Abstract: The present invention relates to a process of isolation of bioactive eupalitin (3-O-O-D-galactopyranoside) of formula 1 possessing anti-osteoporosis activity by extraction of powdered leaves of Boerhaavia diffusa, with better yield:

Abstract: A method of treating Restless Leg Syndrome, includes administering to a subject an iron complex having an iron release rate greater than IDI. The iron release rate is determined at a concentration of at least 2,000 ?g/dl.

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: The present invention relates to a method by which saccharide compounds can be prepared in a very easy way. This method comprises the steps of: (a) attaching at least one saccharide to a cyclic or acyclic diene, (b) reacting the saccharide-containing diene obtained in step (a) or a commercially available saccharide-containing diene with a dienophile by Diels-Alder reaction.

Abstract: The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N3; X1 is hydrogen, —CH2O—, —CH2NH—, —CH3, —CH2N3 or —COO—; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N3, and E is absent when X1 is hydrogen, CH3 or N3.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: Compounds that are modified polysaccharides having pendant aldehyde functionalities are disclosed. Each of the aldehyde functionalities is attached through a linker to a position corresponding to a hydrogen atom of a different hydroxyl group of unmodified polysaccharide. Also disclosed is a method for introducing an amine-reactive functionality into a dextran. The method comprises (a) reacting the dextran with an alkylating agent having a functionality that reacts with an hydroxyl group of the dextran thereby forming an alkylated dextran wherein the alkylating agent has an olefin group and (b) treating the alkylated dextran to convert the olefin group to an amine-reactive functionality. A polysaccharide can be conjugated to a biomolecule by carrying out the above method and reacting the amine-reactive functionality with an amine functionality on the biomolecule to produce polysaccharide conjugated to the biomolecule.

Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.

Abstract: Azithromycin in the form of a monohydrate comprising from 4.0% to 6.5% of water, a process for its preparation and its use in pharmaceutical compositions.

Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.

Abstract: The present invention relates to a composition comprising a catechin compound, ascorbic acid, proline and lysine. The present invention also relates to a method for treating neoplastic disease using a composition comprising a catechin compound, ascorbic acid, proline and lysine.

Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.

Abstract: A protected 2?-deoxycytidine is purified by precipitating the protected 2?-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the protected 2?-deoxycytidine and water, and by recovering the protected 2?-deoxycytidine: wherein R1 represents a 4-methoxytrityl, 4, 4?-dimethoxytrityl, or triphenylmethyl group; and B1 represents a cytosine group having a protected amino group. The compound represented by general formula (3) is, in particular, a protected 2?-deoxycytidine represented by formula (4): The 2?-deoxycytidine is used as a raw material for antisense DNA.

Abstract: Process for the production of polysaccharide ethers, e.g. cellulose ethers, are disclosed wherein salts formed during the process, e.g., sodium nitrate or sodium acetate, are converted to their corresponding acids and bases by means of an electric current, preferably in combination with a bipolar membrane and suitable catiion and/or anion membranes. The acids and bases recovered from the process can be recycled, thereby avoiding the need to provide for disposal of salts.

Abstract: A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryimidine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of TNF? to TNF?-RI.

Abstract: A method for the prophylaxis or treatment of an inflammatory bowel disease is provided, comprising administering to a patient having or at risk of developing an inflammatory bowel disease a therapeutically or preventatively effective amount of one or more ribofuranose derivatives having the Formula (I): wherein R is a group selected from a carboxamide, an amidine, and pharmaceutically acceptable acid addition salts thereof, and the configuration at the C2 carbon of the ribofuranose moiety is D or L. The one or more ribofuranose derivatives (I) may be used in combination with further active agents such as antivirals or agents effective against inflammatory bowel disease.

Abstract: Compositions and methods are provided for use in the treatment of cancer.

Abstract: The instant invention provides a method of treating or preventing osteoarthritis, joint effusion, joint inflammation and pain, synovitis, lameness, post operative arthroscopic surgery, deterioration of proper joint function including joint mobility, the reduction or inhibition of metabolic activity of chondrocytes, the activity of enzymes that degrade cartilage, the reduction or inhibition of the production of Hyaluronic acid, said method comprising orally administering to a mammalian species a therapeutically effective amount of Hyaluronic Acid or pharmaceutically acceptable salts thereof. Additionally, compositions containing hyaluronic acid; chondroitin sulfate, and glucosamine sulfate in a paste formulation are also disclosed which can be administered on their own or can be used as a feed additive.

Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.

Abstract: A method for forming II-type cellulose, which comprises introducing together a slurry having water and a I-type cellulose dispersed therein and water in the state of high temperature and high pressure to a tubular reactor (28) contacting the I-type cellulose with a hot water in a supercritical state or subcritical state for a predetermined time in the tubular reactor (28), to thereby cleave a part of the hydrogen bonds in the I-type cellulose and dissolve the I-type cellulose into the water in a supercritical state or subcritical state, cooling a cellulose solution discharged from the tubular reactor (28) in a cooler (30) to room temperature or lower, followed by allowing to stand, to thereby precipitate crystals of II-type cellulose having a molecular weight lower than that of the I-type cellulose, and separating the resultant II-type cellulose from a solvent. The method allows the preparation of pure II-type cellulose by the use of a simple process.