Abstract: Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.

Abstract: Compounds having a phosphorus group structure of: wherein: R is alkyl, modified lower alkyl; and Ri and Ri are each independently H, alkyl, modified alkyl, or aryl; are provided. Also provided are polynucleotide compositions that include these compounds and methods of using the compounds in synthesis of the same.

Abstract: The present invention provides a process for producing a N4-acyl-5?-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.

Abstract: Provided is a hydroxyl-protected alcohol of the formula R—O—Pg, wherein Pg is a protecting group of the formula: wherein Y, Z, W, R1, R1a, R2, R2a, R3, R3a, R4, R4a, a, b, c, d, e and f are defined herein and R is a nucleosidyl group, an oligonucleotidyl group with 2 to about 300 nucleosides, or an oligomer with 2 to about 300 nucleosides. Also provided is a deprotection method, which includes heating the hydroxyl-protected alcohol at a temperature effective to cleave thermally the hydroxyl-protecting group therefrom.

Abstract: Disclosed herein are methods of using an adenosine analog or derivative for treating heart failure, increasing cardiac muscle contractility, increasing cardiac diastolic relaxation, and increasing vasodilation.

Abstract: The present invention provides solid support media for use in oligomer synthesis, methods of producing the media, and methods of using the media. In some embodiments, the processes of the invention comprise (a) providing an organic phase comprising an olefin monomer, a cross-linker, a functionalizing reagent and an initiator; and (b) contacting the organic phase with an aqueous phase under conditions of time and temperature effective to form the polymeric bead.

Abstract: A production method for conveniently producing a 5?-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a 2?,3?,5?-triacyloxynucleoside compound represented by the formula [I] to selective deacylation in an alcohol represented by the formula [II] using a base selected from the group consisting of alkali metal hydroxide, alkali metal alkoxide and alkali metal carbonate: wherein each symbol in the formula is as defined in the specification.

Abstract: Methods for deprotecting and derivatizing oligonucleotides that are non-covalently bound to a solid support are described. The methods include providing a plurality of oligonucleotides linked to one or more hydrophobic separation functions, wherein the plurality includes protected oligonucleotides, precipitating the plurality of oligonucleotides on a hydrophobic solid support using an organic solvent to produce non-covalently immobilized oligonucleotides, and deprotecting the immobilized oligonucleotides.

Abstract: The present invention is directed to the use of N-acetyl-D-glucosamine to treat organ lesions caused by toxicants and drugs. The present invention is also directed to a method for treating organ lesions caused by toxicant comprising administering to a patient suffering from organ lesions a pharmaceutical composition comprising N-acetyl-D-glucosamine or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to methods for the treatment of a sleep disorder comprising administering a compound of formula (I): wherein all variables are as defined herein.

Abstract: Compositions comprising inorganic phosphate and the nucleotides adenosine diphosphate and adenosine monophosphate; and their use for neutralizing effects of excess incident energy on the human body, particularly effects of ionizing radiation from nuclear or radiological energy sources, are disclosed and claimed.

Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds of Formula II in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases. wherein X is S, N, O or CR; Y is CRR?, O, NR6, CRR?—CRR? or CR?CR; Z is NR6, O, S, CRR? or CRR?—CRR?; R1-R3 are independently selected from the group consisting of H, C1-C8 alkyl, C1-C8 alkoxy, amino, hydroxy, halosubstituted alky and halo; R4 is Q is CR, NR6 or R5 is H or benzyl; R6 is H, C1-C8 alkyl, C1-C8 alkoxy, OH or halo; and R and R? are independently H, C1-C8 alkyl, C1-C8 alkoxy, OH or halo, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen or C1-4alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4-alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N—C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n—wherein n is zero, one or two; with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to —NR3—; processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

Abstract: Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.

Abstract: Methods and uses are described for treating or preventing diseases of humans or non-human animals by reducing the amount of active leukotriene B4 (LTB4) in those in need of such treatment using LTB4 hydroxylases. In certain embodiments, LTB4 hydroxylase is administered in combination with nicotinamide adenine dinucleotide phosphate and/or an NADPH-cytochrome P-450 reductase. The invention is particularly useful for treating or preventing respiratory diseases that are caused or exacerbated by inflammation.

Abstract: Compositions and methods for maintaining healthy mobile joints and cartilage in humans and animals are disclosed. The composition comprises glucosamine and chondroitin dispersed in a controlled-release matrix system capable of releasing the glucosamine and chondroitin over a designated time period. In another aspect, the invention provides compositions and methods for maintaining health mobile joints and cartilage in humans and animals without adversely affecting glucose regulation.

Abstract: The present invention provides a 4?-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: (wherein X represents a halogen atom, R1 represents an ethynyl group or a cyano group, and R2 represents hydrogen, a phosphate residue, or a phosphate derivative residue). The present invention also provides a pharmaceutical composition containing the derivative and a pharmaceutically acceptable carrier therefor. Such derivative is useful as medicine for the treatment of Acquired Immune Deficiency Syndrome (AIDS).

Abstract: A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting group, B is a purine or pyrimidine nucleobase, and R1 is C1-6 alkyl. The compounds of formula (I) are inhibitors of HCV polymerase useful in the treatment of HCV infection.

Abstract: The present invention provides an improved phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole. Further provided are improved methods of oligonucleotide synthesis wherein a phosphoramidite activator comprising a solution of 5-benzylmercaptotetrazole in acetonitrile and N-alkyimidazole is used to prepare internucleoside linkages.

Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2, and L are defined in the description.