Abstract: (?)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (?)-OddC) or its derivative and its use to treat cancer in animals, including humans.

Abstract: A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.

Abstract: The present invention relates generally to molecular assemblies, more particularly to an assay for the detection of G-protein coupled receptor (GPCR) molecular assemblies and bead-based detection of ligand-GPCR complexes and to methods for identifying compounds as agonists, partial agonists or antagonists of the binding of G-protein coupled receptors to G-protein and for use of these compounds in the treatment of conditions or disease states in a mammalian subject or patient, including humans, where G-protein coupled receptor binding to G-protein is implicated.

Abstract: The present invention relates to a method of treating or preventing kidney disease in an animal subject including administering an effective amount of C-reactive protein to the animal subject. The kidney disease may be associated with systemic lupus erythematosus.

Abstract: The present invention is directed to methods of treating patients for pain by administering noribogaine. Noribogaine may also be used to treat patients for the symptoms associated with withdrawal from drug dependency. In the latter case, the noribogaine treatment should be supplemented with the administration of an opioid antagonist such as naloxone.

Abstract: The present invention relates to a method for reducing adhesions associated with post-operative surgery. The present method comprises administering or affixing a polymeric composition preferably comprising chain extended, coupled or crosslinked polyester/poly(oxyalkylene) ABA triblocks or AB diblocks having favorable EO/LA ratios to a site in the body which has been subjected to trauma, e.g. by surgery, excision or inflammatory disease. In the present invention, the polymeric material provides a barrier to prevent or reduce the extent of adhesions forming.

Abstract: The invention provides a catalytic, chemospecific and stereospecific method of oxidizing a wide variety of substrates without unwanted side reactions. Essentially, the method of the instant invention, under relatively mild reaction conditions, catalytically, stereospecifically and chemospecifically inserts oxygen into a hydrocarbon C—H bond. Oxidation (oxygen insertion) at a tertiary C—H bond to form an alcohol (and in some cases a hemiacetal) at the tertiary carbon is favored. The stereochemistry of an oxidized tertiary carbon is preserved. Ketones are formed by oxidizing a secondary C—H bond and ring-cleaved diones are formed by oxidizing cis tertiary CH bonds.

Abstract: The present invention provides a general approach for G protein coupled receptors that may be used to define agonists and antagonists, and the specificity of receptor coupling to G protein subunits. Methods of the present invention use small volumes (microliters) and are compatible with high throughput flow cytometry. When assays of the present invention are multiplexed, the specificity of the interactions of a receptor with many G proteins may be determined simultaneously.

Abstract: An isolated peptide fragment of the VapA protein that binds antibodies specific for Rhodococcus equi and the VapA protein. In a preferred form the peptide contains an amino acid sequence of 5 or more amino acid residues that is identical to or homologous to the amino acid sequence of at least one region of the VapA protein that is responsible for immunological recognition. Methods of diagnosing a vertebrate for the presence of R. equi using the peptide and methods of vaccinating a vertebrate against R. equi using the peptide are also claimed.

Abstract: The instant invention relates to novel surfactant-free, multiphase sunscreen compositions that provide protection from the sun, have a unique visual appeal, and provide skin conditioning and moisturization. In a two-phase embodiment of the instant invention, the compositions are comprised of (1) a first layer comprising a high-density ester and sunscreen, and (2) a second aqueous layer, which is usually the top layer. In a three-phase embodiment of the instant invention, the compositions are comprised of (1) a first layer comprising a high-density ester and and sunscreen, (2) a second aqueous layer, and (3) a third oily layer. The high-density ester layer usually has a specific gravity that is greater than that of the aqueous layer and the aqueous layer usually has a specific gravity that is greater than the oily layer. In preferred embodiments, each phase is substantially clear and has a volume approximately equal to that of the other phase(s).

Abstract: A display and method of preparing 7-transmembrane and other receptors for real-time kinetic analysis of binding interactions. The invention includes display on beads and in micelles for multi-well and flow cytometric analysis. The invention is useful for ligand discovery and drug action discovery, and G-protein response in particular.

Abstract: A member of a new class of bacterial toxin has been isolated and characterised. The bacterial toxin is of the AB5 type and is characterised in that it has a subtilase domain. It is cytotoxic to Vero cells, and toxicity in vivo in mice occurs in a number of different sites. Mutation of the serine active residue results in greater than 99% reduction in activity. The protein has been purified and antibodies have been prepared for both the A subunit and B subunits, and ELISA detection methods have been developed. The nucleic acid sequence has been determined and primers specific for the toxin have been used for a preliminary screen of a range of patient samples to ascertain the extent to which the toxin is present.

Abstract: The present invention relates to a new aziridine derivative that is represented herein by general chemical formulae (Ia) or (Ib), and to their preparation method. In the said chemical formulae, R2 and R3 can be the same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aryl, or amino protective group; and amino protective group is, for example, (Ph)3C, and FMOC(9-fluorenylmethyloxycarbonyl), alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl, aryl or aralkyl.

Abstract: A display and method of preparing 7-transmembrane and other receptors for real-time kinetic analysis of binding interactions. The invention includes display on beads and in micelles for multi-well and flow cytometric analysis. The invention is useful for ligand discovery and drug action discovery, and G-protein response in particular.

Abstract: Methods of treating diabetes in an animal and food compositions useful for treating diabetes are described. In one aspect of the invention, the method includes treating the animal with a therapeutically effective amount of CLA including 9,11-octadecadienoic acid and 10,12-octadecadienoic acid, isomers thereof, esters thereof, salts thereof or mixtures thereof. In another aspect of the invention, a food composition comprising a food product having a therapeutically effective amount of a purified CLA isomer, including cis,cis-9,11-octadecadienoic acid, trans,cis-10,12-octadecadienoic acid or a mixture of purified cis,trans-9,11-octadecadienoic acid and trans,cis-9,11-octadecadienoic acid is described.

Abstract: The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 15?-estradiol ester compounds is presented which exhibit excellent biological activity for use in pharmaceutical compositions for the treatment of symptomology associated with menopause. The present invention is therefore directed to compounds according to the structure: where X is R is H, a C1 to C5 alkyl group, optionally substituted with at least one halogen group, such as CH2CH2F, or other group (e.g., CH2CHF2, CH2CF3 or CF3 group); and m is from 0–5, preferably from 0–2.

Abstract: A novel amphiphilic lipid compound having a cleavable, vinyl ether linked hydrophilic headgroup is described. Also described are liposomes containing the vinyl ether lipid compound, which may be triggered to release their contents and/or permeablize or fuse with target lipid membranes. The cleavable vinyl ether linkage allows the hydrophilic headgroup to be dissociated from the hydrophobic tailgroup(s) of the lipid compound to facilitate phase transitions in the lipid bilayer.

Abstract: The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2?,3?dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(?-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-?-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.

Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2?-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

Abstract: A therapeutic agent capable of of binding to the F?-G? loop of domain 4 of the common c Chain of the receptor for GM-CSF, IL-3, and IL-5. The amino acid Tyr421 which is located in the F?-G? loop is critical in the high affinity binding and stimulation of function of GM-CSF, IL-3 and IL-5 to the common c chain of the receptors. Other receptors for cytokines also show hydrophobic amino acids in analogous positions and it is probable that they too play a pivotal role in binding of respective cytokines to them and in modulating function. Agents capable of binding to the F?-G? loops are suggested and should be of therapeutic value.