shown to mimic the action of insulin and to modulate its action.

Abstract: The present invention is drawn to hyaluronic acid fractions having molecular weights in the range of from about 20,000 to about 60,000 daltons, wherein these hyaluronic acid fractions possess osteoinductive activity. The present invention further includes pharmaceutical compositions comprising such hyaluronic acid fractions to be used in the treatment of various types of bone disorders, as well as methods of treating such disorders using the pharmaceutical compositions.

Abstract: A method for enhancing the solubilization and/or complexation of a drug which is insoluble or sparingly soluble in water with cyclodextrin, comprising combining the drug with cyclodextrin together with a selected hydroxy-carboxylic or polycarboxylic acid.

Abstract: Provided is a biomaterial comprising an interpenetrating polymer network (IPN), wherein one of the polymer components is an acidic polysaccharide or a semi-synthetic derivative thereof. The polysaccharide can be hyaluronic acid, and the second polymer component can be a non-toxic, non-carcinogenic synthetic chemical polymer. The derivative can be a total or partial hyaluronic acid ester or a hyaluronic acid salt. The ester or salt can be formed with a pharmacologically active molecule. Methods for preparing the IPN are also disclosed. The acidic polysaccharide or derivative thereof and the synthetic chemical polymer comprising the IPN can be cross-linked, or the synthetic chemical polymer can be grafted onto the acidic polysaccharide. The cross-linking or grafting can be achieved using compounds capable of generating radicals, or via functional groups on the acidic polysaccharide and the synthetic chemical polymer. The IPN can be formed prior to cross-linking or grafting.

Abstract: The present invention provides a composition of matter comprising a biosynthetic anti-inflammatory oligosaccharide, comprising the structure of: sugar - sugar - X - R; wherein said sugar is selected from the group consisting of N-acetylneuraminic acid, galactose, N-acetylglucosamine, N-acetylgalactosamine, fucose and mannose; wherein X is a bridging atom selected from the group consisting of oxygen, sulfur, nitrogen and carbon; and wherein R is an aglycone selected from the group consisting of naphthol, naphthalenemethane, indenol, a heterocyclic derivative of indenol, a heterocyclic derivative of naphthol and a heterocyclic derivative of naphthalenemethanol. Also provided is a method of treating an inflammatory disease in an individual comprising the step of administering to said individual a therapeutically effective dose of the novel composition of the present invention.

Abstract: A method of treating a mammal for a condition of the skin or exposed tissue selected from the group consisting of basal cell carcinoma and actinic keratosis is provided. The method consists essentially of topically administering to the site of the condition, more than once per day over a period of days sufficient to treat the condition, a non-toxic effective dosage amount of a composition consisting essentially of(a) a non-steroidal anti-inflammatory drug (NSAID) in an amount sufficient to block prostaglandin synthesis,(b) hyaluronic acid or a pharmaceutically acceptable salt thereof in an amount effective to transport said NSAID into the skin or exposed tissue at the site of the condition. The concentration of the hyaluronic add or salt thereof is between 1-3% by weight of the composition. The molecular weight of the hyaluronic acid or salt thereof is between 150,000 and 750,000 Daltons. A pharmaceutical excipient suitable for topical application is included.

Abstract: The present invention relates to a purified, easily produced poly-.beta.-1.fwdarw.4-N-acetylglucosamine (p-GlcNAc) polysaccharide species useful in drug compositions. The p-GlcNAc of the invention is a polymer of high molecular weight whose constituent monosaccharide sugars are attached in a .beta.-1.fwdarw.4 conformation, and which is free of proteins, and substantially free of single amino acids, and other organic and inorganic contaminants. In addition, derivatives and reformulations of p-GlcNAc are described. The present invention further relates to methods for the purification of the p-GlcNAc of the invention from microalgae, preferably diatom, starting sources. Still further, the invention relates to methods for the derivatization and reformulation of the p-GlcNAc. Additionally, the present invention relates to the uses of pure p-GlcNAc, its derivatives, and/or its reformulations.

Abstract: A method of producing a carboxylic acid glucuronide by reacting a carboxylic acid precursor with a blocked sugar epoxide precursor is disclosed. Also disclosed are: deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC carboxylic acid glucuronide having a deuterated hydrocarbon chain; 5'-deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC-carboxylic acid or 5'-deuterated .DELTA..sup.8 - or .DELTA..sup.9 -THC glucuronide. The compositions are useful as GC-MS standards; in methods for preparing antibodies reactive with a THC glucuronide; and, in GC-MS diagnostic methods for THC metabolites.

Abstract: Partially acylated cyclodextrins of the formula I ##STR1## where R denotes hydrogen or R1, wherein R1 can be identical or different and denotes acetyl, propionyl, butyryl, 2-alkoxyacetyl, 2-chloroacetyl, 2-fluoroacetyl, 2-N-acetylaminoacetyl, methacryloyl or acryloyl, and the DS for R1, measured by means of .sup.1 H NMR spectroscopy, is between 0.30 and 1.20; and a process for preparing partially acylated .beta.-cyclodextrins and also a process for their use.

Abstract: Two pharmaceutically useful fractions of hyaluronic acid are obtained comprising a first fraction with a molecular weight between 50,000 and 100,000 which is useful for wound healing, and a second fraction having a molecular weight between 500,000 and 730,000 which is useful for intraocular and intraarticular injections. In addition, pharmaceutical preparations for topical administration are provided containing a pharmacologically active substance together with hyaluronic acid or a molecular weight fraction thereof. The hyaluronic acid may be in the form of the free acid or may be a salt with an alkali or alkaline earth metal, magnesium, aluminum or ammonium, or in the form of a salt with one or more pharmacologically active substances.

Abstract: Hepatocytes spheroids can be formed by culturing hepatocytes in a culture vessel using a lipid-bound glycosaminoglycan as a culture substrate. Floating spheroids of hepatocytes can be obtained efficiently, which are capable of maintaining liver-specific functions and of keeping the spheroid form stably for a prolonged period of time.